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haloperidol

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Description

Haloperidol is a butyrophenone antipsychotic medication. It is used to treat schizophrenia, Tourette syndrome, acute psychosis, and severe agitation. Haloperidol works by blocking the action of dopamine in the brain. It was first synthesized in 1958 by Paul Janssen and his team at Janssen Pharmaceutica. Haloperidol is a potent antipsychotic and has a long half-life. It is typically administered orally, but can also be given intravenously or intramuscularly. Haloperidol has a number of side effects, including extrapyramidal symptoms (EPS) such as tremors, rigidity, and akathisia. It can also cause sedation, drowsiness, and dry mouth. In rare cases, haloperidol can cause neuroleptic malignant syndrome (NMS), a life-threatening condition characterized by high fever, muscle rigidity, and altered mental status. Haloperidol is a widely used and effective antipsychotic medication. It is an important treatment option for patients with schizophrenia, Tourette syndrome, and other mental illnesses. Haloperidol is studied for its potential to treat a variety of other conditions, including obsessive-compulsive disorder, bipolar disorder, and chronic pain. It has also been studied as a potential treatment for Alzheimer's disease and Parkinson's disease.'

Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

diphenylprolinol silyl ether: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3559
CHEMBL ID54
CHEBI ID5613
SCHEMBL ID8264
MeSH IDM0009771
PubMed CID129696643
MeSH IDM0009771

Synonyms (296)

Synonym
BIDD:GT0128
AC-19691
MLS001146904
BRD-K67783091-001-05-5
BRD-K67783091-001-04-8
gtpl86
nsc-615296
pernox
4-[4-(p-chlorophenyl)-4-hydroxypiperidino]-4'-fluorobutyrophenone
sernel
1-(3-p-fluorobenzoylpropyl)-4-p-chlorophenyl-4-hydroxypiperidine
4'-fluoro-4-[4-hydroxy-4-(4'-chlorophenyl)piperidino]butyrophenone
1-butanone, 4-[4-(4-chlorophenyl)-4-hydroxy-1-piperidinyl]-1-(4-fluorophenyl)-
haldol
brotopon
einalon s
aloperidolo
lealgin compositum
serenace
aloperidol
r 1625
4-(4-hydroxy-4'-chloro-4-phenylpiperidino)-4'-fluorobutyrophenone
halojust
mixidol
halol
halopoidol
linton
ulcolind
nsc170973
mcn-jr-1625
.gamma.-[4-(p-chlorphenyl)-4-hydroxpiperidino]-p-fluorbutyrophenone
serenase
aloperidon
galoperidol
halopal
wln: t6ntj a3vr df& dq dr dg
butyrophenone, 4-[4-(p-chlorophenyl)-4-hydroxypiperidino]-4'-fluoro-
4-[4-(para-chlorophenyl)-4-hydroxypiperidino]-4'-fluorobutyrophenone
aldo
serenelfi
r-1625
eukystol
aloperidin
sernas
uliolind
nsc-170973
MLS000028450 ,
smr000058303
DIVK1C_000654
KBIO1_000654
peluces
einecs 200-155-6
aloperidolo [dcit]
brn 0331267
haloperidolum [inn-latin]
butyrophenone, 4-(4-(p-chlorophenyl)-4-hydroxypiperidino)-4'-fluoro-
gamma-(4-(p-chlorophenyl)-4-hydroxypiperidino)-p-fluorbutyrophenone
hsdb 3093
4'-fluoro-4-(4-hydroxy-4-p-chlorophenylpiperidino)butyrophenone
haldol solutab
nsc 615296
gamma-(4-(p-chlorophenyl)-4-hydroxypiperidino)-p-fluorobutyrophenone
butyrophenone, 4'-fluoro-4-(4-(p-chlorophenyl)-4-hydroxypiperidino)-
c21h23clfno2
4-(4-(4-chlorophenyl)-4-hydroxy-1-piperidinyl)-1-(4-fluorophenyl)-1-butanone
4-(4-(p-chlorophenyl)-4-hydroxypiperidino)-4'-fluorobutyrophenone
nsc 170973
fortunan
dozic
keselan
aloperidolo [italian]
1-butanone, 4-(4-(4-chlorophenyl)-4-hydroxy-1-piperidinyl)-1-(4-fluorophenyl)-
ccris 1630
EU-0100583
haloperidol, powder
haloperidol (jp17/usp/inn)
D00136
SPECTRUM_000861
PROBES1_000255
PROBES2_000296
BPBIO1_000144
PRESTWICK_250
NCGC00015500-01
lopac-h-1512
NCGC00023875-02
NCGC00016234-01
cas-52-86-8
tocris-0931
SPECTRUM5_000788
BPBIO1_001231
QTL1_000042
PRESTWICK2_000115
BSPBIO_000130
IDI1_000654
LOPAC0_000583
PRESTWICK3_000115
CMAP_000037
4-[4-(4-chlorophenyl)-4-hydroxy-1-piperidinyl]-1-(4-fluorophenyl)-1-butanone
nsc615296
4-[4-(4-chlorophenyl)-4-hydroxy-1-piperidyl]-1-(4-fluorophenyl)butan-1-one
chembl54 ,
bdbm21398
haloperidol, 1
AB00052008
4-[4-(4-chloro-phenyl)-4-hydroxy-piperidin-1-yl]-1-(4-fluoro-phenyl)-butan-1-one;propionate(hcl)
52-86-8
haloperidol
C01814
4'-fluoro-4-(4-(p-chlorophenyl)-4-hydroxypiperidinyl)butyrophenone
gamma-(4-(p-chlorophenyl)-4-hydroxpiperidino)-p-fluorbutyrophenone
4-(4-(para-chlorophenyl)-4-hydroxypiperidino)-4'-fluorobutyrophenone
DB00502
4-[4-(4-chlorophenyl)-4-hydroxy-1-piperidyl]-1-(4-fluorophenyl)-butan-1-one
4'-fluoro-4-(4-hydroxy-4-(4'-chlorophenyl)piperidino)butyrophenone
BSPBIO_002096
OPREA1_509923
NCGC00023875-08
NCGC00023875-05
NCGC00023875-09
NCGC00023875-06
KBIO2_004958
KBIO3_001316
KBIO2_003909
KBIOSS_001341
KBIOGR_002390
KBIO2_002390
KBIO3_002869
KBIOGR_000980
KBIO2_001341
KBIOSS_002395
KBIO2_007526
KBIO2_006477
SPECTRUM4_000570
PRESTWICK0_000115
SPECTRUM2_001268
NINDS_000654
SPBIO_002069
PRESTWICK1_000115
SPECTRUM3_000448
SPBIO_001236
SPECTRUM1500325
BIOMOL-NT_000035
NCGC00015500-02
NCGC00023875-04
NCGC00023875-07
4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-one
CHEBI:5613 ,
haloperidolum
NCGC00015500-06
HMS2091J09
HMS2089M15
H 1512 ,
NCGC00015500-14
AKOS000280660
L000288
haloperidol decanoate impurity, haloperidol-
HMS502A16
FT-0669100
FT-0669101
lnepoxffqsencj-uhfffaoysa-
inchi=1/c21h23clfno2/c22-18-7-5-17(6-8-18)21(26)11-14-24(15-12-21)13-1-2-20(25)16-3-9-19(23)10-4-16/h3-10,26h,1-2,11-15h2
4-[4-(4-chlorophenyl)-4-hydroxypiperidino]-4'-fluorobutyrophenone
H0912
HMS1920D03
HMS1568G12
NCGC00015500-10
HMS2095G12
HMS3261F08
NCGC00254503-01
tox21_300475
VU0239704-10
nsc757054
pharmakon1600-01500325
nsc-757054
tox21_110162
dtxcid2014150
dtxsid4034150 ,
bioperidolo
halopidol
halosten
sigaperidol
pekuces
halidol
HMS2234P08
CCG-36042
CCG-39111
NCGC00015500-15
NCGC00015500-04
NCGC00015500-05
NCGC00015500-03
NCGC00015500-09
NCGC00015500-13
NCGC00015500-08
NCGC00015500-07
NCGC00015500-17
NCGC00015500-16
NCGC00015500-11
NCGC00015500-12
haloperidol [usan:usp:inn:ban:jan]
j6292f8l3d ,
5-21-02-00377 (beilstein handbook reference)
unii-j6292f8l3d
177716-59-5
epoxy resins
LP00583
haloperidol [who-dd]
haloperidol [usan]
haloperidol [ep monograph]
haloperidol [mi]
haloperidol [vandf]
vesalium component haloperidol
neurodol
haloperidol [jan]
haloperidol [hsdb]
haloperidol [who-ip]
haloperidol [usp monograph]
haloperidol decanoate impurity, haloperidol- [usp impurity]
haloperidol [usp-rs]
haloperidol [orange book]
haloperidolum [who-ip latin]
haloperidol [mart.]
haloperidol component of vesalium
haloperidol [inn]
haloperidol [usp impurity]
haloperidol decanoate impurity g [ep impurity]
HMS3370H11
HY-14538
CS-1971
SCHEMBL8264
NCGC00015500-19
tox21_110162_1
ac250
gamma-[4-(p-chlorophenyl)-4-hydroxypiperidino]-p-fluorobutyrophenone
AB00052008-21
AB00052008-22
NCGC00261268-01
tox21_500583
W-105791
mcm-jr-1625
.gamma.-(4-(p-chlorophenyl)-4-hydroxpiperidino)-p-fluorbutyrophenone
sc 170973
STL417208
picroside-iii
4-(4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl)-1-(4-fluorophenyl)butan-1-one
AB00052008_24
AB00052008_23
OPERA_ID_446
mfcd00051423
FT-0697842
haloperidol, united states pharmacopeia (usp) reference standard
haloperidol, european pharmacopoeia (ep) reference standard
HMS3657I13
AT13670
haloperidol for peak identification, european pharmacopoeia (ep) reference standard
haloperidol for system suitability, european pharmacopoeia (ep) reference standard
haloperidol, pharmaceutical secondary standard; certified reference material
haloperidol 1.0 mg/ml in methanol
SR-01000003076-2
SR-01000003076-11
SR-01000003076-8
sr-01000003076
MRF-0000027
SBI-0050565.P004
HMS3712G12
SW196557-4
duraperidol
S1920
haloperidol (haldol)
Q251347
BRD-K67783091-003-03-6
SDCCGSBI-0050565.P005
BCP33202
NCGC00015500-32
A899749
STR04750
NCGC00015500-24
STARBLD0018801
haloperidol for peak identification
haloperidol for system suitability
CHA71659
BH166165
Z1590789254
ps14 - haloperidol
SY052276
haloperidol (usp impurity)
haloperidol (mart.)
haloperidol (usp monograph)
haloperidol (usp-rs)
haloperidol (usan:usp:inn:ban:jan)
4-(4-(4-chlorophenyl)-4-hydroxy-1-piperidyl)-1-(4-fluorophenyl)-butan-1-one
haloperidol (ep monograph)
n05ad01
haloperidolum (inn-latin)
4-(4-hydroxy-4'-chloro-4-phenylpiperidino)-4'-fluorbutyrophenone
haloperidol, 1mg/ml in methanol
diphenylprolinol silyl ether

Research Excerpts

Overview

Haloperidol is a commonly used antipsychotic drug and may increase neuronal oxidative stress associated with the side effects, including tardive dyskinesia and neurite withdraw. It is known to antagonize dopamine D2 receptors, which are abundantly expressed in the striatum. Haloperidl is a rapid and effective treatment for acute, severe, benign headache in ED patients aged 18 to 55 years.

ExcerptReferenceRelevance
"Haloperidol is a commonly used antipsychotic drug and may increase neuronal oxidative stress associated with the side effects, including tardive dyskinesia and neurite withdraw. "( Resveratrol prevents haloperidol-induced mitochondria dysfunction through the induction of autophagy in SH-SY5Y cells.
Boz, Z; Chen, X; Hu, M; Huang, XF; Tang, R; Wang, R; Yu, Y; Zheng, K; Zheng, M; Zheng, P, 2021
)
2.38
"Haloperidol (HPL) is a typical antipsychotic drug used to treat acute psychotic conditions, delirium, and schizophrenia. "( Enhancement of Haloperidol Binding Affinity to Dopamine Receptor via Forming a Charge-Transfer Complex with Picric Acid and 7,7,8,8-Tetracyanoquinodimethane for Improvement of the Antipsychotic Efficacy.
Alamri, A; Alamri, AS; Alhabeeb, AA; Alhomrani, M; Alkhatabi, HA; Alsanie, WF; Alyami, H; Alzahrani, AS; Alzahrani, O; Felimban, RI; Gaber, A; Habeeballah, H; Raafat, BM; Refat, MS; Shakya, S, 2022
)
2.52
"Haloperidol is a widely used antipsychotic agent that exerts antipsychotic effects through a strong antagonism of dopamine D2 receptors. "( Haloperidol Prevents Oxytosis/Ferroptosis by Targeting Lysosomal Ferrous Ions in a Manner Independent of Dopamine D2 and Sigma-1 Receptors.
Furuta, K; Hirata, Y; Hirayama, T; Nagasawa, H; Oh-Hashi, K; Oka, K; Takemori, H; Watanabe, H; Yamamoto, S, 2022
)
3.61
"Haloperidol is a neuroleptic medication that is used to treat a wide range of neuropsychiatric conditions. "( Inhibition of drug induced Parkinsonism by chronic supplementation of quercetin in haloperidol-treated wistars.
Arshad, M; Farhan, M; Rafi, H; Rafiq, H; Rehman, S; Shakeel, S, 2022
)
2.39
"Haloperidol is a typical antipsychotic medication used in the treatment of schizophrenia that is known to antagonize dopamine D2 receptors, which are abundantly expressed in the striatum."( Chronic treatment with D2-antagonist haloperidol leads to inhibitory/excitatory imbalance in striatal D1-neurons.
Anjo, SI; Baltazar, G; Bessa-Neto, D; Coelho, JF; Cotter, D; Dunn, MJ; Manadas, B; Mendes, VM; Monteiro, P; Rodrigues, D; Santa, C, 2023
)
1.9
"haloperidol is a rapid and effective treatment for acute, severe, benign headache in ED patients aged 18 to 55 years."( Treatment of Headache in the Emergency Department: Haloperidol in the Acute Setting (THE-HA Study): A Randomized Clinical Trial.
Aldy, K; Arnall, E; McCoy, JJ; Petersen, J, 2020
)
1.53
"Haloperidol is a typical antipsychotic drug commonly used to treat a broad range of psychiatric disorders related to dysregulations in the neurotransmitter dopamine (DA). "( Haloperidol Interactions with the dop-3 Receptor in Caenorhabditis elegans.
Aschner, M; Fachinetto, R; Ferrer, B; Krum, BN; Martins, AC; Milne, GL; Queirós, L; Soares, FAA, 2021
)
3.51
"Haloperidol is an antipsychotic agent recently described as an antinociceptive drug able to mediate the antagonism of sigma-1 receptors while morphine is an opioid used in the treatment of neuropathic pain. "( Haloperidol potentiates antinociceptive effects of morphine and disrupt opioid tolerance.
Blanco-Hernández, Y; Espinosa-Juárez, JV; López-Muñoz, FJ; Mena-Valdés, LC, 2021
)
3.51
"Haloperidol (HALO) is a weak base with very low aqueous solubility that is used as an antipsychotic drug. "( β-Cyclodextrin-based ternary complexes of haloperidol and organic acids: the effect of organic acids on the drug solubility enhancement.
Chantasart, D; Rakkaew, P; Suksiriworapong, J, 2018
)
2.19
"Haloperidol (HAL) is a compound that shows a high affinity with these receptors, acting as an antagonist."( Haloperidol Decreases Hyperalgesia and Allodynia Induced by Chronic Constriction Injury.
Espinosa-Juárez, JV; Jaramillo-Morales, OA; López-Muñoz, FJ, 2017
)
2.62
"Haloperidol decanoate is a typical antipsychotic drug used as maintenance therapy for schizophrenia and mood disorders formulated as an ester for intramuscular injection. "( An acute oral intoxication with haloperidol decanoate.
Dekkers, BGJ; Eck, RJ; Ter Maaten, JC; Touw, DJ, 2017
)
2.18
"Haloperidol is an antipsychotic agent that primarily acts as an antagonist of D2 dopamine receptors. "( Haloperidol Affects Plasticity of Differentiated NG-108 Cells Through σ1R/IP
Babula, P; Csaderova, L; Hudecova, S; Krizanova, O; Kubickova, J; Lencesova, L; Novakova, M; Rozborilova, E; Stracina, T, 2018
)
3.37
"Haloperidol is an antipsychotic agent and acts as dopamine D2 receptor (D2R) antagonist, as a prototypical ligand of sigma1 receptors (Sig1R) and it increases expression of type 1 IP"( Disruption of dopamine D1/D2 receptor complex is involved in the function of haloperidol in cardiac H9c2 cells.
Babula, P; Chovancova, B; Krizanova, O; Kubickova, J; Lencesova, L; Lopusna, K; Novakova, M; Novakova, Z; Rezuchova, I; Szadvari, I, 2017
)
2.13
"Haloperidol is a first-generation antipsychotic used in the treatment of psychoses, especially schizophrenia. "( Haloperidol-Induced Preclinical Tardive Dyskinesia Model in Rats.
Cavalcanti, DMLP; Cavalcanti, JRLP; da Silva, ANA; da Silva, MSM; de Araújo, DP; de Sales, LGP; Guzen, FP; Pinheiro, FI, 2019
)
3.4
"Haloperidol (Hal) is an antipsychotic related to movement disorders. "( Influence of magnesium supplementation and L-type calcium channel blocker on haloperidol-induced movement disturbances.
Burger, ME; da Silva Barcelos, RC; Kronbauer, M; Metz, VG; Milanesi, LH; Roversi, K; Rubert Rossato, D, 2019
)
2.19
"Haloperidol is a classic antipsychotic drug known for its propensity to cause extrapyramidal side effects. "( Brain and liver oxidative stress after sertraline and haloperidol treatment in mice.
Abdel-Salam, OM; Khadrawy, YA; Sleem, AA; Youness, ER, 2013
)
2.08
"Haloperidol is a benchmark, accessible antipsychotic drug against which the effects of newer treatments are gauged."( Haloperidol dose for the acute phase of schizophrenia.
Adams, CE; Donnelly, L; Rathbone, J, 2013
)
3.28
"Haloperidol is a dopamine D2 receptor antagonist that induces catalepsy when systemically administered to rodents. "( Dopaminergic mechanisms underlying catalepsy, fear and anxiety: do they interact?
Brandão, ML; Colombo, AC; de Oliveira, AR; Reimer, AE, 2013
)
1.83
"Haloperidol (Hal) is a ligand that can target sigma 2 receptors over-expressed in non-small cell lung cancer. "( Feasibility of haloperidol-anchored albumin nanoparticles loaded with doxorubicin as dry powder inhaler for pulmonary delivery.
Hassanzadeh, F; Mardani, A; Rostami, M; Varshosaz, J, 2015
)
2.21
"Haloperidol is an efficacious antipsychotic drug that has serious, unpredictable motor side effects that limit its utility and cause noncompliance in many patients. "( Genetics of adverse reactions to haloperidol in a mouse diallel: a drug-placebo experiment and Bayesian causal analysis.
Adkins, DE; Barrick, CJ; Crowley, JJ; de Villena, FP; Kim, Y; Lenarcic, AB; Miller, DR; Quackenbush, CR; Shaw, GS; Sullivan, PF; Valdar, W, 2014
)
2.13
"Haloperidol is a potent antipsychotic drug but has a high propensity to cause adverse effects. "( Haloperidol versus placebo for schizophrenia.
Adams, CE; Bergman, H; Irving, CB; Lawrie, S, 2013
)
3.28
"Haloperidol (HAL) is a butyrophenone antipsychotic agent which is highly lipophilic."( Evaluation of intravenous lipid emulsion on haloperidol-induced hypotension in rabbits.
Hosseinzadeh, H; Mohammadpour, AH; Moshiri, M; Vahabzadeh, M, 2016
)
1.42
"Haloperidol is a benchmark drug for the pharmacological treatment of schizophrenia, but the genetics of its efficacy is yet to be elucidated."( Genome-wide association study supports the role of the immunological system and of the neurodevelopmental processes in response to haloperidol treatment.
Drago, A; Friedl, M; Giegling, I; Hartmann, AM; Konte, B; Rujescu, D; Schäfer, M; Serretti, A, 2014
)
2.05
"Haloperidol (HLP) is a potent antipsychotic drug that is commonly used for the treatments of schizophrenia and bipolar disorders but has a tendency to cause adverse effects. "( Evaluation of the in vitro cytogenotoxicity profile of antipsychotic drug haloperidol using human peripheral blood lymphocytes.
Gajski, G; Garaj-Vrhovac, V; Gerić, M, 2014
)
2.08
"Haloperidol is an effective antipsychotic drug for treatment of schizophrenia, but prolonged use can lead to debilitating side effects. "( Neurochemical Metabolomics Reveals Disruption to Sphingolipid Metabolism Following Chronic Haloperidol Administration.
Batman, AM; Beardsley, PM; Crowley, JJ; McClay, JL; van den Oord, EJ; Vann, RE; Vunck, SA, 2015
)
2.08
"Haloperidol is a neuroleptic drug used for a medication of various psychoses and deliria. "( Long-Term Haloperidol Treatment Prolongs QT Interval and Increases Expression of Sigma 1 and IP3 Receptors in Guinea Pig Hearts.
Axmanova, M; Konecny, P; Krizanova, O; Masarik, M; Novakova, M; Olejnickova, V; Polanska, H; Slaninova, I; Stracina, T, 2015
)
2.26
"Haloperidol is a representative typical antipsychotic drug and has potent dopamine receptor antagonistic functions; however, atypical antipsychotics have been developed and characterized an important advance in the treatment of schizophrenia and other psychotic disorders."( Investigation into effects of antipsychotics on ectonucleotidase and adenosine deaminase in zebrafish brain.
Bogo, MR; Bonan, CD; Oliveira, Rda L; Seibt, KJ; Senger, MR, 2015
)
1.14
"Haloperidol is an effective antipsychotic agent, but it causes Parkinsonian-like extrapyramidal symptoms in the majority of treated subjects. "( A Pharmacogenetic Discovery: Cystamine Protects Against Haloperidol-Induced Toxicity and Ischemic Brain Injury.
Clark, JD; Dill, DL; Giffard, R; Nishimura, T; Nishimura, Y; Peltz, G; Sahbaie, P; Wu, M; Xiong, X; Xu, D; Xu, LJ; Zhang, H; Zheng, M, 2016
)
2.12
"Haloperidol is a commonly prescribed antipsychotic drug currently administered as oral and injectable preparations. "( Intranasal haloperidol-loaded miniemulsions for brain targeting: Evaluation of locomotor suppression and in-vivo biodistribution.
Amin, MM; El-Setouhy, DA; Elzanfaly, ES; Ibrahim, AB; Khowessah, OM, 2016
)
2.27
"Haloperidol is an antipsychotic drug that inhibits the dopamine D2 receptor among others. "( Haloperidol aggravates transverse aortic constriction-induced heart failure via mitochondrial dysfunction.
Bhuiyan, MS; Fukunaga, K; Hasegawa, H; Kanai, H; Shinoda, Y; Tagashira, H, 2016
)
3.32
"Haloperidol is an antipsychotic. "( Haloperidol Versus Ondansetron for Treatment of Established Nausea and Vomiting Following General Anesthesia: A Randomized Clinical Trial.
Aouad, MT; Barakat, HB; Korjian, S; Siddik-Sayyid, SM; Yazbeck-Karam, VG, 2017
)
3.34
"Haloperidol is a classical antipsychotic drug, which produces extra-pyrimidal Parkinson's symptoms (EPS)."( Antagonism of haloperidol-induced swim impairment in L-dopa and caffeine treated mice: a pre-clinical model to study Parkinson's disease.
Barodia, SK; Luthra, PM; Raghubir, R, 2009
)
1.43
"Haloperidol (HAL) is a widely used neuroleptic drug for the treatment of acute and chronic psychosis. "( Effect of alpha lipoic acid on the tardive dyskinesia and oxidative stress induced by haloperidol in rats.
Himabindhu, G; Thaakur, S, 2009
)
2.02
"Haloperidol is a commonly used, typical, antipsychotic drug (APD) that acts strongly against positive symptoms, but has fewer therapeutic effects on, or may even aggravate, negative symptoms and cognitive deficits in patients with schizophrenia. "( Haloperidol promotes proliferation but inhibits differentiation in rat oligodendrocyte progenitor cell cultures.
Kong, J; Li, N; Li, X; Mei, F; Niu, J; Wang, H; Xiao, L, 2010
)
3.25
"Haloperidol is a potent dopamine receptor antagonist and used to treat psychotic disorders, such as schizophrenia. "( Neonatal ventral hippocampus lesion induces increase in nitric oxide [NO] levels which is attenuated by subchronic haloperidol treatment.
Aguilar-Alonso, P; Baltazar-Gaytán, E; Bringas, ME; Flores, G; León-Chávez, BA; Negrete-Díaz, JV; Newton, S; Vazquez-Roque, RA, 2010
)
2.01
"Haloperidol is an antipsychotic drug associated with the development of movement disorders. "( Haloperidol-loaded polysorbate-coated polymeric nanocapsules increase its efficacy in the antipsychotic treatment in rats.
Barcelos, RC; Beck, RC; Benvegnú, DM; Boufleur, N; Bürger, ME; Ourique, AF; Pase, CS; Reckziegel, P, 2011
)
3.25
"Haloperidol is a butyrophenone derivative commonly used in many hospital units as an antipsychotic agent."( Evidence of Haldol (haloperidol) long-term intoxication.
Gerace, E; Pellegrino, S; Salomone, A; Vincenti, M, 2012
)
1.42
"Haloperidol (HP) is a widely prescribed antipsychotic drug used for the treatment of mental disorders. "( Alpha-phenyl-N-tert-butylnitrone prevents oxidative stress in a haloperidol-induced animal model of tardive dyskinesia: investigating the behavioural and biochemical changes.
Daya, RP; Mishra, RK; Skoblenick, K; Sookram, CD; Tan, ML, 2011
)
2.05
"Haloperidol is a butyrophenone neuroleptic agent characterized as a high-affinity dopamine antagonist, originally used for the treatment of schizophrenia. "( Role of haloperidol in palliative medicine: an update.
Prommer, E, 2012
)
2.26
"Haloperidol is a preferred agent for the treatment of delirium in this population because of its rapid onset of action and lack of hemodynamic effects."( Haloperidol dosing strategies in the treatment of delirium in the critically ill.
Ensom, MH; Loh, GW; Mabasa, VH; Wang, EH, 2012
)
2.54
"Haloperidol is a recognised D2 receptor antagonist, and these findings suggest that music, by contrast, enhances DA activity and turnover in the brain."( Changes caused by haloperidol are blocked by music in Wistar rat.
del Río, MC; García-Mayórgaz, ÁD; Montilla, P; Quero, I; Tasset, I; Túnez, I, 2012
)
1.43
"Haloperidol (HAL) is an antipsychotic drug that has high affinities to the dopamine D(2), but low affinities to D(1) receptors in the brain. "( Chronic haloperidol-induced spatial memory deficits accompany the upregulation of D(1) and D(2) receptors in the caudate putamen of C57BL/6 mouse.
Rose, GM; Xu, H; Yang, HJ, 2012
)
2.26
"Haloperidol is a benchmark, accessible antipsychotic against which the effects of newer treatments are gauged."( Haloperidol dose for the acute phase of schizophrenia.
Adams, CE; Hamill, KM; Marti, J; Roque, M; Waraich, PS, 2002
)
3.2
"Haloperidol is a typical antipsychotic drug with inhibitory effects on dopamine and calcium homeostasis. "( Modulation of the negative inotropic effect of haloperidol by drugs with positive inotropic effects in isolated rabbit heart.
Bolukbaşi-Hatip, F; Hatip-Al-Khatib, I, 2002
)
2.01
"Haloperidol (HAL) is a typical neuroleptic that acts primarily as a D2 dopamine receptor antagonist. "( Haloperidol- and clozapine-induced oxidative stress in the rat brain.
Bromberg, E; Caldana, F; Dal-Pizzol, F; Laranja, DC; Lima, MN; Moreira, JC; Polydoro, M; Quevedo, J; Roesler, R; Schröder, N, 2004
)
3.21
"Haloperidol is a widely used antipsychotic drug, which exerts its effects via antagonizing the dopaminergic D2 receptors. "( Chronic treatment of haloperidol causes vasoconstriction on basilar arteries of rats, dose dependently.
Aydin, MD; Aydin, N; Bakuridze, K; Gepdiremen, A; Halici, Z; S Ahin, O; Unal, B, 2004
)
2.09
"Haloperidol (HAL) is a typical neuroleptic that acts primarily as a D2 dopamine receptor antagonist."( Haloperidol and clozapine, but not olanzapine, induces oxidative stress in rat brain.
Dal-Pizzol, F; Lima, MS; Martins, MR; Moreira, JC; Quevedo, J; Reinke, A, 2004
)
2.49
"Haloperidol is a receptor D2 antagonist frequently used in the treatment of schizophrenic patients. "( Haloperidol treatments increased macrophage activity in male and female rats: influence of corticosterone and prolactin serum levels.
Dorce, VA; Lourenço, GA; Palermo-Neto, J, 2005
)
3.21
"Haloperidol is a representative of typical antipsychotics that are still in clinical use and which can lead to abnormal motor activity following repeated administration. "( Enhanced 5-HT2C receptor signaling is associated with haloperidol-induced "early onset" vacuous chewing in rats: implications for antipsychotic drug therapy.
Bieganski, GJ; Guillen, V; Mignon, L; Wolf, WA, 2005
)
2.02
"Haloperidol is a high potency typical neuroleptic used in the treatment of schizophrenia but produces muscles related side effects commonly known as EPS."( Effects of tryptophan and valine administration on behavioral pharmacology of haloperidol.
Ahmed, SW; Ali, O; Haleem, DJ; Kamil, N; Obaid, R; Saify, ZS, 2005
)
1.28
"Haloperidol is a prototype of typical APDs, and the other three drugs are atypical APDs, which are effective in reducing negative symptoms and cognitive deficits of schizophrenia, cause less side effects, and are more tolerable compared to haloperidol."( Haloperidol and atypical antipsychotics share a same action of decreasing P75(NTR) mRNA levels in PC12 cells.
Bai, O; Li, XM; Xu, H, 2006
)
2.5
"Haloperidol is a classical neuroleptic drug that is still in clinical use and can lead to abnormal motor activity following repeated administration. "( Haloperidol induces calcium ion influx via L-type calcium channels in hippocampal HN33 cells and renders the neurons more susceptible to oxidative stress.
Choi, JH; Kim, EK; Kim, HS; Kim, YS; Ryu, SH; Suh, PG; Yumkham, S, 2006
)
3.22
"Haloperidol is a potent antipsychotic drug but has a high propensity to cause adverse effects. "( Haloperidol versus placebo for schizophrenia.
Adams, CE; Joy, CB; Lawrie, SM, 2006
)
3.22
"Haloperidol (HAL) is a typical antipsychotic drug and known to cause extrapyramidal symptoms (EPS) that may be associated with the blockade of dopamine D2-receptors in nigrostriatal pathway by the drug. "( Quetiapine reverses altered locomotor activity and tyrosine hydroxylase immunoreactivity in rat caudate putamen following long-term haloperidol treatment.
He, J; Jiang, W; Li, X; Li, XM; Xu, H; Yan, B; Zhang, Y, 2007
)
1.99
"Haloperidol is a widely used neuroleptic drug for the treatment of acute and chronic psychosis. "( Effect of spirulina maxima on the haloperidol induced tardive dyskinesia and oxidative stress in rats.
Jyothi, B; Thaakur, SR, 2007
)
2.06
"Haloperidol is a typical antipsychotic with potent dopamine D(2) receptor antagonism."( Haloperidol and clozapine differentially regulate signals upstream of glycogen synthase kinase 3 in the rat frontal cortex.
Ahn, YM; Jeon, WJ; Juhnn, YS; Kang, UG; Kim, SH; Kim, Y; Kim, YS; Roh, MS; Seo, MS, 2007
)
2.5
"Haloperidol is a classical neuroleptic drug that is still in use and can lead to abnormal motor activity such as tardive dyskinesia (TD) following repeated administration. "( Protective effect of L-type calcium channel blockers against haloperidol-induced orofacial dyskinesia: a behavioural, biochemical and neurochemical study.
Bishnoi, M; Chopra, K; Kulkarni, SK, 2008
)
2.03
"Haloperidol (HAL) is a typical neuroleptic that acts primarily as a D(2) dopamine receptor antagonist."( Antipsychotic-induced oxidative stress in rat brain.
Dal-Pizzol, F; Gomes, KM; Martins, MR; Petronilho, FC; Quevedo, J; Streck, EL, 2008
)
1.07
"Haloperidol was observed to be an effective analgesic, alone and in combination with opiates, in a patient with severe radiation fibrosis and necrosis. "( Haloperidol analgesia.
Cohen-Cole, SA; Daw, JL, 1981
)
3.15
"Haloperidol seemed to be an effective and useful agent for motor manifestations of the disease."( [Effectiveness of haloperidol in the treatment of chorea minor].
Ejiri, K; Fuchigami, T; Fujita, Y; Harada, K; Hiyoshi, K; Miyakawa, M; Moriuchi, R; Ohkubo, O, 1995
)
1.35
"Haloperidol is a widely prescribed antipsychotic that acts as a dopamine D2 receptor antagonist. "( The effects of haloperidol on dopamine receptor gene expression.
Fox, CA; Mansour, A; Watson, SJ, 1994
)
2.08
"Haloperidol (HAL) is a potent butyrophenone antipsychotic agent which is reversibly metabolized to reduced haloperidol (RHAL). "( Effect of quinidine on the interconversion kinetics between haloperidol and reduced haloperidol in humans: implications for the involvement of cytochrome P450IID6.
Fossler, MJ; Hawes, EM; Hubbard, JW; Korchinski, ED; McKay, G; Midha, KK; Young, D, 1993
)
1.97
"Haloperidol seemed to be an effective and tolerable agent in controlling the motor manifestations of the disease."( Sydenham's chorea: a new look at an old disease.
al-Eissa, A,
)
0.85
"Haloperidol thus appears to be a partial agonist for the strychnine-insensitive glycine site associated with the NMDA receptor-channel complex."( Haloperidol interacts with the strychnine-insensitive glycine site at the NMDA receptor in cultured mouse hippocampal neurones.
Fletcher, EJ; MacDonald, JF, 1993
)
2.45
"Haloperidol decanoate is a long-acting depot antipsychotic agent used for the treatment of schizophrenic patients. "( A practical loading dose method for converting schizophrenic patients from oral to depot haloperidol therapy.
Chang, WH; Jann, MW; Lin, HN; Piao-Chien, C; Wei, FC, 1996
)
1.96
"Haloperidol (HAL) is a widely used and clinically effective neuroleptic. "( [Erythrocyte ketone reductase activity, total plasma haloperidol and acute psychoses].
Cottencin, O; Dutoit, D; Erb, F; Goudemand, M; Leroux, JM; Pommery, J; Thomas, P; Vaiga, G,
)
1.82
"Haloperidol (HPD) is a dopamine receptor blocker and a major causative agent of neuroleptic malignant syndrome. "( Regulation of NK activity by the administration of bromocriptine in haloperidol-treated mice.
Habu, S; Hozumi, K; Nishimura, T; Nozaki, H, 1996
)
1.97
"Haloperidol is a substrate of CYP3A4 and an inhibitor, as well as a stimulator, of CYP2D6."( Pharmacokinetics of haloperidol: an update.
Ishizaki, T; Kudo, S, 1999
)
1.35
"Haloperidol is a typical neuroleptic giving extrapyramidal side effects (EPS), whereas the atypical compound clozapine does not."( Differential patterns of induction of NGFI-B, Nor1 and c-fos mRNAs in striatal subregions by haloperidol and clozapine.
Brené, S; Olson, L; Ringholm, A; Werme, M, 2000
)
1.25
"1. Haloperidol is a drug used in the management of several psychotic disorders and its use has been linked to Neuroleptic Malignant Syndrome. "( Methyl p-hydroxybenzoate (E-218) a preservative for drugs and food is an activator of the ryanodine receptor Ca(2+) release channel.
Babini, E; Cavagna, D; Prestipino, G; Treves, S; Zorzato, F, 2000
)
0.93
"Haloperidol is a potent antipsychotic drug but with a high propensity to cause adverse effects. "( Haloperidol versus placebo for schizophrenia.
Adams, CE; Joy, CB; Lawrie, SM, 2001
)
3.2
"Haloperidol (H) is a neuroleptic drug that has one known biologically active metabolite, reduced haloperidol (RH). "( Liquid chromatographic determination of reduced haloperidol and haloperidol concentrations in packed red blood cells from humans.
Dysken, MW; Herzan, LA; Vatassery, GT,
)
1.83
"Haloperidol was shown to be a powerful therapeutic agent when administered for 4 weeks and free of side effects; at doses ranging from 0.25 to 4.0 mg/day (M = 0.844), there was a clinically and statistically significant reduction of a variety of symptoms."( The effects of haloperidol on discrimination learning and behavioral symptoms in autistic children.
Adams, P; Anderson, LT; Campbell, M; Perry, R; Shell, J; Small, AM, 1989
)
1.35
"Haloperidol decanoate is a depot preparation of haloperidol, a commonly used butyrophenone derivative with antipsychotic activity. "( Haloperidol decanoate. A preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in psychosis.
Beresford, R; Ward, A, 1987
)
3.16
"Haloperidol is a safe and efficacious drug for use with disruptive patients in the emergency setting."( Haloperidol for sedation of disruptive emergency patients.
Clinton, JE; Ruiz, E; Stelmachers, Z; Sterner, S, 1987
)
2.44

Effects

Haloperidol has a relatively weak effect on aggression when given alone and can also cause side effects such as early dyskinesia and epileptic seizures. It has a broad action in basal ganglia, causing changes in SNR and in the mediodorsal nucleus.

Haloperidol has long been used for the treatment of delirium. Has a relatively weak effect on aggression when given alone. Can also cause side effects such as early dyskinesia and epileptic seizures.

ExcerptReferenceRelevance
"Haloperidol has a relatively weak effect on aggression when given alone and can also cause side effects such as early dyskinesia and epileptic seizures."( The Use of Rapid Tranquilization in Aggressive Behavior.
Hirsch, S; Steinert, T, 2019
)
1.24
"Haloperidol, in contrast, has a broad and potent action in basal ganglia, causing changes in SNR and in the mediodorsal nucleus, while also altering GAD mRNA in RtN, potentially reflective of its dyskinetic and antipsychotic actions."( Traditional and new antipsychotic drugs differentially alter neurotransmission markers in basal ganglia-thalamocortical neural pathways.
Gao, XM; Hashimoto, T; Sakai, K; Tamminga, CA, 2001
)
1.03
"Haloperidol has long been used for the treatment of delirium."( Dexmedetomidine versus haloperidol for sedation of non-intubated patients with hyperactive delirium during the night in a high dependency unit: study protocol for an open-label, parallel-group, randomized controlled trial (DEX-HD trial).
Harada, H; Ikeda, K; Kamei, J; Kato, T; Kitajima, N; Kuriyama, A; Maeda, J; Matsuyama, A; Minami, T; Mizota, T; Ohtsuru, S; Sakai, Y; Sato, Y; Takatani, Y; Ueno, K; Watanabe, H; Yamaji, K; Yamashita, Y, 2023
)
1.94
"Haloperidol has a relatively weak effect on aggression when given alone and can also cause side effects such as early dyskinesia and epileptic seizures."( The Use of Rapid Tranquilization in Aggressive Behavior.
Hirsch, S; Steinert, T, 2019
)
1.24
"Haloperidol (HL) has successfully been used for nausea and abdominal pain in emergency departments (EDs). "( Haloperidol Use in the Emergency Department for Gastrointestinal Symptoms: Nausea, Vomiting, and Abdominal Pain.
Jehangir, A; Malik, Z; Parkman, HP; Repanshek, ZD; Reznick-Lipina, K; Shahsavari, D; Weiner, M, 2021
)
3.51
"Haloperidol (HP) has been shown to have analgesic & antiemetic properties."( Haloperidol undermining gastroparesis symptoms (HUGS) in the emergency department.
Croft, B; Darracq, MA; Ramirez, R; Stalcup, P, 2017
)
2.62
"Haloperidol has been utilized in the palliative care setting for similar symptoms."( Randomized Controlled Double-blind Trial Comparing Haloperidol Combined With Conventional Therapy to Conventional Therapy Alone in Patients With Symptomatic Gastroparesis.
Cardenas-Turanzas, M; Chambers, KA; Chathampally, Y; Paniagua, L; Patel, S; Roldan, CJ, 2017
)
1.43
"Haloperidol has been extensively used in various psychiatric conditions. "( Haloperidol induces pharmacoepigenetic response by modulating miRNA expression, global DNA methylation and expression profiles of methylation maintenance genes and genes involved in neurotransmission in neuronal cells.
Banerjee, M; Swathy, B, 2017
)
3.34
"Haloperidol and ketorolac have been recommended as therapies that may decrease opioid use for treatment of pain in emergency department patients. "( Does administration of haloperidol or ketorolac decrease opioid administration for abdominal pain patients? A retrospective study.
Bebarta, VS; Heard, K; Hoppe, JA; Monte, AA, 2020
)
2.31
"Haloperidol has immunomodulatory effects when used to treat patients with schizophrenia and also is used to sedate critically ill patients in the intensive care unit. "( Haloperidol suppresses murine dendritic cell maturation and priming of the T helper 1-type immune response.
Fujino, Y; Goto, Y; Kashiwa, Y; Matsumoto, A; Ohta, N; Yamamoto, S, 2015
)
3.3
"Haloperidol has been shown to be effective for migraine treatment."( A Randomized Controlled Trial of Intravenous Haloperidol vs. Intravenous Metoclopramide for Acute Migraine Therapy in the Emergency Department.
Bruner, DI; Frumkin, K; Gaffigan, ME; Pritchard, A; Wason, C, 2015
)
1.4
"Haloperidol has the opposite effect - its long-term administration decreases the number of DCX-positive cells."( Effects of neuroleptics administration on adult neurogenesis in the rat hypothalamus.
Pałasz, A; Rojczyk, E; Wiaderkiewicz, R, 2015
)
1.14
"Haloperidol has been included in the World Health Organisation's list of essential medicines."( The consolidation of neuroleptic therapy: Janssen, the discovery of haloperidol and its introduction into clinical practice.
Alamo, C; López-Muñoz, F, 2009
)
1.31
"Haloperidol has long been used to manage agitation in dementia, but it is associated with increased side effects. "( Multifocal myoclonus induced by haloperidol.
Benito-León, J; Bermejo-Pareja, F; Domínguez, C, 2009
)
2.08
"Haloperidol has some efficacy in the treatment of N/V in this patient group. "( The efficacy of haloperidol in the management of nausea and vomiting in patients with cancer.
Douglas, C; Gilshenan, K; Hardy, JR; O'Shea, A; Welch, L; White, C, 2010
)
2.15
"haloperidol has been shown to cause the life-threatening ventricular tachyarrhythmia torsades de pointes."( Influence of i.v. haloperidol on ventricular repolarization and monophasic action potential duration in anesthetized dogs.
Amin, NB; Borzak, S; Mishima, T; Rasty, S; Sabbah, HN; Tisdale, JE, 2004
)
1.38
"Haloperidol has also been reported to interact with calcium homeostasis through dopamine-2 and sigma-1 receptors, and other, yet unknown mechanisms."( Haloperidol attenuates beta-amyloid-induced calcium imbalance in human fibroblasts.
Janka, Z; Kálmán, J; Kemény, L; Kenderessy, AS; Kis, E; Palotás, A; Palotás, M; Penke, B; Vincze, G,
)
2.3
"Haloperidol (HP) has been hypothesized to potentiate increases in oxidative stress or free radical-mediated levels of toxic metabolites in rat striatum while simultaneous upregulating dopamine (DA)-D2 receptors leading to presumed DA supersensitivity."( Electron spin resonance spectroscopy reveals alpha-phenyl-N-tert-butylnitrone spin-traps free radicals in rat striatum and prevents haloperidol-induced vacuous chewing movements in the rat model of human tardive dyskinesia.
Fairfax, DF; Gupta, SK; Henry, P; Khan, RF; Mishra, RK; N-Marandi, S; Rogoza, RM, 2004
)
1.25
"Haloperidol has been used extensively for the treatment of many psychiatric illnesses as well as for control of agitated patients. "( Potentiation of haloperidol neurotoxicity in acute hyperthyroidism: report of a case.
Chu, H; Hsu, YD; Lin, JC, 2004
)
2.11
"Haloperidol has been shown to enhance attentional selectivity in conditioning procedures. "( Haloperidol can increase responding to both discrete and contextual cues in trace conditioned rats.
Cassaday, HJ; Nelson, AJ; Norman, C, 2005
)
3.21
"Haloperidol has been found to be very efficient in controlling agitation with or without pain, nausea and/or vomiting of central origin, intestinal obstruction, and delirium."( Stability of tramadol and haloperidol for continuous subcutaneous infusion at home.
Azuara, ML; Barcia, E; Martín, A; Negro, S; Sánchez, Y, 2005
)
1.35
"Haloperidol has been shown to induce the expression of the transcription factor nuclear factor-kappaB (NFkappaB)."( Role of nigral NFkappaB p50 and p65 subunit expression in haloperidol-induced neurotoxicity and stereotyped behavior in rats.
Aguilar, E; Bonastre, M; Marin, C; Saldaña, M, 2006
)
1.3
"Haloperidol (HP) has been reported to undergo cytochrome P450 (P450)-mediated metabolism to potentially neurotoxic pyridinium metabolites; however, the chemical pathways and specific enzymes involved in these reactions remain to be identified. "( Cytochrome P450-mediated metabolism of haloperidol and reduced haloperidol to pyridinium metabolites.
Avent, KM; DeVoss, JJ; Gillam, EM, 2006
)
2.05
"Haloperidol (HAL) has been hypothesized to increase oxidative stress, while clozapine (CLO) would produce less oxidative damage."( Effects of chronic haloperidol and/or clozapine on oxidative stress parameters in rat brain.
Agostinho, FR; Dal-Pizzol, F; Jornada, LK; Quevedo, J; Roesler, R; Schröder, N, 2007
)
1.39
"Haloperidol has been shown to induce rapid and transient expression of c-fos messenger RNA and Fos protein in striatal neurons via dopamine D2 receptors. "( Haloperidol-induced Fos expression in striatum is dependent upon transcription factor cyclic AMP response element binding protein.
Heckers, S; Konradi, C, 1995
)
3.18
"Haloperidol has recently been found to be metabolized to its pyridinium ion (HP+). "( Comparison of cytotoxicity of a quaternary pyridinium metabolite of haloperidol (HP+) with neurotoxin N-methyl-4-phenylpyridinium (MPP+) towards cultured dopaminergic neuroblastoma cells.
Fang, J; Yu, PH; Zuo, D, 1995
)
1.97
"Haloperidol has become the drug of choice for sedation of the acutely agitated, delirious adult patient in the critical care setting because of its well-documented efficacy and lack of major side effects. "( The use of haloperidol in the agitated, critically ill pediatric patient with burns.
Brown, RL; Greenhalgh, DG; Henke, A; Warden, GD,
)
1.96
"Haloperidol (HAL) has been widely used in the elderly. "( Symptom change and extrapyramidal side effects during acute haloperidol treatment in chronic geriatric schizophrenics.
Pardo, M; Pollack, S; Weisbard, JJ, 1997
)
1.98
"Haloperidol has been found to be metabolized to a pyridinium ion (HP+; 4-(4-chlorophenyl)-1-[4-(4-fluorophenyl)-4-oxobutyl]-pyridinium). "( Effects of a quaternary pyridinium metabolite of haloperidol (HP+) on the viability and catecholamine levels of cultured PC12 cells.
Fang, J; Yu, PH, 1997
)
1.99
"Haloperidol treatment has been shown to produce oxidative stress in patients with acute psychosis. "( Haloperidol-induced extrapyramidal reaction: lack of protective effect by vitamin E.
Eranti, VS; Gangadhar, BN; Janakiramaiah, N, 1998
)
3.19
"Haloperidol has been reported to induce polymorphic ventricular arrhythmias associated with QT prolongation. "( Effect of magnesium sulfate on the haloperidol-induced QT prolongation assessed in the canine in vivo model under the monitoring of monophasic action potential.
Hashimoto, K; Satoh, Y; Sugiyama, A; Tamura, K, 2000
)
2.03
"Haloperidol and clozapine have been widely used to alleviate schizophrenic symptoms, but their physiological effects in the prefrontal cortex (PFC) are not known. "( Haloperidol and clozapine increase neural activity in the rat prefrontal cortex.
Baeg, EH; Chung, Y; Chung, YK; Jang, J; Jung, MW; Kim, HT; Kim, SU; Kim, YB; Mook-Jung, I, 2001
)
3.2
"Haloperidol, in contrast, has a broad and potent action in basal ganglia, causing changes in SNR and in the mediodorsal nucleus, while also altering GAD mRNA in RtN, potentially reflective of its dyskinetic and antipsychotic actions."( Traditional and new antipsychotic drugs differentially alter neurotransmission markers in basal ganglia-thalamocortical neural pathways.
Gao, XM; Hashimoto, T; Sakai, K; Tamminga, CA, 2001
)
1.03
"Haloperidol has been used for decades to control agitation in dementia, but its effectiveness remains unclear."( Haloperidol for agitation in dementia.
Colford, J; Lonergan, E; Luxenberg, J, 2002
)
2.48
"Haloperidol has the shortest onset of action, being effective within 30 minutes of intravenous administration."( Comparison of droperidol, haloperidol and prochlorperazine as postoperative anti-emetics.
Bennett, G; Loeser, EA; Machin, R; Stanley, TH, 1979
)
1.28
"Oral haloperidol has no influence on the dopamine skin reaction, but increases the blanching in areas of antihistamine treatment."( Dopamine effects on the microcirculation and veins of the skin after local application and their changes by antagonistic drugs.
Dreesen, R; Stüttgen, G, 1979
)
0.71
"Haloperidol has proved to be remarkably safe in this high dose regimen."( Higher than usual dosage of haloperidol: a pilot study in 'back ward' schizophrenics.
Declercq, H; Tanghe, A, 1976
)
1.27
"Haloperidol has strong dopamine-blocking effects, and the hypothalamic inhibitory mechanism for PRL release is believed to be dopamine-mediated."( Selective neuroendocrine effects of low-dose haloperidol in normal adult men.
Gouin, PR; O'Connor, D; Poland, RE; Rubin, RT; Tower, BB, 1976
)
1.24
"Haloperidol disposition has been associated with reversible metabolism: it is reversibly reduced to its metabolite, reduced haloperidol, which has less pharmacologic activity than the parent compound. "( Reversible metabolism of haloperidol and reduced haloperidol in Chinese schizophrenic patients.
Chang, WH; Jann, MW; Lam, YW, 1990
)
2.03
"Haloperidol has been used extensively for the treatment of psychotic disorders, and it has been suggested that the monitoring of plasma haloperidol concentration is clinically useful. "( Pharmacokinetics of haloperidol.
Davis, CM; Froemming, JS; Jann, MW; Lam, YW, 1989
)
2.04
"Haloperidol decanoate has no intrinsic activity: its pharmacodynamic actions are those of haloperidol--primarily that of central antidopamine activity."( Haloperidol decanoate. A preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in psychosis.
Beresford, R; Ward, A, 1987
)
2.44

Actions

Haloperidol did not increase DCFDs (adjusted RR 0.98 [95% CI 0.73-1.31], p = 0.87) It did not cause significant EPS after administration and blocked the increase in rearing time, rearings and crossings.

ExcerptReferenceRelevance
"Haloperidol did not increase DCFDs (adjusted RR 0.98 [95% CI 0.73-1.31], p = 0.87)."( Efficacy of haloperidol to decrease the burden of delirium in adult critically ill patients: the EuRIDICE randomized clinical trial.
Boer, DP; Brouwers, AJBW; Devlin, JW; Gommers, DAMPJ; Hunfeld, NGM; Lens, JA; Osse, RJ; Ponssen, HH; Rietdijk, WJR; Schoonderbeek, JF; Simons, KS; Slooter, AJC; Smit, L; Trogrlic, Z; van den Boogaard, M; van der Jagt, M, 2023
)
2.01
"Haloperidol did not increase the sedation level (RR: 1.88, 95% CI: 0.76-4.63) and mortality (RR: 0.97, 95% CI: 0.83-1.18)."( Haloperidol for preventing delirium in ICU patients: a systematic review and meta-analysis.
Buonanno, P; Iacovazzo, C; Kotfis, K; Marra, A; Servillo, G; Vargas, M, 2021
)
2.79
"Haloperidol-induced increase in malondialdehyde and nitrite generation as well as deficits in antioxidant enzymes activities were attenuated by chronic administration of vinpocetine."( Vinpocetine prevents haloperidol-induced cognitive and working memory deficits through attenuation of oxidative and nitrosative stress in mice.
Adeyemi, OO; Isaac, AI; Ishola, IO, 2020
)
1.6
"Haloperidol induced increase in global DNA methylation which was found to be associated with corresponding increase in expression of various epigenetic modifiers that include DNMT1, DNMT3A, DNMT3B and MBD2. "( Haloperidol induces pharmacoepigenetic response by modulating miRNA expression, global DNA methylation and expression profiles of methylation maintenance genes and genes involved in neurotransmission in neuronal cells.
Banerjee, M; Swathy, B, 2017
)
3.34
"Haloperidol did not cause significant EPS after administration."( Secondary nonmotor negative symptoms in healthy volunteers after single doses of haloperidol and risperidone: a double-blind, crossover, placebo-controlled trial.
Arnaiz, JA; Bernardo, M; Fernández de Bobadilla, R; Gassó, P; Lafuente, A; Mas, S, 2013
)
1.34
"Haloperidol blocked the increase in rearing time, rearings and crossings."( Differential effect of clozapine and haloperidol on rats treated with methylphenidate in the open field test.
Campos-Rodriguez, UE; Cano-Cruz, MA; Saldívar-González, JA, 2009
)
1.35
"Haloperidol-induced increase of striatal enkephalin mRNA is totally abolished in NGFI-B KO mice whereas the increase of neurotensin mRNA expression is reduced by 50%."( The transcription factor NGFI-B (Nur77) and retinoids play a critical role in acute neuroleptic-induced extrapyramidal effect and striatal neuropeptide gene expression.
Beaudry, G; Ethier, I; Lévesque, D; Milbrandt, J; Rouillard, C; St-Hilaire, M, 2004
)
1.04
"Only haloperidol was able to increase the number of Fos immunoreactive neurons (FIr) in the dorsal striatum (vehicle: 0.07 +/- 0.07/0.1 mm(2), haloperidol: 28.3 +/- 8.9/0.1 mm(2), p < 0.01)."( Cannabidiol increases Fos expression in the nucleus accumbens but not in the dorsal striatum.
Del Bel, EA; Guimarães, FS; Guimarães, VM; Zuardi, AW, 2004
)
0.78
"haloperidol, produce significant increases in dopamine and acetylcholine release in the medial prefrontal cortex in rats, effects believed to be related to the ability to improve cognitive function."( Aripiprazole, a novel antipsychotic drug, preferentially increases dopamine release in the prefrontal cortex and hippocampus in rat brain.
Dai, J; Ichikawa, J; Li, Z; Meltzer, HY, 2004
)
1.04
"Haloperidol promotes acute dystonia (3 RCTs n=93, RR 4.7 CI 1.7 to 44, NNH 5 CI 3 to 9), akathisia (4 RCTs n=333, RR 2.6 CI 1.4 to 4.8, NNH 7 CI 3 to 25) and parkinsonism (4 RCTs n=163, RR 11.7 CI 2.9 to 47, NNH 3 CI 2 to 5)."( Haloperidol versus placebo for schizophrenia.
Adams, CE; Joy, CB; Lawrie, SM, 2006
)
2.5
"Haloperidol failed to increase PPI in subjects exhibiting low levels of PPI, but attenuated PPI in those subjects with high sensorimotor gating levels."( Haloperidol differentially modulates prepulse inhibition and p50 suppression in healthy humans stratified for low and high gating levels.
Csomor, PA; Feldon, J; Geyer, MA; Stadler, RR; Vollenweider, FX; Yee, BK, 2008
)
2.51
"Haloperidol can inhibit DOI-induced HTR in mice, but fluoxetine can not."( [Roles of fluoxetine and haloperidol in mouse models of DOI-induced head twitch response].
Dai, XM; Lu, Y; Ma, HW; Yao, Y, 2007
)
1.36
"of haloperidol; this increase persists for 8 hr or longer."( Increase of neurotensin content elicited by neuroleptics in nucleus accumbens.
Costa, E; Govoni, S; Hong, JS; Yang, HY, 1980
)
0.78
"Haloperidol prevented the increase of blood flow in the external layer but did not affect the cortical hemodynamic shift or the depressing influence of talinolol on the channel transport of sodium."( [Effect of a blockade of the beta 1-adrenoreceptors on the hemodynamics, oxygen tension and sodium reabsorption in the rat kidney].
Kriukova, RA; Kuz'min, OB, 1984
)
0.99
"The haloperidol-induced increase in the efflux of DOPAC and HVA was markedly attenuated in the 6-OHDA-pretreated rats."( 6-Hydroxydopamine and 5,7-dihydroxytryptamine selectively reduce dopamine and 5-hydroxytryptamine metabolites in cerebroventricular perfusates of rats.
Moore, KE; Nielsen, JA, 1983
)
0.75
"Haloperidol failed to increase prolactin in newborn female rats; at 4 days, a significant increase was evidenced, and from then onwards the response rose markedly with age."( A developmental study of adenohypophyseal dopaminergic receptors and of haloperidol-induced prolactin release in rats.
Becú de Villalobos, D; Cardinali, DP; Libertun, C; Vacas, MI, 1984
)
1.22
"Haloperidol was found to inhibit monoamine oxidase (MAO) activity in sonicated platelets by 50% (IC50) at a concentration of 10(-4) M. "( Haloperidol inhibition of monoamine oxidase in vivo and in vitro.
Giller, E; Hall, H; Reubens, L; Wojciechoswki, J, 1984
)
3.15
"The haloperidol induced increase in apomorphine induced stereotypy and [3H]spiroperidol binding could be antagonized by EB treatment during the withdrawal phase of the haloperidol treatment."( Hypophysectomy induced hypersensitivity to dopamine: antagonism by estrogen.
Diamond, BI; Fields, JZ; Gordon, JH; Perry, KO, 1981
)
0.74
"The haloperidol-induced increase in the concentration of dopamine in pituitary stalk plasma appeared to be PRL mediated, since this effect of haloperidol was significantly attenuated in rats which had been pretreated with antiserum to PRL."( Release of dopamine from tuberoinfundibular neurons into pituitary stalk blood after prolactin or haloperidol administration.
Gudelsky, GA; Porter, JC, 1980
)
0.96
"The haloperidol-induced increase in AP1 binding activity and intracellular Ca2+ was not reproduced by two other dopamine D2 receptor antagonists, sulpiride and (+)-butaclamol."( Induction of c-fos, jun B and egr-1 expression by haloperidol in PC12 cells: involvement of calcium.
Aunis, D; Esteve, L; Haby, C; Humblot, N; Rodeau, JL; Zwiller, J, 1995
)
1.03
"The haloperidol-induced increase in evoked dopamine release from the nucleus accumbens was less than that from the striatum."( Differential effects of dopamine antagonists on evoked dopamine release from slices of striatum and nucleus accumbens in rats.
Takaki, T; Tanaka, M; Yamada, S; Yokoo, H, 1995
)
0.77
"haloperidol) by their lower liability for producing motor side-effects."( Different effects of subchronic clozapine and haloperidol on dye-coupling between neurons in the rat striatal complex.
Grace, AA; O'Donnell, P, 1995
)
1.27
"The haloperidol-induced increase of Fos-like immunoreactive (Fos-li) neurons in the basal ganglia was compared in the C57BL/6J (B6) and DBA/2J (D2) inbred mouse strains. "( Genetics, haloperidol, and the Fos response in the basal ganglia: a comparison of the C57BL/6J and DBA/2J inbred mouse strains.
Hitzemann, B; Hitzemann, R; Patel, N, 1998
)
1.26
"This haloperidol-induced increase in striatal DOPAC was similar after one injection and after 21 days of haloperidol administration."( Chronic verapamil modifies striatal and frontal cortex dopamine levels.
Guarneros, A; Sitges, M, 1998
)
0.76
"The haloperidol-induced increase in DOPAC and HVA was less intense in primiparous rats than that in nulliparous ovariectomized rats."( Reproductive experience reduces striatal dopaminergic responses in freely moving female rats.
Cruz-Casallas, PE; Felicio, LF; Florio, JC; Hucke, EE, 1998
)
0.78
"Haloperidol did not produce a consistent effect on dopamine release in the principal sulcus, although it increased dopamine release in the caudate."( Clozapine preferentially increases dopamine release in the rhesus monkey prefrontal cortex compared with the caudate nucleus.
Bradberry, CW; Goldman-Rakic, PS; Inglis, FM; Jedema, HP; Moghaddam, B; Pivirotto, PJ; Roth, RH; Youngren, KD, 1999
)
1.02
"Haloperidol was found to increase the response time of the rats and had a modest effect on the motor components of the task."( Intra-striatal haloperidol and scopolamine injections: effects on choice reaction time performance in rats.
Blokland, A; Honig, W, 1999
)
1.38
"Haloperidol did not increase NT/NN mRNA expression in the nucleus accumbens until postnatal day 15 and did not increase NT concentrations in this brain region until postnatal day 21."( The effects of acute antipsychotic drug administration on the neurotensin system of the developing rat brain.
Kinkead, B; Nemeroff, CB; Owens, MJ, 2000
)
1.03
"Haloperidol promotes acute dystonia (three trials, n=135, RR 4.7 CI 1.7 to 44, NNH 5 CI 3 to 9 - not assuming those who left early from placebo suffered dystonis), akathisia (three trials, n=129, RR 6.5 CI 1.5 to 28, NNH 6 CI 4 to 14) and parkinsonism (four trials, n=165, RR 8.9 CI 2.6 to 31, NNH 3 CI 2 to 5)."( Haloperidol versus placebo for schizophrenia.
Adams, CE; Joy, CB; Lawrie, SM, 2001
)
2.47
"Haloperidol alone did not lower body temperature, but it potentiated the body temperature lowering effect of NT77L."( Neurotensin analog selective for hypothermia over antinociception and exhibiting atypical neuroleptic-like properties.
Boules, M; Fauq, A; Jackson, J; McCormick, D; McMahon, B; Richelson, E; Stewart, J; Warrington, L, 2001
)
1.03
"Haloperidol induced an increase in the serotonin transporter in the striatum and the core of the nucleus accumbens."( Chronic clozapine, but not haloperidol, treatment affects rat brain vesicular monoamine transporter 2.
Rehavi, M; Roz, N; Weizman, A, 2002
)
1.33
"Haloperidol caused an increase in dopa and no change in 5-HTP formation."( Agonist--antagonist interaction on dopamine receptors in brain, as reflected in the rates of tyrosine and tryptophan hydroxylation.
Carlsson, A; Kehr, W; Lindqvist, M, 1977
)
0.98
"Haloperidol appeared to enhance and atropine to inhibit the degree of tolerance."( Enhanced naloxone potency and the development of narcotic tolerance.
Takemori, AE; Tulunay, FC; Yano, I, 1979
)
0.98
"Haloperidol at the lower dose produced no significant changes but, at the higher dose, yielded relatively large (42%-143%) increases of NT concentrations in accumbens, caudate, and substantia nigra."( Effects of the isomers of N-n-propylnorapomorphine and haloperidol on regional concentrations of neurotensin in rat brain.
Baldessarini, RJ; Bissette, G; Campbell, A; Kilts, CD; Levant, B; Nemeroff, CB, 1991
)
1.25
"Haloperidol prevented the increase in the methamphetamine-induced release of ACh, whereas the increased release of ACh produced by YM-14673 was partially antagonized by haloperidol."( Effects of a new thyrotropin releasing hormone analogue, YM-14673, on the in vivo release of acetylcholine as measured by intracerebral dialysis in rats.
Okada, M, 1991
)
1
"Haloperidol did not produce any significant change."( Amphetamine and alpha-methyl-p-tyrosine affect the exercise-induced imbalance between the availability of tryptophan and synthesis of serotonin in the brain of the rat.
Chaouloff, F; Elghozi, JL; Guezennec, Y; Laude, D; Merino, D; Serrurrier, B, 1987
)
0.99
"The haloperidol-induced increase in dopamine synthesis (measured as the accumulation of DOPA after inhibition of aromatic amino acid decarboxylate) was antagonized by clonidine in the striatum as well as in the dopamine rich limbic regions."( Activation of alpha 2-adrenoreceptors enhances haloperidol-induced suppression of operant behavior.
Engel, JA; Goldstein, M; Johannessen, K; Liljequist, S, 1986
)
1.01
"Haloperidol appeared to produce lower levels of psychopathology than flupenthixol but similar levels of side effects."( Flupenthixol in chronic schizophrenic inpatients: a controlled comparison with haloperidol.
Beninger, RJ; Delva, NJ; Ehmann, TS, 1987
)
1.22
"Haloperidol caused an increase in both antagonist (3H-spiperone) labeled receptors and agonist (3H-N,n-propylnorapomorphine) labeled ones, whereas tiapride acted on the agonist binding sites and sulpiride acted on the antagonist binding sites."( Effect of long-term dosing with tiapride on brain dopamine receptors and metabolism in rats. Comparative study with sulpiride and haloperidol.
Kohjimoto, Y; Kuwaki, T; Nomura, Y; Ono, T; Satoh, H; Shibayama, F; Shirakawa, K, 1987
)
1.2
"Haloperidol induced an increase in unitary discharges parallel to the elevation of the catecholamine level."( Simultaneous monitoring of electrochemical and unitary neuronal activities by a single carbon fiber microelectrode.
Ikeda, M; Matsushita, A; Miyazaki, H, 1985
)
0.99

Treatment

Haloperidol treatment increased binding (+35%) to D2 dopamine receptors in the nucleus accumbens, where RWJ 37796 treatment had a considerably smaller effect (+12) Haloperidl treatment was withdrawn for up to 6 weeks and patients were evaluated for symptom recurrence.

ExcerptReferenceRelevance
"Haloperidol-treated rats were divided into groups of DSS rats and non-DSS rats based on their voluntary locomotion data."( Upregulation of heat-shock protein HSP-70 and glutamate transporter-1/glutamine synthetase in the striatum and hippocampus in haloperidol-induced dopamine-supersensitivity-state rats.
Hashimoto, K; Hirose, Y; Iyo, M; Kanahara, N; Kimura, H; Kimura, M; Niitsu, T; Oda, Y; Shirayama, Y; Yoshino, K, 2021
)
1.55
"Haloperidol treatment reduced the locomotor activity and increased the number of VCM in rats."( Reversal of haloperidol-induced orofacial dyskinesia and neuroinflammation by isoflavones.
Boeck, CR; da Silva Schmitz, I; de Lima, VB; Dorneles, GP; Mezzomo, NF; Peroza, LR; Romao, PRT; Schaffer, LF, 2022
)
1.82
"haloperidol. Changes in treatment performance seem more frequent when SUCRA is employed as outcome measures in the spie charts."( Estimating and visualising the trade-off between benefits and harms on multiple clinical outcomes in network meta-analysis.
Chiocchia, V; Cipriani, A; Furukawa, TA; Leucht, S; Salanti, G; Schneider-Thoma, J; Siafis, S, 2023
)
1.63
"haloperidol in the treatment of severe benign headache in the ED."( Treatment of Headache in the Emergency Department: Haloperidol in the Acute Setting (THE-HA Study): A Randomized Clinical Trial.
Aldy, K; Arnall, E; McCoy, JJ; Petersen, J, 2020
)
1.53
"Haloperidol 1 mg/kg pretreatment prevented ketamine-dependent increases in fast sniffing and instead HFO coupling to slower basal respiration."( Nasal respiration is necessary for ketamine-dependent high frequency network oscillations and behavioral hyperactivity in rats.
Hunt, MJ; Jurkiewicz, G; Średniawa, W; Whittington, MA; Wójcik, DK; Wróbel, J; Żygierewicz, J, 2020
)
1.28
"Haloperidol-treated rats were divided into groups of DSP rats and non-DSP rats based on locomotion data."( Alterations in glutamatergic signaling in the brain of dopamine supersensitivity psychosis and non-supersensitivity psychosis model rats.
Fujita, Y; Hashimoto, K; Iyo, M; Kanahara, N; Nakata, Y; Niitsu, T; Oda, Y; Oishi, K; Shirayama, Y; Takase, M, 2017
)
1.18
"Haloperidol treatment significantly upregulated the levels of serotonin 5-HT"( Deficient striatal adaptation in aminergic and glutamatergic neurotransmission is associated with tardive dyskinesia in non-human primates exposed to antipsychotic drugs.
Blanchet, PJ; Calon, F; Gasparini, F; Gomez-Mancilla, B; Hernandez, G; Lévesque, C; Lévesque, D; Mahmoudi, S, 2017
)
1.18
"Haloperidol treatment significantly suppressed all of these behaviors in wildtype mice but not in DD mice."( Light/dark phase-dependent spontaneous activity is maintained in dopamine-deficient mice.
Fujita, M; Hagino, Y; Ikeda, K; Kasai, S; Kobayashi, K; Takamatsu, Y; Takeda, T; Tanaka, M, 2017
)
1.18
"Five haloperidol-treated animals developed mild TD movements similar to those found in humans."( Haloperidol-induced striatal Nur77 expression in a non-human primate model of tardive dyskinesia.
Blanchet, PJ; Lévesque, D; Mahmoudi, S, 2013
)
2.29
"Haloperidol treatment along with high, but not low, estradiol replacement was effective in reducing amphetamine-induced locomotor activity in sensitized rats."( Estrogen potentiates the behavioral and nucleus accumbens dopamine response to continuous haloperidol treatment in female rats.
Brake, WG; Madularu, D; Shams, WM, 2014
)
1.34
"Five haloperidol-treated animals developed mild TD movements, and no TD was observed in the clozapine group."( Upregulation of dopamine D3, not D2, receptors correlates with tardive dyskinesia in a primate model.
Blanchet, PJ; Lévesque, D; Mahmoudi, S, 2014
)
0.86
"Haloperidol treatment stimulated the expression of ABCA1 (+51%) and other genes involved in reverse cholesterol transport, that is, CYP7A1 (+98%) in livers of LDL receptor knockout mice."( Haloperidol inhibits the development of atherosclerotic lesions in LDL receptor knockout mice.
Hoekstra, M; Nahon, JE; Reuwer, AQ; van der Sluis, RJ; Van Eck, M, 2015
)
2.58
"Haloperidol treatment lowered the susceptibility of hyperlipidaemic LDL receptor knockout mice to develop atherosclerotic lesions. "( Haloperidol inhibits the development of atherosclerotic lesions in LDL receptor knockout mice.
Hoekstra, M; Nahon, JE; Reuwer, AQ; van der Sluis, RJ; Van Eck, M, 2015
)
3.3
"Haloperidol decanoate-treated animals, acting as controls for possible antipsychotic effects, did not have significantly altered neuronal EAAT2b mRNA levels."( Glutamate transporter splice variant expression in an enriched pyramidal cell population in schizophrenia.
Bauer, D; Haroutunian, V; Hasselfeld, K; McCullumsmith, RE; Meador-Woodruff, JH; O'Donovan, SM; Roussos, P; Simmons, M, 2015
)
1.14
"Haloperidol treatment caused the significant decrease in the relative heart rate and the prolongation of QT interval of the isolated hearts from the haloperidol-treated animals, compared to the hearts isolated from control animals."( Long-Term Haloperidol Treatment Prolongs QT Interval and Increases Expression of Sigma 1 and IP3 Receptors in Guinea Pig Hearts.
Axmanova, M; Konecny, P; Krizanova, O; Masarik, M; Novakova, M; Olejnickova, V; Polanska, H; Slaninova, I; Stracina, T, 2015
)
1.54
"Haloperidol treatment (9 µM) was able to decrease ATP hydrolysis (35%), whereas there were no changes in hydrolysis of ADP and AMP in brain membranes after antipsychotic exposure."( Investigation into effects of antipsychotics on ectonucleotidase and adenosine deaminase in zebrafish brain.
Bogo, MR; Bonan, CD; Oliveira, Rda L; Seibt, KJ; Senger, MR, 2015
)
1.14
"Haloperidol-treated rats did not have altered expression of these subunits, suggesting the changes we observed in schizophrenia are likely not due to chronic antipsychotic treatment."( Protein Expression of Proteasome Subunits in Elderly Patients with Schizophrenia.
Haroutunian, V; Meador-Woodruff, JH; Rubio, MD; Scott, MR, 2016
)
1.16
"Haloperidol treatment for 21 days impaired muscle co-ordination, motor activity and grip strength with an increased in orofacial dyskinetic movements."( Beneficial effects of lycopene against haloperidol induced orofacial dyskinesia in rats: Possible neurotransmitters and neuroinflammation modulation.
Datta, S; Deshmukh, R; Jamwal, S; Kumar, P, 2016
)
1.42
"Haloperidol treatment increased the baseline dopamine levels in both non-sensitised and sensitised rats."( Dopamine dynamics during emotional cognitive processing: Implications of the specific actions of clozapine compared with haloperidol.
Inada, K; Ishigooka, J; Kawano, M; Kawano, T; Muraoka, H; Oshibuchi, H; Tsutsumi, T; Yamada, M, 2016
)
1.36
"haloperidol-treated SIR animals."( The α2C-adrenoceptor antagonist, ORM-10921, has antipsychotic-like effects in social isolation reared rats and bolsters the response to haloperidol.
Cockeran, M; Dreyer, W; Harvey, BH; Sallinen, J; Shahid, M; Uys, M, 2016
)
1.36
"Both haloperidol treatment and 6-OHDA injection reduced significantly PSA-NCAM, synaptophysin and GAD67 expression in the mPFC."( Dopamine acting through D2 receptors modulates the expression of PSA-NCAM, a molecule related to neuronal structural plasticity, in the medial prefrontal cortex of adult rats.
Blasco-Ibáñez, JM; Castillo-Gómez, E; Crespo, C; Gómez-Climent, MA; Guirado, R; Martínez-Guijarro, FJ; Nácher, J; Varea, E, 2008
)
0.8
"Haloperidol treatment significantly induced the catalepsy as observed from increased descent time measured in the bar test."( Neuroprotective effect of naphtha[1,2-d]thiazol-2-amine in an animal model of Parkinson's disease.
Alam, MM; Anwer, T; Azam, F; Barodia, SK, 2009
)
1.07
"Haloperidol treatment (0.2 microM) doubled QKI-7 mRNA levels in U343 cells after 6 hours (p-value < 0.02). "( Haloperidol changes mRNA expression of a QKI splice variant in human astrocytoma cells.
Carlström, EL; Jazin, E; Jiang, L; Saetre, P, 2009
)
3.24
"Haloperidol and clozapine treatment disrupted pup approach, pup retrieval, pup licking and nest building."( The receptor mechanisms underlying the disruptive effects of haloperidol and clozapine on rat maternal behavior: a double dissociation between dopamine D(2) and 5-HT(2A/2C) receptors.
Li, M; Zhao, C, 2009
)
1.32
"Haloperidol treatment of rats increased levels of SNAP-25 (mean 24%, P=0.003), syntaxin (mean 18%, P=0.010), and VAMP (mean 16%, P=0.001), whereas clozapine increased only the VAMP level (mean 13%, P=0.004)."( A novel mechanism and treatment target for presynaptic abnormalities in specific striatal regions in schizophrenia.
Barakauskas, VE; Barr, AM; Beasley, CL; Davceva, N; Dwork, AJ; Falkai, P; Honer, WG; Ilievski, B; Jakovski, Z; Li, HY; Mancevski, B; Mann, JJ; Rosokilja, G; Thornton, AE; Wong, H; Ypsilanti, AR, 2010
)
1.08
"Haloperidol treatment significantly reduced female proceptive behaviors in a dose-dependent manner."( Conditioned ejaculatory preference in male rats paired with haloperidol-treated females.
Girard-Bériault, F; Greggain-Mohr, JA; Ismail, N; Laroche, C; Ménard, S; Pfaus, JG, 2010
)
1.32
"With haloperidol treatment both strains of rats showed a significantly greater maximum increase on MAP-induced dopamine release compared with respective control rats."( Effects of dopamine antagonists on methamphetamine-induced dopamine release in high and low alcohol preference rats.
Hishida, S; Kasuda, S; Kinoshita, H; Matsui, K; Minami, T; Nishiguchi, M; Nishio, H; Ouchi, H; Takahashi, M; Yamamura, T, 2010
)
0.82
"Haloperidol treatment affects the expression of IP3 receptors of type 1 and 2 in cardiac atria, but not in cardiac ventricles."( Haloperidol increases expression of the inositol 1,4,5-trisphosphate receptors in rat cardiac atria, but not in ventricles.
Fialova, K; Krizanova, O; Novakova, M; Sedlakova, B; Sirova, M, 2010
)
2.52
"Haloperidol treatment reduced the voluntary activity and energy expenditure of DR mice and induced insulin resistance in these mice."( Pharmacological modulation of dopamine receptor D2-mediated transmission alters the metabolic phenotype of diet induced obese and diet resistant C57Bl6 mice.
de Leeuw van Weenen, JE; Parlevliet, ET; Pijl, H; Romijn, JA; Schröder-van der Elst, JP; van den Berg, SA; Willems van Dijk, K, 2011
)
1.09
"Haloperidol open treatment was efficacious, and relapse was greater on placebo than with haloperidol continuation. "( A 6-month, randomized, double-blind, placebo-controlled pilot discontinuation trial following response to haloperidol treatment of psychosis and agitation in Alzheimer's disease.
Cunqueiro, K; Devanand, DP; Marder, K; Pelton, GH; Sackeim, HA, 2011
)
2.03
"In haloperidol treated rats, MP significantly reversed the reduction in mean corpuscular haemoglobin (MCH) and mean corpuscular haemoglobin concentration (MCHC) values and increased the red blood cell (RBC) count and packed cell volume (PCV)."( Effects of the hydroethanolic extract of Mucuna pruriens (L.) DC (Fabaceae) on haematological profile in normal and haloperidol treated rats.
Akindele, AJ; Busayo, FI,
)
0.85
"Haloperidol and vehicle treated male mice heterozygous (HET) or homozygous (HOM) for the mutation, or wild type (WT), were evaluated for open field locomotion, catalepsy duration, pole test performance and rota-rod latency to fall."( Alteration in RGS2 expression level is associated with changes in haloperidol induced extrapyramidal features in a mutant mouse model.
Broner, EC; Greenbaum, L; Kohn, Y; Lerer, B; Lifschytz, T; Slonimsky, A; Zozulinsky, P, 2012
)
1.34
"Haloperidol treatment during pre- and post-natal period affects maternal behavior and this may have long-term effects on the offspring. "( The effect of haloperidol on maternal behavior in WAG/Rij rats and its consequences in the offspring.
Dobryakova, YV; Dubynin, VA; Luijtelaar, GV, 2011
)
2.17
"Both haloperidol and nicotine treatment decreased the transporter and α6β2* nAChRs (the asterisk indicates the possible presence of other nicotinic subunits in the receptor complex) when given alone, with no further decline with combined drug treatment."( Nicotine reduces antipsychotic-induced orofacial dyskinesia in rats.
Bordia, T; McIntosh, JM; Quik, M, 2012
)
0.83
"Haloperidol treatment of primary astrocytes resulted in coordinated increases in QKI7 and GFAP expression."( RNA-binding protein QKI regulates Glial fibrillary acidic protein expression in human astrocytes.
Emilsson, L; Feuk, L; Halvardson, J; Jazin, E; Lindholm Carlström, E; Radomska, KJ; Reinius, B, 2013
)
1.11
"Haloperidol pretreatment blocked the PPI tolerance produced by repeated apomorphine injections."( Sensorimotor gating effects produced by repeated dopamine agonists in a paradigm favoring environmental conditioning.
Feifel, D; Johnstone-Miller, E; Morgan, CJ; Priebe, K, 2002
)
1.04
"Haloperidol treatment was not associated with significant weight gain."( Weight and blood pressure change during clozapine treatment.
Ball, P; Baymiller, SP; Buchanan, RW; McMahon, RP,
)
0.85
"Haloperidol treatment markedly reduced locomotor activity but its cardiovascular effects were limited to a more rapid return of heart rate towards baseline levels."( Acute effects of antipsychotic drugs on cardiovascular responses to stress.
van den Buuse, M, 2003
)
1.04
"Haloperidol-treated schizophrenia subjects exhibited an additional and consistent pattern of reduced attention (fixation) to salient features for neutral and happy."( Emotion perception in schizophrenia: an eye movement study comparing the effectiveness of risperidone vs. haloperidol.
Gordon, E; Green, MJ; Harris, AW; Loughland, CM; Williams, LM, 2003
)
1.25
"Haloperidol treatment (1.5 mg/kg/day i.p., 21 days) also significantly increased the density of alpha(1)-adrenoceptor binding in the thalamus (73%), but had no effect on alpha(1)-adrenoceptor levels in any other region examined."( Differential region-specific regulation of central alpha 1-adrenoceptor binding following chronic haloperidol and clozapine administration in the rat.
Cahir, M; King, DJ; Mawhinney, T, 2004
)
1.26
"In haloperidol-treated rats on the LSD, both plasma gamma-MSH and NIL gamma-MSH content were greater than in vehicle-treated rats (P<0.05) and did not increase further on the HSD; MAP was also no different."( Suppression of gamma-melanocyte-stimulating hormone secretion is accompanied by salt-sensitive hypertension in the rat.
Almog, S; Humphreys, MH; Mayan, H; Ni, XP, 2003
)
0.83
"Haloperidol treatment slightly attenuated basal NF-kappaB activity."( Different effects of five dopamine receptor subtypes on nuclear factor-kappaB activity in NG108-15 cells and mouse brain.
Fukunaga, K; Takeuchi, Y, 2004
)
1.04
"haloperidol treatment (Simpson-Angus Scale total score mean change: -0.61 olanzapine vs 0.70 haloperidol; P < 0.001; Barnes Akathisia Scale global score mean change: -0.27 olanzapine vs 0.01 haloperidol; P < 0.05)."( Intramuscular olanzapine and intramuscular haloperidol in acute schizophrenia: antipsychotic efficacy and extrapyramidal safety during the first 24 hours of treatment.
Alaka, K; Battaglia, J; Birkett, M; Bitter, I; Breier, A; Chouinard, G; Ferchland-Howe, I; Jones, B; Lindborg, SR; Meehan, K; Morris, PL; Pickard, A; Roth, J; Taylor, CC; Wright, P, 2003
)
1.3
"Haloperidol treatment in mice induced a strong cataleptic state within 1 h of injection, reaching a maximal plateau after 2 h and lasting for 4 h."( Quercetin, a bioflavonoid, reverses haloperidol-induced catalepsy.
Kulkarni, SK; Naidu, PS, 2004
)
1.32
"haloperidol-treated schizophrenic patients discharged from the hospital."( Relapse in patients with schizophrenia: a comparison between risperidone and haloperidol.
de Sena, EP; Miranda-Scippa, A; Oliveira, IR; Quarantini, Lde C; Santos-Jesus, R, 2003
)
1.27
"Haloperidol-treated patients exhibited significantly greater increases in Extrapyramidal Symptom Rating Scale at end of IM treatment and at endpoint (P<0.0001)."( Ziprasidone and haloperidol in the treatment of acute exacerbation of schizophrenia and schizoaffective disorder: comparison of intramuscular and oral formulations in a 6-week, randomized, blinded-assessment study.
Benattia, I; Brook, S; Romano, SJ; Siu, CO; Walden, J, 2005
)
1.4
"Haloperidol-treated patients exhibited significant decreases in gray matter volume, whereas olanzapine-treated patients did not."( Antipsychotic drug effects on brain morphology in first-episode psychosis.
Charles, C; Green, AI; Gu, H; Gur, RE; Hamer, RM; Kahn, RS; Keefe, RS; Lieberman, JA; McEvoy, J; Perkins, D; Sharma, T; Tohen, M; Tollefson, GD; Zipursky, R, 2005
)
1.05
"Haloperidol pretreatment significantly modified haloperidol challenge effect on regional dopamine metabolite contents."( Poor evidence for depolarization block but uncoupling of nigral from striatal dopamine metabolism after chronic haloperidol treatment in the rat.
Chrapusta, SJ; Egan, MF, 2006
)
1.27
"Haloperidol treatment had no significant effect on CB(1) receptor or [(35)S]GTPgammaS binding levels in globus pallidus."( Subchronic haloperidol increases CB(1) receptor binding and G protein coupling in discrete regions of the basal ganglia.
Andersson, M; Fuxe, K; Strömberg, I; Terasmaa, A, 2005
)
1.44
"Haloperidol-treated patients also showed improvements from baseline in episodic memory, vigilance, and visuomotor speed but not in executive functioning or verbal fluency."( Treatment of cognitive impairment in early psychosis: a comparison of risperidone and haloperidol in a large long-term trial.
Davidson, M; Eerdekens, M; Harvey, PD; Rabinowitz, J, 2005
)
1.27
"Haloperidol-treated patients improved only on domains of learning/memory."( One-year double-blind study of the neurocognitive efficacy of olanzapine, risperidone, and haloperidol in schizophrenia.
Breier, A; Gold, JM; Keefe, RS; Purdon, SE; Rock, SL; Young, CA, 2006
)
1.28
"haloperidol in treatment of acute migraine headache in a double-blind, randomized, placebo-controlled study design."( Haloperidol in the acute treatment of migraine: a randomized, double-blind, placebo-controlled study.
Honkaniemi, J; Liimatainen, S; Rainesalo, S; Sulavuori, S, 2006
)
2.5
"Haloperidol posttreatment induced decreases in the accumulation of [125I] o- and m-BON."( In vivo evaluation of radioiodinated 1-[2-(3,4-dimethoxyphenyl)ethyl]-4-(3-phenylpropyl)-piperazine derivatives as new ligands for sigma receptor imaging using single photon emission computed tomography.
Hirata, M; Mori, T; Ohmomo, Y; Soga, S; Umeda, T, 2006
)
1.06
"Haloperidol and clozapine treatment significantly decreased the nigral expression of bax (p<0.05, p<0.01, respectively)."( Differential nigral expression of Bcl-2 protein family in chronically haloperidol and clozapine-treated rats: role in neurotoxicity and stereotyped behavior.
Aguilar, E; Bonastre, M; Marin, C; Saldaña, M, 2007
)
1.29
"In haloperidol treated animals, the tumor uptake of [123I]14d was not significantly different to controls, while significant reduction of [123I]25 uptake was observed, supporting that [123I]14d uptake relates to melanin interaction, whereas part of the mechanism of [123I]25 uptake is related to its sigma 1-receptor affinity."( Synthesis and evaluation of novel radioiodinated benzamides for malignant melanoma.
Ballantyne, P; Berghofer, P; Chapman, J; Dikic, B; Greguric, I; Jackson, T; Katsifis, A; Liu, X; Loc'h, C; Mattner, F; Pham, TQ, 2007
)
0.85
"Haloperidol treatment produced VCM in 40% of the treated rats and the concomitant treatment with V."( Valeriana officinalis does not alter the orofacial dyskinesia induced by haloperidol in rats: role of dopamine transporter.
Avila, DS; Burger, ME; Calixto, JB; Fachinetto, R; Ferreira, J; Pereira, RP; Rocha, JB; Villarinho, JG; Wagner, C, 2007
)
1.29
"Haloperidol treatment also reduces aggregates formation, an effect that is maintained over time."( Haloperidol protects striatal neurons from dysfunction induced by mutated huntingtin in vivo.
Betuing, S; Brouillet, E; Caboche, J; Charvin, D; Déglon, N; Deyts, C; Luthi-Carter, R; Pagès, C; Perrin, V; Régulier, E; Roze, E, 2008
)
2.51
"Haloperidol pretreatment did not reduce any of the behavioral effects of Delta-9-THC."( Effects of haloperidol on the behavioral, subjective, cognitive, motor, and neuroendocrine effects of Delta-9-tetrahydrocannabinol in humans.
Bhakta, S; Blaise, R; Braley, G; Cooper, T; D'Souza, DC; Oliver, S; Perry, E; Pittman, B; Ranganathan, M; Vendetti, M; Zimolo, Z, 2008
)
1.46
"Haloperidol treatment resulted in a decreased number of motor patterns which were not directed by exteroceptive stimuli (non-exteroceptively directed motor patterns)."( Caudate nucleus and programming behaviour in cats: role of dopamine in switching motor patterns.
Cools, AR; Jaspers, R; Schwarz, M; Sontag, KH, 1984
)
0.99
"Haloperidol treatment did not affect the binding affinity of these receptors."( Dopaminergic stimulation of pituitary but not hypothalamic estrogen receptors in ovariectomized rats.
Carrillo, AJ; Chamness, GC; Steger, RW, 1983
)
0.99
"Haloperidol treatment resulted in no changes in the GABA content, a significant decrease in the glutamate content of the striatum and a significant increase in the aspartate content in the frontal cortex."( Effects of subchronic treatment of methamphetamine haloperidol on the rat brain levels of GABA, glutamate and aspartate.
Kaiya, H; Kondo, T; Namba, M; Okada, Y; Sanpei, F; Takeuchi, K; Yoshida, H, 1983
)
1.24
"Haloperidol treatment significantly increased striatal gamma-aminobutyric acid content and glutamic acid decarboxylase activity by 17% and 16% respectively."( Behavioural and biochemical alterations following haloperidol treatment and withdrawal: the animal model of tardive dyskinesia reexamined.
Lapierre, YD; Rastogi, RB; Rastogi, SK; Singhal, RL, 1983
)
1.24
"When haloperidol-treated guinea-pigs received cycloheximide (24 and 12 h before death), there was a substantial decrease in the response indicating that the biosynthesis and release of endorphins are increased by haloperidol."( Haloperidol treatment increases the biosynthesis and release of endorphins in guinea-pig ileum.
Milanés, MV; Puig, MM; Vargas, ML, 1984
)
2.17
"With haloperidol treatment, symptoms decreased in all cases (21 to 88%) and clinical improvement was associated with an increased level of CSF HVA, often returning to the normal range."( Dopaminergic dsyfunction in Tourette syndrome.
Butler, IJ; Coyle, JT; Seifert, WE; Singer, HS; Tune, LE, 1982
)
0.72
"Haloperidol treatment also increases the metabolites in both dark and light while apomorphine decreases both metabolites in dark and light and partially antagonizes the increase induced by haloperidol."( Activation of dopamine-containing amacrine cells of retina: light-induced increase of acidic dopamine metabolites.
Cohen, J; Hadjiconstantinou, M; Neff, NH, 1983
)
0.99
"Haloperidol pretreatment dose-dependently potentiated the analgesic action of morphine and interfered with tissue morphine levels."( Behavioral and pharmacokinetic interaction between morphine and haloperidol in the rat.
Adamus, A; Melzacka, M; Vetulani, J,
)
1.09
"Haloperidol treatment also increased salivation induced by L-noradrenaline as determined by dose-response relationships."( Salivary secretion induced by L-DOPA in haloperidol-treated rats.
Dvorkin, MA; Medina, JH; Pazo, JH; Tumilasci, OR, 1984
)
1.26
"Haloperidol pretreatment prevents stereotyped behaviour induced by 2-amino-7-phosphonoheptanoic acid, but does not change the effect on the electroshock test."( Anticonvulsant action of 2-amino-7-phosphonoheptanoic acid in the substantia nigra.
De Sarro, G; Meldrum, BS; Reavill, C, 1984
)
0.99
"Haloperidol or lithium treatment increased the relative amount of preproenkephalin A synthesized by 67-98% or 25-29%, respectively."( Regulation of methionine-enkephalin precursor messenger RNA in rat striatum by haloperidol and lithium.
Hong, JS; Sabol, SL; Yoshikawa, K, 1983
)
1.21
"Haloperidol treatment resulted in a 52% increase in 3H-dopamine binding in the septum, whereas phenobarbital treatment caused no significant change."( Increased mesolimbic dopamine binding following chronic haloperidol treatment.
Kamer, RS; Kaplan, LJ; Solomon, PR; Turi, AR, 1981
)
1.23
"In haloperidol-treated rats, higher doses of GBL are needed in order to increase the rate of dopa accumulation."( Long-term application of haloperidol: effects on dopamine and acetylcholine receptors.
Kummer, P; Stock, G, 1981
)
1.08
"Haloperidol treatment promoted tumor growth even after ovariectomy and returned tumor PGE2 values to control levels."( Hormone dependence of 7,12-dimethylbenz[a]anthracene-induced mammary tumor growth: correlation with prostaglandin E2 content.
Abou-Issa, H; Foecking, MK; Kibbey, WE; Matthews, RH; Minton, JP, 1982
)
0.99
"Haloperidol pretreatment in one pair of twins abolished the excitation response but did not reduce increases in cortisol and growth hormone."( Behavioral, biochemical and neuroendocrine responses to amphetamine in normal twins and 'well-state' bipolar patients.
Brown, GM; Dibble, ED; Ebert, M; Gershon, ES; Gold, P; Guroff, JJ; Jimerson, DC; Jimerson, SS; Kessler, LR; Nurnberger, JI; Simmons, S; Storch, FI, 1982
)
0.99
"Haloperidol treatment was able to partially block the effects of the ICV administered beta-[Tyr9]melanotropin-(9-18) on both the extinction and open-field activity."( The interaction between beta-[Tyr9]melanotropin-(9-18), haloperidol and amphetamine in different behavior tests of rats.
Coy, DH; Schally, AV; Telegdy, G; Vécsei, L, 1982
)
1.23
"Haloperidol pretreatment on either day prevented these increases after L-DOPA."( Brain catecholamine concentration during the first week of development in rats.
Korányi, L; Phelps, CP; Tamásy, V, 1982
)
0.99
"haloperidol-treated rats (1, 2.5, 5, 10 mg/kg i.p.) display exaggeraged bracing reactions to passive displacement as well as to stimuli which do not actively challenge stable equilibrium."( Morphine versus haloperidol catalepsy in the rat: a behavioral analysis of postural support mechanisms.
De Ryck, M; Schallert, T; Teitelbaum, P, 1980
)
1.33
"Only haloperidol pretreatment was observed to significantly alter the rats' ability to discriminate apomorphine."( Lack of effect of choline and narcotic antagonists upon apomorphine discrimination.
Schechter, MD, 1980
)
0.72
"Like haloperidol-pretreated rats they were able to maintain uncomfortable postures on the vertical grid or horizontal bar; although signs of rigidity were noticed, the rats would fail to remain self-supporting when placed across metal bookends ("bridge" test)."( Pharmacologic analysis of the postictal immobility syndrome in the rat.
Kofman, O; Mintz, M; Myslobodsky, MS, 1981
)
0.72
"Haloperidol treatment had no effect on the poor performance following hippocampal damage, but it impaired that of sham-controls on both measures."( Impairments of search behaviour in rats after haloperidol treatment, hippocampal or neocortical damage suggest a mesocorticolimbic role in cognition.
Oades, RD, 1981
)
1.24
"Haloperidol treatment (2 hours) accelerated striatal DA turnover similarly in all age groups, by about 100%."( Aging and haloperidol-induced dopamine turnover in the nigro-striatal pathway of C57BL/6J mice.
Finch, CE; Osterburg, HH; Severson, JA, 1981
)
1.39
"Haloperidol treatment led to a stimulatory effect in striatum, medial and lateral preoptic nuclei, and interpeduncular nucleus."( beta-Endorphin and met-enkephalins: their distribution, modulation by estrogens and haloperidol, and role in neuroendocrine control.
Barden, N; Cusan, L; Dupont, A; Labrie, F; Mérand, Y; Vaudry, H, 1980
)
1.21
"Haloperidol treatment significantly increased dyskinetic movements and striatal dopamine D2 receptor density compared with controls."( Suppression of oro-facial movements by rolipram, a cAMP phosphodiesterase inhibitor, in rats chronically treated with haloperidol.
Fukui, S; Hashimoto, K; Inada, T; Iyo, M; Sasaki, H, 1995
)
1.22
"Haloperidol treatment also increased binding (+35%) to D2 dopamine receptors in the nucleus accumbens, where RWJ 37796 treatment had a considerably smaller effect (+12)."( The effect of chronic treatment with a novel aryl-piperazine antipsychotic on monoamine receptors in rat brain.
Offord, SJ; Ordway, GA; Shapiro, LA, 1995
)
1.01
"Haloperidol treatment was withdrawn for up to 6 weeks and patients were evaluated for symptom recurrence."( Increases in CSF levels of interleukin-2 in schizophrenia: effects of recurrence of psychosis and medication status.
Gurklis, J; Kelley, ME; McAllister, CG; Miller, AL; Peters, JL; Rehn, TJ; van Kammen, DP; Yao, J, 1995
)
1.01
"The haloperidol-treated group showed a significant increase in the predrug bolus counts from week 5, suggesting a conditioned response to the cage environment."( Effect of prolonged treatment with haloperidol on "emotional" defecation and movement in rats in a well-habituated environment.
Loneragan, C; Sachdev, P; Westbrook, F, 1994
)
1.05
"Both haloperidol and clozapine treatment reduced the weight gain of the rats."( Differential Fos-protein induction in rat forebrain regions after acute and long-term haloperidol and clozapine treatment.
Koch, T; Korf, J; Sebens, JB; Ter Horst, GJ, 1995
)
0.97
"This haloperidol treatment also induced a significantly increase in the frequency of involuntary chewing movements and tongue protrusions, which are considered as a model of tardive dyskinesia."( Rolipram, a selective c-AMP phosphodiesterase inhibitor suppresses oro-facial dyskinetic movements in rats.
Fukui, S; Hashimoto, K; Inada, T; Iyo, M; Kitao, Y; Maeda, Y; Sasaki, H, 1995
)
0.75
"Haloperidol-treated animals exhibited late onset increases in small amplitude oral movements and an increase in the percentage of oral movements in the 1-2 Hz range, accompanied by a decrease in oral movements in the higher frequency range (> 6 Hz) as determined by fast fourier analysis."( Chronic haloperidol, but not clozapine, produces altered oral movements and increased extracellular glutamate in rats.
Chapman, MA; See, RE, 1994
)
1.44
"Haloperidol-treated rats showed an increase of DA, DOPAC, and HVA overflow in the PFC and the NAC-C."( Dopamine increase in the prefrontal cortex correlates with reversal of haloperidol-induced catalepsy in rats.
Baptista, T; Fernandez, R; Hernandez, L; Murzi, E; Tucci, S, 1994
)
1.24
"The haloperidol pretreatment attenuated the extracellular increase in glutamate produced by METH and blocked subsequent neurotoxicity to DA neurons."( Methamphetamine-induced neurotoxicity: roles for glutamate and dopamine efflux.
Stephans, SE; Yamamoto, BK, 1994
)
0.77
"Haloperidol treatment did not affect basal phosphoinositide turnover in the three brain regions."( Effect of chronic haloperidol treatment on dopamine-induced inositol phosphate formation in rat brain slices.
Chuang, DM; Kirch, DG; Li, R; Wyatt, RJ, 1994
)
1.34
"Haloperidol treatment produced a 77% increase in apomorphine-induced sterotypy."( Dopamine D1 receptor stimulation but not dopamine D2 receptor stimulation attenuates haloperidol-induced behavioral supersensitivity and receptor up-regulation.
Chase, TN; Marin, C, 1993
)
1.23
"The haloperidol-treated rats in the high-dose condition had significantly more bolus counts in the 2 hours after the injection than were observed in the groups treated with domperidone (a peripheral dopamine D2 receptor antagonist) or placebo."( Neuroleptic-induced defecation in rats as a model for neuroleptic dysphoria.
Loneragan, C; Sachdev, P; Westbrook, F, 1993
)
0.77
"The haloperidol-treated group consisted of two women and 15 men, three inpatients and 14 outpatients, and seven patients with a comorbid chronic tic disorder."( Haloperidol addition in fluvoxamine-refractory obsessive-compulsive disorder. A double-blind, placebo-controlled study in patients with and without tics.
Goodman, WK; Heninger, GR; Leckman, JF; Lee, NC; McDougle, CJ; Price, LH, 1994
)
2.21
"Haloperidol treatment was found to increase the number of binding sites of D2 dopamine receptors in striatum, olfactory tubercle, hypothalamus and anterior pituitary, while Bmax of D2 receptors in hippocampus was decreased by haloperidol treatment."( Effects of long-term treatment of haloperidol on D2 dopamine receptors in various areas of rat brain.
Ichinowatari, N; Mamiya, G; Ohtakeno, S; Watanabe, H; Watanabe, M, 1993
)
1.29
"haloperidol in the treatment of agitated psychiatric patients in need of rapid tranquilization."( A double-blind randomized clinical trial of rapid tranquilization with I.M. clonazepam and I.M. haloperidol in agitated psychotic patients with manic symptoms.
Annable, L; Chouinard, G; Holobow, N; Szkrumelak, N; Turnier, L, 1993
)
1.23
"Haloperidol-treated rats showed more response strategies based on visual or auditory cues, and less spatial response strategies than control rats."( Haloperidol affects stimulus-dependent strategies and not reward-dependent strategies.
Coenders, CJ; Kerbusch, SM; Vossen, JM, 1993
)
2.45
"Haloperidol treatment significantly reduced plasma Mg but not plasma Ca or P levels."( Effects of haloperidol on human plasma magnesium.
Durst, R; Gardner, EL; Jabotinsky-Rubin, K; Lerner, J; Levitin, LA; Moscovich, DG; Silver, H; Van Praag, H,
)
1.24
"Haloperidol treatment disrupted the sustained attention task performance by decreasing the number of behavior-initiated stimulus presentations, decreasing the number of reinforcers earned, increasing the proportion of errors of omission and increasing reaction time to the target stimulus."( Effects of chronic haloperidol on reaction time and errors in a sustained attention task: partial reversal by anticholinergics and by amphetamine.
Brockel, BJ; Fowler, SC, 1995
)
1.34
"Haloperidol treatment (1 mg/kg/day for 21 days) increased apomorphine-induced stereotypies but did not modify striatal c-fos levels."( Striatal c-fos levels do not correlate with haloperidol-induced behavioral supersensitivity.
Bonastre, M; Marin, C; Tolosa, E, 1996
)
1.28
"4. Haloperidol treatment decreased NGF levels in mouse hypothalamus and this effect did not differ at the two time points tested."( Haloperidol treatment decreases nerve growth factor levels in the hypothalamus of adult mice.
Alleva, E; Aloe, L; Cirulli, F; Della Seta, D, 1996
)
2.25
"Haloperidol pretreatment, but not amphetamine or MK-801, increased calmodulin in striatal but not limbic forebrain membranes."( Haloperidol and MK-801 block increases in striatal calmodulin resulting from repeated amphetamine treatment.
Gnegy, ME; Hewlett, GH; Pimputkar, G, 1996
)
2.46
"In haloperidol-treated rats hypersensitivity of the dopaminergic system developed at the end of 2 weeks' administration, as evidenced by depression of dopamine metabolism."( Different effects of chronic administration of haloperidol and pimozide on dopamine metabolism in the rat brain.
Antkiewicz-Michaluk, L; Karolewicz, B; Michaluk, J; Vetulani, J, 1996
)
1.06
"Haloperidol animals pretreated with L-NAME i.p."( Nitric oxide synthesis inhibition attenuates haloperidol-induced supersensitivity.
Bozarth, MA; Pudiak, CM, 1997
)
1.28
"Haloperidol treatment for 21 days resulted in an increase in angiotensin II AT1 receptor levels in the nucleus accumbens, accompanied by an increase in dopamine D2 receptors, but no change in dopamine D1 receptors."( Upregulation of angiotensin II AT1 receptors in the mouse nucleus accumbens by chronic haloperidol treatment.
Chai, SY; Jenkins, TA; Mendelsohn, FA, 1997
)
1.24
"All haloperidol-treated rats developed oral dyskinesias at a significantly higher rate than rats treated with water (p = 0.0007) or those treated with clozapine (p = 0.0017)."( The dose-response characteristics of rat oral dyskinesias with chronic haloperidol or clozapine administration.
Cooper, TB; Gao, XM; Hashimoto, T; Tamminga, CA, 1997
)
1.01
"Haloperidol-associated treatment-limiting adverse events were experienced by 41% of the patients."( Relative efficacy of haloperidol and pimozide in children and adolescents with Tourette's disorder.
Jackson, C; Nesbitt, L; Sallee, FR; Sethuraman, G; Sine, L, 1997
)
1.34
"Haloperidol-treated rats had higher bolus counts than vehicle-treated rats, and this increase was significantly reversed by the lipophilic but not the hydrophilic beta-antagonists."( The effects of beta-adrenoceptor antagonists on a rat model of neuroleptic-induced akathisia.
Sachdev, PS; Saharov, T, 1997
)
1.02
"A haloperidol-treated patient with chronic schizophrenia had a near-arrhythmic circadian rest-activity cycle, whereas rhythms of 6-sulphatoxy-melatonin and core body temperature were of normal amplitude and phase-advanced. "( A schizophrenic patient with an arrhythmic circadian rest-activity cycle.
Cajochen, C; Nussbaum, P; Wirz-Justice, A, 1997
)
1.02
"In haloperidol-treated rats, tyrosine hydroxylase-positive cell counts were normal in ventral tegmental area but were decreased in substantia nigra by 34% at two weeks withdrawal and by 52% at four weeks withdrawal; cell counts were almost fully recovered by 12 weeks withdrawal."( Haloperidol induces persistent down-regulation of tyrosine hydroxylase immunoreactivity in substantia nigra but not ventral tegmental area in the rat.
Garside, S; Levinson, AJ; Mazurek, MF; Rosebush, PI, 1998
)
2.26
"Haloperidol treatment increased the [3H]spiperone-binding by 28%, the levels of D2L and D2S receptor mRNA by 41% and 38%, respectively, and the level of prolactin mRNA by 26%."( Differential effects on D2 dopamine receptor and prolactin gene expression by haloperidol and aripiprazole in the rat pituitary.
Hide, I; Hirose, T; Inoue, A; Kikuchi, T; Koga, N; Nakata, Y; Seto, M; Sugita, S, 1998
)
1.25
"Haloperidol-treated rats displayed a significant emergence of NMDA stimulated oral activity (nondirected oral movements, oral tremor, audible teeth grinding, and directed oral movements)."( Emergence of oral and locomotor activity in chronic haloperidol-treated rats following cortical N-methyl-D-aspartate stimulation.
Grimm, JW; Kruzich, PJ; See, RE, 1998
)
1.27
"Haloperidol pretreatment was unable to alter this pattern of behavior (i.e., rats still ran quickly when presented with the scent that predicted food availability)."( Haloperidol does not affect motivational processes in an operant runway model of food-seeking behavior.
Ettenberg, A; McFarland, K, 1998
)
2.46
"Haloperidol-treated animals show potentiated LI, and it has been suggested that this is due to retarded switching to respond according to the stimulus-reinforcer contingency."( Haloperidol-induced potentiation of latent inhibition: interaction with parameters of conditioning.
Feldon, J; Ruob, C; Weiner, I, 1998
)
2.46
"Haloperidol treatment has been shown to produce oxidative stress in patients with acute psychosis. "( Haloperidol-induced extrapyramidal reaction: lack of protective effect by vitamin E.
Eranti, VS; Gangadhar, BN; Janakiramaiah, N, 1998
)
3.19
"Haloperidol-treated first-episode patients experienced statistically significantly more extrapyramidal symptoms than haloperidol-treated multiple-episode patients."( Olanzapine versus haloperidol treatment in first-episode psychosis.
Beasley, C; Grundy, S; Lieberman, JA; Sanger, TM; Tohen, M; Tollefson, GD, 1999
)
1.36
"Haloperidol treatment did not alter glutamate concentrations."( Cerebrospinal fluid glutamate inversely correlates with positive symptom severity in unmedicated male schizophrenic/schizoaffective patients.
Bardgett, M; Csernansky, JG; Faull, KF; Faustman, WO; Pfefferbaum, A, 1999
)
1.02
"Haloperidol-treated patients showed dose-dependently (Pearson r = 0.64; P < 0.05) a significantly higher (P < 0.05) mean occupancy rate of 84% (range 67-94)."( In vivo 123I IBZM SPECT imaging of striatal dopamine-2 receptor occupancy in schizophrenic patients treated with olanzapine in comparison to clozapine and haloperidol.
Asenbaum, S; Barnas, C; Brücke, T; Fischer, P; Kasper, S; Küfferle, B; Pezawas, L; Tauscher, J; Tauscher-Wisniewski, S, 1999
)
1.22
"Haloperidol treatment for 34 weeks increased the optical density of preproenkephalin messenger RNA in individual striatal neurons and enkephalin peptide in the neuropil, regardless of the level of oral dyskinesia produced."( The relationship between oral dyskinesias produced by long-term haloperidol treatment, the density of striatal preproenkephalin messenger RNA and enkephalin peptide, and the number of striatal neurons expressing preproenkephalin messenger RNA in rats.
Andreassen, OA; Finsen, B; Jørgensen, HA; Ostergaard, K; Sørensen, JC; West, MJ, 1999
)
1.26
"Haloperidol pretreatment dramatically potentiated the dopamine-releasing effect of amphetamine administration."( Comparison of effects of haloperidol administration on amphetamine-stimulated dopamine release in the rat medial prefrontal cortex and dorsal striatum.
Pehek, EA, 1999
)
1.33
"Haloperidol treatment generated a 248% increase in SMP O2- production rate when measured in the presence of NADH plus rotenone."( Nitric oxide, superoxide, and hydrogen peroxide production in brain mitochondria after haloperidol treatment.
Arnaiz, SL; Boveris, A; Coronel, MF, 1999
)
1.25
"Haloperidol treatment seemed to alleviate inflammation in rheumatoid arthritis. "( Old drug, new tricks: haloperidol inhibits secretion of proinflammatory cytokines.
Al-Saffar, Z; Bacon, PA; Golding, SP; Hutchinson, D; McLaughlin, PJ; Moots, RJ; Young, SP, 1999
)
2.06
"Haloperidol pretreatment reduced impairments in executive cognitive functions produced by ketamine as measured by proverb interpretations and the Wisconsin Card Sorting Test."( Interactive effects of subanesthetic ketamine and haloperidol in healthy humans.
Abi-Dargham, A; Abi-Saab, D; Bennett, A; Bowers, MB; Cassello, K; Charney, DS; D'Souza, DC; Heninger, GR; Karper, LP; Krystal, JH; Vegso, S, 1999
)
1.28
"In haloperidol-pretreated rats, quinpirole induced intense head-down sniffing, rearing, grooming and object-directed oral activity."( Differential behavioural effect of quinpirole in neuroleptic-pretreated rats - role of alpha(1)-adrenoceptor.
Obuchowicz, E, 1999
)
0.82
"The haloperidol treatment produced an area specific increase in Galpha(i)3 mRNA in the frontal cortex and a decrease of Galpha(i)3 in the striatum."( Haloperidol treatment selectively affects expression of Galpha(i)3 subunit mRNA in specific regions of the rat brain.
Kowalska, M; Kreiner, G; Nalepa, I; Sanak, M; Vetulani, J,
)
2.05
"Haloperidol treatment is likewise shown to increase (897)Ser-NR1 phosphorylation in rats in vivo."( Intracellular modulation of NMDA receptor function by antipsychotic drugs.
Barczak, A; Carlson, RR; Coyle, JT; Heckers, S; Huganir, RL; Kang, S; Konradi, C; Leveque, JC; Li, XM; Macías, W; Rajadhyaksha, A, 2000
)
1.03
"Haloperidol treatment produced a significant reduction in mu-receptor binding in the globus pallidus (P<0.05). "( Decreased mu-opioid receptor binding in the globus pallidus of rats treated with chronic haloperidol.
Baca, SM; Bower, CM; Egan, MF; Hamid, EH; Hyde, TM; Zaka, M, 2000
)
1.97
"Haloperidol-pretreated animals showed markedly impaired active avoidance, deficits which were improved by 2.5 and 5 mg/kg but not by 10 mg/kg clozapine pretreatment."( Low-dose clozapine pretreatment partially prevents haloperidol-induced deficits in conditioned active avoidance.
Feldon, J; Murphy, CA, 2000
)
1.28
"Haloperidol is the treatment of choice, but sometimes psychotic episodes were so intense that anticonvulsants had to be withdrawn, as this occurred in one of the reported cases."( [Forced normalization].
Domzał, TM,
)
0.85
"Haloperidol pretreatment inhibited the smoking-induced increase in absolute beta frequency."( Effects of haloperidol pretreatment on the smoking-induced EEG/mood activation response profile.
Ilivitsky, V; Knott, VJ; Mahoney, C; Walker, D, 2001
)
1.42
"The haloperidol-treated group had significantly lower CSF-uncorrected and CSF-corrected left frontal NAA than the normal controls, with the clozapine group having intermediate concentrations."( Effects of chronic haloperidol and clozapine treatments on frontal and caudate neurochemistry in schizophrenia.
Blanchard, J; Brooks, WM; Bustillo, JR; Hart, BL; Jung, RE; Keith, SJ; Lauriello, J; Petropoulos, H; Rowland, LM, 2001
)
1.12
"Haloperidol-treated patients showed a worsening on Simpson-Angus scale while there was no significant change in this measure in risperidone-treated patients."( A double-blind randomised comparison of risperidone and haloperidol in the treatment of behavioural and psychological symptoms in Chinese dementia patients.
Chan, WC; Chiu, HF; Choy, CN; Lam, LC; Leung, VP; Li, SW, 2001
)
1.28
"Haloperidol-treated animals displayed a supersensitive response to dexamphetamine."( The demonstration of a change in adrenergic receptor sensitivity in the central nervous system of mice after withdrawal from long-term treatment with haloperidol.
Dunstan, R; Jackson, DM, 1976
)
1.18
"In haloperidol-treated animals the levels of homovanillic acid were significantly elevated in animals receiving tyrosine."( Brain tyrosine level controls striatal dopamine synthesis in haloperidol-treated rats.
Scally, MC; Ulus, I; Wurtman, RJ, 1977
)
1.01
"Haloperidol-treated animals administered saline or acid-vehicle were, in five of six experiments, more active than animals withdrawn from vehicle-treatment."( Long-term haloperidol-treatment of mice: a change in beta-adrenergic receptor responsiveness.
Dunstan, R; Jackson, DM, 1979
)
1.38
"Haloperidol pretreatment reduced this response in three patients and eliminated the euphoriant and activating response in the remaining seven patients."( Haloperidol and lithium blocking of the mood response to intravenous methylphenidate.
Belmaker, RH; Ebstein, RP; Wald, D, 1978
)
2.42
"2. Haloperidol treated mice (premedicated with reserpine plus alpha-methyl-p-tyrosine) displayed an increased locomotor response to apomorphine and to apomorphine plus clonidine, but neither haloperidol- or vehicle-treated animals revealed any stimulant response to clonidine."( The effect of apomorphine and clonidine on locomotor activity in mice after long term treatment with haloperidol.
Dunstan, R; Jackson, DM,
)
0.86
"Haloperidol treatment for stuttering was examined in a double-blind cross-over study of 26 adult volunteers with long-standing stuttering. "( Haloperiodl in the treatment of stuttering.
Campbell, L; Kelly, P; Murray, TJ; Stefanik, K, 1977
)
1.7
"The haloperidol treatment enhanced the apomorphine-induced reduction of the striatal HVA content at the withdrawal stage in the 24-day-old and 34-day-old rat."( Developmental change in striatal concentration of homovanillic acid and 3,4-dihydroxyphenylacetic acid in response to apomorphine and haloperidol treatment.
Komori, T; Nomura, Y; Okuda, S; Segawa, T, 1979
)
0.94
"In haloperidol-pretreated rats the pattern of elimination of apomorphine from the striatum changed, revealing the presence of two compartments; this was not observed in the limbic forebrain, from which the elimination was linear, both in the presence and absence of haloperidol."( Haloperidol-induced changes in the regional cerebral pharmacokinetics of apomorphine.
Daniel, W; Melzacka, M; Vetulani, J; Wiszniowska, G,
)
2.09
"Haloperidol-treated animals administered methylhyoscine (1 mg/kg i.p.) and various doses of physostigmine (5 to 1215 microgram/kg) displayed significantly less depression of locomotor activity than vehicle-treated animals."( The demonstration of a change in responsiveness of mice to physostigmine and atropine after withdrawal from long-term haloperidol pretreatment.
Dunstan, R; Jackson, DM, 1977
)
1.19
"Haloperidol pre-treatment blocked the effects of apomorphine on PRL, TSH, and GH secretion."( Differential effects of dopamine agonists and haloperidol on release of prolactin, thyroid stimulating hormone, growth hormone and luteinizing hormone in rats.
Meites, J; Moore, KE; Mueller, GP; Simpkins, J, 1976
)
1.24
"Haloperidol-treated rats developed statistically significant behavioral hypersensitivity relative to vehicle-treated controls (p < 0.01)."( Synaptic plasticity in the rat striatum following chronic haloperidol treatment.
Carvey, PM; Kao, LC; Kerns, JM; Klawans, HL; Sierens, DK, 1992
)
1.25
"In haloperidol-treated rats, unlike naive animals, activation of neostriatal D2 dopamine receptors induced a potent presynaptic inhibition of glutamate-mediated excitatory synaptic potentials."( Chronic neuroleptic treatment: D2 dopamine receptor supersensitivity and striatal glutamatergic transmission.
Bernardi, G; Calabresi, P; De Murtas, M; Mercuri, NB, 1992
)
0.8
"In haloperidol-treated epileptic rats, LCMRglc decreased to levels comparable to those measured in untreated control rats."( Mapping of cerebral energy metabolism in rats with genetic generalized nonconvulsive epilepsy.
Boyet, S; Marescaux, C; Nehlig, A; Vergnes, M, 1992
)
0.8
"Haloperidol treatment increased the level of labeling in the entopeduncular nucleus and clozapine treatment increased labeling in the globus pallidus suggesting that these drugs exert different regulatory effects on pallidal neurons."( Clozapine and haloperidol have differential effects on glutamic acid decarboxylase mRNA in the pallidal nuclei of the rat.
Chesselet, MF; Mercugliano, M; Salama, AI; Saller, CF; U'Prichard, DC, 1992
)
1.37
"Haloperidol (HAL) treatment failed to block the stimulant-induced increase in kindling acquisition indicating that changes in dopamine (DA) are not necessary for the AMPH/kindling synergism to develop."( Amphetamine sensitization and amygdala kindling: pharmacological evaluation of catecholaminergic and cholinergic mechanisms.
Kirkby, RD; Kokkinidis, L, 1991
)
1
"Haloperidol treatment (1 mg/kg) produced significant increases in the concentrations of NT in the nucleus accumbens and caudate nucleus but not in the other brain regions studied."( Effects of CI-943, a potential antipsychotic drug, and haloperidol on regional brain neurotensin concentrations.
Bissette, G; Davis, MD; Heffner, TG; Levant, B; Nemeroff, CB, 1991
)
1.25
"Haloperidol treatment did not modify the number of medium-sized enkephalinergic neurons expressing the D2 receptor mRNA."( Striatal neurons express increased level of dopamine D2 receptor mRNA in response to haloperidol treatment: a quantitative in situ hybridization study.
Bernard, V; Bloch, B; Le Moine, C, 1991
)
1.23
"Haloperidol-treated patients reported significantly more drowsiness and increased sleep during treatment (p = 0.026 and 0.012, respectively)."( A double blind comparative multicentre study of remoxipride and haloperidol in schizophrenia.
Andersen, J; Birket-Smith, M; Fensbo, C; Fogh, M; Hansen, NR; Kristensen, M; Kørner, A; Møller-Nielsen, EM; Ostergaard, P; Thiesen, S, 1990
)
1.24
"Haloperidol treated patients reported more tiredness and drowsiness than remoxipride treated patients."( A double-blind multicentre study comparing remoxipride, two and three times daily, with haloperidol in schizophrenia.
Beckmann, H; Bunse, J; Dittmann, V; Klieser, E; König, P; Laux, G; Schöny, HW; Schröder, HG; Schubert, H; Unterweger, B, 1990
)
1.22
"Haloperidol-treated patients reported greater increases in sleep and salivation than remoxipride-treated patients."( A double-blind comparative study of remoxipride and haloperidol in schizophrenic and schizophreniform disorders.
Cosyns, P; de Bleeker, E; Deleu, G; Lotstra, F; Masson, A; Mendlewicz, J; Mertens, C; Parent, M; Peuskens, J; Suy, E, 1990
)
1.25
"Haloperidol-treated patients reported also significantly more concentration difficulties."( Remoxipride and haloperidol in schizophrenia: a double-blind multicentre study.
Ahlfors, UG; Appelberg, B; Hagert, U; Harma, P; Katila, H; Mahlanen, A; Mehtonen, OP; Naukkarinen, H; Outakoski, J; Rimön, R, 1990
)
1.35
"Haloperidol treatment for 3 or 7 days decreased K(+)-stimulated DA release by maximally 35%, but a 14-day treatment was not effective."( Decrease in the evoked release of endogenous dopamine and dihydroxyphenylacetic acid from rat striatal slices after withdrawal from repeated haloperidol.
Sumi, T; Umeda, Y, 1990
)
1.2
"This haloperidol treatment was subthreshold for inducing either dopamine autoreceptor supersensitivity or postsynaptic supersensitivity as evidenced by equivalent metabolic reductions in chronically treated neuroleptic versus vehicle groups, and an absence of stereotypical responding in either condition."( Behavioral evidence for dopamine receptor subsensitivity following chronic haloperidol.
Lynch, MR,
)
0.82
"Haloperidol treatment (14 or 21 days) provoked an increase in mRNA content for D2 receptor and preproenkephalin A in the striatum."( Dopamine receptor gene expression by enkephalin neurons in rat forebrain.
Bloch, B; Fouque, B; Guitteny, AF; Le Moine, C; Normand, E; Teoule, R, 1990
)
1
"Haloperidol pretreatment did not antagonize the MK-801-induced stimulation of locomotion."( The NMDA antagonist MK-801 causes marked locomotor stimulation in monoamine-depleted mice.
Carlsson, A; Carlsson, M, 1989
)
1
"Haloperidol treatment (2 mg/kg/day, i.p., 3 weeks), which has been reported to increase enkephalin levels in the striatum, induced a 23% decrease in striatal (posterior level A= +8.4-8.6 mm) NEP labeling (but no change of mu- and delta-sites)."( Effects of repeated treatment with haloperidol on rat striatal neutral endopeptidase, and on mu- and delta-opioid binding sites: comparison with chronic morphine and chronic kelatorphan.
Delay-Goyet, P; Roques, BP; Zajac, JM, 1989
)
1.28
"Haloperidol treatment did not affect the concentration of somatostatin-like immunoreactivity in the two brain areas."( Long-term haloperidol treatment decreases somatostatin binding in rat brain.
Arilla, E; Colas, B; Lopez-Ruiz, MP; Perez-Oso, E, 1989
)
1.4
"Haloperidol treatment for seven days produced a 25 to 125% increase in [3H]-spiroperidol binding to striatal DA receptors in a dose-dependent fashion."( Striatal dopamine receptor supersensitivity after long-term haloperidol treatment of hypophysectomized rats.
Camillo, MA; DeLucia, R; Scavone, C, 1989
)
1.24
"Haloperidol pretreatment failed to significantly modify the mydriasis produced by phenylephrine or atropine."( Mechanism of haloperidol-induced miosis.
Chauhan, BS; Jain, IP; Lal, BB; Rastogi, CK; Srivastava, YP; Tripathi, CD, 1989
)
1.37
"Haloperidol pretreatment attenuated cocaine-induced increases in systolic and diastolic blood pressure but not heart rate."( Effects of intravenous cocaine are partially attenuated by haloperidol.
Jaffe, JH; Kumor, KM; Sherer, MA, 1989
)
1.24
"In haloperidol-pretreated rats, ascorbate significantly lowered sniffing and forepaw shuffling throughout the amphetamine response."( Ascorbate antagonizes the behavioral effects of amphetamine by a central mechanism.
Basse-Tomusk, A; Block, M; Carpenter, M; Gardiner, TW; Rebec, GV; White, LK, 1988
)
0.79
"Haloperidol treatment masked withdrawal-exacerbated tardive dyskinesia more than molindone did; this difference (measured by percent change in AIMS scores) was significant (p = .04) when the dose was 200% but not 100% of the prestudy neuroleptic dose."( Molindone and haloperidol in tardive dyskinesia.
Benarroche, CL; Glazer, WM; Hafez, HM, 1985
)
1.35
"Haloperidol pretreatment accelerated this decay, confirming the increase in brain dopamine turnover induced by neuroleptics."( Study of dopamine turnover by monitoring the decline of dopamine metabolites in rat CSF after alpha-methyl-p-tyrosine.
Laude, D; Mignot, E, 1985
)
0.99
"Haloperidol treatment, on the other hand, had no significant effect on dopamine and a biphasic effect on adrenaline content."( Adrenal catecholamine concentration after chronic treatment with bromocriptine and haloperidol.
Baksi, SN; Hughes, MJ; Strahlendorf, HK, 1986
)
1.22
"Haloperidol treatment significantly increased the specific activity of the secretory vesicle-associated acetyltransferase without affecting the specific activity of the enzymes present in the endoplasmic reticulum or cytosol."( Coordinate regulation of peptide acetyltransferase activity and proopiomelanocortin gene expression in the intermediate lobe of the rat pituitary.
Chappell, MC; Millington, WR; Mueller, GP; O'Donohue, TL; Roberts, JL, 1986
)
0.99
"In haloperidol-pretreated animals subjected to VE (n = 7), plasma ANF was 81 +/- 8 pg ml-1 during VE, significantly higher than in the control animals."( Atrial natriuretic factor, urinary catechol compounds and electrolyte excretion in rats during normal hydration and isotonic volume expansion. Influence of dopamine receptor blockade.
Ande'n, NE; Grabowska-Ande'n, M; Hansell, P; Ulfendahl, HR, 1988
)
0.79
"Haloperidol pretreatment resulted in an increase in the density of striatal D-2 dopamine receptors, but did not alter the density of cerebral cortical 3H-imipramine binding sites or beta-adrenergic receptors."( Chronic antidepressant treatment and mouse brain 3H-imipramine binding.
Anderson, B; Severson, JA, 1986
)
0.99
"Haloperidol treatment did not block heroin reward."( The dopamine hypothesis of opiate reward challenged.
Ramsey, N; Van Ree, JM, 1987
)
0.99
"Haloperidol pretreatment blocked place preferences induced by AMP but not by MPD."( The effects of haloperidol on amphetamine- and methylphenidate-induced conditioned place preferences and locomotor activity.
Fibiger, HC; Martin-Iverson, MT; Mithani, S; Phillips, AG, 1986
)
1.35
"Haloperidol treatment decreased chorea but did not affect gait patterns."( The gait abnormality of Huntington's disease.
Koller, WC; Trimble, J, 1985
)
0.99
"Haloperidol pretreatment marginally increased the effect of CBZ against PTZ induced seizures, but not against electrically induced seizures (MES and MET tests)."( Influence of dopaminergic receptor supersensitivity on anticonvulsant action of carbamazepine.
David, J; Joseph, T; Kadlimatti, SH; Nadig, RS; Somaja, L,
)
0.85
"Haloperidol treatment dramatically increased the number of dark melanotropes and the amount of POMC mRNA in each cell and eliminated the cellular heterogeneity in both staining properties and the distribution of POMC mRNA."( Dopaminergic regulation of the biosynthetic activity of individual melanotropes in the rat pituitary intermediate lobe: a morphometric analysis by light and electron microscopy and in situ hybridization.
Chronwall, BM; Hook, GR; Millington, WR, 1988
)
1
"With haloperidol pretreatment the uptake was lower, probably mainly showing the remaining unspecific binding."( Dopamine receptors in pituitary adenomas: PET visualization with 11C-N-methylspiperone.
Antoni, G; Bergström, K; Bergström, M; Hartvig, P; Långström, B; Lundberg, PO; Lundqvist, H; Muhr, C,
)
0.59
"The haloperidol decanoate-treated rats showed lower levels of DOPAC and/or HVA than the rats of the other two groups."( [Effect of haloperidol decanoate on the dopaminergic system in the rat brain].
Fujiwara, Y; Harada, T; Kashihara, K; Ogawa, T; Otsuki, S; Sato, M, 1986
)
1.14
"Haloperidol-treated rats show brisk righting, bracing, and clinging reflexes, effects suggesting that motor subsystems subserving static postural support are dominant over those involved in more phasic locomotor and orienting movements."( Forelimb placing and hopping reflexes in haloperidol- and morphine-treated cataleptic rats.
Wolgin, DL, 1985
)
1.26
"Haloperidol treatment increased enkephalins, the precursor, and PE-mRNA content in the striatum, suggesting that this drug might increase enkephalin steady state by increasing transcription, translation, or both processes."( Use of mRNA hybridization and radioimmunoassay to study mechanisms of drug-induced accumulation of enkephalins in rat brain structures.
Costa, E; Mocchetti, I; Schwartz, JP, 1985
)
0.99
"In haloperidol-treated rats, bracing, i.e., resistance to displacement along a horizontal surface, was found to involve four components: gripping by the digits, extension by the limbs, stiffening of the body axis and arching the vertebral column towards the displacing force. "( Fractionation of the cataleptic bracing response in rats.
Chen, YC; Pellis, SM; Teitelbaum, P, 1985
)
0.89
"The treatment of haloperidol-treated rats with quercetin was successful in reversing the haloperidol alterations."( Inhibition of drug induced Parkinsonism by chronic supplementation of quercetin in haloperidol-treated wistars.
Arshad, M; Farhan, M; Rafi, H; Rafiq, H; Rehman, S; Shakeel, S, 2022
)
1.27
"Treatment with haloperidol should be carefully considered, especially in older patients and patients at risk of CVD or pneumonia, since the risk of death appears to be lower with non-haloperidol agents."( Mortality Risk Associated with Haloperidol Use Compared with Other Antipsychotics: An 11-Year Population-Based Propensity-Score-Matched Cohort Study.
Besag, FMC; Blais, JE; Chan, EW; Chang, WC; Chen, EYH; Lao, KSJ; Lee, EHM; Wong, AYS; Wong, ICK, 2020
)
1.18
"Mice treated with haloperidol develop many of the features of TD, including jaw tremors, tongue protrusions, and vacuous chewing movements (VCMs)."( Antipsychotic Behavioral Phenotypes in the Mouse Collaborative Cross Recombinant Inbred Inter-Crosses (RIX).
Crowley, JJ; DeCristo, DM; Giusti-Rodríguez, P; Manuel de Villena, FP; Miller, DR; Nonneman, RJ; Quackenbush, CR; Ryan, A; Shaw, GD; Sullivan, PF; Xenakis, JG; Zhabotynsky, V; Zou, F, 2020
)
0.88
"Pretreatment with haloperidol inhalation inhibited the MK-801-induced or memantine-induced increase in locomotor activity."( Effects of haloperidol inhalation on MK-801- and memantine-induced locomotion in mice.
Ishihara, T; Kitamura, N; Matsumoto, Y; Murakami, S; Okamoto, M; Suemitsu, S; Takahashi, Y; Ueno, H; Wani, K, 2020
)
1.27
"Treatment haloperidol administered later in the ICU course was less protective of death."( Association Between Incident Delirium Treatment With Haloperidol and Mortality in Critically Ill Adults.
Briesacher, BA; Devlin, JW; Duprey, MS; Griffith, JL; Pickkers, P; Saczynski, JS; van den Boogaard, M; van der Hoeven, JG, 2021
)
1.25
"Treatment with haloperidol according to a dose-titration protocol MEASUREMENTS AND MAIN RESULTS:: Thirteen children (median age [range] 8.3 yr [0.4-13.8 yr]) received haloperidol, predominantly IV (median dose [range] 0.027 mg/kg/d [0.005-0.085 mg/kg/d]). "( Monitoring Haloperidol Plasma Concentration and Associated Adverse Events in Critically Ill Children With Delirium: First Results of a Clinical Protocol Aimed to Monitor Efficacy and Safety.
de Wildt, SN; Ista, E; Jessurun, N; Slooff, VD; Tibboel, D; van Beusekom, BS; van den Dungen, DK, 2018
)
1.22
"Treatment with haloperidol alone reduced the locomotor activity in the open-field test that was prevented by co-treatment with gabapentin."( Gabapentin reduces haloperidol-induced vacuous chewing movements in mice.
Ceretta, APC; de Freitas, CM; de Moraes Reis, E; Dotto, MM; Fachinetto, R; Machado-de-Ávila, RA; Reinheimer, JB; Schaffer, LF; Scussel, R, 2018
)
1.15
"Mice treated with haloperidol showed an increase in microglial activation and inflammatory mediators in the striatum."( Cannabidiol prevents haloperidol-induced vacuos chewing movements and inflammatory changes in mice via PPARγ receptors.
Cunha, TM; Del Bel, EA; Guimarães, FS; Prado, DS; Raisman-Vozari, R; Sepulveda-Diaz, JE; Sonego, AB; Tirapelli, CR; Vale, GT, 2018
)
1.12
"Pretreatment with haloperidol also reduced the facilitatory effect of apomorphine more effectively in RLA than RHA rats."( Dopamine is involved in the different patterns of copulatory behaviour of Roman high and low avoidance rats: studies with apomorphine and haloperidol.
Argiolas, A; Corda, MG; Giorgi, O; Melis, MR; Piludu, MA; Sanna, F, 2014
)
0.93
"Pretreatment of haloperidol significantly reduced the radiotracer accumulation of [(99m)Tc]23 or [(99m)Tc]24 in the brain."( Novel cyclopentadienyl tricarbonyl (99m)tc complexes containing 1-piperonylpiperazine moiety: potential imaging probes for sigma-1 receptors.
Brust, P; Cui, M; Deuther-Conrad, W; Jia, B; Jia, H; Li, D; Liu, B; Lu, J; Steinbach, J; Wang, X; Xie, Y, 2014
)
0.74
"Treatment with haloperidol has been shown, in studies using death certificates and prescription files, to be associated with an excess of sudden cardiac deaths, and regulatory warnings highlight this risk in patients with dementia. "( Haloperidol and sudden cardiac death in dementia: autopsy findings in psychiatric inpatients.
Correll, CU; Grudnikoff, E; Ifteni, P; Kane, JM; Koppel, J; Kremen, N; Manu, P, 2015
)
2.21
"Rats treated with haloperidol decanoate (HAL; 21mg/kg every 3weeks, IM) for 12weeks were concurrently treated with LA (10 or 20mg/kg, PO)."( Lipoic acid and haloperidol-induced vacuous chewing movements: Implications for prophylactic antioxidant use in tardive dyskinesia.
Andreazza, AC; Fletcher, PJ; Lister, J; Navaid, B; Nesarajah, Y; Nobrega, JN; Remington, G; Teo, C; Wilson, AA; Wilson, VS, 2017
)
1.12
"Rats treated with haloperidol orally at a dose of for a period of 5 weeks developed VCMs, which increased progressively as the treatment continued for 5 weeks."( Report: Protective effects of rice bran oil in haloperidol-induced tardive dyskinesia and serotonergic responses in rats.
Haleem, DJ; Haleem, MA; Samad, N, 2016
)
1.01
"Treatment with haloperidol or LY379268 normalized novelty-induced locomotor hyperactivity in GLAST KO."( Loss of glial glutamate and aspartate transporter (excitatory amino acid transporter 1) causes locomotor hyperactivity and exaggerated responses to psychotomimetics: rescue by haloperidol and metabotropic glutamate 2/3 agonist.
Heilig, M; Holmes, A; Karlsson, RM; Tanaka, K, 2008
)
0.88
"treated with haloperidol (1.0 mg/kg) or ziprasidone (4.0 mg/kg) for 15 days."( Haloperidol (but not ziprasidone) withdrawal potentiates sensitization to the hyperlocomotor effect of cocaine in mice.
Alvarez, Jdo N; Carvalho, Rde C; Frussa-Filho, R; Fukushiro, DF; Ribeiro, LT; Ricardo, VP, 2008
)
2.14
"The treatment with haloperidol more often results in movement disorders, sleepiness, inhibition, sexual dysfunction and cholinolytic effects."( [Peculiarities of neuroleptic syndrome in women treated with typical and atypical neuroleptics].
Chitaia, NN; Danilov, DS; Tiuvina, NA, 2009
)
0.67
"Treatment with haloperidol reduced the inhibitory effect of SRIF on adenylyl cyclase (AC) activity."( Effects of the antipsychotic drug haloperidol on the somastostatinergic system in SH-SY5Y neuroblastoma cells.
Arilla-Ferreiro, E; Busto, R; Cano, S; Dávalos, A; de la Peña, G; Hernández-Pinto, AM; Lasunción, MA; Puebla-Jiménez, L; Sánchez-Wandelmer, J, 2009
)
0.97
"Pretreatment with haloperidol (0.2 mg/kg, i.p.) alone also decreased locomotion, increased cataleptic activity and immobility time in the tail suspension test."( Central nervous system effects of the essential oil of the leaves of Alpinia zerumbet in mice.
de Araújo, FY; de Moraes, MO; de Oliveira, GV; de Sousa, FC; Leal, LK; Macêdo, DS; Moura, BA; Silva, MI; Vasconcelos, SM; Viana, GS, 2009
)
0.68
"Pretreatment with haloperidol, spiperone, pimozide, aripiprazole and risperidone markedly inhibited high potassium-evoked dopamine release."( Haloperidol, spiperone, pimozide and aripiprazole reduce intracellular dopamine content in PC12 cells and rat mesencephalic cultures: Implication of inhibition of vesicular transport.
Akaike, A; Izumi, Y; Kume, T; Matsuo, T; Sawada, H; Takada-Takatori, Y; Wakita, S, 2010
)
2.13
"Treatment with haloperidol did not affect bone density."( The atypical anti-psychotic clozapine decreases bone mass in rats in vivo.
Callon, K; Cheng, A; Cornish, J; Costa, JL; Gamble, G; Grey, A; Lin, JM; Shepherd, PR; Smith, G; Vickers, MH; Watson, M, 2011
)
0.71
"Rats treated with haloperidol at doses of 0.5-5.0 mg/kg exhibited impaired motor coordination and a decrease in exploratory activity in an open field."( Reversal of haloperidol-induced motor deficits by mianserin and mesulergine in rats.
Haleem, DJ; Shireen, E, 2011
)
1.07
"Pretreatment with haloperidol (0.2-1.0 mg/kg i.p.) prevented the development of morphine tolerance and dependence in a dose-dependent manner."( Haloperidol disrupts opioid-antinociceptive tolerance and physical dependence.
Chen, Y; Tang, L; Wang, ZJ; Yang, C, 2011
)
2.14
"Treatment with haloperidol resulted in more side effects."( Aripiprazole and haloperidol in the treatment of delirium.
Boettger, S; Breitbart, W; Friedlander, M; Passik, S, 2011
)
1.05
"Rats treated with haloperidol or haloperidol plus NGB 2904 or nafadotride developed catalepsy sensitization with repeated conditioning."( Reduced expression of haloperidol conditioned catalepsy in rats by the dopamine D3 receptor antagonists nafadotride and NGB 2904.
Banasikowski, TJ; Beninger, RJ, 2012
)
1.02
"Treatment with haloperidol should be avoided in extremely slow and extremely rapid metabolizers of CYP2D6 substrates. "( The impact of the CYP2D6 polymorphism on haloperidol pharmacokinetics and on the outcome of haloperidol treatment.
Brockmöller, J; Kirchheiner, J; Müller-Oerlinghausen, B; Roots, I; Sachse, C; Schmider, J; Walter, S, 2002
)
0.93
"Treatment with haloperidol resulted in an acute elevation of cortical APP both in therapeutic and toxic doses, however, it had no significant chronic impact on APP."( Effect of haloperidol and risperidone on amyloid precursor protein levels in vivo.
Hugyecz, M; Janka, Z; Kálmán, J; Molnár, J; Pákáski, M; Palotás, A; Palotás, M; Penke, B, 2003
)
1.06
"Pretreatment with haloperidol blocked the [(18)F]FE-SA5845 binding to give PET-images with low and uniform uptake in the brain."( Evaluation of [18F]fluorinated sigma receptor ligands in the conscious monkey brain.
Elsinga, PH; Harada, N; Ishiwata, K; Kakiuchi, T; Kawamura, K; Kimura, Y; Kobayashi, T; Tsukada, H; Vaalburg, W, 2004
)
0.65
"Treatment with haloperidol also led the reduction of phosphorylation levels of Akt, and activated caspase-3."( Neurotoxic potential of haloperidol in comparison with risperidone: implication of Akt-mediated signal changes by haloperidol.
Hashimoto, E; Ozawa, H; Saito, T; Tateno, M; Ukai, W, 2004
)
0.97
"Pretreatment with haloperidol or risperidone abolished the effects of acute d-amphetamine on NT-LI and NPY-LI."( Effects of acute and subchronic d-amphetamine on ventral striatal concentrations of neurotensin and neuropeptide Y in rats treated with antipsychotic drugs.
Gruber, SH; Mathé, AA; Nomikos, GG, 2006
)
0.66
"Rats treated with haloperidol at a dose of 1 mg/kg exhibited impaired motor coordination and a decrease in exploratory activity."( Reversal of haloperidol-induced extrapyramidal symptoms by buspirone: a time-related study.
Haleem, DJ; Haleem, MA; Samad, N, 2007
)
1.04
"treated with haloperidol (1.0 mg/kg) and/or ziprasidone (4.0 mg/kg) for 15 days."( Haloperidol (but not ziprasidone) withdrawal enhances cocaine-induced locomotor activation and conditioned place preference in mice.
Alvarez, Jdo N; Chinen, CC; de Castro, JP; Frussa-Filho, R; Fukushiro, DF; Tatsu, JA, 2007
)
2.14
"Pre-treatment with haloperidol plus 8.0 mg/kg of CPA and 25 and 50 mg/kg of LH reverted the treatment effect."( Involvement of the histaminergic system on appetitive learning and its interaction with haloperidol in goldfish.
Mattioli, R; Medalha, CC, 2007
)
0.88
"Treatment with haloperidol could significantly increase the PI than the treatment with risperidone (p<0.01) throughout the treatment course."( Effects of haloperidol and risperidone on cerebrohemodynamics in drug-naive schizophrenic patients.
Chou, YH; Lee, SM; Li, MH; Wan, FJ; Yen, MH, 2008
)
1.08
"Rats treated with haloperidol at a dose of 1 mg/kg twice a day for 2 weeks displayed VCMs with twitching of facial musculature that increased in a time dependent manner as the treatment continued to 5 weeks."( Reversal of haloperidol-induced tardive vacuous chewing movements and supersensitive somatodendritic serotonergic response by buspirone in rats.
Haleem, DJ; Haleem, MA; Samad, N, 2007
)
1.04
"Treatment with haloperidol increases oxyradicals which are implicated in TD."( Effect of spirulina maxima on the haloperidol induced tardive dyskinesia and oxidative stress in rats.
Jyothi, B; Thaakur, SR, 2007
)
0.96
"Pretreatment with haloperidol (4 mg/kg, i.p.) resulted in a synergistic hypothermic effect."( Serotonergic neurotransmission mediates hypothermia induced by the N-phenylpiperazine antipsychotic prototypes LASSBio-579 and LASSBio-581.
Barreiro, EJ; Betti, AH; Conrado, DJ; Fraga, CA; Kliemann, M; Neves, G; Rates, SM; Tasso, L, 2008
)
0.67
"Treatment with haloperidol and clozapine attenuated the detrimental performance effects of these challenges, with clozapine exhibiting more robust attenuation."( Detection of the moderately beneficial cognitive effects of low-dose treatment with haloperidol or clozapine in an animal model of the attentional impairments of schizophrenia.
Martinez, V; Sarter, M, 2008
)
0.91
"Pretreatment with haloperidol (0.0032 or 0.01 mg/kg, i.m.) antagonized the effects of low doses of cocaine on the number of infusions in the self-administration component, whereas only the 0.01-mg/kg dose antagonized the effects of high doses of cocaine on the number of infusions."( Differential antagonism of cocaine self-administration and cocaine-induced disruptions of learning by haloperidol in rhesus monkeys.
Moerschbaecher, JM; Roussell, AM; Winsauer, PJ, 2008
)
0.88
"The treatment with haloperidol worsened the adverse effects of chronic social stress having effects similar to stress on reward and motivation-related behaviours."( Pharmacological validation of a chronic social stress model of depression in rats: effects of reboxetine, haloperidol and diazepam.
Abumaria, N; Flügge, G; Fuchs, E; Havemann-Reinecke, U; Hiemke, C; Rüther, E; Rygula, R; Zernig, G, 2008
)
0.88
"Rats treated with haloperidol also showed an increase in 5-HIAA levels, possibly due to enhanced serotonin turnover."( Dopamine and serotonin metabolites in rat cerebroventricular fluid following withdrawal of haloperidol or electroshock treatment.
Barkai, AI; Kowalik, S; Reches, A, 1984
)
0.81
"Pretreatment with haloperidol or metoclopramide reduced the intensity of stereotyped behaviour induced by fencamfamine, while phenoxybenzamine increased this behaviour."( On the mechanism of central stimulation action of fencamfamine.
Aizenstein, ML; Bernardi, MM; DeLucia, R; Scavone, C, 1984
)
0.59
"Pretreatment with haloperidol attenuated the hypothermia in a dose-dependent manner."( Effects of dopaminergic and serotonergic drugs on ethanol-induced hypothermia.
Horita, A; Lai, H; Yamawaki, S, 1984
)
0.59
"Treatment with haloperidol is useful for 80% to 85% of patients but associated with troublesome side effects in one-half of those treated."( Tics in childhood.
Golden, GS, 1983
)
0.61
"RA treatment of haloperidol-treated rats significantly (p less than 0.001) blocked the stimulatory effect of haloperidol on mammary carcinoma development."( Retinoid feeding, hormone inhibition, and/or immune stimulation and the progression of N-methyl-N-nitrosourea-induced rat mammary carcinoma: suppression by retinoids of peptide hormone-induced tumor cell proliferation in vivo and in vitro.
Aylsworth, CF; DeHoog, JV; Scieszka, KM; Welsch, CW, 1984
)
0.6
"Pretreatment with haloperidol, 1.0 and 2.0 mg/kg ip 1 h beforehand in post-lesion week 9, converted the biphasic response into an enhanced, uniphasic one."( Apomorphine-induced biphasic circling behaviour in 6-hydroxydopamine-lesioned rats. A pharmacological kindling phenomenon.
Coward, DM, 1983
)
0.59
"Treatment with haloperidol, but not sulpiride or clozapine, caused inhibition of stereotyped behaviour induced by apomorphine (0.125-0.25 mg/kg SC)."( Differential alterations in striatal dopamine receptor sensitivity induced by repeated administration of clinically equivalent doses of haloperidol, sulpiride or clozapine in rats.
Hall, MD; Jenner, P; Kilpatrick, G; Marsden, CD; Rupniak, NM, 1984
)
0.81
"Pre-treatment with haloperidol enhanced both behavioral responses to central DA injection, while pre-treatment with thioridazine did not enhance either behavior."( Chronic administration of three neuroleptics: effects of behavioral supersensitivity mediated by two different brain regions in the rat.
Davis, KL; Guerin, JJ; Halperin, R, 1983
)
0.58
"Pretreatment with haloperidol (0.5 and 1.0 mg/kg SC) also significantly antagonized the circling behavior induced by GABA and muscimol."( Circling behavior induced by intranigral injections of GABA and muscimol in rats.
Kaakkola, S; Kääriäinen, I, 1980
)
0.58
"Pretreatment with haloperidol (0.1 or 0.2 mg/kg) during the conditioning phase blocked the establishment of place preference even though the animals consumed the food in the drugged state."( Attenuation by haloperidol of place preference conditioning using food reinforcement.
Fibiger, HC; Phillips, AG; Spyraki, C, 1982
)
0.94
"Pretreatment with haloperidol (0.15 or 1.0 mg/kg) antagonized the place preference produced by amphetamine (1.5 mg/kg)."( Dopaminergic substrates of amphetamine-induced place preference conditioning.
Fibiger, HC; Phillips, AG; Spyraki, C, 1982
)
0.59
"Pretreatment with haloperidol (1 mg/kg) partially blocked the PCP-induced hyperactivity but pretreatment with methysergide (3 mg/kg) did not."( Effects of phencyclidine on aggressive behavior in mice.
Miczek, KA; Tyler, CB, 1982
)
0.59
"Pretreatment with haloperidol did not change the toxicity of reserpine."( Effects of preceding sensibilization by reserpine and haloperidol on toxicity of dopaminergic agonists.
Schmidt, J; Westermann, KH, 1980
)
0.83
"Treatment with haloperidol produced a marked improvement in the symptoms, some of which are seldom reported."( Gilles de la Tourette's syndrome: case report.
Shenken, LI, 1980
)
0.6
"Treatment with haloperidol is effective but associated with a high incidence of side effects."( Tics and tremors.
Golden, GS; Hood, OJ, 1982
)
0.6
"Pretreatment with haloperidol (0.5 and 1.0 mg/kg s.c.) significantly but not completely antagonized the circling response to baclofen."( Circling behaviour induced by intranigral injection of baclofen in rats.
Kaakkola, S, 1980
)
0.58
"Pretreatment with haloperidol reduced the salivary secretion to L-dopa in normal animals (unoperated glands), while the response to dopamine was unaffected."( Studies on the mechanisms of L-dopa-induced salivary secretion.
Medina, JH; Pazo, JH; Tumilasci, OR, 1981
)
0.59
"Treatment with haloperidol had no effect on NT concentrations in any brain region in 10-day-old rat pups."( Ontogeny of the effect of antipsychotic drug treatment on neurotensin concentrations in the rat brain.
Kinkead, B; Nemeroff, CB; Owens, MJ, 1995
)
0.63
"Pretreatment with haloperidol (2 mg/kg) significantly decreases the radioactivity measured in the brain 30-120 min after injection of [3H]4-PPBP."( In vivo labeling of sigma receptors in mouse brain with [3H]4-phenyl-1-(4-phenylbutyl)piperidine.
Hashimoto, K; London, ED; Scheffel, U, 1995
)
0.61
"Treatment with haloperidol and (+) butaclamol, which have a high affinity for dopamine D2 receptors, also tended to reduce the myocardial uptake of radioactivity, while (-)-butaclamol, which has no affinity for dopamine D2 receptors, caused no change in uptake."( Myocardial accumulation of a dopamine D2 receptor-binding radioligand, 2'-iodospiperone.
Iida, Y; Iwasaki, Y; Konishi, J; Magata, Y; Saji, H; Tanahashi, K; Yokoyama, A; Yonekura, Y, 1993
)
0.63
"Pretreatment with haloperidol (13 to 130 nmol/kg sc), but not equimolar doses of UH 232, prevented the disruption of PPI produced by the highest dose (0.6 mumol/kg sc) of each agonist."( Effects of D3/D2 dopamine receptor agonists and antagonists on prepulse inhibition of acoustic startle in the rat.
Caine, SB; Geyer, MA; Swerdlow, NR, 1995
)
0.61
"Pretreatment with haloperidol (HALO) 0.5 or 1.0 mg/kg IP before PCA blocked the facilitatory phase of the response."( Opposite effects of PCA and chlorimipramine on ICSS and on its facilitation by amphetamine.
Olds, ME, 1994
)
0.61
"Pretreatment with haloperidol suppressed both the antiparkinsonian effects and the hyperactivity induced by apomorphine."( Effects of terguride, a partial D2 agonist, on MPTP-lesioned parkinsonian cynomolgus monkeys.
Akai, T; Kuno, S; Mizuta, E; Yamaguchi, M, 1993
)
0.61
"Treatment with haloperidol also increased the size of the striatal catechol peak but was responsible for a reduction of the neuropeptidergic signal."( Functional in vivo interaction between growth hormone and dopamine systems are correlated to changes in striatal somatostatin levels as detected by voltammetry.
Crespi, F, 1993
)
0.63
"Treatment with haloperidol caused initial increases in urinary homovanillic acid (HVA) output that returned toward baseline by the 5th week."( Studies of catecholamine metabolism in schizophrenia/psychosis--II.
Berman, N; Bowden, CL; Contreras, SA; Javors, MA; Maas, JW; Miller, AL; Seleshi, E; Weintraub, SE, 1993
)
0.63
"Treatment with haloperidol or chlorpromazine was associated with an extremely low prevalence of extrapyramidal side effects."( A double-blind trial of haloperidol, chlorpromazine, and lorazepam in the treatment of delirium in hospitalized AIDS patients.
Breitbart, W; Corbera, K; Derevenco, M; Grau, C; Jacobson, P; Lund, S; Marotta, R; Platt, MM; Raymond, S; Weisman, H, 1996
)
0.94
"Pretreatment with haloperidol significantly antagonized quinpirole-induced elevation in striatal ACh (p<0.01) and cerebellar cGMP(p<0.05), and haloperidol had no significant effect on oxotremorine-induced agonist responses."( Comparative dopaminergic and muscarinic antagonist activity of clozapine and haloperidol.
Ellerbrock, BR; Sethy, VH; Wu, H, 1996
)
0.85
"Pretreatment with haloperidol prevented both inhibitory and potentiative effects of substance P-(1-7) whereas thiothixine did not, suggesting inhibitory as well as potentiative modulation of NMDA by sigma receptor activity."( Evidence that the NH2-terminus of substance P modulates N-methyl-D-aspartate-induced activity by an action involving sigma receptors.
Hornfeldt, CS; Kitto, KF; Larson, AA, 1996
)
0.62
"Pretreatment with haloperidol or SCH 23390 without cocaine enhanced the locomotor-activating effects of the subsequent cocaine challenge injection."( Cocaine-induced behavioral sensitization: effects of haloperidol and SCH 23390 treatments.
Ellison, T; Mattingly, BA; Rase, K; Rowlett, JK, 1996
)
0.87
"Treatment with haloperidol, a dopamine receptor D-2 antagonist, for one month resulted in an increase in the mean percentage of asymmetric synapses containing a discontinuous, or perforated, postsynaptic density (PSD) [Meshul et al. "( Activation of corticostriatal pathway leads to similar morphological changes observed following haloperidol treatment.
Allen, C; Buckman, JF; Feller, DJ; Meshul, CK; Riggan, JP, 1996
)
0.87
"Pretreatment with haloperidol, a non-selective antagonist of the D2 family of receptors, significantly (P < 0.01) blocked 7-OH-DPAT- and quinpirole-induced increases in ACh."( D2 and D1 dopaminergic activity of 7-OH-DPAT.
Ellerbrock, BR; Fici, GJ; Sethy, VH; Wu, H, 1996
)
0.62
"Treatment with haloperidol and lithium was unsuccessful but the addition of carbamazepine produced a dramatic response. "( A patient with mania and photoconvulsive epilepsy.
Corbett, AJ; Reid, WG; Roxanas, MG, 1996
)
0.65
"When treated with haloperidol, RIIbeta mutant mice fail to induce either c-fos or neurotensin mRNA and the acute cataleptic response is blocked."( Loss of haloperidol induced gene expression and catalepsy in protein kinase A-deficient mice.
Adams, MR; Brandon, EP; Chartoff, EH; Dorsa, DM; Idzerda, RL; McKnight, GS, 1997
)
1.05
"Treatment with haloperidol caused a marked reduction of radioactivity uptake in all the brain regions examined."( Fluorine-18 radiolabelling, biodistribution studies and preliminary PET evaluation of a new memantine derivative for imaging the NMDA receptor.
Ametamey, SM; Leenders, KL; Parsons, CG; Quack, G; Samnick, S; Schubiger, PA; Vontobel, P,
)
0.47
"Rats treated with haloperidol did not have a larger mean striatum area than the control group on either D1- or D2-like ligand autoradiograms."( Effects of chronic treatment with typical and atypical antipsychotic drugs on the rat striatum.
Alvir, JM; Bilder, R; Chakos, M; Creese, I; Kinon, BJ; Lee, H; Lieberman, JA; Redmond, M; Tarazi, FI; Wu, H, 1999
)
0.63
"The treatment with haloperidol also did not affect sigma 1-receptor mRNA detected by the RNase protection assay."( [Functional characterization of a sigma receptor and its gene expression by haloperidol].
Inoue, A; Nakata, Y; Sugita, S, 1999
)
0.85
"Pretreatment of haloperidol increased the striatal arc mRNA levels."( Effect of atypical antipsychotics on phencyclidine-induced expression of arc in rat brain.
Hashimoto, K; Hirano, M; Hondo, H; Kuroki, T; Motomura, K; Nakahara, T; Tsutsumi, T; Uchimura, H; Ueki, H, 2000
)
0.64
"Treatment with haloperidol did not affect the levels of sigma(1) receptor mRNA in any brain region in either species."( Repeated haloperidol treatment decreases sigma(1) receptor binding but does not affect its mRNA levels in the guinea pig or rat brain.
Hide, I; Ichimoto, H; Inoue, A; Nakata, Y; Shoji, H; Sugita, S, 2000
)
1.06
"Treatment with haloperidol did not produce significant changes in GAP-43 mRNA expression."( Differential effects of amphetamine and phencyclidine on the expression of growth-associated protein GAP-43.
Kanazir, S; Rakic, L; Ruzdijic, S; Veskov, R; Vukosavic, S, 2001
)
0.65
"Pretreatment with haloperidol, but not with clozapine, significantly reduced the effects of dopamine and theophylline."( Effects of chemical stimulation of the mesolimbic dopamine system upon locomotor activity.
Honig, WM; Pijnenburg, AJ; Van der Heyden, JA; Van Rossum, JM, 1976
)
0.58
"Pretreatment with haloperidol or reserpine prevented the increase of striatal cAMP following cerebral hemisection."( Cyclic AMP content and regulation of tyrosine-3-mono-oxygenase in rat striatum.
Costa, E; Guidotti, A; Zivkovic, B, 1976
)
0.58
"Treatment with haloperidol in all patients and with dipropylacetic acid in three patients did not appear to modify the CSF, HVA, and 5HIAA concentrations, the plasma DBH activity, or the DA uptake."( Biochemical aspects of Huntington's chorea.
Algeri, S; Branciforti, A; Calderini, G; Caraceni, T; Consolazione, A; Dall'olio, A; Girotti, F; Morselli, PL; Riva, E; Spreafico, R, 1977
)
0.6
"Pretreatment with haloperidol (2 mg intramuscularly) or sulpiride (100 mg intramuscularly) 30 minutes prior to apomorphine treatment, prevented the therapeutic effect of this compound."( Apomorphine hydrochloride-induced improvement in Huntington's chorea: stimulation of dopamine receptor.
Cianchetti, C; Corsini, GU; Gessa, G; Mangoni, A; Masala, C; Onali, P, 1978
)
0.58
"Treatment with haloperidol produces a good or excellent response in three quarters of the patients."( Tourette syndrome. The pediatric perspective.
Golden, GS, 1977
)
0.6
"Treatment with haloperidol suggested as a most effective method of symptomatic treatment."( Gilles de la Tourett's disease, a single case study: a discussion on aetiology and treatment.
Izadi, C; Naraghi, MM, 1978
)
0.6
"Pretreatment with haloperidol (1 mg/kg) abolishes the increase in water intake but does not prevent the increase in food intake."( An effect of haloperidol on the increased food and water intake induced in rabbits by 2-deoxy-D-glucose.
Anderson, J; Sharman, DF; Stephens, DB, 1979
)
0.95
"Pretreatment with haloperidol significantly depressed the accumulation of apomorphine in the caudate nucleus and hippocampus, but not in the cerebellum."( Accumulation of apomorphine in caudate nucleus and hippocampus of the rabbit.
Melzacka, M; Rurak, A; Smiałowski, A; Vetulani, J, 1979
)
0.58
"Pretreatment with haloperidol (400 microgram, i.c.v.) attenuated the thermoregulatory effects of i.c.v."( Comparison of the thermoregulatory responses to intracerebroventricularly injected dopamine, noradrenaline and 5-hydroxytryptamine in the goat.
De Roij, TO; Frens, J; Vianen-Meijerink, M; Woutersen-Van-Nijnanten, F, 1978
)
0.58
"Pretreatment with haloperidol also reversed the depression caused by apomorphine."( Antagonism by haloperidol of locomotor depression induced by small doses of apomorphine.
Strömbom, U, 1977
)
0.94
"Rats treated with haloperidol or bearing subcutaneous implants of prolactin-secreting tumors had elevated CSF prolactin levels compared to those observed in control rats. "( Prolactin in human and rat serum and cerebrospinal fluid.
Login, IS; MacLeod, RM, 1977
)
0.59
"Pretreatment with haloperidole nullified the effect of apomorphine."( [Nigrostriatally induced motor reactions in the rat. I. Rotational behavior and posture asymetry after intracerebral injection of apomorphine and dopamine].
Staib, AH; Westermann, KH, 1976
)
0.58
"Pretreatment with haloperidol, 5 mg/kg i.p."( Effect of (+) amphetamine on monoamine synthesis and metabolism after axotomy in rat forebrain.
Kehr, W; Speckenbach, W, 1976
)
0.58
"Pretreatment with haloperidol (0.16 mg/kg) or pimozide (0.08 mg/kg) but not with phentolamine (10mg/kg) effectively blocked amphetamine-dopa jumping."( Narcotic withdrawal like mouse jumping produced by amphetamine and L-DOPA.
Colpaert, FC; Laduron, P; Lal, H, 1975
)
0.58
"Treatment with haloperidol (4 mg/kg/day) or morphine (60 mg/kg/day) given daily for six days before surgery promoted recovery and reduced the incidence of death."( Effects of haloperidol, methyltyrosine and morphine on recovery from lesions of lateral hypothalamus.
Anderson, CD; Gianutsos, G; Hynes, MD; Lal, H,
)
0.86
"Pretreatment with haloperidol (0.05 and 0.1 mg/kg, SC) failed to alter hourly or daily self-injection rates."( Influence of dopaminergic and serotonergic neurons on intravenous ethanol self-administration in the rat.
Lyness, WH; Smith, FL, 1992
)
0.61
"Pretreatment with haloperidol also markedly reduced the antitussive effects of (+/-)-pentazocine and dextromethorphan."( Involvement of haloperidol-sensitive sigma-sites in antitussive effects.
Hitosugi, H; Iwamoto, Y; Kamei, J; Kasuya, Y; Kawashima, N; Misawa, M, 1992
)
0.96
"Pretreatment with haloperidol (0.2 mg/kg) significantly attenuated the elevations in corticosterone and ACTH elicited by cocaine, as well as the elevation in ACTH produced by GBR12909."( Monoamine mediation of cocaine-induced hypothalamo-pituitary-adrenal activation.
Borowsky, B; Kuhn, CM, 1991
)
0.6
"Pretreatment with haloperidol (i.p.) abolished the effect of Ruthenium Red after injection into the caudoventromedial nigra but only partially reduced it after administration into the central nigra."( Circling behavior induced by intranigral administration of ruthenium red and 4-aminopyridine in the rat.
Flores-Hernández, J; Tapia, R, 1990
)
0.6
"Pretreatment with haloperidol (0.05 and 0.1 mg/kg s.c.) attenuated the effect induced by median raphe 8-OH-DPAT (0.5 microgram) complementing previous results with dorsal raphe 8-OH-DPAT."( Dopamine receptor blockade in nucleus accumbens or caudate nucleus differentially affects feeding induced by 8-OH-DPAT injected into dorsal or median raphe.
Fletcher, PJ, 1991
)
0.6
"Pretreatment with haloperidol or clozapine caused a significant reduction of the 60 mM potassium-evoked release, compared with a saline treated control group (control 21.0 fmol; haloperidol 2.8 fmol; clozapine 8.8 fmol) and an increase of tissue levels after haloperidol treatment by 43%."( Calcitonin gene-related peptide in the amygdaloid complex of the rat: immunohistochemical and quantitative distribution, and drug effects on calcium dependent, potassium-evoked in vitro release.
Haring, C; Humpel, C; Javorsky, F; Krobath, J; Saria, A; Skofitsch, G, 1991
)
0.6
"Treatment with haloperidol (0.015-0.06 mg/kg IM) did not induce chewing."( Drug-induced purposeless chewing: animal model of dyskinesia or nausea?
Iversen, SD; Rupniak, NM; Tye, SJ, 1990
)
0.62
"Pretreatment with haloperidol, 0.1 or 0.2 mg kg-1 SC at -40 min, or remoxipride 8 mg kg-1 IP at -30 min, did not antagonize the PCP-induced disruption of discriminative performance, nor was the PCP-induced increase in number of intertrial crosses antagonized."( Phencyclidine-induced disruption of an aversely motivated two-choice successive discrimination in the rat.
Ahlenius, S; Ericson, E, 1990
)
0.6
"Pretreatment with haloperidol (0.1 mg kg-1, 30 min) significantly attenuated the effects of equi-effective doses of buspirone, gepirone and ipsapirone, indicating that these drugs interact with dopaminergic systems to increase feeding."( The involvement of 5-hydroxytryptaminergic and dopaminergic mechanisms in the eating induced by buspirone, gepirone and ipsapirone.
Davies, M; Fletcher, PJ, 1990
)
0.6
"Treatment with haloperidol led to improvement in the characteristic tics of Tourette's disorder as well as to improvement in these three complex-associated behaviors."( Tourette's disorder and associated complex behaviors: a case report.
McDougle, CJ; Rohrbaugh, RM; Southwick, SM,
)
0.47
"Treatment with haloperidol normalized the low ratio."( Preliminary evidence of reduced combined output of dopamine and its metabolites in chronic schizophrenia.
Bigelow, LB; Karoum, F; Karson, CN; Lawson, WB; Wyatt, RJ, 1987
)
0.61
"Pretreatment with haloperidol or the partial lesioning of nigrostriatal neurons enhanced the effect of tyrosine on dopamine release, and haloperidol also prolonged this effect."( Dopamine release in rat striatum: physiological coupling to tyrosine supply.
Acworth, IN; During, MJ; Wurtman, RJ, 1989
)
0.6
"Pretreatment with haloperidol, alpha-methyl-p-tyrosine (alpha-MT) and amino-oxyacetic acid (AOAA) but not atropine, inhibited the ability of both YM-14673 and TRH to increase SMA."( Effects of a new TRH analogue, YM-14673, on spontaneous motor activity in rats.
Kobayashi, M; Shimizu, M; Yamamoto, M,
)
0.45
"Treatment with haloperidol resulted in significantly more severe movement disorder in pinealectomized rats than in unoperated control rats."( Increased incidence and severity of neuroleptic-induced movement disorder in pinealectomized rats.
Fisher, H; Sandyk, R, 1989
)
0.62
"Pretreatment with haloperidol (2.5 micrograms into VLS) had no effect on PS/Ach-induced mouth movements."( Cholinergic stimulation of the ventrolateral striatum elicits mouth movements in rats: pharmacological and regional specificity.
Bakshi, VP; Delfs, JM; Kelley, AE; Lang, CG, 1989
)
0.6
"Pretreatment with haloperidol reduced subject ratings of pleasant sensations but had no effect on drug "rush." Haloperidol (8 mg) has a small and limited effect on the subjective response to cocaine when given 20 min before cocaine."( Effects of intravenous cocaine are partially attenuated by haloperidol.
Jaffe, JH; Kumor, KM; Sherer, MA, 1989
)
0.84
"Pretreatment with haloperidol (0.5 mg/kg, i.p.) had no effect on increase in spontaneous release of ACh brought about by cerulein administration (100 micrograms/kg, i.p.)."( Effect of cerulein on in vivo release of acetylcholine from the rat striatum.
Kito, S; Shimoyama, M, 1989
)
0.6
"Pretreatment with haloperidol counteracted the effects of apomorphine and B-HT 920."( Increased investigative activity after presynaptic dopaminergic stimulation measured by a fixed-interval recording procedure.
Höglund, AU; Meyerson, BJ, 1985
)
0.59
"Pretreatment with haloperidol antagonized the anoretic effect induced by fencamfamine."( Reduction of food intake by fencamfamine in rats.
Aizenstein, ML; DeLucia, R; Planeta, Cda S; Scavone, C, 1987
)
0.6
"Pretreatment with haloperidol, an antagonist of both D-1 and D-2 dopamine receptors, metoclopramide and molindone, the selective D-2 dopamine receptor antagonists, effectively antagonised bromocriptine-induced climbing behaviour."( Antagonism of bromocriptine-induced cage climbing behaviour in mice by the selective D-2 dopamine receptor antagonists, metoclopramide and molindone.
Balsara, JJ; Bapat, TR; Chandorkar, AG; Gada, VP; Nandal, NV,
)
0.45
"Treatment with haloperidol increased plasma prolactin moderately whilst nalbuphine raised it markedly 1 and 2.5 h post injection."( Psychomotor, respiratory and neuroendocrinological effects of nalbuphine and haloperidol, alone and in combination, in healthy subjects.
Saarialho-Kere, U, 1988
)
0.84
"Pretreatment with haloperidol (0.020 mg/kg) in a dose which preferentially acts at presynaptic sites reversed the effects of low doses of apomorphine, bromocriptine or pergolide on sleep and W."( Biphasic effects of dopamine D-2 receptor agonists on sleep and wakefulness in the rat.
D'Angelo, L; Fernández, M; Hawkins, M; Jantos, H; Monti, JM, 1988
)
0.6
"Pretreatment with haloperidol and sulpiride blocked the effects induced by ciladopa."( Evaluation of ciladopa hydrochloride as a potential anti-Parkinson drug.
Fields, JZ; Gordon, JH; Koller, WC; Perlow, MJ, 1986
)
0.59
"Treatment with haloperidol, bromocriptine and morphine altered the relationship, favoring immunoreactive more than bioactive hormone, and reversing the pretreatment Nb2BA/RIA ratio."( Comparison between rat prolactin radioimmunoassay and bioassay values under different experimental and physiological conditions.
Casanueva, FF; Friesen, HG; Owens, RE, 1985
)
0.61
"Pretreatment with haloperidol failed to alter the stimulus properties of dl-cathinone."( Comparative discriminative stimulus properties of dl-cathinone, d-amphetamine, and cocaine in rats.
Huang, D; Wilson, MC, 1986
)
0.59
"Treatment with haloperidol 5 mg IM caused significant improvement while placebo treatment did not."( Treatment of phenylcyclohexylpyrrolidine (PHP) psychosis with haloperidol.
Giannini, AJ; Loiselle, RH; Malone, DW; Price, WA, 1985
)
0.85

Toxicity

The neurologic side effect profile of low-dose risperidone is comparable with that of haloperidol in patients receiving APDs for the first time. Olanzapine and clozapine are afflicted with the highest risk of inducing weight gain. There is a clear increased risk of extrapyramidal adverse effects for haloperids compared with placebo.

ExcerptReferenceRelevance
" The total incidence of serious adverse events in the short-term double-blind programme was approximately 2% for both remoxipride and haloperidol."( Safety evaluation in both short- and long-term treatment of schizophrenia with remoxipride.
Englund, A; Lawrie, V; Lewander, T; Morrison, D; Schlachet, A; Westerbergh, SE, 1990
)
0.48
" The results support the hypothesis of a positive correlation between the CSF HVA and the hypokinetic-rigid side effect and a negative correlation between the pretherapeutic dopamine turnover and the risk of neuroleptic Parkinsonism."( Hypokinetic-rigid extrapyramidal side effects of neuroleptics: the relationship of the silent period in EMG and HVA and 5-HIAA in CSF.
Baslo, A; Eroğlu, L; Hizal, A; Yazici, J; Yazici, O, 1986
)
0.27
" The results counter sporadic clinical reports suggesting a toxic interaction between lithium and neuroleptic drugs."( Safety of the combination of lithium and neuroleptic drugs.
Goldney, RD; Spence, ND, 1986
)
0.27
"Malathion-induced marked potentiation of BPMC toxicity (about fivefold) was analyzed by measuring LD50 as an index of acute toxicity."( Contribution of monoaminergic nervous system in potentiation of 2-sec-butylphenyl N-methylcarbamate (BPMC) toxicity by malathion in male mice.
Shirasu, Y; Takahashi, H; Tanaka, J; Tsuda, S, 1987
)
0.27
"Neurochemical effects of electroconvulsive shock (ECS) in three neurotransmitter-receptor systems were studied in relation to the mechanism of action and adverse effects of ECT."( Electroconvulsive shock and neurotransmitter receptors: implications for mechanism of action and adverse effects of electroconvulsive therapy.
Lerer, B, 1984
)
0.27
" The authors reviewed a further case of adverse drug response following the concomitant use of lithium and haloperidol."( The question of lithium/neuroleptic toxicity.
Jeffries, J; Remington, G; Wilkins, J, 1984
)
0.48
"Amine-curing agent for epoxy resin, bis(4-amino-3-methylcyclohexyl)methane, has been suspected of inducing toxic symptoms in man which resemble collagen disease such as scleroderma or polymyositis."( [Subacute toxicity of an amine-curing agent for epoxy resin].
Matsumoto, M; Nakayama, E; Nishizawa, H; Ohsawa, M; Ohshima, S; Okuda, H; Sasaki, N; Shibata, T, 1984
)
0.27
" Other adverse effects were assessed using the UKU Side Effects Scale."( Extrapyramidal side effects and tolerability of risperidone: a review.
Owens, DG, 1994
)
0.29
" Other adverse events interfering with the patients' social roles also interfere with the patients' willingness to comply with treatment."( Compliance with antipsychotic drug treatment: influence of side effects.
Fleischhacker, WW; Günther, V; Kurz, M; Meise, U, 1994
)
0.29
" This suggests that glutamate also mediates the toxic effects of METH."( Methamphetamine-induced neurotoxicity: roles for glutamate and dopamine efflux.
Stephans, SE; Yamamoto, BK, 1994
)
0.29
" Although HPP+ was less potent than MPP+ on the dopaminergic system, the two compounds displayed comparable toxic effects on the serotonergic system."( MPP(+)-like neurotoxicity of a pyridinium metabolite derived from haloperidol: in vivo microdialysis and in vitro mitochondrial studies.
Castagnoli, N; D'Engelbronner, J; Igarashi, K; Rollema, H; Skolnik, M; Usuki, E, 1994
)
0.53
"The toxic effects of modified endodontic sealers, Fillcanal, N-Rickert, FS, and Sealer 26, were assessed."( Cytotoxicity of some modified root canal sealers and their leachable components.
Araki, K; Barbosa, SV; Spångberg, LS, 1993
)
0.29
" It seemed sensible to investigate whether or not HP+ might be toxic towards dopaminergic neurons and perhaps associated with some of the residual moto-function side effects of haloperidol."( Comparison of cytotoxicity of a quaternary pyridinium metabolite of haloperidol (HP+) with neurotoxin N-methyl-4-phenylpyridinium (MPP+) towards cultured dopaminergic neuroblastoma cells.
Fang, J; Yu, PH; Zuo, D, 1995
)
0.72
" However, there were no adverse effects on the copulation index in any of the treated groups."( Collaborative work to determine an optimal administration period and optimal parameters for detection of effects on male fertility in rats--male reproductive toxicity study of haloperidol.
Imanishi, M; Takagi, S; Takeuchi, M; Yoneyama, M, 1995
)
0.48
" Gross toxic side effects (seizures, catatonia, confusion) and Neuroleptic Induced Deficit Syndrome in conjunction with blood levels over 30 ng/ml were identified in 13 of our 43 patients."( Haloperidol dose and blood level variability: toxicity and interindividual and intraindividual variability in the nonresponder patient in the clinical practice setting.
Clark, L; Dabiri, L; Darby, JK; Mosbacher, D; Pasta, DJ, 1995
)
1.73
" Serious adverse events did not occur."( Pramipexole as adjunct to haloperidol in schizophrenia. Safety and efficacy.
Barnas, C; Heiden, A; Kasper, S; Laakmann, G; Pfolz, H; Volz, HP; Zeit, H, 1997
)
0.6
" The proportion of patients failing to reach at least 20% improvement on the positive and negative syndrome scale (PANSS) or brief psychiatric rating scale (BPRS), the proportion of patients discontinuing treatment because of adverse effects and the number of patients who needed antiparkinsonian medication were abstracted for use as outcome measures."( Risperidone versus haloperidol in the treatment of schizophrenia: a meta-analysis comparing their efficacy and safety.
Bacaltchuk, J; de Castro-e-Silva, E; de Oliveira, IR; de Sena, EP; Miranda-Scippa, AM; Pereira, EL; Ribeiro, MG, 1996
)
0.62
" The adverse effects of risperidone may be due to the lack of development of acute tolerance to its powerful serotonergic (5-HT2A) antagonism, which could be responsible for the disruption of brainstem physiology in regions controlling saccadic eye movements."( Adverse effects of risperidone on eye movement activity: a comparison of risperidone and haloperidol in antipsychotic-naive schizophrenic patients.
Bauer, KS; Haas, GL; Keshavan, MS; Kroboth, PD; Schooler, NR; Sweeney, JA, 1997
)
0.52
" Significant adverse events included somnolence, weight gain, and asymptomatic treatment-emergent transaminase elevation."( Safety of olanzapine.
Beasley, CM; Tollefson, GD; Tran, PV, 1997
)
0.3
"Most traditional neuroleptics have a narrow therapeutic-to-toxic index, and thus, the novel antipsychotics are the result of a search to substantially widen the distance between the dose that treats psychosis and the one that produces adverse effects."( The relationship of pharmacology to side effects.
Casey, DE, 1997
)
0.3
"Very little is known about the pharmacokinetics of neuroleptic drugs in breast-feeding mothers and their infants or about possible adverse effects in the infants."( Neuroleptic drugs in breast-milk: a study of pharmacokinetics and of possible adverse effects in breast-fed infants.
Craggs, M; Kumar, R; Smith, B; Yoshida, K, 1998
)
0.3
" Concentrations of haloperidol in the adult range were found in plasma from 2 of 5 infants assayed by EIA but there was no evidence of any acute or delayed adverse effects."( Neuroleptic drugs in breast-milk: a study of pharmacokinetics and of possible adverse effects in breast-fed infants.
Craggs, M; Kumar, R; Smith, B; Yoshida, K, 1998
)
0.63
"This research explored the effects of haloperidol (HP) metabolites on biogenic amine uptake and release, and compared them to those of MPTP and its toxic metabolite, MPP+."( Effects of haloperidol metabolites on neurotransmitter uptake and release: possible role in neurotoxicity and tardive dyskinesia.
Barlow, RL; Bempong, J; Bloomquist, JR; Kirby, ML; Wright, AM, 1998
)
0.96
"In order to study the putative monoamine oxidase (MAO) inhibitory side effect of neuroleptics and simultaneous changes in platelet serotonin content both MAO-B activity and serotonin (5-HT) content in platelets of 30 healthy volunteers and 50 schizophrenic patients treated with neuroleptics were investigated."( MAO inhibitory side effects of neuroleptics and platelet serotonin content in schizophrenic patients.
Borcsiczky, D; Magyar, K; Máté, M; Mészáros, Z; Tarcali, J; Tekes, K, 1998
)
0.3
" AH26 had a severe cytotoxic effect whilst Topseal and AH-Plus showed a markedly lower toxic influence on the cells during the experimental period."( Cytotoxicity of three resin-based root canal sealers: an in vitro evaluation.
Beltes, P; Geromichalos, GD; Kortsaris, AH; Koulaouzidou, EA; Papazisis, KT, 1998
)
0.3
"To compare the side effect profile of risperidone with that of oral haloperidol in patients with no previous exposure to antipsychotic drugs (APDs)."( Neurologic side effects in neuroleptic-naive patients treated with haloperidol or risperidone.
Mazurek, MF; Rosebush, PI, 1999
)
0.77
"Early studies suggested that the APD risperidone may have a side effect profile comparable with that of placebo."( Neurologic side effects in neuroleptic-naive patients treated with haloperidol or risperidone.
Mazurek, MF; Rosebush, PI, 1999
)
0.54
"The neurologic side effect profile of low-dose risperidone is comparable with that of haloperidol in patients receiving APDs for the first time."( Neurologic side effects in neuroleptic-naive patients treated with haloperidol or risperidone.
Mazurek, MF; Rosebush, PI, 1999
)
0.76
" Safety was monitored by open adverse event reporting, the Simpson-Angus Scale, the Barnes Akathisia Scale and the Abnormal Involuntary Movement scale."( Safety profile of amisulpride in short- and long-term use.
Coulouvrat, C; Dondey-Nouvel, L; Rein, W, 2000
)
0.31
" Adverse events were mainly psychiatric in nature, and occurred with similar frequency in each group (amisulpride 254/370, 69%; haloperidol 82/118, 70%)."( Long-term safety and efficacy of amisulpride in subchronic or chronic schizophrenia. Amisulpride Study Group.
Colonna, L; Dondey-Nouvel, L; Rein, W; Saleem, P, 2000
)
0.51
"The relationship between Taq1 A polymorphism of dopamine D(2) receptor (DRD(2)) gene and extrapyramidal adverse effects of bromperidol and nemonapride, which are both antipsychotic drugs with selective and potent DRD(2) antagonistic property, was investigated in Japanese schizophrenic inpatients."( No relationship between Taq1 a polymorphism of dopamine D(2) receptor gene and extrapyramidal adverse effects of selective dopamine D(2) antagonists, bromperidol, and nemonapride in schizophrenia: a preliminary study.
Kaneko, S; Kondo, T; Mihara, K; Nagashima, U; Ono, S; Otani, K; Suzuki, A, 2000
)
0.31
" This was likely because of the fact that glutamate, now toxic at much lower concentrations, was able to reach and activate dendritic receptors under these conditions."( NMDA and glutamate evoke excitotoxicity at distinct cellular locations in rat cortical neurons in vitro.
Aizenman, E; Blitzblau, RC; Du, S; Leszkiewicz, DN; Rosenberg, PA; Sinor, JD; Venneti, S, 2000
)
0.31
" The results obtained in this study showed the high cytotoxcity of the new AH Plus root canal sealer, which was shown to be equally or more toxic to the standard AH26 and Diaket materials."( Cytotoxic effect of four root filling materials.
Anić, I; Karlović, Z; Marsan, T; Miletić, I; Osmak, M; Pezelj-Ribarić, S, 2000
)
0.31
" The present study aims to investigate the relationship between the -141C Ins/Del polymorphism and extrapyramidal adverse effects of bromperidol and nemonapride, antipsychotic drugs with a selective and potent DRD2 antagonistic property, in schizophrenic inpatients."( No relationship between--141C Ins/Del polymorphism in the promoter region of dopamine D2 receptor and extrapyramidal adverse effects of selective dopamine D2 antagonists in schizophrenic patients: a preliminary study.
Kaneko, S; Kondo, T; Mihara, K; Ono, S; Otani, K; Suzuki, A; Yasui, N, 2001
)
0.31
" We conducted a survey of Spanish psychiatrists in mental health centers and outpatient treatment units to assess the severity scores that they would assign to a list of the most common adverse events (AEs) that usually occur with antipsychotic treatment."( Global index of safety (GIS): a new instrument to assess drug safety.
Badía, X; Gómez, JC; Kind, P; Sacristán, JA, 2001
)
0.31
" These preliminary results suggest that crossover from haloperidol to risperidone is generally safe and effective and may produce favorable moods in agitated dementia patients."( Shifting from haloperidol to risperidone for behavioral disturbances in dementia: safety, response predictors, and mood effects.
Chang, WH; Chang, YC; Chiu, CC; Huang, MC; Lane, HY; Su, MH, 2002
)
0.92
" Adverse events were recorded during the trial period."( Efficacy and safety of zotepine for the treatment of Taiwanese schizophrenic patients: a double-blind comparison with haloperidol.
Hwang, TJ; Lin, HN; Lin, SK, 2001
)
0.52
" Calcium hydroxide-based sealer was the least toxic sealer amongst the chemicals tested in both cultures."( Cytotoxicity of resin-, zinc oxide-eugenol-, and calcium hydroxide-based root canal sealers on human periodontal ligament cells and permanent V79 cells.
Chang, YC; Chou, MY; Huang, FM; Tai, KW, 2002
)
0.31
"The effects of haloperidol, risperidone, and thioridazine on the pharmacokinetics and side-effect profile of quetiapine were investigated in 36 patients with schizophrenia, schizoaffective disorder, or bipolar disorder in a single-center, two-period, multiple-dose, open-label, randomized trial."( The safety and pharmacokinetics of quetiapine when coadministered with haloperidol, risperidone, or thioridazine.
Alva, G; Arvanitis, LA; Bera, R; Potkin, SG; Thyrum, PT; Yeh, C, 2002
)
0.9
"The novel antipsychotic medications offer a more favorable extrapyramidal side effect profile than conventional agents."( Sexual side effects of novel antipsychotic medications.
Marder, SR; Pierre, JM; Saunders, CS; Wirshing, DA; Wirshing, WC, 2002
)
0.31
"Sexual side effects are common clinically pertinent adverse effects associated with both novel and conventional antipsychotic medications."( Sexual side effects of novel antipsychotic medications.
Marder, SR; Pierre, JM; Saunders, CS; Wirshing, DA; Wirshing, WC, 2002
)
0.31
"Aripiprazole, effective against positive and negative symptoms, is a safe and well-tolerated potential treatment for schizophrenia and schizoaffective disorder."( Efficacy and safety of aripiprazole and haloperidol versus placebo in patients with schizophrenia and schizoaffective disorder.
Ali, MW; Carson, WH; Ingenito, GG; Kane, JM; McQuade, RD; Saha, AR; Zimbroff, DL, 2002
)
0.58
" Safety was assessed through the collection of spontaneous adverse events and a specific extrapyramidal symptoms questionnaire (EPS)."( Safety of olanzapine versus conventional antipsychotics in the treatment of patients with acute schizophrenia. A naturalistic study.
Alvarez, E; Bobes, J; Cañas, F; Carrasco, JL; Gascón, J; Gibert, J; Gómez, JC; Gutiérrez, M; Sacristán, JA, 2003
)
0.32
" Oral dose did not significantly correlate with any of these efficacy or side-effect measures."( Usefulness of plasma haloperidol levels for monitoring clinical efficacy and side effects in Alzheimer patients with psychosis and behavioral dyscontrol.
Bell, K; Cooper, TB; Devanand, DP; Liu, X; Marder, K; Marston, K; Pelton, GH,
)
0.45
" Both sealers had a low toxic influence on the cells during the experimental period."( A comparison of the in vitro cytotoxicity of two root canal sealers.
Kalayci, A; Oztan, MD; Yilmaz, S; Zaimoğlu, L, 2003
)
0.32
" Safety assessments included adverse event (AE) reports, EPS scales, ECGs, weight, and prolactin, glucose and cholesterol levels."( Aripiprazole in the treatment of schizophrenia: safety and tolerability in short-term, placebo-controlled trials.
Ali, M; Iwamoto, T; Kaplita, S; Marcus, R; Marder, SR; McQuade, RD; Safferman, AZ; Saha, A; Stock, E, 2003
)
0.32
" AH Plus was also shown to be toxic in concentrations of 16."( Examination of cytotoxicity and mutagenicity of AH26 and AH Plus sealers.
Anić, I; Garaj-Vrhovac, V; Jukić, S; Miletić, I; Osmak, M; Zeljezić, D, 2003
)
0.32
" Adverse events and scores on EPS rating scales were assessed."( A comparison of the efficacy and safety of olanzapine versus haloperidol during transition from intramuscular to oral therapy.
Birkett, M; Breier, A; Lindborg, SR; Meehan, K; Morris, P; Taylor, CC; Wright, P, 2003
)
0.56
" Although the nature of adverse events differed between the two agents, retention in the study was greater with olanzapine."( Comparative efficacy and safety of atypical and conventional antipsychotic drugs in first-episode psychosis: a randomized, double-blind trial of olanzapine versus haloperidol.
Green, AI; Gur, RE; Hamer, RM; Kahn, R; Lieberman, JA; McEvoy, J; Perkins, D; Sharma, T; Tohen, M; Tollefson, G; Wei, H; Zipursky, R, 2003
)
0.51
" Time to discontinuation due to adverse events or lack of efficacy was significantly greater with aripiprazole than with haloperidol (p=0."( Efficacy and safety of aripiprazole vs. haloperidol for long-term maintenance treatment following acute relapse of schizophrenia.
Ali, M; Archibald, D; Carson, WH; Ingenito, G; Kasper, S; Lerman, MN; Marcus, R; McQuade, RD; Pigott, T; Saha, A, 2003
)
0.79
" The aim of this study is to explore the adverse effects of conventional and atypical antipsychotic drugs and their associated factors."( Adverse effects of risperidone and haloperidol treatment in schizophrenia.
Chong, MY; Lung, FW; Yen, YC, 2004
)
0.6
" The safety and tolerability were assessed with the Extrapyramidal Symptom Rating Scale, the UKU Side-Effect Rating Scale and clinical laboratory assessments."( Adverse effects of risperidone and haloperidol treatment in schizophrenia.
Chong, MY; Lung, FW; Yen, YC, 2004
)
0.6
" The most frequent adverse effects for both groups were tremor and rigidity."( Adverse effects of risperidone and haloperidol treatment in schizophrenia.
Chong, MY; Lung, FW; Yen, YC, 2004
)
0.6
" While typical antipsychotics are often switched to atypical agents when adverse effects become limiting, there is little preclinical information to support this strategy, both in terms of efficacy and side effects."( Combined treatment of quetiapine with haloperidol in animal models of antipsychotic effect and extrapyramidal side effects: comparison with risperidone and chlorpromazine.
Matsuoka, N; Mutoh, S; Shirakawa, K; Tada, M, 2004
)
0.59
" Adverse events related to movement disorders were reported in 3%."( Long-acting injectable risperidone: safety and efficacy in stable patients switched from conventional depot antipsychotics.
Eerdekens, E; Eerdekens, M; Jacko, M; Turner, M, 2004
)
0.32
"In contrast with the Parkinson's-like effects associated with the mitochondrial neurotoxin N-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and the neuroleptic agent haloperidol, there exist no reports on adverse central nervous system (CNS) effects with the structurally related N-substituted-4-arylpiperidin-4-ol derivative and antidiarrheal agent loperamide."( Identification of an N-methyl-4-phenylpyridinium-like metabolite of the antidiarrheal agent loperamide in human liver microsomes: underlying reason(s) for the lack of neurotoxicity despite the bioactivation event.
Kalgutkar, AS; Nguyen, HT, 2004
)
0.52
" Data included safety assessments with an extrapyramidal symptoms (EPS) questionnaire and the report of spontaneous adverse events, plus clinical assessments with the Brief Psychiatric Rating Scale (BPRS) and the Clinical Global Impressions-Severity of Illness (CGI-S)."( Safety and effectiveness of olanzapine in monotherapy: a multivariate analysis of a naturalistic study.
Alvarez, E; Bobes, J; Cañas, F; Carrasco, JL; Ciudad, A; Gascón, J; Gibert, J; Gómez, JC; Gutiérrez, M, 2005
)
0.33
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" Adverse effects from the use of haloperidol such as prolonged QTc, dystonic reactions, and torsades de pointes were recorded."( Pharmacologic treatment of acute pediatric methamphetamine toxicity.
Ruha, AM; Yarema, MC, 2006
)
0.62
" No serious adverse effects were observed from the use of these agents."( Pharmacologic treatment of acute pediatric methamphetamine toxicity.
Ruha, AM; Yarema, MC, 2006
)
0.33
"The aim of this study was to determine the risk of adverse events for risperidone and haloperidol in delirium patients."( Comparison of the risk of adverse events between risperidone and haloperidol in delirium patients.
Hoshino, S; Miyaji, S; Miyaoka, H; Sakai, Y; Yamamoto, H; Yamamoto, K, 2007
)
0.8
" Extrapyramidal symptom-related adverse events were lower for aripiprazole (1."( Efficacy and safety of oral aripiprazole compared with haloperidol in patients transitioning from acute treatment with intramuscular formulations.
Allen, MH; Crandall, DT; Currier, GW; Daniel, DG; Manos, G; McQuade, R; Oren, D; Pikalov, AA; Zimbroff, DL, 2007
)
0.59
"Acutely agitated patients with schizophrenia or schizoaffective disorder treated with aripiprazole IM or haloperidol IM demonstrated similar effective and safe transition to their respective oral formulations."( Efficacy and safety of oral aripiprazole compared with haloperidol in patients transitioning from acute treatment with intramuscular formulations.
Allen, MH; Crandall, DT; Currier, GW; Daniel, DG; Manos, G; McQuade, R; Oren, D; Pikalov, AA; Zimbroff, DL, 2007
)
0.8
"In the filter diffusion test, freshly mixed Epiphany and AH Plus were rated severely toxic and RoekoSeal and EndoREZ nontoxic."( Toxicity evaluation of root canal sealers in vitro.
Bruzell, E; Lodiene, G; Morisbak, E; Ørstavik, D, 2008
)
0.35
"The multi-methacrylate resin-based (Epiphany) root canal sealer was significantly more toxic to L-929 cells than the silicone-based Roeko Seal and the single methacrylate-based EndoREZ root canal sealers."( Toxicity evaluation of root canal sealers in vitro.
Bruzell, E; Lodiene, G; Morisbak, E; Ørstavik, D, 2008
)
0.35
" The aim of this study is to investigate the adverse effects of antipsychotic drugs on fatty liver."( Gene expression on liver toxicity induced by administration of haloperidol in rats with severe fatty liver.
Hanagama, M; Inoue, H; Kamiya, M; Nata, M; Shinone, K, 2008
)
0.59
" The most common adverse events were insomnia (18."( Long-term efficacy and safety of iloperidone: results from 3 clinical trials for the treatment of schizophrenia.
Di Marino, M; Kane, JM; Laska, E; Lauriello, J; Wolfgang, CD, 2008
)
0.35
" In addition, adverse events were also evaluated."( [A naturalistic, observational study of outpatients with schizophrenia: efficacy and safety results after 6 months. The International Schizophrenia Outpatient Health Outcomes study, IC-SOHO].
Agoston, T; István, S; Tamás, T; Zoltán, J, 2007
)
0.34
" During the assessment periods Positive and Negative Syndrome Scale (PANSS) was administered to monitor the progress in psychopathology and Udvalg for Kliniske Undersogelser (UKU) side effects rating scale was applied to rate the treatment emergent adverse effects."( An open, randomized, comparative study of efficacy and safety of risperidone and haloperidol in schizophrenia.
Adhikari, SR; Gurung, CK; Koirala, NR; Nepal, MK; Sharma, VD; Tamrakar, SM,
)
0.36
" MetaSEAL was more toxic than AH Plus Jet during the first week."( In vitro cytotoxicity evaluation of a self-adhesive, methacrylate resin-based root canal sealer.
Brackett, MG; Cotti, E; Dettori, C; Huffman, BP; Lockwood, PE; Mai, S; Pashley, DH; Pinna, L; Tay, FR, 2008
)
0.35
" Sample size was reduced from 311 to 156 patients, thereby decreasing the number of patients exposed to placebo from 54 to 30 and the number exposed to the active control with a known side effect from 126 to 60."( Bayesian adaptive non-inferiority with safety assessment: retrospective case study to highlight potential benefits and limitations of the approach.
Baker, R; Breier, A; Dunayevich, E; Lindborg, S; Seaman, J; Spann, M, 2009
)
0.35
" Safety and tolerability evaluations included incidence of treatment-emergent adverse events and extrapyramidal symptom assessments (SAS, BARS, and AIMS), and metabolic profile changes including weight and BMI."( The efficacy, safety, and tolerability of aripiprazole for the treatment of schizoaffective disorder: results from a pooled analysis of a sub-population of subjects from two randomized, double-blind, placebo-controlled, pivotal trials.
Assunção-Talbott, S; Eudicone, JM; Glick, ID; Mankoski, R; Marcus, RN; Tran, QV, 2009
)
0.35
" It may potentially have a lower incidence of adverse events than other antipsychotic agents."( The efficacy and safety of blonanserin compared with haloperidol in acute-phase schizophrenia: a randomized, double-blind, placebo-controlled, multicentre study.
Garcia, E; Nakamura, H; Peris, F; Robert, M; Sato, N; Terazawa, Y, 2009
)
0.6
" Patients were assessed weekly for clinical efficacy, adverse events, extrapyramidal symptoms (EPS) and drug compliance, and were assessed biweekly for other safety variables."( The efficacy and safety of blonanserin compared with haloperidol in acute-phase schizophrenia: a randomized, double-blind, placebo-controlled, multicentre study.
Garcia, E; Nakamura, H; Peris, F; Robert, M; Sato, N; Terazawa, Y, 2009
)
0.6
"The ranking of the most to the least toxic material was: Acroseal > Epiphany = AH Plus >> COP."( The induction of cytotoxicity, oxidative stress, and genotoxicity by root canal sealers in mammalian cells.
Camargo, CH; Camargo, SE; Hiller, KA; Schmalz, G; Schweikl, H; Valera, MC, 2009
)
0.35
"The RealSeal sealer was significantly more toxic to MG63 cells than the AH Plus within 3 days, whereas RealSeal core material was similar with gutta-percha."( Cytotoxicity of RealSeal on human osteoblast-like MG63 cells.
Dong, G; Liang, J; Xu, P; Ye, L; Zheng, L, 2010
)
0.36
" Treatment with antipsychotics in this limited pilot trial did not improve the number of days alive without delirium or coma, nor did it increase adverse outcomes."( Feasibility, efficacy, and safety of antipsychotics for intensive care unit delirium: the MIND randomized, placebo-controlled trial.
Bernard, GR; Canonico, AE; Carson, SS; Dittus, RS; Ely, EW; Girard, TD; Meltzer, HY; Pandharipande, PP; Pun, BT; Schmidt, GA; Shintani, AK; Thompson, JL; Wright, PE, 2010
)
0.36
" Treatment-related adverse events (AEs) occurred in 44% and 52%, 57%, and 41% of the asenapine at 5 and 10 mg BID, haloperidol, and placebo groups, respectively."( Efficacy and safety of asenapine in a placebo- and haloperidol-controlled trial in patients with acute exacerbation of schizophrenia.
Alphs, L; Cohen, M; Kane, JM; Panagides, J; Zhao, J, 2010
)
0.82
"AH Plus root canal sealer was significantly more toxic to L-929 cells than MTA and iRoot SP."( Ex vivo cytotoxicity of a new calcium silicate-based canal filling material.
Li, Z; Peng, B; Zhang, W, 2010
)
0.36
" Patients reported similar levels of adverse events and treatment-emergent adverse events (TEAEs), except for extrapyramidal syndrome-related TEAEs, which were more common in the risperidone-treated group."( A double-blind, randomized study comparing the efficacy and safety of sertindole and risperidone in patients with treatment-resistant schizophrenia.
Buckley, PF; Daniel, DG; Kane, JM; Potkin, SG, 2011
)
0.37
" We both investigated the antipsychotic effect (Positive and Negative Syndrome Scale) and motor side effect (Extrapyramidal Symptom Rating Scale) at baseline and days 3, 7, 14, 21 and 28."( Glutamatergic gene variants impact the clinical profile of efficacy and side effects of haloperidol.
Dolžan, V; Drago, A; Giegling, I; Hartmann, AM; Möller, HJ; Plesničar, BK; Rujescu, D; Sander, T; Schäfer, M; Serretti, A; Stassen, HH; Toliat, MR, 2011
)
0.59
" The present study investigates the molecular etiology of haloperidol neurotoxicity and the role of curcumin, a well-known anti-oxidant, in ameliorating these adverse effects."( Protective effect of curcumin and its combination with piperine (bioavailability enhancer) against haloperidol-associated neurotoxicity: cellular and neurochemical evidence.
Bishnoi, M; Chopra, K; Kulkarni, SK; Rongzhu, L, 2011
)
0.83
" Diluted eluates of Activ GP and Epiphany were generally less toxic than the undiluted ones."( Cytotoxicity of 5 endodontic sealers on L929 cell line and human dental pulp cells.
Bayırlı, G; Bayrak, OF; Ersev, H; Karapınar-Kazandağ, M; Sahin, F; Tanalp, J; Yalvaç, ME, 2011
)
0.37
" Based on adverse drug reaction (ADR) reports of QT prolongation and torsades de pointes, regulatory agencies recommended the use of continuous telemetry or advising against the intravenous administration in general."( Comparative safety of antipsychotics in the WHO pharmacovigilance database: the haloperidol case.
Guglielmo, BJ; Meier, CR; Meyer-Massetti, C; Rätz Bravo, AE; Vaerini, S, 2011
)
0.6
"While regulatory agencies advise against the use of intravenous haloperidol, review of VigiBase does not reveal that the intravenous route is any more likely to be associated with cardiac adverse events."( Comparative safety of antipsychotics in the WHO pharmacovigilance database: the haloperidol case.
Guglielmo, BJ; Meier, CR; Meyer-Massetti, C; Rätz Bravo, AE; Vaerini, S, 2011
)
0.83
"The objective of the study was to examine the efficacy and the degree of adverse effects connected with atypical neuroleptic drugs and haloperidol by using a previously described Bayesian statistical method that includes both direct and indirect comparisons simultaneously."( A review and Bayesian meta-analysis of clinical efficacy and adverse effects of 4 atypical neuroleptic drugs compared with haloperidol and placebo.
Aursnes, I; Gaasemyr, J; Klemp, M; Natvig, B; Skomedal, T; Tvete, IF, 2011
)
0.78
" When the risk of adverse effects is analyzed, olanzapine and clozapine are afflicted with the highest risk of inducing weight gain and haloperidol with extrapyramidal symptoms."( A review and Bayesian meta-analysis of clinical efficacy and adverse effects of 4 atypical neuroleptic drugs compared with haloperidol and placebo.
Aursnes, I; Gaasemyr, J; Klemp, M; Natvig, B; Skomedal, T; Tvete, IF, 2011
)
0.78
" Safety measures included treatment-emergent adverse events (TEAEs), weight and extrapyramidal symptoms (EPSs)."( Efficacy and safety of olanzapine in the treatment of Japanese patients with bipolar I disorder in a current manic or mixed episode: a randomized, double-blind, placebo- and haloperidol-controlled study.
Higuchi, T; Kanba, S; Katagiri, H; Takahashi, M; Takita, Y; Tohen, M, 2012
)
0.57
"Extrapyramidal symptoms (EPSs) are common adverse effects of antipsychotics."( The association study of polymorphisms in DAT, DRD2, and COMT genes and acute extrapyramidal adverse effects in male schizophrenic patients treated with haloperidol.
Bozina, N; Mihaljević-Peles, A; Muck-Seler, D; Nikolac-Perkovic, M; Sagud, M; Vuksan-Cusa, B; Zivković, M, 2013
)
0.59
"Root canal sealing materials may have toxic potential in vitro depending on the cell line, cytotoxicity assay, material chemistry, and degree of polymer curing."( Detection of leachables and cytotoxicity after exposure to methacrylate- and epoxy-based root canal sealers in vitro.
Bruzell, EM; Kopperud, HM; Lodienė, G; Ørstavik, D, 2013
)
0.39
" The safety was evaluated by the Udvalg Kliniske Undersogelser side effect rating scale."( Efficacy and safety of haloperidol versus atypical antipsychotic medications in the treatment of delirium.
Choi, SH; Choi, WJ; Kim, JJ; Park, JY; Park, KM; Seok, JH; Yoon, HJ, 2013
)
0.7
" Fifteen subjects experienced a few adverse events, but there were no significant differences in adverse event profiles among the four groups."( Efficacy and safety of haloperidol versus atypical antipsychotic medications in the treatment of delirium.
Choi, SH; Choi, WJ; Kim, JJ; Park, JY; Park, KM; Seok, JH; Yoon, HJ, 2013
)
0.7
"Haloperidol, risperidone, olanzapine, and quetiapine were equally efficacious and safe in the treatment of delirium."( Efficacy and safety of haloperidol versus atypical antipsychotic medications in the treatment of delirium.
Choi, SH; Choi, WJ; Kim, JJ; Park, JY; Park, KM; Seok, JH; Yoon, HJ, 2013
)
2.14
" Long-term use leads to various adverse side effects, especially to severe impairment of extrapyramidal nerve tracts and in particular, altered QT interval and increased incidence of arrhytmias."( Haloperidol cytotoxicity and its relation to oxidative stress.
Adam, V; Babula, P; Gumulec, J; Kizek, R; Masarik, M; Novakova, M; Polanska, H; Raudenska, M; Stracina, T; Sztalmachova, M, 2013
)
1.83
" The cytotoxicity evaluation revealed that ZnO QDs at higher concentrations decreased cell viability but were generally safe at 30 ppm or below."( Synthesis of water-dispersible zinc oxide quantum dots with antibacterial activity and low cytotoxicity for cell labeling.
Hsu, SH; Huang, S; Lee, DS; Lem, KW; Lin, YY; Nguyen, DH, 2013
)
0.39
" The goal of this study was to compare QTc prolongation, adverse events, and effectiveness of droperidol and haloperidol among a cohort of agitated patients in the prehospital setting."( Comparison of droperidol and haloperidol for use by paramedics: assessment of safety and effectiveness.
Caruso, EH; Colwell, CB; Gaither, JB; Haukoos, JS; Johnston, JB; Macht, M; Marquez, KD; McVaney, KE; Mull, AC; Shupp, AM,
)
0.63
" We reviewed emergency department (ED) electrocardiograms when available (haloperidol, n = 78, 25%; droperidol, n = 178, 76%) for QTc length (in milliseconds), medical records for clinically relevant adverse events (defined a priori as systolic blood pressure (SBP) <90 mmHg, seizure, administration of anti-dysrhythmic medications, cardioversion or defibrillation, bag-valve-mask ventilation, intubation, cardiopulmonary arrest, and prehospital or in-hospital death)."( Comparison of droperidol and haloperidol for use by paramedics: assessment of safety and effectiveness.
Caruso, EH; Colwell, CB; Gaither, JB; Haukoos, JS; Johnston, JB; Macht, M; Marquez, KD; McVaney, KE; Mull, AC; Shupp, AM,
)
0.65
" There were no statistically significant differences in adverse events in the droperidol group as compared to the haloperidol group."( Comparison of droperidol and haloperidol for use by paramedics: assessment of safety and effectiveness.
Caruso, EH; Colwell, CB; Gaither, JB; Haukoos, JS; Johnston, JB; Macht, M; Marquez, KD; McVaney, KE; Mull, AC; Shupp, AM,
)
0.63
"In this cohort of agitated patients treated with haloperidol or droperidol in the prehospital setting, there was no significant difference found in QTc prolongation, adverse events, or need for repeat sedation between haloperidol and droperidol."( Comparison of droperidol and haloperidol for use by paramedics: assessment of safety and effectiveness.
Caruso, EH; Colwell, CB; Gaither, JB; Haukoos, JS; Johnston, JB; Macht, M; Marquez, KD; McVaney, KE; Mull, AC; Shupp, AM,
)
0.68
" Both groups reported insomnia as the most common treatment-emergent adverse event, and no serious adverse event was reported."( A double-blind, randomized comparison study of efficacy and safety of intramuscular olanzapine and intramuscular haloperidol in patients with schizophrenia and acute agitated behavior.
Chan, HY; Chen, CK; Chen, JJ; Chen, YS; Chou, SY; Ree, SC; Su, LW, 2014
)
0.61
"Haloperidol (HLP) is a potent antipsychotic drug that is commonly used for the treatments of schizophrenia and bipolar disorders but has a tendency to cause adverse effects."( Evaluation of the in vitro cytogenotoxicity profile of antipsychotic drug haloperidol using human peripheral blood lymphocytes.
Gajski, G; Garaj-Vrhovac, V; Gerić, M, 2014
)
2.08
"At all experimental conditions, the extracts of freshly mixed GuttaFlow 2 were nontoxic, whereas the extracts of freshly mixed and set AH Plus and RealSeal sealers were toxic to HGF cells (P < ."( In vitro cytotoxicity of guttaflow 2 on human gingival fibroblasts.
Huang, Y; Liu, J; Mandal, P; Sah, SK; Zhao, J, 2014
)
0.4
"Both GuttaFlow 2 and MTA evoked a less toxic response to HGF cells than AH Plus and RealSeal sealer."( In vitro cytotoxicity of guttaflow 2 on human gingival fibroblasts.
Huang, Y; Liu, J; Mandal, P; Sah, SK; Zhao, J, 2014
)
0.4
" Secondary outcome measures include delirium severity and duration assessed with the Delirium Rating Scale Revised 98; number of delirium-free days; adverse events; hospital length-of-stay; all-cause mortality; new institutionalisation; (Instrumental) Activities of Daily Living assessed with the Katz Index of ADL, and Lawton IADL scale; cognitive function assessed with the Six-item Cognitive Impairment Test, and the Dutch short form Informant Questionnaire on Cognitive Decline in the Elderly."( Efficacy and safety of haloperidol prophylaxis for delirium prevention in older medical and surgical at-risk patients acutely admitted to hospital through the emergency department: study protocol of a multicenter, randomised, double-blind, placebo-control
Anten, S; Bet, PM; Boelaarts, L; de Graaf, K; de Vries, OJ; Diepeveen, SH; Kamper, AM; Kramer, MH; Kuipéri, E; Lagaay, AM; Nanayakkara, PW; Pons, D; Schrijver, EJ; Siegel, A; van de Ven, PM; van Marum, RJ; van Strien, AM; Verburg, A, 2014
)
0.71
"The aim of this study was to compare the efficacy and side-effect profile of the typical antipsychotic haloperidol with that of the atypical antipsychotics risperidone, olanzapine, and aripiprazole in the management of delirium."( Haloperidol, risperidone, olanzapine and aripiprazole in the management of delirium: A comparison of efficacy, safety, and side effects.
Boettger, S; Breitbart, W; Jenewein, J, 2015
)
2.07
"The Memorial Delirium Assessment Scale (MDAS), the Karnofsky Performance Status (KPS) scale, and a side-effect rating were recorded at baseline (T1), after 2-3 days (T2), and after 4-7 days (T3)."( Haloperidol, risperidone, olanzapine and aripiprazole in the management of delirium: A comparison of efficacy, safety, and side effects.
Boettger, S; Breitbart, W; Jenewein, J, 2015
)
1.86
"Haloperidol, risperidone, aripiprazole, and olanzapine were equally effective in the management of delirium; however, they differed in terms of their side-effect profile."( Haloperidol, risperidone, olanzapine and aripiprazole in the management of delirium: A comparison of efficacy, safety, and side effects.
Boettger, S; Breitbart, W; Jenewein, J, 2015
)
3.3
"The reports submitted to the US Food and Drug Administration (FDA) Adverse Event Reporting System (FAERS) from 1997 to 2011 were reviewed to assess serious adverse events induced by the administration of antipsychotics to children."( Antipsychotics-associated serious adverse events in children: an analysis of the FAERS database.
Brown, JB; Kadoyama, K; Kimura, G; Miki, I; Nakamura, T; Nisiguchi, K; Okuno, Y; Sakaeda, T, 2015
)
0.42
" Signals in the data that signified a drug-associated adverse event were detected via quantitative data mining algorithms."( Antipsychotics-associated serious adverse events in children: an analysis of the FAERS database.
Brown, JB; Kadoyama, K; Kimura, G; Miki, I; Nakamura, T; Nisiguchi, K; Okuno, Y; Sakaeda, T, 2015
)
0.42
" Significant signals of the QT prolongation adverse event were detected only for ziprasidone and risperidone."( Antipsychotics-associated serious adverse events in children: an analysis of the FAERS database.
Brown, JB; Kadoyama, K; Kimura, G; Miki, I; Nakamura, T; Nisiguchi, K; Okuno, Y; Sakaeda, T, 2015
)
0.42
"It was suggested that there is a level of diversity in the strength of the association between various first- and second-generation antipsychotics with associated serious adverse events, which possibly lead to fatal outcomes."( Antipsychotics-associated serious adverse events in children: an analysis of the FAERS database.
Brown, JB; Kadoyama, K; Kimura, G; Miki, I; Nakamura, T; Nisiguchi, K; Okuno, Y; Sakaeda, T, 2015
)
0.42
"While antipsychotic-induced extrapyramidal symptoms (EPS) and akathisia remain important concerns in the treatment of patients with schizophrenia, the relationship between movement disorder rating scales and spontaneously reported EPS-related adverse events (EPS-AEs) remains unexplored."( Relating Spontaneously Reported Extrapyramidal Adverse Events to Movement Disorder Rating Scales.
Fleischhacker, WW; Karayal, ON; Kemmler, G; Kolluri, S; Vanderburg, D; Widschwendter, CG, 2015
)
0.42
" Haloperidol administration was not associated with treatment-limiting side-effects, but few studies used a systematic approach to identify adverse events."( Efficacy and safety of haloperidol for in-hospital delirium prevention and treatment: A systematic review of current evidence.
de Graaf, K; de Vries, OJ; Maier, AB; Nanayakkara, PW; Schrijver, EJ, 2016
)
1.66
" Moreover, its use is less toxic and safer."( Comparison of Pharmacological Potency and Safety of Glutamate Blocker IEM-1913 and Memantine.
Gmiro, VE; Serdyuk, SE; Veselkina, OS, 2015
)
0.42
" Generally, the antipsychotics significantly enhanced NRG1/ErbB signaling with increased expression of NRG1 and phosphorylation of ErbB4 and ErbB2 in the brain and myocardium, except that clozapine partly blocked the cardiac NRG1/ErbB2 activation, which could be associated with its more severe cardiac adverse actions."( Effects of prolonged antipsychotic administration on neuregulin-1/ErbB signaling in rat prefrontal cortex and myocardium: implications for the therapeutic action and cardiac adverse effect.
Cai, H; Dang, R; Guo, Y; Jiang, P; Liang, D; Lv, C; Yang, R, 2016
)
0.43
" The aim of the present study was to evaluate the adverse effects of BADGE on Rhinella arenarum by means of standardized bioassays at embryo-larval development."( Developmental toxicity of bisphenol A diglycidyl ether (epoxide resin badge) during the early life cycle of a native amphibian species.
Aronzon, CM; Hutler Wolkowicz, I; Pérez Coll, C; Svartz, GV, 2016
)
0.43
"Haloperidol was more effective than levosulpiride injection for psychotic symptoms, aggression, and severity of agitation in acute psychosis, but extrapyramidal adverse effects were less frequent with levosulpiride as compared with those receiving haloperidol."( Efficacy and Safety of Levosulpiride Versus Haloperidol Injection in Patients With Acute Psychosis: A Randomized Double-Blind Study.
Bains, HS; Kumar, A; Lavania, S; Praharaj, SK; Sinha, V,
)
1.84
"Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites."( Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
Jones, LH; Nadanaciva, S; Rana, P; Will, Y, 2016
)
0.43
"Driven by the need of pharmacovigilance centres and companies to routinely collect and review all available data about adverse drug reactions (ADRs) and adverse events of interest, we introduce and validate a computational framework exploiting dominant as well as emerging publicly available data sources for drug safety surveillance."( Exploiting heterogeneous publicly available data sources for drug safety surveillance: computational framework and case studies.
Jaulent, MC; Koutkias, VG; Lillo-Le Louët, A, 2017
)
0.46
" We acquired data from the FDA Adverse Event Reporting System (FAERS), PubMed and Twitter."( Exploiting heterogeneous publicly available data sources for drug safety surveillance: computational framework and case studies.
Jaulent, MC; Koutkias, VG; Lillo-Le Louët, A, 2017
)
0.46
" Pachymic acid could be a viable therapeutic agent to overcome the potential adverse effects associated with root canal sealers."( A Comparative Evaluation of the Effect of the Addition of Pachymic Acid on the Cytotoxicity of 4 Different Root Canal Sealers-An In Vitro Study.
Arun, S; Mahalaxmi, S; Rajkumar, K; Sampath, V, 2017
)
0.46
"Purpose To evaluate glass-fiber-based guidewires that are safe for magnetic resonance (MR) imaging-guided endovascular interventions by using a phantom and an in vivo swine model."( Glass-Fiber-based MR-safe Guidewire for MR Imaging-guided Endovascular Interventions: In Vitro and Preclinical in Vivo Feasibility Study.
Buecker, A; Massmann, A; Schneider, GK, 2017
)
0.46
"These results suggest that epigenetic changes at the striatal Drd2 promoter drive age-related increases in antipsychotic side effect susceptibility, and HDAC inhibitors may be an effective adjunct treatment strategy to reduce side effects in aged populations."( Histone deacetylase inhibitors reverse age-related increases in side effects of haloperidol in mice.
Csernansky, JG; Dong, H; Fang, D; Fisher, DW; Montalvo-Ortiz, JL; Rodríguez, G, 2017
)
0.68
" On hospital admission, serum level of lithium was far above toxic level."( Hypertensive bipolar: chronic lithium toxicity in patients taking ACE inhibitor.
Abdul Aziz, MF; Masiran, R, 2017
)
0.46
"As delirium in critically ill children is increasingly recognized, more children are treated with the antipsychotic drug haloperidol, while current dosing guidelines are lacking solid evidence and appear to be associated with a high risk of adverse events."( Monitoring Haloperidol Plasma Concentration and Associated Adverse Events in Critically Ill Children With Delirium: First Results of a Clinical Protocol Aimed to Monitor Efficacy and Safety.
de Wildt, SN; Ista, E; Jessurun, N; Slooff, VD; Tibboel, D; van Beusekom, BS; van den Dungen, DK, 2018
)
1.08
" Daily, adverse events were systematically assessed, haloperidol plasma concentrations were measured, and delirium symptoms followed."( Monitoring Haloperidol Plasma Concentration and Associated Adverse Events in Critically Ill Children With Delirium: First Results of a Clinical Protocol Aimed to Monitor Efficacy and Safety.
de Wildt, SN; Ista, E; Jessurun, N; Slooff, VD; Tibboel, D; van Beusekom, BS; van den Dungen, DK, 2018
)
1.12
" In all patients, pediatric delirium resolved, but five of 13 patients developed possible adverse event."( Monitoring Haloperidol Plasma Concentration and Associated Adverse Events in Critically Ill Children With Delirium: First Results of a Clinical Protocol Aimed to Monitor Efficacy and Safety.
de Wildt, SN; Ista, E; Jessurun, N; Slooff, VD; Tibboel, D; van Beusekom, BS; van den Dungen, DK, 2018
)
0.87
"Prospective systematic monitoring of adverse event in critically ill children receiving haloperidol revealed a significant proportion of possible adverse events."( Monitoring Haloperidol Plasma Concentration and Associated Adverse Events in Critically Ill Children With Delirium: First Results of a Clinical Protocol Aimed to Monitor Efficacy and Safety.
de Wildt, SN; Ista, E; Jessurun, N; Slooff, VD; Tibboel, D; van Beusekom, BS; van den Dungen, DK, 2018
)
1.09
"Based on findings from 34 blinded, randomized controlled trials, common acute adverse effects of second-generation antipsychotics and haloperidol were headache, dizziness, insomnia, and somnolence."( Evidence-Based Review Of Pharmacotherapy For Acute Agitation. Part 2: Safety.
Zun, LS, 2018
)
0.68
" The current report presents adverse events in an infant exposed to a combination of risperidone and haloperidol through breast milk."( Adverse Events in a Breastfed Infant Exposed to Risperidone and Haloperidol.
Uguz, F, 2019
)
0.97
" There was a significant difference between aripiprazole and placebo in the incidence rate of adverse events (AEs) for somnolence (RR = 6."( Safety of aripiprazole for tics in children and adolescents: A systematic review and meta-analysis.
Cui, H; Mao, J; Yang, C; Yi, Q; Zhang, L, 2019
)
0.51
" In terms of safety profiles, haloperidol was not associated with increased risk for QTc prolongation, extrapyramidal symptoms, or adverse events."( Efficacy and safety of haloperidol for delirium prevention in adult patients: An updated meta-analysis with trial sequential analysis of randomized controlled trials.
Chen, R; Chen, Z; Deng, Y; Guo, H; Hou, Y; Liu, G; Su, Y; Wei, X; Wen, S; Ye, Z; Zheng, D; Zuo, L, 2020
)
1.16
" A disproportionality analysis was performed to detect a signal for reporting "infective-pneumonia" and "pneumonia-aspiration" and antipsychotics using reports submitted between 2004 and 2019 to the FDA adverse events spontaneous reporting system (FAERS) database."( Exploring a Safety Signal of Antipsychotic-Associated Pneumonia: A Pharmacovigilance-Pharmacodynamic Study.
Cepaityte, D; Egberts, T; Kouvelas, D; Leucht, S; Papazisis, G; Siafis, S, 2021
)
0.62
" Secondary outcomes included the proportion of patients who required rescue medications for agitation within 4 hours of initial IV olanzapine or IV haloperidol administration, incidence of adverse events and ICU length of stay."( A Retrospective Comparison of the Effectiveness and Safety of Intravenous Olanzapine Versus Intravenous Haloperidol for Agitation in Adult Intensive Care Unit Patients.
Abdallah, GT; Eche, IJ; Eche, IM; Hsu, D; Knoph, KN; Patel, P; Wang, M; Wong, A; Yankama, TT, 2022
)
1.14
" This material has been utilized to fabricate fire safe epoxy thermosets (EP)."( From herbicide to flame retardant: The lamellar-like phosphorus-bridged amitrole toward high fire safety epoxy resin with light smoke and low toxicity.
Ai, YF; Bai, WB; Jian, RK; Lin, YC; Liu, XD; Xie, RR, 2022
)
0.72
" The release of toxic gases (CO and HCN) and volatile organic compounds in the EP was also effectively inhibited at the same time."( Covalent grafting diazotized black phosphorus with ferrocene oligomer towards smoke suppression and toxicity reduction.
Qiu, S; Song, L; Wang, J; Yang, W; Zhou, Y; Zou, B, 2022
)
0.72
"Retrospective studies using spontaneous reporting system databases have provided a great understanding of adverse drug reactions (ADRs) in the real world, complementing the data obtained from randomized controlled trials."( Characteristics of adverse reactions among antipsychotic drugs using the Korean Adverse Event Reporting System database from 2010 to 2019.
Byeon, SJ; Chung, SJ; Oh, S, 2022
)
0.72
"Data were collected from the Korea Adverse Event Reporting System database between 2010 and 2019."( Characteristics of adverse reactions among antipsychotic drugs using the Korean Adverse Event Reporting System database from 2010 to 2019.
Byeon, SJ; Chung, SJ; Oh, S, 2022
)
0.72
"In total, 5067 adverse events associated with antipsychotic drugs were reported."( Characteristics of adverse reactions among antipsychotic drugs using the Korean Adverse Event Reporting System database from 2010 to 2019.
Byeon, SJ; Chung, SJ; Oh, S, 2022
)
0.72
" The frequent detection of bisphenols in maternal and fetal samples has raised concerns about their toxic effects on human embryonic development, especially on the development of the central nervous system."( Development of human retinal organoid models for bisphenol toxicity assessment.
Fang, Y; Gao, H; Ge, L; Gong, J; Kang, J; Li, M; Xu, H; Yang, C; Yang, J, 2022
)
0.72
"To compare the risk for in-hospital adverse events associated with oral haloperidol, olanzapine, quetiapine, and risperidone in older patients after major surgery."( Comparative Safety Analysis of Oral Antipsychotics for In-Hospital Adverse Clinical Events in Older Adults After Major Surgery : A Nationwide Cohort Study.
Bateman, BT; Ely, EW; Inouye, SK; Jones, RN; Kim, DH; Lee, SB; Levin, R; Marcantonio, ER; Metzger, E; Pandharipande, PP; Park, CM; Pisani, MA, 2023
)
1.14
"These results suggest that atypical antipsychotics and haloperidol have similar rates of in-hospital adverse clinical events in older patients with postoperative delirium who receive an oral low-to-moderate dose antipsychotic drug."( Comparative Safety Analysis of Oral Antipsychotics for In-Hospital Adverse Clinical Events in Older Adults After Major Surgery : A Nationwide Cohort Study.
Bateman, BT; Ely, EW; Inouye, SK; Jones, RN; Kim, DH; Lee, SB; Levin, R; Marcantonio, ER; Metzger, E; Pandharipande, PP; Park, CM; Pisani, MA, 2023
)
1.16

Pharmacokinetics

The extent and clinical significance of the pharmacokinetic interaction between fluoxetine and haloperidol was studied in 13 schizophrenic patients with prominent negative symptoms. A pharmacodynamic model was set up to quantitatively describe the time-dependent adaptation of HVA accumulation in the whole rat brain.

ExcerptReferenceRelevance
" Then, the principal pharmacokinetic data of haloperidol are exposed with a special emphasis on the lack of information about the correlations between plasma levels and clinical effects."( [Value of pharmacokinetic data during the treatment of psychoses with haloperidol].
Cottereau, MJ; Cuche, H; Deniker, P; Lôo, H; Zarifian, E, 1979
)
0.75
" These data were used to determine the pharmacokinetic factor(s) that correlate best with HL and RHL concentrations in hair."( Steady-state pharmacokinetics of haloperidol and reduced haloperidol in schizophrenic patients: analysis of factors determining their concentrations in hair.
Hasegawa, K; Hirayama, H; Matsuno, H; Nakashima, M; Sato, H; Uematsu, T, 1992
)
0.56
" The mean elimination half-life of 54."( Pharmacokinetics of haloperidol and reduced haloperidol in Chinese schizophrenic patients after intravenous and oral administration of haloperidol.
Chang, WH; Chen, H; Jann, MW; Lam, YW, 1992
)
0.61
" A pharmacodynamic model was set up to quantitatively describe the time-dependent adaptation of HVA accumulation in the whole rat brain during constant haloperidol administration."( A pharmacodynamic model to predict the time dependent adaptation of dopaminergic activity during constant concentrations of haloperidol.
Cheng, YF; Paalzow, LK, 1990
)
0.68
" This means that it has a long half-life measurable in months rather than weeks."( Single-dose pharmacokinetics of fluphenazine after fluphenazine decanoate administration.
Cooper, TB; Levinson, DF; Lo, ES; Simpson, GM; Stephanos, MJ; Yadalam, KG, 1990
)
0.28
" Results suggested an absorption half-life of 4 weeks, although, in three cases steady state was only achieved after 11 monthly injections."( Pharmacokinetics of haloperidol and fluphenazine decanoates in chronic schizophrenia.
McCreadie, RG; Whitehead, A; Wiles, DH, 1990
)
0.6
" The authors examined the possibilities of a pharmacokinetic effect of alprazolam on neuroleptic plasma levels and of a clinical effect of alprazolam."( Neuroleptic augmentation with alprazolam: clinical effects and pharmacokinetic correlates.
Angrist, B; Cooper, T; Douyon, R; Peselow, E; Rotrosen, J, 1989
)
0.28
" However, there is large interindividual, but not intraindividual, variability in plasma haloperidol concentrations and most pharmacokinetic parameters."( Pharmacokinetics of haloperidol.
Davis, CM; Froemming, JS; Jann, MW; Lam, YW, 1989
)
0.82
" The distributions of these pharmacokinetic parameters about their respective means were each leptokurtotic and skewed toward higher values."( Intersubject variation in the pharmacokinetics of haloperidol and reduced haloperidol.
Chakraborty, BS; Ganes, DA; Hawes, EM; Hubbard, JW; Keegan, DL; Korchinski, ED; McKay, G; Midha, KK, 1989
)
0.53
" The plasma RHAL:HAL ratios on days 6 and 7 were higher than and positively correlated with those at Tmax after a single dose of HAL and were negatively correlated with the HAL:RHAL ratios at Tmax after a single dose of RHAL."( Pharmacodynamics and pharmacokinetics of haloperidol and reduced haloperidol in schizophrenic patients.
Chang, WH; Chen, CT; Chen, TY; Hu, WH; Jann, MW; Lam, YW; Lin, SK; Yeh, EK, 1989
)
0.54
" The enanthate produces peak plasma concentrations on days 2 to 3 and declines with an apparent elimination half-life (i."( Clinical pharmacokinetics of the depot antipsychotics.
Ereshefsky, L; Jann, MW; Saklad, SR,
)
0.13
" Moreover pharmacokinetic data increasingly have been clinically applied."( Chemotherapy with neuroleptics. Clinical and pharmacokinetic aspects with a particular view to depot preparations.
Knudsen, P, 1985
)
0.27
"Precise pharmacokinetic data of long-acting neuroleptics: apparent half life (T 1/2), time of peak plasma concentration (Tmax), bioavailability, has been a major contribution to determine optimal dosage of the drug."( [Clinical pharmacokinetics of haloperidol decanoate. Comparison with other prolonged-action neuroleptics].
Levron, JC; Ropert, R,
)
0.42
" Both agents possess similar pharmacodynamic properties which are consistent with central antidopaminergic activity."( Bromperidol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in psychoses.
Benfield, P; Clark, BG; Jue, SG; Ward, A, 1988
)
0.27
" Serum levels of haloperidol were determined by high performance liquid chromatography and serum concentration data obtained were submitted to pharmacokinetic analysis."( Pharmacokinetics of haloperidol in psychotic patients.
Bondesson, U; Cheng, YF; Ekblom, B; Eriksson, K; Eriksson, SO; Lindberg, A; Lindström, L; Paalzow, LK, 1987
)
0.94
" Haloperidol decanoate has no intrinsic activity: its pharmacodynamic actions are those of haloperidol--primarily that of central antidopamine activity."( Haloperidol decanoate. A preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in psychosis.
Beresford, R; Ward, A, 1987
)
2.63
" Within each interval between doses, haloperidol plasma levels were maximal within the first week after each dose, decaying with an average half-life of three weeks."( Pharmacology, pharmacokinetics and clinical development of haloperidol decanoate.
Gelders, YG, 1986
)
0.79
" The pharmacokinetic parameters of both the distribution and elimination phases were similar in each forebrain region for both haloperidol and amphetamine."( Unilateral cerebral drug administration: pharmacokinetics of haloperidol and amphetamine.
Hyde, JF; Jerussi, TP, 1987
)
0.72
" A possible increase in anticholinergic symptoms and a pharmacokinetic interaction are reported in literature."( Combination therapy with haloperidol and orphenadrine in schizophrenia. A clinical and pharmacokinetic study.
Altamura, AC; Buccio, M; Cazzullo, CL; Colombo, G; Terzi, A,
)
0.43
" We conclude that hypophysectomy may enhance the ability of haloperidol to induce striatal dopamine receptor supersensitivity in the rat, and that this may be due to differences in the pharmacokinetic handling of haloperidol between sham-operated and hypophysectomized animals."( Hypophysectomy may non-selectively alter pharmacokinetic parameters to enhance the ability of haloperidol to increase striatal dopamine receptor density in the rat.
Jenner, P; Marsden, CD; Simpson, MD, 1986
)
0.73
" The program enables the analysis of pharmacokinetic drug level profiles with a high degree of precision."( STRITERFIT, a least-squares pharmacokinetic curve-fitting package using a programmable calculator.
Schwerzel, E; Thornhill, DP, 1985
)
0.27
"The pharmacokinetic behaviour of haloperidol (0."( Pharmacokinetics and effects of haloperidol in the isolated mouse.
Baumann, GH; Zetler, G, 1985
)
0.83
"The future of depot neuroleptic therapy is discussed in terms of pharmacokinetic and pharmacodynamic research opportunities."( Future of depot neuroleptic therapy: pharmacokinetic and pharmacodynamic approaches.
Davis, CM; Ereshefsky, L; Jann, MW; Richards, A; Saklad, SR; Seidel, DR, 1984
)
0.27
" Four to 5 Cmin were monitored just before the morning valproic acid dose for 3 to 4 days preceding the kinetic study."( The effects of neuroleptics (haloperidol and chlorpromazine) on the pharmacokinetics of valproic acid in schizophrenic patients.
Chiba, K; Iizuka, R; Ishizaki, T; Kobayashi, K; Saito, M, 1984
)
0.56
" The results indicate that the analgesic effect of morphine in the tail-flick test is correlated better with the spinal than cerebral morphine levels and that potentiation of morphine analgesia by haloperidol is due, at least in part, to pharmacokinetic interaction."( Behavioral and pharmacokinetic interaction between morphine and haloperidol in the rat.
Adamus, A; Melzacka, M; Vetulani, J,
)
0.56
" After a bolus administration, plasma and brain concentrations were significantly higher at later time points, the plasma elimination half-life was significantly longer and the estimated plasma clearance was lower in 32- to 34- than in 3- to 4-month-old animals."( Age effects on haloperidol pharmacokinetics in male, Fischer-344 rats.
Kapetanovic, IM; Rapoport, SI; Sweeney, DJ, 1982
)
0.62
" The biological half-life of 15."( Haloperidol pharmacokinetics: a preliminary study in rhesus monkeys using a new radioimmunoassay procedure.
Barrow, A; Forrest, TJ; Jackson, LS; Palmer, RF; Stafford, JE, 1981
)
1.71
"The investigation was designed to study plasma drug concentration and prolactin response determined by two different doses of haloperidol, a standard one and four-fold higher the other, and to explore the relationships between clinical effects and pharmacokinetic and physiological variables in psychotic patients."( [Standard and high doses of haloperidol. Clinical, pharmacokinetic and pharmacodynamic aspects].
Birkner, R; Delgado, S; Duran, E; Haverbeck, C; Katz, I; Kohen, P; Schilkrut, R,
)
0.63
" Most traditional antipsychotic drugs have similar pharmacokinetic profiles that differ from the newer agents in several key respects."( Brief comparison of the pharmacokinetics and pharmacodynamics of the traditional and newer antipsychotic drugs.
DeVane, CL, 1995
)
0.29
"A pharmacodynamic interactional study with omeprazole was undertaken in rats."( Pharmacodynamic interactions of omeprazole with CNS active drugs in rats.
Chakrabarti, A; Chandrashekhar, SM; Garg, SK, 1995
)
0.29
" Mean pharmacokinetic parameters of haloperidol in the presence of alosetron and placebo treatments were not significantly (P > ."( Effect of alosetron (a new 5-HT3 receptor antagonist) on the pharmacokinetics of haloperidol in schizophrenic patients.
Gupta, SK; Kunka, RL; Lloyd, T; Metz, A; Perel, JM; Rudolph, G, 1995
)
0.79
"The purpose of the study was to investigate clinical and pharmacokinetic parameters concerning perphenazine decanoate (PD) and haloperidol decanoate (HD) with an interval of 3 weeks during a study period of 51 weeks."( A long-term cross-over pharmacokinetic study comparing perphenazine decanoate and haloperidol decanoate in schizophrenic patients.
Dencker, SJ; Giös, I; Mårtensson, E; Nordén, T; Nyberg, G; Persson, R; Roman, G; Stockman, O; Svärd, KO, 1994
)
0.72
" To deal with pharmacokinetic aspects two main topics are discussed in this paper: (A) the interindividual differences in bioavailability and metabolism and (B) the plasma level-clinical response relationship."( A multidimensional (pharmacokinetic and clinical-biological) approach to neuroleptic response in schizophrenia. With particular reference to drug resistance.
Altamura, AC, 1993
)
0.29
"A double-blind, placebo-controlled study using 12 healthy men was designed to evaluate pharmacokinetic and pharmacodynamic interactions when nefazodone and haloperidol are coadministered."( Investigation of pharmacokinetic and pharmacodynamic interactions after coadministration of nefazodone and haloperidol.
Barbhaiya, RH; Breul, HP; Greene, DS; Midha, KK; Shukla, UA, 1996
)
0.7
"The pharmacokinetic interaction between buspirone and haloperidol was evaluated in schizophrenic patients in two different groups."( Lack of pharmacokinetic interaction between buspirone and haloperidol in patients with schizophrenia.
Chang, TP; Chang, WH; Chen, JS; Chien, CP; Huang, HF; Jann, MW; Juang, DJ; Lam, YW; Lin, SK; Wei, FC, 1996
)
0.79
" These pharmacokinetic changes were not due to the changes in the rate of MAP metabolism."( Effects of haloperidol and cocaine pretreatments on brain distribution and kinetics of [11C]methamphetamine in methamphetamine sensitized dog: application of PET to drug pharmacokinetic study.
Fujiwara, T; Funaki, Y; Hishinuma, T; Ido, T; Ishiwata, S; Itoh, M; Iwata, R; Mizugaki, M; Nakamura, H; Numachi, Y; Sato, M; Tomioka, Y; Yanai, K; Yoshida, S, 1997
)
0.69
"The extent and clinical significance of the pharmacokinetic interaction between fluoxetine and haloperidol was studied in 13 schizophrenic patients with prominent negative symptoms."( Interaction between fluoxetine and haloperidol: pharmacokinetic and clinical implications.
Avenoso, A; Campo, G; Caputi, AP; Facciolă, G; Ferlito, M; Perucca, E; Spinà, E; Zuccaro, P, 1997
)
0.79
"The objective of this study was to examine neuroleptic effectiveness among Asians and Caucasians, and to investigate inter-ethnic pharmacodynamic differences."( An investigation of ethnic and gender differences in the pharmacodynamics of haloperidol.
Bean, G; Beiser, M; Zhang-Wong, J; Zipursky, RB, 1998
)
0.53
"Pharmacokinetic and pharmacodynamic interactions between the gastrokinetic drug cisapride and the antipsychotic drugs bromperidol and haloperidol were studied in 29 schizophrenic inpatients."( No pharmacokinetic but pharmacodynamic interactions between cisapride and bromperidol or haloperidol.
Furukori, H; Inoue, Y; Ishida, M; Kaneko, S; Kondo, T; Mihara, K; Nagashima, U; Otani, K; Suzuki, A; Yasui, N, 1999
)
0.73
" The aim of this study was to investigate possible pharmacokinetic interactions of neuroleptic haloperidol with the beta-blocker carteolol and the anticholinergic biperiden."( Pharmacokinetic and pharmacodynamic interactions among haloperidol, carteolol hydrochloride and biperiden hydrochloride.
Aoki, S; Hisazumi, H; Isawa, S; Kudo, S; Kumagai, Y; Miura, S; Murasaki, M; Uchiumi, M; Yoshioka, M, 1999
)
0.77
" Pharmacokinetic interactions occur between haloperidol and various drugs given concomitantly, for example, carbamazepine, phenytoin, phenobarbital, fluoxetine, fluvoxamine, nefazodone, venlafaxine, buspirone, alprazolam, rifampicin (rifampin), quinidine and carteolol."( Pharmacokinetics of haloperidol: an update.
Ishizaki, T; Kudo, S, 1999
)
0.89
"Retrospective population pharmacokinetic study."( Population pharmacokinetics of haloperidol using routine clinical pharmacokinetic data in Japanese patients.
Anai, M; Goto, Y; Higuchi, S; Hokazono, T; Ichimaru, R; Maki, T; Matsunaga, K; Ohdo, S; Yukawa, E; Yukawa, M, 2002
)
0.6
"Routine clinical pharmacokinetic data gathered from patients receiving haloperidol were analysed to estimate population pharmacokinetic parameters with the nonlinear mixed effects model (NONMEM) computer program."( Population pharmacokinetics of haloperidol using routine clinical pharmacokinetic data in Japanese patients.
Anai, M; Goto, Y; Higuchi, S; Hokazono, T; Ichimaru, R; Maki, T; Matsunaga, K; Ohdo, S; Yukawa, E; Yukawa, M, 2002
)
0.83
"The final pharmacokinetic model was CL = 42."( Population pharmacokinetics of haloperidol using routine clinical pharmacokinetic data in Japanese patients.
Anai, M; Goto, Y; Higuchi, S; Hokazono, T; Ichimaru, R; Maki, T; Matsunaga, K; Ohdo, S; Yukawa, E; Yukawa, M, 2002
)
0.6
" Despite a statistically significant greater mean elimination half-life (19."( Pharmacokinetics and QT interval pharmacodynamics of oral haloperidol in poor and extensive metabolizers of CYP2D6.
Arefayene, M; Desai, M; Desta, Z; Flockhart, DA; Gorski, JC; Li, L; Liu, Y; Tanus-Santos, JE, 2003
)
0.56
" A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals."( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004
)
0.32
" By allometric scaling of in vivo animal data, clearance of PNU-96391 in humans was over-predicted by 4-fold, half-life was under-predicted by 3-fold, and volume of distribution was accurately predicted."( Comparison of prediction methods for in vivo clearance of (S,S)-3-[3-(methylsulfonyl)phenyl]-1-propylpiperidine hydrochloride, a dopamine D2 receptor antagonist, in humans.
Black, ML; Duncan, JN; Toth, LN; Yamazaki, S, 2004
)
0.32
", reference drug), and also to estimate the pharmacokinetic parameters of haloperidol in Korean volunteers."( Pharmacokinetics and bioequivalence of haloperidol tablet by liquid chromatographic mass spectrometry with electrospray ionization.
Kwon, JT; Kwon, KI; Yun, MH, 2005
)
0.83
" Recent studies with a 103-compound dataset suggested that scaling from monkey pharmacokinetic data tended to be the most accurate method for predicting human clearance."( Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
Evans, CA; Jolivette, LJ; Nagilla, R; Ward, KW, 2006
)
0.33
" The pharmacokinetics of haloperidol and its pharmacodynamic effects measured for QTc prolongation and neurologic side effects were evaluated after a single dose of 5 mg haloperidol following a pretreatment of placebo or itraconazole at 200 mg/d for 10 days in a randomized crossover manner."( Combined effects of itraconazole and CYP2D6*10 genetic polymorphism on the pharmacokinetics and pharmacodynamics of haloperidol in healthy subjects.
Cha, IJ; Jung, HJ; Kim, KA; Park, JY; Shim, JC; Shin, JG; Shon, JH; Yoon, YR, 2006
)
0.85
"We have presented pharmacokinetic parameters of bromperidol (BP) in 14 healthy Korean subjects."( Pharmacokinetic parameters of bromperidol in Korean subjects.
Kim, HG; Kim, JW; Kim, YG; Lee, SY, 2006
)
0.33
"3 mg/kg haloperidol, however, exhibited similar pharmacodynamic effects in both genotypes."( Pharmacodynamic consequences of P-glycoprotein-dependent pharmacokinetics of risperidone and haloperidol in mice.
Henken, S; Hiemke, C; Kirschbaum, KM; Schmitt, U, 2008
)
1
" The results showed that [(3)H]PB28 and the corresponding unlabelled PB28 had superimposed pharmacodynamic properties."( Tritium radiolabelling of PB28, a potent sigma-2 receptor ligand: pharmacokinetic and pharmacodynamic characterization.
Abate, C; Berardi, F; Colabufo, NA; Contino, M; Ferorelli, S; Inglese, C; Perrone, R, 2008
)
0.35
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" Noncompartmental analysis was used to estimate pharmacokinetic parameters."( Comparison of intranasal administration of haloperidol with intravenous and intramuscular administration: a pilot pharmacokinetic study.
Archer, SM; Ashford, JW; Miller, JL; Rudy, AC; Wermeling, DP, 2008
)
0.61
"A simple and rapid RP-HPLC-DAD method was developed and validated for simultaneous determination of the dopamine antagonists haloperidol, its diazepane analog, and the dopamine agonist bromocriptine in rat plasma, to perform pharmacokinetic drug-interaction studies."( Simultaneous RP-HPLC-DAD quantification of bromocriptine, haloperidol and its diazepane structural analog in rat plasma with droperidol as internal standard for application to drug-interaction pharmacokinetics.
Ablordeppey, SY; Billups, J; Jackson, TL; Jones, C; Spencer, SD, 2010
)
0.81
" Pharmacokinetic parameters in brain and plasma were determined for SYA013."( Evaluation of the behavioral and pharmacokinetic profile of SYA013, a homopiperazine analog of haloperidol in rats.
Ablordeppey, SY; Boateng, B; Bricker, B; Jackson, T; Zhu, XY, 2012
)
0.6
" blood pressure, heart rate, body temperature) can be reduced, possibly due to a pharmacodynamic interaction at the serotonin reuptake transporter (SERT)."( Pharmacokinetics and pharmacodynamics of 3,4-methylenedioxymethamphetamine (MDMA): interindividual differences due to polymorphisms and drug-drug interactions.
Hondebrink, L; Meulenbelt, J; Rietjens, SJ; Westerink, RH, 2012
)
0.38
" Here we tested the pharmacodynamic consequences of these properties in a P-gp deficient mouse model by studying the effects of aripiprazole and of ziprasidone on motor coordination."( Pharmacodynamic effects of aripiprazole and ziprasidone with respect to p-glycoprotein substrate properties.
Frisch, J; Hiemke, C; Holthoewer, D; Kirschbaum, KM; Schmitt, U, 2013
)
0.39
"Evidence was given that P-gp substrate properties have pharmacodynamic consequences for aripiprazole but not for ziprasidone and thus affect dopamine receptor related motor behaviour."( Pharmacodynamic effects of aripiprazole and ziprasidone with respect to p-glycoprotein substrate properties.
Frisch, J; Hiemke, C; Holthoewer, D; Kirschbaum, KM; Schmitt, U, 2013
)
0.39
"Volume of distribution is one of the most important pharmacokinetic properties of a drug candidate."( Volume of Distribution in Drug Design.
Beaumont, K; Di, L; Maurer, TS; Smith, DA, 2015
)
0.42
" With the aid of the efficient and reliable simultaneous LC-ESI-MS/MS assay this pharmacokinetic study provided insights into their therapeutic targets of these three iridoid glycosides as well as valuable experimental basis for an expansion of their clinical indications."( A pre-clinical pharmacokinetic study in rats of three naturally occurring iridoid glycosides, Picroside-I, II and III, using a validated simultaneous HPLC-MS/MS assay.
Liu, L; Liu, M; Ma, B; Qi, H; Wang, Y; Wu, Z; Xue, B; Yao, D; Ying, H; Zhang, Q; Zhu, J, 2015
)
0.42
"This review gives an overview of how the pharmacokinetics in terminally ill patients may differ from the average population and discusses the effect of terminal illness on each of the four pharmacokinetic processes absorption, distribution, metabolism, and elimination."( Pharmacokinetic considerations and recommendations in palliative care, with focus on morphine, midazolam and haloperidol.
Baar, FP; de Winter, BC; Franken, LG; Koch, BC; Mathôt, RA; Tibboel, D; van Esch, HJ; van Gelder, T; van Zuylen, L, 2016
)
0.65
" We therefore designed a population pharmacokinetic study to gain more insight into the pharmacokinetics of haloperidol in terminally ill patients and to find clinically relevant covariates that may be used in developing an individualised dosing regimen."( Population pharmacokinetics of haloperidol in terminally ill adult patients.
Baar, FPM; de Winter, BCM; Franken, LG; Koch, BCP; Masman, AD; Mathot, RAA; Tibboel, D; van Gelder, T, 2017
)
0.95
"2), a population pharmacokinetic analysis was conducted with 87 samples from 28 terminally ill patients who received haloperidol either orally or subcutaneously."( Population pharmacokinetics of haloperidol in terminally ill adult patients.
Baar, FPM; de Winter, BCM; Franken, LG; Koch, BCP; Masman, AD; Mathot, RAA; Tibboel, D; van Gelder, T, 2017
)
0.95
" This resulted in an average terminal half-life of haloperidol of around 30 h."( Population pharmacokinetics of haloperidol in terminally ill adult patients.
Baar, FPM; de Winter, BCM; Franken, LG; Koch, BCP; Masman, AD; Mathot, RAA; Tibboel, D; van Gelder, T, 2017
)
0.99
" Studies reporting the pharmacokinetic parameters of CYP1A2-metabolized antipsychotic drugs in individuals who were genotyped for CYP1A2 genetic polymorphisms were retrieved."( Impact of CYP1A2 genetic polymorphisms on pharmacokinetics of antipsychotic drugs: a systematic review and meta-analysis.
Hanprasertpong, N; Koonrungsesomboon, N; Na Takuathung, M; Teekachunhatean, S, 2019
)
0.51
" With this review, we aim to provide an overview of the pharmacodynamic interactions between ketamine and mood stabilizers, benzodiazepines, monoamine oxidase-inhibitors, antipsychotics, and psychostimulants."( Pharmacodynamic Interactions Between Ketamine and Psychiatric Medications Used in the Treatment of Depression: A Systematic Review.
Bakker, IM; Kamphuis, J; Schoevers, RA; Smith-Apeldoorn, SY; Touw, DJ; Veraart, JKE; Visser, BAE, 2021
)
0.62
" More studies are needed to provide insight into pharmacodynamic interactions with ketamine."( Pharmacodynamic Interactions Between Ketamine and Psychiatric Medications Used in the Treatment of Depression: A Systematic Review.
Bakker, IM; Kamphuis, J; Schoevers, RA; Smith-Apeldoorn, SY; Touw, DJ; Veraart, JKE; Visser, BAE, 2021
)
0.62

Compound-Compound Interactions

The aim of this work was to investigate the effect on antioxidant potential of some commonly used drugs. Volunteers who were given haloperidol combined with sleep deprivation exhibited an elevation of the duration and density of the STW. The aim of the research is to estimate the influence of lithium on the parameters of oxidative stress and viability of SH-SY5Y cell lines.

ExcerptReferenceRelevance
") alone or in combination with haloperidol (0."( Effects produced by acute and chronic treatment with granisetron alone or in combination with haloperidol on midbrain dopamine neurons.
Ashby, CR; Minabe, Y; Wang, RY, 1992
)
0.79
"Effects of cocaine, alone and in combination with the dopaminergic antagonists, SCH 23390 and haloperidol were studied in squirrel monkeys trained to respond under fixed-interval schedules of electric-shock presentation."( Behavioral effects of cocaine alone and in combination with selective dopamine antagonists in the squirrel monkey.
Katz, JL; Witkin, JM, 1991
)
0.5
"To assess the roles of substance P in neurologic or psychiatric illnesses, effects of acute or chronic (40- or 80-day dietary) treatment with trihexyphenidyl and carbamazepine alone or in combination with haloperidol on substance P content were investigated in the rat brain."( Effects of chronic treatment with trihexyphenidyl and carbamazepine alone or in combination with haloperidol on substance P content in rat brain: a possible implication of substance P in affective disorders.
Mataga, N; Mitsushio, H; Takashima, M; Toru, M, 1988
)
0.68
" Serum triiodothyronine (T3) and T4 by radioimmunoassay showed that PTU alone and in combination with Li lowered serum T4, while a high level of T4 by its supplement was suppressed by co-administration of Li."( Effect of lithium carbonate administration singly or in combination with some psychotropic drugs on the radioiodide uptake by mouse thyroid.
Akamatsu, S; Kamata, N; Kawada, J; Kurata, M; Kuwae, T; Minakuchi, K; Nishida, M; Takasugi, M; Teraoka, K, 1989
)
0.28
"Lithium (250 mg/kg IP) administered in combination with haloperidol (2-5 mg/kg IP) or thyrotropin-releasing hormone (TRH) (10 or 20 mg/kg, IP) evoked jumping in mice."( Lithium in combination with haloperidol or thyrotropin-releasing hormone induces jumping in mice.
Furukawa, T; Ushijima, I; Yamada, K, 1982
)
0.8
" This suggests that scanning electron microscopy combined with energy dispersive X-ray microanalysis is useful for detecting carbon particles in the cytoplasm at an ultrastructural level in semi-thin epoxy sections subsequent to ion etching and that this method may be applicable to other cell markers, such as gold particles to track cells in the field of cell development and cell differentiation."( A new method for detecting and localizing cell markers endocytosed by fibroblasts in epoxy resin semi-thin sections using scanning electron microscopy combined with energy dispersive X-ray microanalysis after ion-etching.
Aoyagi, S; Fujiwara, T; Isshiki, N; Kon, K; Shimizu, D; Tsunokuni, H, 2000
)
0.31
" The volunteers who were given haloperidol combined with sleep deprivation exhibited an elevation of the duration and density of the STW, without significant alterations of the other REM sleep phasic phenomena such as rapid eye movement."( Sawtooth waves during REM sleep after administration of haloperidol combined with total sleep deprivation in healthy young subjects.
Peres, CA; Pinto, LR; Remesar-Lopez, AJ; Russo, RH; Tufik, S, 2002
)
0.85
"1 mg/kg) in combination with fluvoxamine also caused a selective increase in extracellular DA levels in the cortex."( Sulpiride in combination with fluvoxamine increases in vivo dopamine release selectively in rat prefrontal cortex.
Ago, Y; Baba, A; Matsuda, T; Nakamura, S, 2005
)
0.33
" As ciproxifan and thioperamide are inhibitors of cytochrome P450 enzymes, responsible for metabolizing risperidone and haloperidol, the possibility that the augmentation of antipsychotics by imidazoles resulted from drug-drug interactions was tested."( Lack of cataleptogenic potentiation with non-imidazole H3 receptor antagonists reveals potential drug-drug interactions between imidazole-based H3 receptor antagonists and antipsychotic drugs.
Ballard, ME; Cowart, M; Decker, MW; Esbenshade, TA; Faghih, R; Fox, GB; Hancock, AA; Pan, L; Roberts, S; Rueter, LE; Zhang, M, 2005
)
0.54
"To compare oral risperidone and intramuscular (IM) haloperidol, both in combination with IM lorazepam, in the management of acute agitation and psychosis in the medical emergency department."( Risperidone versus haloperidol, in combination with lorazepam, in the treatment of acute agitation and psychosis: a pilot, randomized, double-blind, placebo-controlled trial.
Currier, GW; McMullan, JT; Veser, BD; Veser, FH; Zealberg, J, 2006
)
0.91
" In this study, we sought to further examine this mechanism using a novel drug-drug conditioning procedure."( An investigation of the behavioral mechanisms of antipsychotic action using a drug-drug conditioning paradigm.
He, W; Li, M; Mead, A, 2009
)
0.35
"To compare the short- and long-term sealing ability of root canal fillings consisting of AH-26 and laterally compacted gutta-percha in combination with a self-etching dentin bonding system and the Epiphany-Resilon system."( Long-term evaluation of the sealing ability of two root canal sealers in combination with self-etching bonding agents.
Economides, N; Gogos, C; Helvatjoglu-Antoniades, M; Kokorikos, I; Kolokouris, I, 2009
)
0.35
"The Epiphany-Resilon system and the group obturated with AH-26 sealer and gutta-percha, in combination with the self-etching bonding system after removal of the smear layer with EDTA, demonstrated similar sealing ability."( Long-term evaluation of the sealing ability of two root canal sealers in combination with self-etching bonding agents.
Economides, N; Gogos, C; Helvatjoglu-Antoniades, M; Kokorikos, I; Kolokouris, I, 2009
)
0.35
"The aim of this work was to investigate the effect on antioxidant potential of some commonly used drugs (morphine, tramadol, bromocriptine, haloperidol and azithromycin) on immobilization stress (IS) combined with cold restraint stress (CRS) in the rat."( Antioxidant effects of some drugs on immobilization stress combined with cold restraint stress.
Janicijevic-Hudomal, S; Kaurinovic, B; Popovic, M; Rasic, J; Trivic, S; Vojnović, M, 2009
)
0.55
" This study was conducted to investigate the efficacy and tolerability of zotepine compared to haloperidol in combination with a mood stabilizer (lithium or valproate) for treatment of acute mania."( A single-blind, comparative study of zotepine versus haloperidol in combination with a mood stabilizer for patients with moderate-to-severe mania.
Chan, HY; Chang, CJ; Chen, CH; Chen, JJ; Chiu, NY; Jou, SH; Juang, YY, 2010
)
0.83
"In combination with a mood stabilizer, zotepine appears to be as effective as haloperidol in treating moderate-to-severe mania in the acute phase, but has the advantages of lowering hyperuricemia and fewer extrapyramidal side-effects."( A single-blind, comparative study of zotepine versus haloperidol in combination with a mood stabilizer for patients with moderate-to-severe mania.
Chan, HY; Chang, CJ; Chen, CH; Chen, JJ; Chiu, NY; Jou, SH; Juang, YY, 2010
)
0.84
" VU0364770 showed efficacy alone or when administered in combination with L-DOPA or an adenosine 2A (A2A) receptor antagonist currently in clinical development (preladenant)."( The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease.
Amalric, M; Blobaum, AL; Bode, J; Bridges, TM; Bubser, M; Conn, PJ; Daniels, JS; Dickerson, JW; Engers, DW; Hopkins, CR; Italiano, K; Jadhav, S; Jones, CK; Lindsley, CW; Morrison, RD; Niswender, CM; Thompson, AD; Turle-Lorenzo, N, 2012
)
0.38
" This practice of polypharmacy increases the possibility for drug-drug interactions."( Drug-drug conditioning between citalopram and haloperidol or olanzapine in a conditioned avoidance response model: implications for polypharmacy in schizophrenia.
Li, M; Sparkman, NL, 2012
)
0.64
"To determine the most common drug-drug interaction (DDI) pairs contributing to QTc prolongation in cardiac intensive care units (ICUs)."( Drug-drug interactions contributing to QT prolongation in cardiac intensive care units.
Armahizer, MJ; Kane-Gill, SL; Seybert, AL; Smithburger, PL, 2013
)
0.39
"We examined whether MK-801 in combination with CA receptor ligands, which inhibit CAergic neuronal activities, could induce anesthesia including LORR."( Selective blockade of N-methyl-D-aspartate channels in combination with dopamine receptor antagonism induces loss of the righting reflex in mice, but not immobility.
Irifune, M; Kanematsu, T; Kikuchi, N; Morioka, N; Morita, K; Nakata, Y; Sakai, N; Shimizu, Y; Yoshida, K, 2015
)
0.42
" In contrast, MK-801 in combination with a small dose of the dopamine (DA) receptor antagonist haloperidol (0."( Selective blockade of N-methyl-D-aspartate channels in combination with dopamine receptor antagonism induces loss of the righting reflex in mice, but not immobility.
Irifune, M; Kanematsu, T; Kikuchi, N; Morioka, N; Morita, K; Nakata, Y; Sakai, N; Shimizu, Y; Yoshida, K, 2015
)
0.64
" This study sought to identify which dose of haloperidol 1mg or 2mg could be combined with dexamethasone without adverse effects in high-risk patients undergoing gynecological laparoscopic surgery."( Haloperidol dose combined with dexamethasone for PONV prophylaxis in high-risk patients undergoing gynecological laparoscopic surgery: a prospective, randomized, double-blind, dose-response and placebo-controlled study.
Baek, J; Joo, J; Moon, YE; Park, YG, 2015
)
2.12
" The aim of this research is to estimate the influence of lithium (alone and in combination with haloperidol) on the parameters of oxidative stress and viability of SH-SY5Y cell lines in neutral and pro-oxidative conditions."( Impact of lithium alone or in combination with haloperidol on oxidative stress parameters and cell viability in SH-SY5Y cell culture.
Gawlik-Kotelnicka, O; Lazarek, J; Mielicki, W; Rabe-Jabłońska, J; Strzelecki, D, 2016
)
0.91
"1) To provide a comparison of the frequency with which FGAs are administered with adjunctive benzodiazepines or anticholinergic medications."( First-generation Antipsychotics Are Often Prescribed in the Emergency Department but Are Often Not Administered with Adjunctive Medications.
Campillo, A; Castillo, E; Hopper, A; Ryan, V; Vilke, GM; Wilson, MP, 2015
)
0.42
"The aim of study was to investigate the effects of pyrroloquinoline quinone (PQQ) combined with d-serine on the modulation of glycine sites in the brain of rats using social recognition test."( Modulation of glycine sites enhances social memory in rats using PQQ combined with d-serine.
Liu, D; Mao, S; Peng, Y; Qin, X; Zhang, R; Zhou, X, 2016
)
0.43
"The aim of this study was to observe potential drug-drug interactions in the medication of Mexican schizophrenic patients."( Potential drug-drug interaction in Mexican patients with schizophrenia.
de la O de la O, ME; Genis, A; González-Castro, TB; Juárez-Rojop, IE; Lilia López-Narváez, M; Nicolini, H; Ocaña-Zurita, MC; Tovilla-Zárate, CA, 2016
)
0.43
"html ) was used in this study to analyse potential drug-drug interactions."( Potential drug-drug interaction in Mexican patients with schizophrenia.
de la O de la O, ME; Genis, A; González-Castro, TB; Juárez-Rojop, IE; Lilia López-Narváez, M; Nicolini, H; Ocaña-Zurita, MC; Tovilla-Zárate, CA, 2016
)
0.43
"In total, 86 of 126 patients were at risk of potential drug-drug interactions."( Potential drug-drug interaction in Mexican patients with schizophrenia.
de la O de la O, ME; Genis, A; González-Castro, TB; Juárez-Rojop, IE; Lilia López-Narváez, M; Nicolini, H; Ocaña-Zurita, MC; Tovilla-Zárate, CA, 2016
)
0.43
" The potential drug-drug interactions observed in the Mexican population are consistent with the concomitant use of antipsychotics, benzodiazepines, and antidepressants prescribed in schizophrenia that could cause central nervous system (CNS) depression and anticholinergic effect."( Potential drug-drug interaction in Mexican patients with schizophrenia.
de la O de la O, ME; Genis, A; González-Castro, TB; Juárez-Rojop, IE; Lilia López-Narváez, M; Nicolini, H; Ocaña-Zurita, MC; Tovilla-Zárate, CA, 2016
)
0.43
" For these people, a number of treatment strategies have emerged, including the prescription of a second anti-psychotic drug in combination with clozapine."( Clozapine combined with different antipsychotic drugs for treatment-resistant schizophrenia.
Barber, S; Cipriani, A; Corsi, M; Olotu, U, 2017
)
0.46
" The present study used a conditioned avoidance response (CAR) test (a behavioral test of antipsychotic effect) and examined the specific drug-drug interactions between nicotine and haloperidol or clozapine."( A drug-drug conditioning paradigm reveals multiple antipsychotic-nicotine interactions.
Feng, M; Li, M; Sparkman, NL; Sui, N, 2017
)
0.65
"Clinical studies that focused on treating schizophrenia showed that Calculus Bovis Sativus (CBS), a substitute of Calculus Bovis, when used in combination with haloperidol could significantly lower the dosage of haloperidol compared with treatment with haloperidol alone, whereas efficacy was maintained."( Investigation of the synergistic effects of haloperidol combined with Calculus Bovis Sativus in treating MK-801-induced schizophrenia in rats.
He, GF; He, GZ; Lei, K; Li, J; Li, XP; Liu, D; Liu, YN; Ren, XH; Zhang, CL, 2018
)
0.94
"To evaluate the clinical curative effect of warm gutta-percha filling technique combined with different sealers in root canal filling."( [Curative effect of warm gutta-percha filling technique combined with different sealers in root canal filling].
Luo, YJ; Shu, Y, 2018
)
0.48
"The root canal sealing effects of warm gutta-percha filling technique combined with iRoot SP or AH plus or Vitapex are good."( [Curative effect of warm gutta-percha filling technique combined with different sealers in root canal filling].
Luo, YJ; Shu, Y, 2018
)
0.48
"This study is aimed at evaluating the effects of FiberSite and glass fiber postsystems on the fracture resistance of endodontically restored teeth, when combined with various root canal sealers."( Comparison of Fracture Resistance of Endodontically Treated Teeth Restored with FiberSite Postsystem and Glass Fiber, Combined with Different Root Canal Sealers.
Eren, B; Gulsahi, K; Kandemir, B; Ozasir, T, 2021
)
0.62
"Pharmacokinetic (PK) drug-drug interactions (DDIs) of oral haloperidol, a first-generation antipsychotic, are systematically reviewed."( Pharmacokinetic drug interactions with oral haloperidol in adults: dose correction factors from a combined weighted analysis.
de Leon, J; Hiemke, C; McGrane, I; Spina, E, 2022
)
1.23
" MATERIAL AND METHODS For this in vitro study, we tested 92 extracted human teeth, which were divided into 3 groups after a preparation technique and obturation with Endomethasone N sealer, glass ionomer cement, and EndoRez sealer in combination with Thermafil obturator."( Evaluation of Apical Leakage After Root Canal Obturation with Glass Ionomer, Resin, and Zinc Oxide Eugenol Sealers Combined with Thermafil.
Ajeti, N; Kuçi, A; Meqa, K; Stavileci, M; Vula, V, 2022
)
0.72
"To determine the clinical efficacy of ultrasonic irrigation combined with epoxy resin-based sealer in single visit root canal treatment of chronic pulpitis."( Effect of Ultrasonic Irrigation Combined with Epoxy Resin Paste in Single Visit Root Canal Treatment in Chronic Pulpitis.
Wang, J; Wang, N; Zhang, CF; Zhu, XY, 2023
)
0.91
"Ultrasonic irrigation combined with epoxy resin-based paste yields better results for chronic pulpitis treatment, reducing postoperative pain, mitigating inflammation levels, and enhancing quality of life."( Effect of Ultrasonic Irrigation Combined with Epoxy Resin Paste in Single Visit Root Canal Treatment in Chronic Pulpitis.
Wang, J; Wang, N; Zhang, CF; Zhu, XY, 2023
)
0.91

Bioavailability

Large doses of haloperidol can safely be given intravenously and intramuscularly. The bioavailability of this agent administered orally ranges from 60 to 65%. Elimination half-life (t1/2 beta) and bioavailability (F) were calculated for both groups.

ExcerptReferenceRelevance
" Data in adult patients illustrate on the one hand possible causes of variability in plasma levels of haloperidol and, on the other hand, the fact that poor bioavailability is not the cause of lack of response in 'resistant' schizophrenic patients."( Clinical significance of monitoring plasma levels of psychotropic drugs.
Morselli, PL; Zarifian, E, 1979
)
0.48
" A relatively small change in absorption rate occurred when the splanchnic blood flow rate was decreased about 35%."( Drug absorption VII: influence of mesenteric blood flow on intestinal drug absorption in dogs.
Crouthamel, WG; Diamond, L; Dittert, LW; Doluisio, JT, 1975
)
0.25
" After oral dosing, bioavailability of haloperidol was 35 +/- 8%, suggesting extensive first pass metabolism."( Pharmacokinetics of haloperidol and reduced haloperidol in Chinese schizophrenic patients after intravenous and oral administration of haloperidol.
Chang, WH; Chen, H; Jann, MW; Lam, YW, 1992
)
0.88
" bioavailability and a relatively long duration of action."( Pharmacology of risperidone (R 64 766), a new antipsychotic with serotonin-S2 and dopamine-D2 antagonistic properties.
Awouters, F; Janssen, PA; Meert, TF; Megens, AA; Niemegeers, CJ; Schellekens, KH, 1988
)
0.27
" Large doses of haloperidol can safely be given intravenously and intramuscularly for rapid neuroleptisation; the bioavailability of this agent administered orally ranges from 60 to 65%."( Pharmacokinetics of haloperidol.
Davis, CM; Froemming, JS; Jann, MW; Lam, YW, 1989
)
0.95
"The bioavailability of a new tablet formulation (5 mg) of haloperidol was estimated relative to two lots of a reference product."( Comparative bioavailability of a new commercial tablet formulation and two lots of a reference formulation of haloperidol.
Chakraborty, BS; Hawes, EM; Hubbard, JW; McKay, G; Midha, KK; Schwede, R, 1989
)
0.73
" The absorption rate constant is slower than the elimination rate constant and therefore, the depot antipsychotics exhibit 'flip-flop' kinetics where the time to steady-state is a function of the absorption rate, and the concentration at steady-state is a function of the elimination rate."( Clinical pharmacokinetics of the depot antipsychotics.
Ereshefsky, L; Jann, MW; Saklad, SR,
)
0.13
" This variation for fluphenazine may be explained by the fact that its pKa value is closer to that of piracetam, thus preventing better bioavailability of the neuroleptic, or its better affinity for DA-1 dopaminergic receptors."( Piracetam interactions with neuroleptics in psychopharmacological tests.
Bourin, M; Larousse, C; Poisson, L, 1986
)
0.27
" Optimal dose has been determined from the bioavailability of the oral formulation and the interval between two injections, it averages 15, 20 times the oral daily dose for haloperidol decanoate."( [Clinical pharmacokinetics of haloperidol decanoate. Comparison with other prolonged-action neuroleptics].
Levron, JC; Ropert, R,
)
0.61
" Lorazepam is an excellent first choice because of its intermediate half-life, absence of active metabolites, and high bioavailability that can be achieved with a number of routes of administration."( Emerging treatment options in the alcohol withdrawal syndrome.
Rosenbloom, A, 1988
)
0.27
" Consequently, for a drug mainly eliminated by hepatic metabolism like haloperidol, the total blood clearance and the extent of oral bioavailability can be affected by changes in hepatic blood flow, hepatic enzyme activities and drug binding."( Pharmacokinetics of haloperidol in psychotic patients.
Bondesson, U; Cheng, YF; Ekblom, B; Eriksson, K; Eriksson, SO; Lindberg, A; Lindström, L; Paalzow, LK, 1987
)
0.83
" Elimination half-life (t1/2 beta) and bioavailability (F) were calculated for both groups from haloperidol serum concentrations determined by gas-liquid chromatography."( Elimination half-life and bioavailability of haloperidol in schizophrenic patients.
Hollister, LE; Magliozzi, JR, 1985
)
0.75
" These preclinical data support its use as an antipsychotic agent and show that it is well absorbed following oral administration with an apparent elimination half-life of approximately 24 h, supporting a once-daily dose regimen."( Bromperidol, a new butyrophenone neuroleptic: a review.
Dubinsky, B; Janssen, PA; McGuire, JL; McKenzie, BE; Niemegeers, CJ; Weintraub, HS, 1982
)
0.26
" In chronic unresponsive schizophrenic patients, poor drug bioavailability is not the major factor for the lack of response, and the possibility that these patients constitute a nosological subgroup is suggested."( Haloperidol plasma level monitoring in neuropsychiatric patients.
Bianchetti, G; Dugas, M; Morselli, PL, 1982
)
1.71
" were in accordance with the bioavailability of haloperidol."( Influence of route of administration on haloperidol plasma levels in psychotic patients.
Bianchetti, G; Deniker, P; Morselli, PL; Poirier-Littre, MF; Zarifian, E, 1980
)
0.78
" The newer antipsychotic agents clozapine and risperidone are also well absorbed and undergo extensive presystemic elimination."( Brief comparison of the pharmacokinetics and pharmacodynamics of the traditional and newer antipsychotic drugs.
DeVane, CL, 1995
)
0.29
" Plasma concentrations of the hormone were determined until 240 min post administration by ELISA, and the absolute bioavailability was estimated to be in the vicinity of 20%."( Epithelial transport and bioavailability of intranasally administered human growth hormone formulated with the absorption enhancers didecanoyl-L-alpha-phosphatidylcholine and alpha-cyclodextrin in rabbits.
Agerholm, C; Bastholm, L; Elling, F; Johansen, PB; Nielsen, MH, 1994
)
0.29
" These results indicate a marked behavioral difference in the effects of haloperidol in drug-naive and chronically treated rats which is not related to an altered bioavailability of the drug and which is dissociated from both basal and haloperidol induced effects on dopamine and acetylcholine release in both brain regions."( Acute versus chronic haloperidol: relationship between tolerance to catalepsy and striatal and accumbens dopamine, GABA and acetylcholine release.
Beck, O; O'Connor, WT; Osborne, PG; Ungerstedt, U, 1994
)
0.84
" To deal with pharmacokinetic aspects two main topics are discussed in this paper: (A) the interindividual differences in bioavailability and metabolism and (B) the plasma level-clinical response relationship."( A multidimensional (pharmacokinetic and clinical-biological) approach to neuroleptic response in schizophrenia. With particular reference to drug resistance.
Altamura, AC, 1993
)
0.29
" Compound 36 is an antagonist of hD4 receptors with good oral bioavailability of 38%, a half life of 2 h, and brain levels 10-fold higher than plasma levels."( 4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor.
Baker, R; Ball, R; Broughton, HB; Collins, I; Davey, WB; Emms, F; Freedman, SB; Leeson, PD; Marwood, R; Patel, S; Ragan, CI; Rowley, M, 1997
)
0.3
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
" Limited oral bioavailability of AC-90179 likely reflects rapid metabolism rather than poor absorption."( Pharmacological characterization of AC-90179 [2-(4-methoxyphenyl)-N-(4-methyl-benzyl)-N-(1-methyl-piperidin-4-yl)-acetamide hydrochloride]: a selective serotonin 2A receptor inverse agonist.
Andersson, CM; Bradley, SR; Brann, MR; Davis, RE; Hacksell, U; Harvey, SC; Kold, H; Makhay, M; Son, T; Spalding, TA; Tolf, BR; Vanover, KE; Veinbergs, I; Weiner, DM, 2004
)
0.32
" The bioavailability and pharmacokinetics of haloperidol tablets were examined on 24 healthy volunteers who received a single oral dose of each preparation in the fasting state in a randomized balanced 2 way crossover design."( Pharmacokinetics and bioequivalence of haloperidol tablet by liquid chromatographic mass spectrometry with electrospray ionization.
Kwon, JT; Kwon, KI; Yun, MH, 2005
)
0.86
" However, limited peptide stability and oral bioavailability have prevented these compounds from being developed as relevant pharmaceuticals."( Design, synthesis, and evaluation of the antipsychotic potential of orally bioavailable neurotensin (8-13) analogues containing non-natural arginine and lysine residues.
Dix, TA; Hadden, MK; Kokko, KP; Mazella, J; Orwig, KS, 2005
)
0.33
"The drug-transporting P-glycoprotein transports drugs against a concentration gradient across the blood-brain barrier back into the plasma and thereby reduces the bioavailability in the brain."( Association between multidrug resistance 1 (MDR1) gene polymorphisms and therapeutic response to bromperidol in schizophrenic patients: a preliminary study.
Kaneda, A; Kaneko, S; Nakagami, T; Saito, M; Tateishi, T; Yasui-Furukori, N, 2006
)
0.33
" New dopamine D4 receptor agonists, exemplified by (E)-1-(4-chlorophenyl)-3-(4-pyridin-2-ylpiperazin-1-yl)propan-1-one O-methyloxime (59a) and (E)-1-(3-chloro-4-fluorophenyl)-3-(4-pyridin-2-ylpiperazin-1-yl)propan-1-one O-methyloxime (64a), exhibited favorable pharmacokinetic profiles and showed oral bioavailability in rat and dog."( 1-aryl-3-(4-pyridine-2-ylpiperazin-1-yl)propan-1-one oximes as potent dopamine D4 receptor agonists for the treatment of erectile dysfunction.
Bhatia, P; Brioni, JD; Chang, R; Donnelly-Roberts, DL; El Kouhen, O; Hakeem, AA; Henry, R; Hollingsworth, PR; Hsieh, GC; Kolasa, T; Marsh, KC; Martino, B; Matulenko, MA; Miller, LN; Moreland, RB; Mortell, K; Nakane, M; Namovic, MT; Patel, MV; Stewart, AO; Terranova, MA; Uchic, ME; Wetter, JM, 2006
)
0.33
"The goal of this study was to identify a structurally distinct D(4)-selective agonist with superior oral bioavailability to our first-generation clinical candidate 1a (ABT-724) for the potential treatment of erectile dysfunction."( Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction.
Brioni, JD; Chang, R; Cowart, MD; Darbyshire, JF; Donnelly-Roberts, DL; El-Kouhen, OF; Gintant, G; Hakeem, AA; Hollingsworth, PR; Hsieh, GC; Kolasa, T; Marsh, KC; Martin, R; Martino, BR; Matulenko, MA; Miller, LN; Moreland, RB; Mortell, K; Nakane, M; Namovic, MT; Nelson, SL; Patel, MV; Rohde, JJ; Stewart, AO; Sullivan, JP; Terranova, MA; Uchic, ME; Wetter, JM, 2006
)
0.33
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34
" In addition, this series of compounds has demonstrated good bioavailability and in vivo efficacy in a rodent model of Parkinson's disease, despite having reduced potency for the rat A2A receptor versus the human A2A receptor."( Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy.
Castro-Palomino, JC; Chen, Y; Crespo, MI; Díaz, JL; Gross, RS; Gual, S; Joswig, T; Lanier, MC; Lechner, SM; Lin, E; Malany, S; Markison, S; Moorjani, M; O'Brien, Z; Prat, M; Rueter, JK; Santos, M; Saunders, J; Slee, DH; Wen, J; Williams, JP; Zhang, X, 2008
)
0.35
" Mean (percent coefficient of variation) haloperidol bioavailability after intranasal administration was 63."( Comparison of intranasal administration of haloperidol with intravenous and intramuscular administration: a pilot pharmacokinetic study.
Archer, SM; Ashford, JW; Miller, JL; Rudy, AC; Wermeling, DP, 2008
)
0.87
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
" Therefore, dissolution rate rather than solubility may be the best predictor of bioavailability for such compounds."( Solution-mediated phase transformation of salts during dissolution: investigation using haloperidol as a model drug.
Bogner, R; Greco, K; Mcnamara, DP, 2011
)
0.59
" Preliminary tests for oral bioavailability also revealed promising results for this new class of potential antipsychotic compounds."( Molecular combination of the dopamine and serotonin scaffolds yield in novel antipsychotic drug candidates - characterization by in vivo experiments.
Enzensperger, C; Fleck, C; Lehmann, J; Mueller, FK; Robaa, D; Schulze, M; Siol, O, 2012
)
0.38
"We describe the discovery of potent and orally bioavailable tetrahydropyridopyrimidine inhibitors of phosphodiesterase 10A by systematic optimization of a novel HTS lead."( Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
Breslin, MJ; Coleman, PJ; Cox, CD; Fandozzi, C; Fuerst, J; Hill, N; Huszar, S; Kandebo, M; Kim, SH; Ma, B; McGaughey, G; Raheem, IT; Renger, JJ; Schreier, JD; Sharma, S; Smith, S; Uslaner, J; Yan, Y, 2012
)
0.38
" This multifunctional drug candidate is orally bioavailable and exhibits good antipsychotic efficacy in vivo."( Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.
Beard, JD; Davis, RE; Hendrick, JP; Lee, T; Li, P; Mates, S; Peng, Y; Robichaud, AJ; Snyder, GL; Tomesch, J; Vanover, KE; Wennogle, LP; Yao, W; Zhang, Q; Zhu, H, 2014
)
0.4
" Upon cytotoxicity test with a human cell line, the succinoglycan dimers displayed little effect up to 1000 μM, suggesting their potential usage to improve solubility and bioavailability of poorly soluble therapeutic agents."( Solubilization of haloperidol by acyclic succinoglycan oligosaccharides.
Cho, E; Choi, JM; Choi, Y; Jung, S; Kim, H; Lee, IS, 2012
)
0.71
", ip) indicate that the liver is the primary site of biotransformation of the compound, suggesting that both 22a and its metabolite(s) are active, compensating probably low bioavailability of the parent molecule."( Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Bednarski, M; Gunia-Krzyżak, A; Marona, H; Nitek, W; Pękala, E; Powroźnik, B; Słoczyńska, K; Walczak, M; Waszkielewicz, AM; Żesławska, E, 2016
)
0.43
"Cell membrane permeability is an important determinant for oral absorption and bioavailability of a drug molecule."( Highly predictive and interpretable models for PAMPA permeability.
Jadhav, A; Kerns, E; Nguyen, K; Shah, P; Sun, H; Xu, X; Yan, Z; Yu, KR, 2017
)
0.46
" Losartan carboxylic acid (LCA), the potent AT1 blocker metabolite of losartan, suffers from poor bioavailability and brain access."( Conjugation to Ascorbic Acid Enhances Brain Availability of Losartan Carboxylic Acid and Protects Against Parkinsonism in Rats.
Prusty, S; Sahu, PK; Singh, VK; Subudhi, BB, 2018
)
0.48
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" Additionally, an ∼85% correlation was obtained between PAMPA pH 5 permeability and in vivo oral bioavailability in mice and rats."( Using in vitro ADME data for lead compound selection: An emphasis on PAMPA pH 5 permeability and oral bioavailability.
Itkin, M; Kabir, M; Mathé, EA; Nguyễn, ÐT; Padilha, EC; Shah, P; Shinn, P; Siramshetty, V; Wang, AQ; Williams, J; Xu, X; Yu, KR; Zhao, T, 2022
)
0.72

Dosage Studied

Daily dosing requirements were less in the elderly for intermittent intravenous lorazepam, haloperidol, and morphine but not for midazolam. 25 years of experience have indicated that haloperodol can be used safely and effectively to manage a variety of psychiatric illnesses. dosage and method of administration are adjusted to individual patients' needs.

ExcerptRelevanceReference
" Therefore, monitoring treatment by dosage adjustment alone is of little value."( Plasma level monitoring of antipsychotic drugs.
Cooper, TB,
)
0.13
" Their plasma levels are not correlated with their dosage in a man to another, but, for some of them, there is lineary relation for one person."( [Relations between the levels of neuroleptics and the doses, the therapeutic effects and the side effects].
Andersson, JC; Davy, JP; Halbecq, JJ; Morel, P; Moulin, M; Poilpre, E, 1978
)
0.26
"The dose-response relationship for d-amphetamine (0."( Actions and interactions of amphetamine on self-stimulation in rats.
Aulakh, CS; Pradhan, SN, 1979
)
0.26
"01) 6 hours after dosing by metoclopramide 40 mg, and haloperidol 5 mg and 10 mg, when compared to placebo."( Metoclopramide and haloperidol in tardive dyskinesia.
Bateman, DN; Dutta, DK; McClelland, HA; Rawlins, MD, 1979
)
0.84
" A dosing strategy for the combbination of clomipramine and haloperidol is described."( [The treatment of chronic pain symptoms with psychotropic drugs (author's transl)].
Kocher, R, 1976
)
0.5
" SHPGE2, PGE2, and C did not cause catalepsy and did not show statistically significant dose-response antagonism of rotational behavior at less than toxic doses."( Neuropharmacological and behavioral evaluation of prostaglandin E2 and 11-thiol-11-desoxy prostaglandin E2 in the mouse and rat.
Bloss, JL; Singer, GH, 1978
)
0.26
" A clearcut dosage schedule for in- and out-patients using imipramine (Tofranil) or chlorimipramine (Anafranil) and haloperidol (Haldol) is established."( [The treatment of chronic pain with psychotropic drugs].
Kocher, R, 1978
)
0.47
"The effect of various antipsychotic drugs on the blockade of dopaminergic receptors in striatum and limbic forebrain was examined by establishing dose-response curves for the increase in HVA and for the antagonism of d-amphetamine-induced rotation in rats with unilateral lesions of the substantia nigra."( On the significance of the increase in homovanillic acid (HVA) caused by antipsychotic drugs in corpus striatum and limbic forebrain.
Dingell, JV; Hill, H; Robinson, SE; Setler, P; Stawarz, RJ; Sulser, F, 1975
)
0.25
" Side effects were common on a dosage of 3 mg haloperidol daily."( Haloperiodl in the treatment of stuttering.
Campbell, L; Kelly, P; Murray, TJ; Stefanik, K, 1977
)
0.52
" This phenomenon may also contribute to explain the complex dose-response curves of apomorphine."( Agonist--antagonist interaction on dopamine receptors in brain, as reflected in the rates of tyrosine and tryptophan hydroxylation.
Carlsson, A; Kehr, W; Lindqvist, M, 1977
)
0.26
"In a double blind chlorpromazine-controlled trial, high dosage haloperidol (100 mg daily) given for three months, appreciably improved the mental state of male chronic 'drug resistant' schizophrenic inpatients in the rehabilitation/long-stay unit of one psychiatric hospital."( High dosage haloperidol in chronic schizophrenia.
MacDonald, IM; McCreadie, RG, 1977
)
0.88
", as needed over a four-hour period (total dosage ranging from 4 to 32 mg."( Relative efficacy of parenteral haloperidol and thiothixene for the emergency treatment of acutely excited and agitated patients.
Stotsky, BA, 1977
)
0.54
" The optimal dosage of bromperidol seemed to lie between 4 and 6 mg/day."( Results of a clinical trial with bromperidol C-C 2489/21.
Weiser, G,
)
0.13
" Patients were treated up to 30 days and the dosage of bromperidol was increased depending on effects and side-effects up to 5 mg per day."( Effects and side-effects of bromperidol in comparison with other antipsychotic drugs.
Woggon, B,
)
0.13
"The high dosage of bromperidol as used in this investigation was a safe and effective agent in the treatment of alcohol-induced delirium tremens."( Interim report: high dosage bromperidol therapy of delirium tremens.
Schmatolla, E,
)
0.13
"Nine refractory chronic psychotics were switched to a lower dosage of, mostly, a long-acting diphenylbutylpiperidine after having been treated with high initial and maintenance doses of Haldol."( A six-month follow-up of refractory chronic psychotics treated with Haldol-AID.
Wouters, J,
)
0.13
" The employed dosage caused no strong sedation."( Double-blind comparison of bromperidol and perphenazine.
Angst, J; Woggon, B, 1978
)
0.26
" With exception of the pancreas, a dosage of dependent increase of the 3H-leucine incorporation was observed in the treated animals."( [Influence of haloperidol on the 3H-leucine incorporation in incretory organs of the mouse (author's transl)].
Hackenberg, P; Lange, E, 1978
)
0.62
" The initial doses varied widely, ranging from 1 to 30 mg, with a maximum total daily dosage of 100 mg."( Overview: efficacy and safety of the rapid neuroleptization method with injectable haloperidol.
Donlon, PT; Hopkin, J; Tupin, JP, 1979
)
0.48
" In the 1-day dosage group the amount of anticholinergics were significantly reduced (2."( [Extrapyamidal side-effects with 1-day dosage of haloperidol (author's transl)].
Matzner, G; Rüther, E; Uriarte, V, 1978
)
0.51
" Dose-response functions were determined for d- and l-amphetamine, alpha-methyltyrosine, and haloperidol."( Free-operant and auto-titration brain self-stimulation procedures in the rat: a comparison of drug effects.
Holtzman, SG; Schaefer, GJ, 1979
)
0.48
" In studying the dose-response relationship there appears to be a relationship between drug dose and polysome disaggregation in both groups of animals, although the effects were always greater in crowded mice."( Effect of crowding on amphetamine-induced disaggregation of brain polyribosomes.
Blackshear, MA; Proctor, CD; Wade, LH, 1979
)
0.26
"A randomized cross-over trial was conducted in 30 restless mentally subnormal patients by increasing the dosage of haloperidol from 10 to 60 mg and of thioridazine from 100 to 600 mg daily."( A controlled double-blind study of haloperidol versus thioridazine in the treatment of restless mentally subnormal patients. Serum levels and clinical effects.
Räisänen, P; Rimón, R; Väisänen, K; Viukari, M,
)
0.62
"A dose-response analysis was performed on D-amphetamine- and methylphenidate-induced changes in neuronal activity in the neostriatum of immobilized, phenidate-induced changes in neuronal activity in the neostriatum of immobilized, locally anesthetized rats."( Dose-dependent biphasic alterations in the spontaneous activity of neurons in the rat neostriatum produced by d-amphetamine and methylphenidate.
Rebec, GV; Segal, DS, 1978
)
0.26
" Similarly, a shift to the left of the haloperidol dose-response curve for the increase in striatal dopamine metabolite levels was observed in rats treated subacutely with the ester as compared to control rats."( Subsensitivity of striatal and mesolimbic dopamine target cells after repeated treatment with apomorphine dipivaloyl ester.
Scatton, B; Worms, P, 1978
)
0.53
"5 mg/kg, 24 h prior to the experiment) the dose-response curve was not significantly affected by haloperidol, a dopamine vascular receptor antagonist (10(-6)-3X10(-6) M)."( Studies on the positive inotropic effect of dopamine in the guinea-pig heart.
Ledda, F; Maccioni, T; Mantelli, L; Mugelli, A; Torrini, M, 1977
)
0.47
" With increase of antidepressants dosage received by a subordinate rat its competing ability becomes enhanced too; this may cause a change in domination."( [Effect of pharmacologic substances on the dominance-submission relationship in a pair of rats].
Kampov-Polevoi, AB, 1978
)
0.26
" When a similar dosage regimen was employed with pregnant rats beginning on day 16 of gestation, levodopa plus carbidopa delayed the average delivery time 12 hr."( Investigation of a dopaminergic mechanism for regulating oxytocin release.
Lewis, PR; Miller, JW; Seybold, VS, 1978
)
0.26
", circling behavior) in a spherical "rotometer" and dose-response relationships were generated using d-amphetamine, apomorphine, L-Dopa, haloperidol, and scopolamine."( Drug-induced rotation in rats without lesions: behavioral and neurochemical indices of a normal asymmetry in nigro-striatal function.
Glick, SD; Jerussi, TP, 1976
)
0.46
" Dose-response analyses of the effects of d-amphetamine, an indirectly acting dopamine agonist, and apomorphine, a directly acting dopamine agonist, revealed a shift in the dose-response curves following chronic morphine treatment, indicating that the animals were supersensitive to these agents."( Alterations in the effects of dopamine agonists and antagonists on general activity in rats following chronic morphine treatment.
Overstreet, DH; Smee, ML, 1976
)
0.26
" Desalivate rats showed a marked attenuation of feeding (and prandial drinking) at low doses, but when wet mash was given instead of pellets and water a normal dose-response relationship was obtained."( Feeding and drinking interactions after acute butyrophenone administration.
Engle, DJ; Rowland, N, 1977
)
0.26
"The dose-response effects of apomorphine and ET-495 (piribedil), 2 specific dopamine (DA) receptor stimulators, and haloperidol, a DA receptor blocker, were tested on the secretion of prolactin (PRL), thyroid stimulating hormone (TSH), growth hormone (GH) and luteinizing hormone (LH) in male rats."( Differential effects of dopamine agonists and haloperidol on release of prolactin, thyroid stimulating hormone, growth hormone and luteinizing hormone in rats.
Meites, J; Moore, KE; Mueller, GP; Simpkins, J, 1976
)
0.72
" A dosage schedule for in- and outpatients has been established, using imipramine (Tofranil) or chlorimipramine (Anafranil), and haloperidol (Haldol)."( The use of psychotropic drugs in the treatment of chronic, severe pains.
Kocher, R, 1976
)
0.46
" Fusaric acid produced a shift to the right and down in the dose-response curves to all tested agonists, and antagonized acetylcholine and serotonin most effectively among these agonists."( Relaxation of isolated rabbit arteries by fusaric (5-butylpicolinic) acid.
Asano, M; Hidaka, H, 1976
)
0.26
" Both At and Sc in a wide range of dosage protect against the tonic phase of convulsions produced by electroshock."( Central action of drugs acting on the cholinergic muscarinic receptor. III. Influence of atropine and scopolamine injected intraventricularly on behavior and levels of biogenic amines in the rat brain.
Kleinrok, Z; Poddubiuk, Z; Zebrowska-Lupina, I, 1975
)
0.25
" Dose-response curves and time-action curves were generated."( Differential sensitivity of two dopaminergic structures in rat brain to haloperidol and to clozapine.
Stanley, ME; Watson, E; Wilk, S, 1975
)
0.49
"There are many reasons why once a day oral dosage may be advantageous in administration of psychotropic drugs to mental patients, such as convenience for the patient, avoided side effects, ease of remembering, all of which contribute to reliable dosage as well as cost savings."( Clinical pharmacology and the prescription of psychotropic medication.
Davis, JM, 1975
)
0.25
"), the respondings were inhibited in proportion to the dosage except in DRL performance, in which only correct response rate decreased at 8 mg/kg."( [Effects of penfluridol, a psychotropic agent, on operant behavior of rats].
Kuribara, H; Okuizumi, K; Shirota, M; Tadokoro, S, 1975
)
0.25
" Intraventricular injection of phenylephrine produced a dose-dependent hypothermia, whereas no dose-response relationship was obtained by isoproterenol."( [Role of brain biogenic amines in the central thermoregulatory mechanism of the rat (author's transl)].
Fukushima, N, 1975
)
0.25
" Dose-response curves of apomorphine-stimulated motor activity and rearing behavior were shifted to the left when determined in mice during the period of withdrawal hyperactivity."( Supersensitivity to dopaminergic agonists induced by haloperidol.
Moore, KE; Thornburg, JE, 1975
)
0.5
" Zuclopenthixol also has the advantage for both patients and nursing staff that dosage is once daily."( Zuclopenthixol, melperone and haloperidol/levomepromazine in the elderly. Meta-analysis of two double-blind trials at 15 nursing homes in Norway.
Elgen, K; Fuglum, E; Nygaard, HA, 1992
)
0.57
" The patient was treated over a period of 48 days with a morphine dosage ranging from 10 to 60 mg/h, which kept her free of pain."( [Continuous ambulatory intravenous morphine infusion for pain therapy in advanced ovarian cancer].
Günter, HH; Hilfrich, J; Kühnle, H; Schönborn, I; Sorge, J; Steffmann, B, 1992
)
0.28
" Multiphasic dose-response relationships between the magnitudes, rates and apparent rate constants of release of DA and the concentration of the autoreceptor antagonist, haloperidol, were observed."( Blockade of dopamine autoreceptors by haloperidol and the apparent dynamics of potassium-stimulated endogenous release of dopamine from and reuptake into striatal suspensions in the rat.
McElvain, JS; Schenk, JO, 1992
)
0.75
"The human scalp hair is a useful tissue that retains the past dosage history over a rather long period of time, acting like a "tape-recorder"."( [Establishment of a method to analyze drugs in the hair and its application for determining patient compliance].
Uematsu, T, 1992
)
0.28
" For corticosterone determinations, mice were dosed on GD 10, and blood was collected at 1, 4, 24, or 48 hr after dosing."( The effect of teratogens on maternal corticosterone levels and cleft incidence in A/J mice.
Hansen, DK; Holson, RR; Sheehan, DM; Sullivan-Jones, P,
)
0.13
" In the previously reported case, factors capable of potentiating NMS included a high dosage of tetrabenazine exceeding the accepted therapeutic range, and co-medication with the dopamine-synthesis inhibitor alpha-methylparatyrosine, while in the present case abrupt introduction of the drug and discontinuation of concomitant neuroleptics may have contributed to this important adverse reaction."( Neuroleptic malignant syndrome related to tetrabenazine introduction and haloperidol discontinuation in Huntington's disease.
Giménez-Roldán, S; Mateo, D; Muñoz-Blanco, JL, 1992
)
0.52
" HD dosage was highly correlated with both RBC H and plasma H, but RBC RH and plasma RH were not significantly related to dosage at any time point."( Haloperidol decanoate pharmacokinetics in red blood cells and plasma.
Dysken, MW; Holden, L; Johnson, SB; Kim, SW; Skare, S; Thomsyck, L; Vatassery, G, 1992
)
1.73
" In the individually treated group the dosage was determined by a senior psychiatrist at the hospital who was not involved in collecting the data of the investigation; neither the nursing staff nor the physicians involved in thus study were informed of the dosages."( [Disagreement in standardized haloperidol treatment in comparison with "adequate individual dosage" of acutely schizophrenic patients].
Klieser, E; Lehmann, E, 1992
)
0.57
" Dosage was chosen and adjusted to the individual patient's condition and response."( Zuclopenthixol and haloperidol in patients with acute psychotic states. A double-blind, multi-centre study.
Eliander, H; Heikkilä, L; Pedersen, V; Turunen, M; Vartiainen, H, 1992
)
0.61
" Dose-response curves were determined at the conclusion of the chronic phase."( Sensitization to haloperidol-induced suppression of milk intake: effect of interdose interval.
Moore, J; Wolgin, DL, 1992
)
0.62
" The study indicates that haloperidol decanoate even in low dosage is effective maintenance therapy is preventing relapse."( Duration of neuroleptic treatment and relapse rate: a 5-year follow-up study with haloperidol decanoate.
Youssef, HA, 1991
)
0.81
" In the presence of a constant dose of prazosin, the dose-response curve for induction of rotation by AMPH was shifted to the right."( Differential modulation of (+)-amphetamine-induced rotation in unilateral substantia nigra-lesioned rats by alpha 1 as compared to alpha 2 agonists and antagonists.
Colpaert, FC; Mavridis, M; Millan, MJ, 1991
)
0.28
" The dose-response curve of haloperidol remained virtually unchanged, apparently because of the potent dopamine-D2 antagonism associated with these doses which may block the potentiating effect of apomorphine."( Functional interaction between serotonin-S2 and dopamine-D2 neurotransmission as revealed by selective antagonism of hyper-reactivity to tryptamine and apomorphine.
Awouters, F; Janssen, PA; Megens, AA; Niemegeers, CJ, 1990
)
0.57
" Interpatient variation in plasma HAL levels at a given dosage was up to sixfold."( Dose-dependent reduced haloperidol/haloperidol ratios in schizophrenic patients.
Chang, WH; Chen, H; Chen, TY; Hwu, HG; Lane, HY; Lin, HN; Lin, SK; Lin, WL; Wei, HL, 1991
)
0.59
"5 mg/kg/infusion), and shifted the dose-response curve for cocaine self-administration to the right."( GR38032F, a serotonin 5-HT3 antagonist, fails to alter cocaine self-administration in rats.
Peltier, R; Schenk, S, 1991
)
0.28
" Both 23390 and raclopride, which were used at low dosage (0."( Antagonism of EEGraphic and behavioural effects of methamphetamine by selective receptor blockers (SCH 23390 and raclopride) in the rabbit.
Albergati, A; Bo, P; Dallocchio, C; Marchioni, E; Savoldi, F, 1991
)
0.28
" The remaining 95 responding or nonresponding patients were then randomly assigned, double-blind, to a dosage of haloperidol two to 10 times higher (mean, 11."( Optimal dose of neuroleptic in acute schizophrenia. A controlled study of the neuroleptic threshold and higher haloperidol dose.
Hogarty, GE; McEvoy, JP; Steingard, S, 1991
)
0.7
" Dose-response studies of the effect of baclofen on prolactin (PRL) secretion were performed in stressed male rats."( Further evidence for the inhibitory action of baclofen on a prolactin-releasing factor.
Libertun, C; Lux-Lantos, V; Rey, E; Somoza, G, 1991
)
0.28
" The dose-response curves were found to be at least biphasic (small doses increased release and large doses inhibited release) and different in shape from dose-response curves for increases in the turnover of dopamine, suggesting that the two processes may not be related."( Effects of acute and chronic systemic administration of some typical antipsychotic drugs on turnover of dopamine and potassium ion-induced release of dopamine in the striatum of the rat in vivo.
Patterson, TA; Schenk, JO, 1991
)
0.28
" A shift in the dose-response function of amphetamine that occurred during these weeks, however, precluded appropriate analysis of haloperidol's effects."( Rebound cue state following a single dose of haloperidol.
Barrett, RJ; Caul, WF; Jones, JR; Murphy, SM; Schmidt, TA, 1991
)
0.75
" Dose-response curves for each drug were shifted to the left in the MPTP-treated mice, suggesting behavioral supersensitivity."( Dopamine receptors and sensorimotor behavior in MPTP-treated mice.
Bruno, JP; Hadjiconstantinou, M; Weihmuller, FB, 1990
)
0.28
" Remoxipride, at both dosage ranges used, thus had comparable therapeutic efficacy to that of haloperidol."( A double-blind multicentre comparison of remoxipride, at two dose levels, and haloperidol.
Agussol, P; Alby, JM; Brion, S; Burnat, G; Castelnau, D; Deluermoz, S; Dufour, H; Ferreri, M; Goudemand, M; Patris, M, 1990
)
0.73
" Because of the interaction between dopamine (DA) and neurotensin (NT) in the target areas of these systems, and in order to study if the different action of typical and atypical neuroleptic drugs could be related to a modification of the DA/NT balance, we investigated DA2 and NT receptor modifications--by means of quantitative receptor autoradiography--after chronic treatment with low dosage of haloperidol, chlorpromazine, thioridazine and clozapine."( DA2/NT receptor balance in the mesostriatal and mesolimbocortical systems after chronic treatment with typical and atypical neuroleptic drugs.
Amato, G; Calzà, L; Giardino, L; Piazza, PV; Zanni, M, 1990
)
0.45
" In the first series of experiments, dose-response curves were constructed for the inhibition of A9 and A10 dopamine cell firing by intravenous administration of the potent dopamine agonist, R-(-)-N-n-propylnorapomorphine (NPA)."( Irreversible receptor inactivation reveals differences in dopamine receptor reserve between A9 and A10 dopamine systems: an electrophysiological analysis.
Cox, RF; Waszczak, BL, 1990
)
0.28
" The distribution of both HP and RHP along the maternal hair paralleled the dosage of HP when hair growth was assumed to be 1 cm per month."( The measurement of haloperidol and reduced haloperidol in neonatal hair as an index of placental transfer of maternal haloperidol.
Matsuno, H; Nakashima, M; Uematsu, T; Yamada, K, 1991
)
0.61
") 20 min before cocaine resulted in a 4- to 8-fold parallel shift to the right in the cocaine dose-response function."( Pharmacological characterization of the discriminative stimulus effects of cocaine in rhesus monkeys.
Anthony, EW; Kleven, MS; Woolverton, WL, 1990
)
0.28
" These behaviors had a similar dose-response and time course and were blocked by the 5-HT2/5-HT1C antagonists mianserin, ritanserin, and methysergide."( Evidence for involvement of 5-HT2 and 5-HT1C receptors in the behavioral effects of the 5-HT agonist 1-(2,5-dimethoxy-4-iodophenyl aminopropane)-2 (DOI).
Pranzatelli, MR, 1990
)
0.28
" After increasing the dosage of prednisone, she recovered almost completely from this episode."( [Cerebral disseminated lupus erythematosus; brain-racking for patient and physician].
de Glas-Vos, JW; Prins, JM, 1990
)
0.28
" This property was reflected by a greater extent of inhibition of the binding of PCP-selective relative to sigma H-selective ligands at a given cation concentration, as well as by lower IC50's and by steeper slopes of the cation dose-response curves."( Differential modulation by cations of sigma and phencyclidine binding sites in rat brain.
Katki, AG; Rodbard, D; Schwarz, S; Zhou, GZ, 1990
)
0.28
"The patients reported in our previous paper were followed further, by analyzing hair samples collected monthly for 4 or 5 months, while growing hair continues to reflect the individual dosage history of haloperidol."( Human scalp hair as evidence of individual dosage history of haloperidol: longer-term follow-up study.
Sato, R; Uematsu, T, 1990
)
0.71
" Dose-response comparisons revealed that MK-801 was 3, 6, 19 and 119 times more potent at activating A10 neurons than PCP, (+)-SKF-10,047, ketamine and (+)-pentazocine, respectively."( Non-competitive N-methyl-D-aspartate antagonists are potent activators of ventral tegmental A10 dopamine neurons.
Ceci, A; French, ED, 1990
)
0.28
"Twenty-five inpatients with acute exacerbations of schizophrenia (by Research Diagnostic Criteria) or schizoaffective disorder underwent a prospective haloperidol dosing procedure and were assigned fixed doses chosen to yield a distribution of haloperidol plasma levels above and below a hypothesized upper therapeutic limit of 18 ng/ml."( Haloperidol plasma levels and acute clinical change in schizophrenia.
Coryell, W; Kelly, M; Miller, DD; Perry, PJ, 1990
)
1.92
" Twelve healthy male volunteers participated in four experimental occasions during each of which they were dosed with one of the following anti-psychotic drugs: chlorpromazine (50 mg), haloperidol (3 mg), sulpiride (400 mg) and placebo."( A comparison of the central nervous system effects of haloperidol, chlorpromazine and sulpiride in normal volunteers.
Cooper, SM; McClelland, GR; Pilgrim, AJ, 1990
)
0.72
" Hair from other patients, in whom the dosage of HL had been changed within a few months prior to sampling, was sectioned into 1 cm-long portions successively from the roots and the concentrations of both compounds in each portion were measured."( The measurement of haloperidol and reduced haloperidol in hair as an index of dosage history.
Matsuno, H; Nakashima, M; Uematsu, T, 1990
)
0.61
" The extract was also able to produce a rightward displacement of the apomorphine dose-response curve for stereotyped behavior and decrease the maximum response possible."( Effects of a Palicourea marcgravii leaf extract on some dopamine-related behaviors of rats.
de Souza-Spinosa, H; Górniak, SL; Palermo-Neto, J, 1990
)
0.28
" Thus, different dose-response curves were generated depending upon whether cathine or vehicle was administered the day before testing."( Discriminative stimulus properties of (+)cathine, an alkaloid of the khat plant.
Pehek, EA; Schechter, MD, 1990
)
0.28
"We have evaluated the efficacy and safety of different dosing regimens of haloperidol decanoate (HLD)."( Kinetics and clinical evaluation of haloperidol decanoate loading dose regimen.
Davis, CM; Ereshefsky, L; Lyman, RC; Saklad, SR; Toney, G; Tran-Johnson, T, 1990
)
0.78
" Prediction of steady-state concentrations on the basis of a mg/kg/day dosage (dose method), although equally precise, generated significantly less information concerning the variance between observed and predicted haloperidol plasma concentrations."( Pharmacokinetic protocol for predicting plasma haloperidol concentrations.
Arndt, SV; Coryell, WH; Kelly, MW; Miller, DD; Perry, PJ, 1990
)
0.72
" We sought to determine whether daily versus weekly dosing of haloperidol for 3 weeks produced distinct effects on DA, dihydroxyphenylacetic acid (DOPAC), and homovanillic acid (HVA) concentrations in multiple brain areas."( Sensitization versus tolerance to the dopamine turnover-elevating effects of haloperidol: the effect of regular/intermittent dosing.
Barnes, DE; Bellows, EP; Csernansky, JG; Lombrozo, L, 1990
)
0.75
" gamma E (beta-LPH-(61-77)), beta-endorphin-(1-17)), and DT gamma E (beta-LPH-(62-77), beta-endorphin-(2-17)) were without effect in the dosage used."( The effect of gamma-type endorphins on alpha-MSH release in the rat.
Andringa-Bakker, EA; de Rotte, AA; de Wied, D; van de Buuse, M; van Wimersma Greidanus, TB, 1985
)
0.27
" The dose-response curves of SKF 38393 were shifted in parallel to the right by butaclamol (3 X 10(-6) and 6 X 10(-6) M) and haloperidol (3 X 10(-6) and 3 X 10(-5) M)."( The relaxing effect of SKF 38393 on the catch contraction of Mytilus smooth muscle.
Ishikawa, T; Murakami, H; Sano, M, 1986
)
0.48
" These were haloperidol, clopenthixol, tefludazine, and setoperone, all tested in the dosage range of ."( Serotonergic aspects of acute extrapyramidal syndromes in nonhuman primates.
Casey, DE, 1989
)
0.66
" Dose-response curves obtained with a holding potential of -140 mV were best fitted by 2:1 stoichiometry in all three drugs and were shifted in the direction of lower concentrations when a holding potential of -90 mV was used."( Block of sodium channels by psychotropic drugs in single guinea-pig cardiac myocytes.
Narahashi, T; Ogata, N, 1989
)
0.28
" In slices from methamphetamine-treated rats, the dose-response curve for the dopamine hyperpolarization was shifted to the left of that seen in neurones from control rats by a factor of approximately 100."( Enhancement of dopamine actions on rat nucleus accumbens neurones in vitro after methamphetamine pre-treatment.
Higashi, H; Inanaga, K; Nishi, S; Uchimura, N, 1989
)
0.28
" Subsequent dose-response studies with other serotonergic and dopaminergic antagonists suggested that dopaminergic receptors are involved in the adaptive response to the irritant."( A role for dopamine as an endogenous protective factor in the rat stomach.
MacNaughton, WK; Wallace, JL, 1989
)
0.28
" However, by the 12th week of dosing with haloperidol all the monkeys showed a profound EPS characterized by limb extensions, head pushing, tongue protrusions and sometimes severe biting movements."( Acute extrapyramidal syndrome in Cebus monkeys: development mediated by dopamine D2 but not D1 receptors.
Chipkin, RE; Coffin, VL; Latranyi, MB, 1989
)
0.54
"In the present experiments, the dose-response effects of the dopamine (DA) receptor antagonists haloperidol, pimozide, clozapine, sulpiride, and metoclopramide, were assessed on patterns of copulatory behavior in intact, sexually active male rats with a high level of sexual experience and performance."( Differential effects of dopamine receptor antagonists on the sexual behavior of male rats.
Pfaus, JG; Phillips, AG, 1989
)
0.5
" The dosage equivalency of haloperidol decanoate (1."( A randomized clinical trial of haloperidol decanoate and fluphenazine decanoate in the outpatient treatment of schizophrenia.
Annable, L; Campbell, W; Chouinard, G, 1989
)
0.86
" As in experiment 1, CCK produced "biphasic" dose-response effects with strong attenuation that persisted throughout the entire 60-min test at both high (1 microgram) and low (1 ng) doses."( CCK-8 injected into the nucleus accumbens attenuates the supersensitive locomotor response to apomorphine in 6-OHDA and chronic-neuroleptic treated rats.
Ettenberg, A; Koob, GF; Weiss, F, 1989
)
0.28
" Subsequent challenge with haloperidol indicated a significant decrease in responsiveness to haloperidol-induced release of DA, but not HVA, in chronically dosed rats."( Repeated haloperidol administration changes basal release of striatal dopamine and subsequent response to haloperidol challenge.
Hong, JS; Stachowiak, MK; Tilson, H; Zhang, W, 1989
)
0.99
" The efficacy of the haloperidol dosage was tested on the amphetamine psychosis model."( The effects of haloperidol on synaptic plasticity in rat's medial prefrontal cortex.
Haselhorst, U; Istomin, VV; Klintzova, AJ; Schenk, H; Uranova, NA, 1989
)
0.95
" A comparison of levels of dopamine binding activity present in serum samples taken immediately prior to dosing on various days during the course of the study suggested that steady-state was achieved within seven days with repeated administration."( Radioreceptor assay of dopamine binding activity in human serum after tiospirone administration.
Hyslop, DK; Shukla, UA; Taylor, DP; Westrick, ML, 1989
)
0.28
" There was no significant difference in Li dosage among these three groups."( Effect of lithium and neuroleptic combination on lithium transport, blood pressure, and weight in bipolar patients.
Ghadirian, AM; Nair, NP; Schwartz, G, 1989
)
0.28
" Acute and long-term haloperidol administration induced significant leftward displacement of the control dose-response curves for picrotoxin but not those for strychnine or 3-mercaptopropionic acid (3-MPA)."( Behavioral aspects of GABAergic-dopaminergic interactions in the central nervous system.
Palermo-Neto, J; Sandoval, MR, 1989
)
0.6
" In these six cases it was demonstrated that the neuroleptics dosage was inappropriate, being either too high or too low as judged from the plasma concentrations."( [Quantitative approach to treatment with incisive neuroleptics by therapeutic monitoring].
Balant-Gorgia, AE; Eisele, R; Garrone, G, 1985
)
0.27
" It is suggested that additional studies, carefully designed, on dosage and plasma levels could help in achieving the lowest possible therapeutic dosage and thus in minimizing side effects."( Blood levels of neuroleptics: state of the art.
Simpson, GM; Yadalam, K, 1985
)
0.27
" Such variations have been attributed to individual metabolism, pharmacologic differences, and age--all of which may need careful consideration in prescribing an appropriate dosage regimen for a given patient."( Interpatient variations in antipsychotic therapy.
Gershon, S; McIntyre, IM, 1985
)
0.27
" The dose-response effect for the duration variable was different for the two lick conditions in that reflexive lick duration was lengthened as dose increased, whereas operant lick duration was lengthened only at the lower doses of these drugs."( Effects of neuroleptics on rate and duration of operant versus reflexive licking in rats.
Fowler, SC; Gramling, SE, 1985
)
0.27
" A dosage reduction might be considered after 2 to 4 weeks' treatment in non-responders who have plasma chlorpromazine concentrations above 100 to 150 micrograms/L or plasma haloperidol concentrations above 20 to 30 micrograms/L."( Plasma level monitoring of antipsychotic drugs. Clinical utility.
Dahl, SG,
)
0.32
" Therefore, it is critical to establish dosing strategies for long-term therapy that emphasize a minimal effective dose."( Dosage strategies with long-acting injectable neuroleptics, including haloperidol decanoate.
Kane, JM, 1986
)
0.5
" The dosage calculation was made from the haloperidol doses previously received by the patients, adjusted in each particular case, with a mean of 73 mg per application (range, 50 to 200 mg)."( [Chronic treatment of schizophrenia with injectable bromperidol decanoate].
Suárez Richards, M, 1985
)
0.53
" This led to the hope that measuring neuroleptic concentrations would allow more effective oral dosing for individual psychotic patients."( Neuroleptic blood levels and clinical response.
Rockland, LH, 1986
)
0.27
" Data were analyzed to determine the effect of anticholinergic prophylaxis, age, sex, and type and dosage of neuroleptic on the incidence of dystonic reactions."( Anticholinergic agents for prophylaxis of neuroleptic-induced dystonic reactions: a prospective study.
Heiser, JF; Morrison, RL; Simpson, GM; Sramek, JJ, 1986
)
0.27
"Precise pharmacokinetic data of long-acting neuroleptics: apparent half life (T 1/2), time of peak plasma concentration (Tmax), bioavailability, has been a major contribution to determine optimal dosage of the drug."( [Clinical pharmacokinetics of haloperidol decanoate. Comparison with other prolonged-action neuroleptics].
Levron, JC; Ropert, R,
)
0.42
" In a sulpiride-treated patient, the dosage was reduced in four steps over a nine-week period and a curvilinear relationship was demonstrated between central D2-dopamine receptor occupancy and serum drug concentrations."( Central D2-dopamine receptor occupancy in schizophrenic patients treated with antipsychotic drugs.
Farde, L; Halldin, C; Sedvall, G; Wiesel, FA, 1988
)
0.27
" Dose-response studies of catalepsy and ptosis were conducted in male Sprague-Dawley rats aged 30, 56, or 100 days."( Decreasing sensitivity to neuroleptic agents in developing rats; evidence for a pharmacodynamic factor.
Baldessarini, RJ; Campbell, A; Teicher, MH, 1988
)
0.27
"This article reviews the role of a new depot antipsychotic dosage form, haloperidol decanoate (HD), in relationship to other comparable pharmacotherapies (oral and injectable)."( Haloperidol decanoate: a depot antipsychotic.
Evans, RL; Hemstrom, CA; Lobeck, FG, 1988
)
1.95
" For remoxipride, the dose-response curve for antagonism of GBL-reversal was superimposable over that for antagonism of apomorphine-induced stereotypies, with an ED50 value about 12 times higher than that for antagonism of apomorphine-induced hyperactivity."( Comparison of the effects of haloperidol, remoxipride and raclopride on "pre"- and postsynaptic dopamine receptors in the rat brain.
Fowler, CJ; Magnusson, O; Mohringe, B; Ogren, SO; Wijkström, A, 1988
)
0.57
" Dose-response quantitative generalization was obtained by using 1 and 2 micrograms/kg caerulein."( Neuroleptic-like properties of cholecystokinin analogs: distinctive mechanisms underlying similar behavioral profiles depending on the route of administration.
De Witte, P; Gewiss, M; Roques, B; Vanderhaeghen, JJ,
)
0.13
"Therapeutic plasma monitoring of haloperidol, a major neuroleptic, measured by radioimmunoassay, has shown a rather good correlation between plasma level and dosage but with large interindividual variation in children as in adults; age seems not to have any effect on haloperidol metabolism."( [Haloperidol. Plasma monitoring and hormonal effects of treatment].
Debray, Q; Dugas, M; Giraud, J; Goyot, C; Grenier, J; Guay, C, 1985
)
1.46
" Time-course and dose-response studies further demonstrated that acetyltransferase activity covaried with POMC mRNA and peptide levels."( Coordinate regulation of peptide acetyltransferase activity and proopiomelanocortin gene expression in the intermediate lobe of the rat pituitary.
Chappell, MC; Millington, WR; Mueller, GP; O'Donohue, TL; Roberts, JL, 1986
)
0.27
" In previous investigations we found that in the same dosage Atriopeptin II increased sodium excretion 10-fold in euvolaemic animals."( Renal effects of atriopeptin II and dopamine receptor blockade in acutely volume-expanded rats.
Hansell, P; Michaelsson, K; Ulfendahl, HR, 1988
)
0.27
"01 to 1 microM were added to the incubation media, GH secretion was consistently inhibited and a dose-response relationship was observed between the cyproheptadine concentrations and the amounts of GH released into the media."( Cyproheptadine-mediated inhibition of growth hormone and prolactin release from pituitary adenoma cells of acromegaly and gigantism in culture.
Fukushima, T; Ishibashi, M; Yamaji, T, 1985
)
0.27
" After injection of 2 mg/kg haloperidol daily for 7 days, the dose-response curve to L-noradrenaline was displaced to the left, with lowering of the threshold and enhancement of the maximal response."( Chronic haloperidol causes increase in salivary response and alpha 1-adrenoceptors in submandibular gland of the rat.
De Robertis, E; De Stein, ML; Medina, JH; Pazo, JH; Tumilasci, OR, 1985
)
1
" The repeated dosing decreased body weight and caused neuromuscular dysfunction."( 3H-dopamine uptake and 3H-haloperidol binding in striatum after administration of methyl mercury to rats.
Komulainen, H; Tuomisto, J, 1985
)
0.57
"1-1 mg/kg SC) also produced jumping behavior, but the dose-response curve for apomorphine was shifted to the right."( Effects of acute and long-term treatments with thyrotropin-releasing hormone on locomotor activity and jumping behavior in mice.
Glavin, GB; Hara, T; Hirano, H; Mizuki, Y; Ushijima, I; Watanabe, K; Yamada, M, 1986
)
0.27
" Also, dosage requirements increase in the presence of other drugs that are enzyme inducers."( Clinical pharmacokinetics of carbamazepine.
Kerr, BM; Levy, RH, 1988
)
0.27
" In the 18-month study, haloperidol was injected intraperitoneally as a solution (HaldolR) at a dosage of 5 mg/kg daily for 5, 10 and 20 consecutive days in 5-week-old mice."( Mutagenic and leukemogenic activity of haloperidol: a negative study.
de Meester, C; Lambotte-Vandepaer, M; Marsboom, R; Van Cauteren, H; Vandenberghe, J; Vanparys, P, 1987
)
0.85
" These determinations demonstrate that the release of haloperidol with the decanoate form is sustained throughout the 4-week dosing interval."( A clinical trial comparing intramuscular haloperidol decanoate and oral haloperidol in chronic schizophrenic patients: efficacy, safety, and dosage equivalence.
Achim, A; Lizondo, E; Nayak, R; Schwartz, G; Suranyi-Cadotte, B; Thavundayil, JX; Vasavan Nair, NP, 1986
)
0.79
" Dosage adjustment after 2 weeks of treatment was made in seven subjects based on poor clinical response or side effects."( Neuroleptic radioreceptor activity and clinical outcome in schizophrenia.
Alexander, H; Bowden, C; Contreras, S; Faber, R, 1987
)
0.27
" After 24 h treatment with amine, the MAO activity of cultured skin fibroblasts was elevated in a dose-response manner."( Increased activity of monoamine oxidase by epoxy resin hardeners.
Yano, E, 1987
)
0.27
"The relationship between chronic oral dosage with a long-acting formulation of propranolol and plasma propranolol levels 22 to 23 hours later is described in 12 adult male patients with organic brain disease."( Plasma propranolol levels and their effect on plasma thioridazine and haloperidol concentrations.
Greendyke, RM; Kanter, DR, 1987
)
0.51
" To characterize the concentration-time profile of the two routes of administration, blood samples were obtained on two separate occasions at steady state during maintenance dosing for each route of administration."( The bioavailability and pharmacokinetics of oral and depot intramuscular haloperidol in schizophrenic patients.
Doose, DR; Nair, NP; Nayak, RK, 1987
)
0.5
"The effects of long-term dosing with tiapride for 21 days on barin dopamine receptors and dopamine turnover were compared with those of sulpiride and haloperidol."( Effect of long-term dosing with tiapride on brain dopamine receptors and metabolism in rats. Comparative study with sulpiride and haloperidol.
Kohjimoto, Y; Kuwaki, T; Nomura, Y; Ono, T; Satoh, H; Shibayama, F; Shirakawa, K, 1987
)
0.68
" Cumulative dosing of methamphetamine and morphine increased response rates without marked changes in avoidance rates in the shuttle avoidance response."( [Effects of psychotropic drugs by the cumulative-dosing procedure on lever-press and shuttle discrete avoidance responses in mice].
Furusawa, K; Kuribara, H; Tadokoro, S, 1987
)
0.27
" All three drugs disrupted performance during both the initial dose-response determination as well as during the redetermination following the regimen."( Effects of dopaminergic agents on eye tracking before and after repeated methamphetamine.
Ando, K; Johanson, CE; Schuster, CR, 1986
)
0.27
" Serum haloperidol levels in these patients decreased to about 60% of the levels seen just prior to the usual morning dosing during the drug holiday."( Drug holidays and serum haloperidol levels in schizophrenic patients.
Couch, L; Fody, EP; Harrison, RH; McMillan, DE; Newton, JE; Reese, WG, 1986
)
1.03
"1-30 mg/kg) elicited yawning that began 15-20 min after injection and lasted for 60 min, and the dose-response curve showed a bell-shaped form."( Desipramine induces yawning behaviour in rats.
Czyrak, A; Klimek, V; Mogilnicka, E; Wedzony, K, 1986
)
0.27
"A study of the liver N-demethylase activity in rats treated with different dosage schedule of morphine, or with a single dose of haloperidol was carried out."( N-demethylase activity in the rat liver following morphine and haloperidol treatment.
Daniel, W; Melzacka, M,
)
0.58
" It was concluded that 4-week intramuscular administration of haloperidol decanoate provides appropriate control of schizophrenic symptoms, but that flupenthixol decanoate should be dosed at shorter intervals."( Haloperidol decanoate and flupenthixol decanoate in schizophrenia. A long-term double-blind cross-over comparison.
Eberhard, G; Hellbom, E, 1986
)
1.95
"0 mg/kg) from saline, and then generalization tests were conducted using a cumulative dosing procedure."( Discriminative stimulus properties of buspirone in the pigeon.
Barrett, JE; Mansbach, RS, 1987
)
0.27
" After cumulative dosage dose-response curves are given for single frequency bands and different brain areas."( Classification of sulpiride, clozapine and haloperidol by toposelective recording from different brain structures in the immobilized rat (stereo-EEG).
Decker, H; Dimpfel, W, 1985
)
0.53
" In contrast, haloperidol failed to exert a similar effect at a dosage (1."( Conditioned taste aversion to chlorpromazine, but not to haloperidol.
Giardini, V, 1985
)
0.88
" For these reasons, we have undertaken a systematic study of haloperidol dose-response curves with particular emphasis on the lowest possible concentrations of drug."( Influences of endogenous dopamine on carotid body discharge and ventilation.
Chow, CM; Read, DJ; Winder, C, 1986
)
0.51
" After these dose-response curve determinations, chronic daily treatment with haloperidol (0."( Effects of drugs on schedule-controlled behavior in rats during chronic haloperidol administration.
McMillan, DE; Rastogi, SK, 1985
)
0.73
" After a diagnosis of "dysmorphic syndrome," haloperidol was prescribed at a dosage of 1 mg twice daily."( The dysmorphic syndrome.
Koblenzer, CS, 1985
)
0.53
" The effects on the overall response and the induction and elicitation phases were evaluated, using two alternative dosage schedules for each agent."( Different effects of psychotropic drugs on delayed hypersensitivity responses in mice.
Descotes, J; Evreux, JC; Tedone, R, 1985
)
0.27
" Tolerance to MA, increased sensitivity to HAL and no consistent sensitivity change to APO were observed when dose-response functions were redetermined starting 1 month after the repeated MA administration."( Sensitivity changes to dopaminergic agents in fine motor control of rhesus monkeys after repeated methamphetamine administration.
Ando, K; Johanson, CE; Schuster, CR; Seiden, LS, 1985
)
0.27
" Prolonged treatment with nomifensin markedly reduced the response of the type I inhibitor both to low and high doses of apomorphine and shifted the dose-response curves to the right."( The responsiveness of the endogenous inhibitor of cAMP-dependent protein kinase to apomorphine in rat striatum after prolonged treatment with nomifensin.
Szmigielska, H; Szmigielski, A; Zalewska, J,
)
0.13
" The dose-response relationship for hyperactivity in grouped mice following the injection of morphine sulphate has been established."( Monoamine mediation of the morphine-induced activation of mice.
Carroll, BJ; Sharp, PT, 1972
)
0.25
" This diabetes insipidus is reversible, non-progressive, unrelated to plasma level, and distinct in attack from lithium-induced hypothyroidism, which may occur at low dosage but is also usually of late onset and reversible or treatable with thyroxine while lithium is continued."( Blood levels and management of lithium treatment.
Crammer, JL; Crane, G; Rosser, RM, 1974
)
0.25
" However, the dose-response curve for pilocarpine was steeper than that for apomorphine."( Apomorphine-induced and pilocarpine-induced hypothermia in mice: drug interactions and changes in drug sensitivity after caudate nucleus lesions.
Glick, SD; Marsanico, RG, 1974
)
0.25
" The ED50s of the effective neuroleptics for this inhibition were similar to those reported for antagonism of amphetamine-induced stereotypic behavior in the rat and the slopes of the dose-response curves were parallel indicating a common site and mechanism of action, presumably blockade of postsynaptic dopaminergic receptors."( Effect of neuroleptics and tricyclic antidepressants upon d-amphetamine discrimination.
Schechter, MD, 1980
)
0.26
"The counterbalanced design in a bioequivalent study of haloperidol indicated an absence of any clinical difference between a new 20-mg dosage form and two 10-mg tablets of haloperidol (Haldol)."( The dopamine radioreceptor assay--a clinical application.
Hanlon, TE; Kurland, AA; Nagaraju, A, 1980
)
0.51
" Each dopamine antagonist displaced the dose-response curve for dopamine-induced suppression of prolactin release to the right in a parallel manner."( Chlorpromazine, haloperidol, metoclopramide and domperidone release prolactin through dopamine antagonism at low concentrations but paradoxically inhibit prolactin release at high concentrations.
Besser, GM; Delitala, G; Grossman, A; Stubbs, WA; Yeo, T, 1980
)
0.61
" The dose-response curves showed potencies similar to those in several animal behavioral paradigms."( Electrophysiologic interactions of antipsychotic drugs with central noradrenergic pathways.
Freedman, R; Geller, HM; Hoffer, BJ; Marwaha, J, 1981
)
0.26
"A case illustrating the worsening of a patient's schizophrenic symptoms following haloperidol dosage increases in presented."( Psychotic exacerbation with haloperidol.
Lee, D; Sramek, JJ; Tornatore, FL, 1981
)
0.78
" The response to 3 x 10(-7) M dopamine was considered as the maximum response to obtain dose-response curves (Takayanagi et al 1981)."( Photoaffinity labelling of dopamine receptors in molluscan smooth muscle.
Iwayama, Y; Takayanagi, I, 1982
)
0.26
" administration of lisuride at the dosage known to be ineffective on the postsynaptic dopamine receptor."( [Suppressive effects of lisuride on the synthesis, release and metabolism of dopamine in rat brain].
Azuma, H; Iwai, K; Kikuta, M; Liu, HJ; Oshino, N; Sato, K, 1982
)
0.26
" Drugs and dosage of peroral and intravenous neuroleptic treatment and possible complications are discussed."( [Inpatient withdrawal treatment of heroin dependence with neuroleptics--an approach to addicts].
Hermann, P; Presslich, O; Schanda, H, 1983
)
0.27
" In the 6th and 8th h after the 10-mg dosage but also after the 40-mg dose some activating properties were observed, as indicated by the decrease in slow waves and increase in slow beta activity and average frequency."( Determination of pharmacodynamics of the new neuroleptic zetidoline by neuroendocrinologic, pharmaco-EEG, and psychometric studies--Part I.
Dubini, A; Grünberger, J; Linzmayer, L; Saletu, B, 1983
)
0.27
" The dosage was adjusted to the clinical response of the patients and the mean dose was 21."( A double-blind controlled trial of pipotiazine, haloperidol and placebo in recently-hospitalized acute schizophrenic patients.
Bechelli, LP; Hetem, G; Ruffino-Netto, A, 1983
)
0.52
" The clinical significance of plasma monitoring of depot fluphenazine, including the development of dosage conversion guidelines, is presented."( Future of depot neuroleptic therapy: pharmacokinetic and pharmacodynamic approaches.
Davis, CM; Ereshefsky, L; Jann, MW; Richards, A; Saklad, SR; Seidel, DR, 1984
)
0.27
") elicited yawning in rats and the dose-response curves of all 3 compounds showed a bell-shaped form."( Effects of apomorphine, TL-99 and 3-PPP on yawning in rats.
Boissard, CG; Delini-Stula, A; Mogilnicka, E, 1984
)
0.27
" The dosage schema can be adapted individually whenever necessary."( [Long-term therapy of chronic schizophrenic patients with haloperidol decanoate].
Roncoroni, D, 1984
)
0.51
" It appears that propericiazine shows an inverted U-shaped dose-response curve."( Prophylactic effect of neuroleptics in symptom-free schizophrenics: a comparative dose-response study of haloperidol and propericiazine.
Hoaki, Y; Koga, I; Nishikawa, T; Tanaka, M; Tsuda, A; Uchida, Y, 1984
)
0.48
"The authors studied high-potency versus low-potency neuroleptic dosing practices for 110 Boston-area psychiatric inpatients and compared the findings with the dosing practices reported in surveys of nearly 16,000 Veterans Administration patients."( Dissimilar dosing with high-potency and low-potency neuroleptics.
Baldessarini, RJ; Cotton, P; Katz, B, 1984
)
0.27
" Administration of nitrazepam with other drugs, except aminopyrine, or of estazolam together with haloperidol exhibited an anticonvulsive pattern different from the case of dosing with either drug alone."( [Pharmacology of a 1H-1, 2, 4-triazolyl benzophenone derivative (450191-S), a new sleep-inducer (III). Behavioral study on interactions of 450191-S and other drugs in mice].
Horiuchi, M; Ibii, N; Yamamoto, K, 1984
)
0.48
"0 mg/kg) were examined in a subchronic (28 day) dosing regimen."( Acute and subchronic effects of neuroleptics on quantitative measures of discriminative motor control in rats.
Ford, KE; Fowler, SC; Gramling, SE; Nail, GL, 1984
)
0.27
" (+) Butaclamol but not (-) butaclamol shifted the dopamine dose-response curve to the right in a parallel fashion, indicating competitive antagonism."( Pharmacological characterization of renal vascular dopamine receptors.
Imbs, JL; Schmidt, M,
)
0.13
" There were also differences in the dose-response curves."( Neuroleptic-induced seizures. An in vitro technique for assessing relative risk.
Luchins, DJ; Oliver, AP; Wyatt, RJ, 1982
)
0.26
" It means that over this dosage range haloperidol potentiates GABA-induced effects."( [Participation of GABA-ergic structures in producing the effects of haloperidol].
Molodavkin, GM; Ostrovskaia, RU, 1980
)
0.77
" Apomorphine, at doses different than the training dose, produced a dose-response relationship, whereas, caffeine (7."( Caffeine potentiation of apomorphine discrimination.
Schechter, MD, 1980
)
0.26
" A dose-response relationship (5-100 mg/kg) for the hypothermic effect of delta 9-THC was seen."( The mechanism of action of delta 9-tetrahydrocannabinol on body temperature in mice.
Davies, JA; Graham, JD, 1980
)
0.26
"3 mg/kg) produced a 3-fold shift to the right of the cyclazocine dose-response curve but did not completely block the cyclazocine-like stimulus effects of either SKF 10,047 or ethylketocyclazocine."( Discriminative stimulus effects of prototype opiate receptor agonists in monkeys.
Holtzman, SG; Teal, JJ, 1980
)
0.26
"Using a double-blind experimental design, two dosage regimens of haloperidol were compared in acutely decompensated, newly admitted schizophrenic patients."( Haloperidol in acute schizophrenic inpatients. A double-blind comparison of two dosage regimens.
Greub, E; Modestin, J; Pia, M; Toffler, G, 1983
)
1.95
"In a double-blind controlled study, 20 acutely psychotic inpatients were treated with different haloperidol dosage regimens."( Plasma/RBC haloperidol ratios and improvement in acute psychotic symptoms.
Depry, D; Janowsky, DS; Munson, E; Neborsky, RJ; Perel, JM, 1984
)
0.88
" This dosage of haloperidol had no effect on tactile placing in normal cats."( Amphetamine and apomorphine restore tactile placing after motor cortex injury in the cat.
Feeney, DM; Hovda, DA, 1983
)
0.61
" The interaction of these compounds was determined by repeated determination of the dose-response function for d-amphetamine in combination with different doses of haloperidol."( The effect of d-amphetamine and haloperidol alone and in combination on milk drinking in rats.
Foltin, RW; Schuster, CR; Woolverton, WL, 1983
)
0.75
" Evidence for this is based on the fact that in our patients and others mentioned in the literature the dosage and blood levels of lithium were not high."( Toxic irreversible encephalopathy induced by lithium carbonate and haloperidol. A report of 2 cases.
Hurwitz, MD; Sandyk, R, 1983
)
0.5
" Overall, 25 years of experience have indicated that haloperidol can be used safely and effectively to manage a variety of psychiatric illnesses, so long as dosage and method of administration are adjusted to individual patients' needs."( Haloperidol: a quarter century of experience.
Ayd, FJ; Settle, EC, 1983
)
1.96
" The suggested importance of treatment schedule rather than cumulative drug dosage in the development of tolerance to haloperidol may have significance to long-term side effects of chronic neuroleptic treatment such as tardive dyskinesia and clinical issues such as drug holidays."( Treatment schedule as a determinant of the development of tolerance to haloperidol.
Carey, RJ; DeVeaugh-Geiss, J, 1984
)
0.71
" Most children suffered side effects on relatively high doses of lithium, and those few who experienced side effects on low dosage had saliva lithium levels that were proportionately high."( Saliva lithium levels in children: their use in monitoring serum lithium levels and lithium side effects.
Anderson, L; Campbell, M; Grega, DM; Perry, R, 1984
)
0.27
" An increase in dosage also had only a transient effect."( Development of tolerance to the therapeutic effect of amantadine on akathisia.
Barreira, P; Lipinski, JF; Zubenko, GS, 1984
)
0.27
"In an open study, 18 patients suffering from an acute episode of schizophrenia and 18 patients with severe mania were given haloperidol at different dosage levels."( Plasma haloperidol levels and therapeutic response in acute mania and schizophrenia.
Balant, L; Balant-Gorgia, AE; Eisele, R; Garrone, G, 1984
)
0.93
" An experimental study of the long-term administrations of haloperidol revealed the formation of adaptation to the drug which can be overcome by a zigzag-like sharp elevation of the dosage followed by rapid reduction to the baseline level."( [Various methods of overcoming secondary resistance to treatment developing in relation to adaptation to psychotropic drugs during long-term treatment (clinico-experimental study)].
Allikmets, LKh; Avrutskiĭ, GIa; Beliakov, AV; Neduva, AA; Zharkovskiĭ, AM, 1984
)
0.51
" Animals of high dosage group showed suppression of body weight increase and loss of muscular strength of limbs in the administration period."( [Subacute toxicity of an amine-curing agent for epoxy resin].
Matsumoto, M; Nakayama, E; Nishizawa, H; Ohsawa, M; Ohshima, S; Okuda, H; Sasaki, N; Shibata, T, 1984
)
0.27
"The drug difference between a low and a high dosage of haloperidol was investigated in 40 acutely ill schizophrenic patients."( Effects of high and low dosage of haloperidol on the brain in relation to schizophrenic thought disorder.
Lehmann, E; Scholz, OB; Winter, M, 1984
)
0.79
" At each dose tested, metoclopramide produced a larger rightward shift of the apomorphine dose-response curve in the control rats than in withdrawn rats."( Kinetic analysis of central nervous system supersensitivity induced in rats by long-term haloperidol administration. I. pA2 determination.
Bernardi, MM; Palermo-Neto, J; Saban, R, 1984
)
0.49
" Metoclopramide and haloperidol are both excellent antiemetics when given in sufficient dosage by an effective route."( Comparison of the antiemetic effect of high-dose intravenous metoclopramide and high-dose intravenous haloperidol in a randomized double-blind crossover study.
Cariffe, P; Gala, KV; Grunberg, SM; Jamin, D; Johnson, K; Krailo, M; Lampenfeld, M; Strych, D, 1984
)
0.81
") was not inhibited at any dosage level in haloperidol-treated rats, and was enhanced by higher doses of nomifensine."( Enhancement of stereotypy induced by nomifensine in rats during continuous chronic haloperidol treatment.
Jenner, P; Marsden, CD; Rupniak, NM, 1984
)
0.76
"Nineteen male patients, under 35 years of age, newly admitted with a diagnosis of schizophrenia, were treated with either chlorpromazine or haloperidol at a fixed dosage for 25 days."( Total and free plasma neuroleptic levels in schizophrenic patients.
Davidson, L; Glaister, J; Jeffries, JJ; Seeman, P; Tang, SW; Toth, R, 1984
)
0.47
" At the end of the trial, the mean dosage of HD administered and BPRS (Brief Psychiatric Rating Scale) mean scores were significantly lower than the initial ones (70."( Haloperidol decanoate in schizophreniform disorders. Clinical and neuroendocrine aspects.
Attenni, M; Casacchia, M; Castellana, F; Ecari, U; Iafrate, A; Meco, G,
)
1.57
" Lever pressing for intracranial self-stimulation (ICSS) was attenuated in a dose-related fashion by TL-99 and 3-PPP, with relatively shallow dose-response relationships."( Avoidance and ICSS behavioral models dissociate TL-99 and 3-PPP from dopamine receptor antagonists.
Fenton, HM; Gerhardt, S; Hall, NR; Liebman, JM; Neale, R; Noreika, L, 1983
)
0.27
"The neurochemical background of clinical experiences that the patients receiving high dosage haloperidol showed no extrapyramidal side effects was investigated by using rats."( [High dosage haloperidol reduces cataleptic response with increased noradrenaline metabolism in the rat brain areas].
Takashima, M; Toru, M, 1983
)
0.85
" The clinical implications for dosage strategies are discussed."( Beyond the therapeutic window: a case presentation.
Butterfield, L; Friedel, RO; Garicano, M; Narasimhachari, N; Schulz, SC, 1984
)
0.27
" Preincubation of the sonicated platelets with haloperidol before the assay did not shift the dose-response curve."( Haloperidol inhibition of monoamine oxidase in vivo and in vitro.
Giller, E; Hall, H; Reubens, L; Wojciechoswki, J, 1984
)
1.97
" Patients were selected based on poor response or the need for high dosage and were rated with the Clinical Global Impression Scale."( Haloperidol and reduced haloperidol plasma levels in selected schizophrenic patients.
Browning, JL; Burch, NR; Davis, CM; Ereshefsky, L; Harrington, CA; Jann, MW; Saklad, SR, 1984
)
1.71
" A total of 30 female patients with a diagnosis of chronic schizophrenia were initially stabilised on the dosage of haloperidol which produced optimum therapeutic response when given once or twice daily."( A clinical and pharmacodynamic evaluation of sulpiride.
Bailey, J; Bishop, M; Coppen, A; Rao, VA, 1981
)
0.47
" These included improvement during a drug-free trial: the absence of a prior history of a speech problem; the patient's marked psychotic state and anxiety: and the high dosage of haloperidol."( Persistent dysarthria with apraxia associated with a combination of lithium carbonate and haloperidol.
Bond, WS; Carvalho, M; Foulks, EF, 1982
)
0.68
" Dose-response curves for d-MA (0."( Altered sensitivity to d-methylamphetamine, apomorphine, and haloperidol in rhesus monkeys depleted of caudate dopamine by repeated administration of d-methylamphetamine.
Finnegan, KT; Ricaurte, G; Schuster, CR; Seiden, LS, 1982
)
0.51
" It is concluded that agonist induction of subsensitivity in the DA system is difficult to reproduce and may depend on highly specific dosage conditions and treatment schedules."( The effect of chronic bromocriptine and L-dopa on spiperone binding and apomorphine-induced stereotypy.
Bannet, J; Belmaker, RH; Globus, M; Lerer, B, 1982
)
0.26
" Mean daily dosage was approximately 112 mg flupenthixol and 18 mg haloperidol."( Flupenthixol versus haloperidol in acute psychosis.
Parent, M; Toussaint, C, 1983
)
0.83
" Following acquisition of the discrimination, dose-response functions were generated for both training-dose groups during 5 min test sessions."( Drug discrimination in rats: evidence for amphetamine-like cue state following chronic haloperidol.
Barrett, RJ; Steranka, LR, 1983
)
0.49
" There appeared to be no difference between the viloxazine-treated group and the placebo-treated group, although the study raised some question as to the adequacies of the dosage utilized since there was an absence of any apparent side effects."( Viloxazine and the depressed schizophrenic--methodological issues.
Kurland, AA; Nagaraju, A, 1981
)
0.26
"A randomized cross-over trial was conducted in 30 restless mentally subnormal patients by increasing the dosage of haloperidol from 10 to 60 mg and that of thioridazine from 100 to 600 mg daily."( Haloperidol, thioridazine and placebo in mentally subnormal patients-serum levels and clinical effects.
Räisänen, P; Rimón, R; Väisänen, K; Viukari, M, 1981
)
1.92
" It appears that although haloperidol disposition can be described by linear kinetics in volunteers, this is not the case in patients in whom a 7--10-fold variability in plasma levels is observed for the same dosage together with the possibility of saturation kinetics and/or first pass effect."( Haloperidol plasma level monitoring in neuropsychiatric patients.
Bianchetti, G; Dugas, M; Morselli, PL, 1982
)
2.01
" The failure of our combination antiemetic regimens to intensify the proven antiemetic efficacy of single agents emphasises the need for re-evaluation of currently used antiemetic agents and their dosage schedules."( Single-agent versus combination antiemetic treatments in patients receiving cytotoxic chemotherapy.
Coates, A; Diekman, J; Fox, RM; Kearsley, JH; Sims, K; Tattersall, MH, 1982
)
0.26
" Solutions prepared from commercial dosage forms of haloperidol (injection, oral liquid concentrate, and tablets) were assayed to verify the accuracy of the HPLC assay to quantify haloperidol."( Stability of haloperidol in 5% dextrose injection.
Das Gupta, V; Stewart, KR, 1982
)
0.88
" Plasma prolactin levels, initially high, increased when the dosage was increased to 100 mg/day but did not increase further."( High doses of haloperidol in schizophrenia. A clinical, biochemical, and pharmacokinetic study.
Bianchetti, G; Cuche, H; Loo, H; Morselli, PL; Scatton, B; Zarifian, E, 1982
)
0.62
" Ten of the studies are dose-response evaluations."( Sleep spindles: pharmacological effects in humans.
Hirshkowitz, M; Karacan, I; Thornby, JI, 1982
)
0.26
" In neither patient, the increase in haloperidol dosage affected paranoid symptoms."( [Use of haloperidol in high doses in schizophrenia. Clinical, biochemical and pharmacokinetic study].
Bianchetti, G; Cuche, H; Loo, H; Morselli, PL; Scatton, B; Zarifian, E, 1982
)
0.97
" After stable discrimination performances were attained (greater than 85%) in each group, dose-response generalizations between the two groups of animals were examined."( Comparative discriminative stimulus effects of 5-methoxy-N,N-dimethyltryptamine and LSD.
Glennon, RA; Rosecrans, JA; Young, R, 1982
)
0.26
" A dose-response relationship was evident as 80-245 mg/kg produced from 3 to 70% fetal anomalies."( Haloperidol teratogenicity in the fetal hamster.
Geber, WF; Gill, TS; Guram, MS, 1982
)
1.71
" These findings constitute biochemical evidence for selective elevation of brain DA during the first postnatal week of life after L-DOPA administration in a dosage that is also capable of enhancing the coordination required for swimming behavior."( Brain catecholamine concentration during the first week of development in rats.
Korányi, L; Phelps, CP; Tamásy, V, 1982
)
0.26
" (2) There were significant correlations between daily dosage and salivary and serum concentrations, and the regression lines were shown in the equivalent exponential form."( Haloperidol concentrations in saliva and serum: determination by the radioimmunoassay method.
Miura, S; Yamazumi, S, 1981
)
1.71
"30 h in one of five dosage levels (0."( Differential time- and dose-dependent effects in the haloperidol blockade of luteinizing hormone release and ovulation.
Johnson, JH; Krieg, RJ, 1981
)
0.51
"Chronic schizophrenic patients were maintained for six months on a dosage of haloperidol adjusted to give optimum clinical effect."( Clinical state, plasma levels of haloperidol and prolactin: a correlation study in chronic schizophrenia.
Bishop, M; Coppen, A; Rao, VA, 1980
)
0.77
" Using a chronic dosing regime, the effects of haloperidol (0."( Time course of chronic haloperidol and clozapine upon operant rate and duration.
Faustman, W; Fowler, S; Walker, C, 1981
)
0.83
"A comparison of a chemical analytic technique (gas chromatography/mass spectrometry) with that of the dopamine receptor blocking assay in a study involving seven schizophrenic patients being administered a fixed dosage of haloperidol (20 mg) demonstrated a high degree of correspondence in the quantification of the plasma levels of the neuroleptic."( A comparison of dopamine receptor blocking assay with plasma drug levels of haloperidol in schizophrenic patients.
Hanlon, TE; Kurland, AA; Nagaraju, A; Ng, KT; Wilkinson, EH, 1981
)
0.68
"6 hr at all three dosage levels."( A new radioimmunoassay for haloperidol: direct measurement of serum and striatal concentrations.
Colburn, WA; Marcum, EA; Miller, RL; Spector, S; Wurzburger, RJ, 1981
)
0.56
" Dose-response relationship of methylphenidate thermal effects exhibits a U-shape curve."( A comparison of the hypothermic effects of methylphenidate and d-amphetamine.
Ben-Uriah, Y; Carasso, RL; Yehuda, S, 1981
)
0.26
"Haloperidol levels were measured by radioreceptor assay in 12 schizophrenic patients during gradual dosage reduction (at 10-day) intervals) from 60 to 0 mg/day."( Haloperidol blood levels during dosage reduction in chronic schizophrenic patients.
Belmaker, RH; Ebstein, RP; Goldman, Z; Hermoni, M; Lerer, B; Zohar, J, 1981
)
3.15
" The same was true for haloperidol plasma levels after chronic dosing in man."( Radioimmunoassay of bromperidol and haloperidol in human and canine plasma.
Belpaire, FM; Bogaert, MG; De Moerloose, P; Van Den Eeckhout, E, 1980
)
0.85
" Serum levels of haloperidol in schizophrenic patients receiving single oral dosing (6 mg/subject) have also been determined."( Determination of haloperidol in human serum by radioimmunoassay.
Hashimoto, M; Itoh, H; Iwaisaki, M; Kagemoto, A; Minaki, Y; Sekine, Y; Suzuki, H; Utsui, Y; Yagi, G, 1980
)
0.94
" This methylamphetamine treatment also attenuated the ability of methylamphetamine and apomorphine to produce increases in locomotor activity without shifting the dose-response curve to the right or left."( The effects of dopaminergic agents on the locomotor activity of rats after high doses of methylamphetamine.
Lucot, JB; Schuster, CR; Seiden, LS; Wagner, GC, 1980
)
0.26
") every 4 weeks with haloperidol decanoate using different dosage schedules which were calculated from the previously prescribed daily oral dose of haloperidol multiplied by a factor of 30, 20 or 10."( Intramuscular haloperidol decanoate for neuroleptic maintenance therapy. Efficacy, dosage schedule and plasma levels. An open multicenter study.
Berghmans, W; Deberdt, R; Driesens, F; Elens, P; Heykants, J; Reyntjens, A; van Wijngaarden, I; Woestenborghs, R, 1980
)
0.94
" Dose-response analysis of receptor occupancy revealed risperidone demonstrated higher binding affinity for 5-HT2 than for D2, while the reverse was observed with haloperidol."( In vivo dopamine-D2 and serotonin-5-HT2 receptor binding study of risperidone and haloperidol.
Kido, H; Mori, H; Sakamoto, H; Shiba, K; Sumiyoshi, T; Suzuki, K; Urasaki, K; Yamaguchi, N; Yokogawa, K, 1994
)
0.71
" Risperidone was found to have a curvilinear dose-response curve with an optimum effect of 4 mg day on the negative, anxious/depressive and cognitive factors and with an optimum effect of 8 mg day on the positive and excited factors."( Changes in single symptoms and separate factors of the schizophrenic syndrome after treatment with risperidone or haloperidol.
Lindström, E; von Knorring, L, 1994
)
0.5
"0 mg/kg induced a significant leftward displacement of the control dose-response curve constructed for apomorphine (0."( Effect of manipulation of the GABA system on dopamine-related behaviors.
Palermo-Neto, J; Sandoval, MR, 1995
)
0.29
"025 mg/kg quinpirole from distilled water, a dose-response curve and time course of the quinpirole discriminative stimulus were determined."( D2-specific discriminative stimuli: parameters, blocking, and rebound.
Barrett, RJ; Caul, WF; Huffman, EM; Jones, JR; Strand, EJ, 1995
)
0.29
" This dosage impaired conditioning of the male animals but did not attain the same effects on females."( Gender differences in the effects of haloperidol on avoidance conditioning in mice.
Arenas, MC; Parra, A; Simón, VM, 1995
)
0.56
" To the extent that the VCM syndrome models TD, the absence of long-term suppression of the VCM syndrome suggests that, at this dosage range, increasing depot neuroleptic doses may not be a useful long-term strategy for TD suppression."( Neuroleptic-induced vacuous chewing movements in rodents: incidence and effects of long-term increases in haloperidol dose.
Egan, MF; Hyde, TM; Kleinman, JE; Wyatt, RJ, 1995
)
0.5
" The dose-response curves for haloperidol to changes in the evoked DA release were found to be biphasic (small doses increased the release and large doses inhibited), which were shifted to the left by longer periods of superfusion with haloperidol."( [Inhibitory effect of haloperidol on evoked dopamine release from striatal slices of the rat].
Takaki, T; Tanaka, M; Yamada, S; Yokoo, H, 1995
)
0.89
" In 53 patients who were treated with two or more haloperidol dosage regimens, steady-state haloperidol and reduced haloperidol drug concentrations obtained from the different regimens were positively correlated with the haloperidol dose (R = ."( Intra- and interethnic variability in reduced haloperidol to haloperidol ratios.
Chang, WH; Chen, H; Davis, CM; Jann, MW; Lam, YW; Lin, SK; Yu, HS, 1995
)
0.8
" This study evaluated the effect of oral alosetron dosing on the pharmacokinetics of haloperidol, the latter being administered daily to 13 schizophrenic patients for 56 days."( Effect of alosetron (a new 5-HT3 receptor antagonist) on the pharmacokinetics of haloperidol in schizophrenic patients.
Gupta, SK; Kunka, RL; Lloyd, T; Metz, A; Perel, JM; Rudolph, G, 1995
)
0.74
" Mice and rats were given A5 intraperitoneally at three different dosage levels."( The influence of antineoplaston A5 on the central dopaminergic structures.
Burzynski, SR; Chodkowska, A; Feldo, M; Juszkiewicz, M; Kleinrok, Z; Majewska, B, 1994
)
0.29
" Dose-response functions for cocaine and haloperidol demonstrated both quantitative and qualitative specificity of the training stimuli."( A three-choice haloperidol-saline-cocaine drug discrimination task in rats.
Gauvin, DV; Goulden, KL; Holloway, FA, 1994
)
0.91
"During a 4-week interval of haloperidol decanoate dosage (dose range = 30-50 mg), the patients' D2 receptor occupancy was determined with positron emission tomography on two occasions."( D2 dopamine receptor occupancy during low-dose treatment with haloperidol decanoate.
Bertilsson, L; Dahl, ML; Farde, L; Halldin, C; Nyberg, S, 1995
)
0.83
"Hair samples were obtained 1-5 months after ingestion of the antimicrobial ofloxacin, which had been given for 1 or 3 days at the commencement of haloperidol administration, or when its dosage was reduced."( Using ofloxacin as a time marker in hair analysis for monitoring the dosage history of haloperidol.
Kosuge, K; Nakano, M; Nakashima, M; Nishimoto, M; Sato, H; Uematsu, T, 1994
)
0.71
" In this case, it seems necessary to diminish the interval between injections than to give higher dosage in order to maintain plasma concentrations."( Do enzyme inducers modify haloperidol decanoate rate of release?
Agenet, C; Barges-Bertocchio, MH; Levron, JC; Pupeschi, G, 1994
)
0.59
" The dose-response curve was bell-shaped which is typical for cognition enhancers."( PRE-084, a sigma selective PCP derivative, attenuates MK-801-induced impairment of learning in mice.
Maurice, T; Nabeshima, T; Parish, DW; Privat, A; Su, TP, 1994
)
0.29
"There is a trend in clinical psychiatric practice to make the dosing schedules of psychotropic medications as simple as possible."( Comparison of haloperidol plasma concentrations between twice-a-day and once-a-day dosing in Chinese schizophrenic patients.
Chang, WH; Chen, CH; Lin, SK, 1993
)
0.65
"Doctors' prescription and dosing behaviour was investigated using data from 9 clinical trials in 550 patients treated with psychotropics."( Correct titration of non-drugs and some other methodological issues.
Beneke, M; Fritze, J; Rasmus, W; Rød, IS, 1994
)
0.29
" In addition, the clinician should consider the dosage schedule of each medication and balance this against the probability of extrapyramidal side effects and noncompliance."( Dose response of prophylactic antipsychotics.
Brauzer, B; Casey, DE; Davis, JM; Gierl, B; Hassan, M; Kane, JM; Marder, SR; Schooler, N, 1993
)
0.29
" D2-DAr binding assays showed 1) that CLG-induced changes in Bmax parallel these behavioral changes and 2) that the biphasic CLG dose-response curve may involve CLG failure at high cumulative doses to lower Bmax."( Prevention and reversal of dopamine receptor supersensitivity by cyclo(leucyl-glycyl) (CLG): biphasic dose-response curves.
Drucker, GE; Engh, K; Fields, JZ; Gordon, JH; Ritzmann, RF; Wichlinski, LJ, 1994
)
0.29
" In the first the effects of captopril on apomorphine-induced behaviour were compared with those of the classical neuroleptic haloperidol, and in the second dose-response curves for the effects of captopril and enalapril on apomorphine-induced behaviour were determined."( The angiotensin converting enzyme inhibitors captopril and enalapril inhibit apomorphine-induced oral stereotypy in the rat.
Banks, RJ; Dourish, CT; Mozley, L, 1994
)
0.49
"Two patients with akathisia developing only after neuroleptic dosage reduction or withdrawal are described."( Withdrawal akathisia: case reports and a proposed classification of chronic akathisia.
Lang, AE, 1994
)
0.29
" Eighteen-day-old rats were 35% and 63% more sensitive than adults to the effects of haloperidol on striatal and accumbens turnover and had steeper dose-response curves."( Developmental differences in acute nigrostriatal and mesocorticolimbic system response to haloperidol.
Baldessarini, RJ; Barber, NI; Campbell, A; Gallitano, AL; Gelbard, HA; Marsh, E; Teicher, MH, 1993
)
0.73
" In vitro protein secretion rates exhibit a dose-response relationship with increases in protein release up to a concentration of 10(-8) to 10(-4) M for various derivatives of bromhexine and 10(-4) M for carbachol."( Lacrimal secretion stimulants: sigma receptors and drug implications.
Barfknecht, CF; Cheng, B; Ignace, CC; Iwai, Y; Newton, RE; Schoenwald, RD; Shirolkar, S; Vidvauns, S; Xia, E, 1993
)
0.29
" In keeping with previous data obtained with other sigma receptor ligands, low doses of sertraline and of clorgyline potentiated selectively with a bell-shaped dose-response curve the effect of N-methyl-D-aspartate (NMDA) on pyramidal neurons in the CA3 region of the rat dorsal hippocampus."( Modification of the N-methyl-D-aspartate response by antidepressant sigma receptor ligands.
Bergeron, R; De Montigny, C; Debonnel, G, 1993
)
0.29
" Using an optimizing dosage regime, the outcome variables studied were aggression frequency and the number and nature of emergent side effects."( Aggression in the demented patient: a double-blind study of loxapine versus haloperidol.
Ancill, RJ; Carlyle, W; Sheldon, L, 1993
)
0.52
"The concentration of chlorpromazine (CPZ) in hair was measured to demonstrate its value as an index of individual dosage history and compliance."( Chlorpromazine in human scalp hair as an index of dosage history: comparison with simultaneously measured haloperidol.
Nakashima, M; Sato, H; Uematsu, T; Yamada, K, 1993
)
0.5
" A dose-response analysis of D2 and 5-HT2 receptor occupancy by the drugs consolidated the higher 5-HT2 binding affinity of clozapine in comparison with haloperidol."( Time course of dopamine-D2 and serotonin-5-HT2 receptor occupancy rates by haloperidol and clozapine in vivo.
Ichimura, F; Kido, H; Mori, H; Sakamoto, H; Shiba, K; Sumiyoshi, T; Suzuki, K; Urasaki, K; Yamaguchi, N; Yokogawa, K, 1993
)
0.71
" The dose-response curves were U-shaped."( Influence of beta-casomorphins on apomorphine-induced hyperlocomotion.
Grecksch, G; Matthies, H; Rüthrich, HL, 1993
)
0.29
") did not shift the apomorphine dose-response curve (0."( Comparison of the effects of the cholecystokinin-B receptor antagonist, PD 134308, and the cholecystokinin-A receptor antagonist, L-364,718, on dopamine neuronal activity in the substantia nigra and ventral tegmental area.
Christoffersen, CL; Meltzer, LT; Razmpour, A; Serpa, KA, 1993
)
0.29
" Body clearance decreased nonsignificantly, and elimination half-life increased significantly after chronic dosing compared with kinetic parameters determined after a single dose."( The assessment and clinical implications of haloperidol acute-dose, steady-state, and withdrawal pharmacokinetics.
Bigelow, LB; DeVane, CL; Khot, V; Kirch, DG; Korpi, ER; Venable, D; Wyatt, RJ, 1993
)
0.55
" Animals that were lesioned and treated with haloperidol chronically had longer durations of catalepsy at the first two dose-response determinations."( Partial 6-hydroxydopamine-induced lesions and haloperidol-induced catalepsy.
Fisher, H; Johnson, SK; Wagner, GC, 1993
)
0.8
"Despite the trend towards lower neuroleptic dosing in the treatment of psychosis, there continue to be patients who are administered doses that are higher than recommended."( Acutely psychotic patients receiving high-dose haloperidol therapy.
Coulter, K; Pollock, B; Reed, K; Remington, G; Voineskos, G, 1993
)
0.54
"Previous data suggest the possibility that haloperidol daily dosing requirements may be confounded by smoking and, at higher doses, capacity-limited metabolism."( Haloperidol dosing requirements: the contribution of smoking and nonlinear pharmacokinetics.
Arndt, SV; Holman, TL; Miller, DD; Perry, PJ; Smith, DA, 1993
)
1.99
"Single administration of the regulating peptide tuftsin Thr- Lys-Pro-Arg (300 micrograms/kg) was shown to affect the state of the transmitter systems in the brain of rats treated with the sedative drug haloperidol in a total dosage of 15 mg/kg within 30 days."( [Effect of the tetrapeptide tuftsin on activity of the monoaminergic system of the brain in experimental pathology].
Dovedov, EL; Monakov, MIu,
)
0.32
" Haloperidol is often administered chronically in clinical situations; hence, it is important to investigate the effects of repeated, as well as acute, dosing with this drug."( Effect of repeated haloperidol administration on phencyclidine discrimination in rats.
Wiley, JL, 1995
)
1.53
" Cognitive function testing was performed before dosing and over a 24-hour period after dosing on Days 1, 2, and 25."( Absence of effect of sertraline on time-based sensitization of cognitive impairment with haloperidol.
Oliver, SD; Rapeport, WG; Wesnes, K; Williams, SA, 1996
)
0.52
"Haloperidol, a neuroleptic, was orally administered at 0, 3, 10, 30 and 60 mg/kg/day in a 4-week dosing study, and 0, 3, 10 and 30 mg/kg/day in a 9-week dosing study, to Sprague-Dawley male rats which were then sacrificed for histopathological examination or mated with untreated females."( Collaborative work to determine an optimal administration period and optimal parameters for detection of effects on male fertility in rats--male reproductive toxicity study of haloperidol.
Imanishi, M; Takagi, S; Takeuchi, M; Yoneyama, M, 1995
)
1.93
" In vivo, risperidone showed the highest potency for 5-HT2A-receptor occupancy; To obtain the same extent of D2-receptor occupancy, a 19-times higher dosage was required."( In vitro receptor binding and in vivo receptor occupancy in rat and guinea pig brain: risperidone compared with antipsychotics hitherto used.
Bonaventure, P; Janssen, PF; Leysen, JE; Schotte, A, 1995
)
0.29
"(-)-Pentazocine is active in the tailflick assay in CD-1 mice, although it shows a biphasic dose-response curve with a peak effect of only 30%."( (-)-Pentazocine analgesia in mice: interactions with a sigma receptor system.
Chien, CC; Pasternak, GW, 1995
)
0.29
" The dose-response curves at which each drug produced vacuous jaw movements are presented and discussed in terms of their predictive capabilities of early onset extrapyramidal side effects."( The effects of raclopride on vacuous jaw movements in rats following acute administration.
Harrington, A; Kaczmarek, HJ; Steinpreis, RE, 1996
)
0.29
" The administration of 5 mg of haloperidol to subjects dosed with nefazodone to steady state led to a modest pharmacokinetic interaction, as indicated by a 36, 13, and 37% increase in mean area under the curve (AUC0-12), highest concentration, and 12-h concentration values for haloperidol, respectively; only the increase in AUC was statistically significant."( Investigation of pharmacokinetic and pharmacodynamic interactions after coadministration of nefazodone and haloperidol.
Barbhaiya, RH; Breul, HP; Greene, DS; Midha, KK; Shukla, UA, 1996
)
0.79
" Patients were maintained on monthly depot treatment for 40 weeks after the loading dose regimen and only one patient relapsed during treatment despite dosage increases."( Haloperidol and reduced haloperidol plasma concentrations after a loading dose regimen with haloperidol decanoate.
Chang, WH; Jann, MW; Lin, HN; Piao-Chien, C; Wei, FC, 1996
)
1.74
" Following systemic (intraperitoneal) administration of apomorphine (a dopamine receptor D1/D2 mixed agonist), SKF 38393 (D1 > D3 > D2 agonist), LY 17155 or quinpirole (D3 > D2 and D1) agonist), haloperidol (a DA-D2 antagonist), and clonidine (noradrenaline receptor alpha 2 agonist), the ICSS response rates evoked from LH-MFB and VTA-SN were compared with vehicle or saline-treated animals on the basis of dose-response functions."( Dose-response functions of apomorphine, SKF 38393, LY 171555, haloperidol and clonidine on the self-stimulation evoked from lateral hypothalamus and ventral tegmentum.
Desiraju, T; Raju, TR; Singh, J, 1996
)
0.72
" Our data indicate a need to establish dose-response curves for the conventional neuroleptics."( Positron emission tomography studies on D2 dopamine receptor occupancy and plasma antipsychotic drug levels in man.
Farde, L; Halldin, C; Nordström, AL; Nyberg, S, 1995
)
0.29
" The results of this preliminary study suggest that, in the management of delirium, appropriate usage of haloperidol on the first day is important as it affects the dosage thereafter."( Usage of haloperidol for delirium in cancer patients.
Akechi, T; Fukue, M; Kagaya, A; Nishida, A; Okamura, H; Oomori, N; Uchitomi, Y; Yamawaki, S, 1996
)
0.93
" The recommended initial dosage was 150 mg bromperidol (one 3 ml ampoule), and this did not in fact have to be increased during the trial."( [Bromperidol decanoate in the residual phase of schizophrenia].
Canova, L; Cocconcelli, C; Faravelli, C; Marchetti, FP; Mariani, G; Rapisarda, V; Smeraldi, E, 1996
)
0.29
" The methods are illustrated on a data set involving alternative dosage regimens for the treatment of schizophrenia using haloperidol and on a regression example."( Pattern-mixture models for multivariate incomplete data with covariates.
Little, RJ; Wang, Y, 1996
)
0.5
" Three notions have been utilized conceptually to explain the distinction between atypical versus typical antipsychotic drugs: 1) dose-response separation between particular pharmacologic functions; 2) anatomic specificity of particular pharmacologic activities; 3) neurotransmitter receptor interactions and pharmacodynamics."( Mechanisms of action of atypical antipsychotic drugs: a critical analysis.
Kinon, BJ; Lieberman, JA, 1996
)
0.29
" Criteria for evaluation were derived from the medical literature and product information, and included the following areas: diagnosis, stabilization on a short-acting form of the antipsychotic, appropriateness of dosage conversion to depot therapy, concomitant administration of short-acting antipsychotics (and duration of concomitant medications), and plasma concentration monitoring."( Evaluation of inpatient depot antipsychotic prescribing.
Crismon, ML; Dorson, PG; Pabis, DJ, 1996
)
0.29
" These patients were receiving a stable dosage of a short-acting antipsychotic prior to conversion to depot therapy (i."( Evaluation of inpatient depot antipsychotic prescribing.
Crismon, ML; Dorson, PG; Pabis, DJ, 1996
)
0.29
"Risperidone had a bell-shaped dose-response curve, with optimal therapeutic responses occurring at a daily dose of 8 mg."( [Risperidone in the treatment of chronic schizophrenia: multicenter study comparative to haloperidol].
Ayuso, JL; Chinchilla, A; Eguiluz, I; Fernández, A; González Pinto, A; Guimon, J; Gutiérrez, M; Herraiz, ML; López Ibor, JJ,
)
0.35
" We discuss a possible relation between serotonin syndrome and a highly dosed combination therapy with moclobemide."( [Depressive stupor--malignant neuroleptic syndrome--serotonin syndrome. A case contribution to a difficult differential diagnosis].
König, F; Löble, M; Wolfersdorf, M, 1996
)
0.29
" Patients were treated with risperidone in two different dosage groups (3 mg and 8 mg) and haloperidol (10-20 mg) and compared with eight healthy control subjects."( Striatal dopamine-2 receptor occupancy in psychotic patients treated with risperidone.
Asenbaum, S; Brücke, T; Gössler, R; Kasper, S; Küfferle, B; Podreka, I; Tauscher, J; Topitz-Schratzberger, A; Vesely, C, 1996
)
0.51
" The dose-response curve at antigen challenge is steep."( Anaphylactic bronchoconstriction in immunized guinea pigs provoked by inhalation and intravenous administration of hexahydrophthalic anhydride and methyltetrahydrophthalic anhydride.
Jonson, B; Welinder, H; Zhang, XD; Zhao, H, 1997
)
0.3
" We have shown that sigma ligands, such as di(2-tolyl)guanidin (DTG), potentiate dose-dependently, with bell-shaped dose-response curves, the neuronal response of pyramidal neurones to N-methyl-D-aspartate (NMDA) in the CA3 region of the rat dorsal hippocampus."( Effect of short-term and long-term treatments with sigma ligands on the N-methyl-D-aspartate response in the CA3 region of the rat dorsal hippocampus.
Bergeron, R; de Montigny, C; Debonnel, G, 1997
)
0.3
" Based on the currently available literature, in any critically ill patient receiving droperidol or haloperidol therapy whose QTc interval lengthens by 25% or more over baseline, therapy should be discontinued or the dosage reduced."( Conduction disturbances associated with administration of butyrophenone antipsychotics in the critically ill: a review of the literature.
Lawrence, KR; Nasraway, SA,
)
0.35
" Analyses indicated that an increasing dose-response curve was observed across the range of all olanzapine dose groups."( Olanzapine versus haloperidol: acute phase results of the international double-blind olanzapine trial.
Beasley, CM; Beuzen, JN; Blin, O; Crawford, AM; Dellva, MA; Hamilton, SH; Tollefson, GD; Tran, PV, 1997
)
0.63
" The implications of the D2 occupancy findings for the optimal dosing of neuroleptics are discussed."( The relationship between D2 receptor occupancy and plasma levels on low dose oral haloperidol: a PET study.
Houle, S; Jones, C; Kapur, S; Reed, K; Remington, G; Roy, P; Zipursky, R, 1997
)
0.52
" The patient developed postural hypotension and the risperidone dosage was held at 2 mg bid."( Fatal cardiac event following initiation of risperidone therapy.
Levenson, JW; Ravin, DS,
)
0.13
" Though our findings confirm that fluoxetine impairs haloperidol clearance, this interaction is unlikely to have adverse clinical consequences, at least in patients chronically stabilized on a low dosage of haloperidol."( Interaction between fluoxetine and haloperidol: pharmacokinetic and clinical implications.
Avenoso, A; Campo, G; Caputi, AP; Facciolă, G; Ferlito, M; Perucca, E; Spinà, E; Zuccaro, P, 1997
)
0.82
"Five fixed doses of the atypical antipsychotic "Seroquel" (quetiapine) were evaluated to delineate a dose-response relationship, as measured by changes from baseline in Brief Psychiatric Rating Scale (BPRS), Clinical Global Impression (CGI), and Modified Scale for the Assessment of Negative Symptoms (SANS) summary scores, and to compare efficacy and tolerability opposite placebo and haloperidol."( Multiple fixed doses of "Seroquel" (quetiapine) in patients with acute exacerbation of schizophrenia: a comparison with haloperidol and placebo. The Seroquel Trial 13 Study Group.
Arvanitis, LA; Miller, BG, 1997
)
0.67
" Compound 6, 3-benzyl-8-methyl-1,2,3,4-tetrahydrochromeno[3,4-c]pyridin-5-one, increased DOPA (L-3,4-dihydroxyphenylalanine) synthesis 84% in the hippocampus and 10% in the striatum of rat brain when dosed orally at 10 mg/kg."( Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents.
Capiris, T; Connor, DT; Heffner, TG; MacKenzie, RG; Miller, SR; Pugsley, TA; Unangst, PC; Wise, LD, 1997
)
0.3
"Thirty-seven newly admitted schizophrenic patients were treated with an open and flexible dosage of chlorpromazine for 3 months after receiving a test dose."( Prediction of drug responses in schizophrenia: a method using a test dose of chlorpromazine.
Minami, H; Miyahara, A; Nakahara, T; Nakane, Y, 1997
)
0.3
" In addition, the polymorphic distribution of RH/HL ratios, suggested by previous investigators, was further tested in each dosage group (for controlling the potential dosage effect on RH/HL ratios)."( Dose-dependent reduced haloperidol/haloperidol ratios: influence of patient-related variables.
Chang, WH; Chang, YC; Hu, OY; Hu, WH; Jann, MW; Lane, HY; Lin, HN, 1997
)
0.61
" Once these movement disorders were induced, they consistently reappeared after further treatment with haloperidol, and once haloperidol dosing was discontinued, the episodes vanished."( The common marmoset (Callithrix jacchus) as a model for neuroleptic-induced acute dystonia.
Fukuoka, T; Kohda, A; Matsuo, M; Nakano, M; Okuno, Y, 1997
)
0.51
" A significantly greater percentage of subjects receiving combined treatment improved on the specific measures 60 minutes after dosing (p<0."( A double-blind study of lorazepam versus the combination of haloperidol and lorazepam in managing agitation.
Bieniek, SA; Dominguez, RA; Ownby, RL; Penalver, A,
)
0.37
" While suspected anaphylaxis needs to be vigorously treated, a history of neuroleptic use and particularly of a recent dosage increase should alert clinicians to the possibility of acute laryngeal dystonia."( Neuroleptic-induced laryngeal dystonia can mimic anaphylaxis.
Ilchef, R, 1997
)
0.3
" Incipient congenic strains of D2R-deficient mice demonstrated an orderly gene dosage reduction in locomotion superimposed on both extremes of parental background locomotor activity."( Locomotor activity in D2 dopamine receptor-deficient mice is determined by gene dosage, genetic background, and developmental adaptations.
Bunzow, JR; Burkhart-Kasch, S; Fang, Y; Gerhardt, GA; Grandy, DK; Kelly, MA; Lessov, CN; Low, MJ; Phillips, TJ; Rubinstein, M; Zhang, G, 1998
)
0.3
" In conclusion, the present studies demonstrate that in the case of sequential dosing olanzapine more effectively enhances DA and NE release in the Pfc than in the subcortical areas, which may have an impact on its atypical antipsychotic actions."( Olanzapine increases in vivo dopamine and norepinephrine release in rat prefrontal cortex, nucleus accumbens and striatum.
Bymaster, FP; Li, XM; Perry, KW; Wong, DT, 1998
)
0.3
" Twenty-one patients meeting DSM-III criteria for schizophrenia were enrolled; all patients had been stabilized for at least 2 weeks on their dosage of neuroleptic medicine before entering the study."( Naltrexone augmentation of neuroleptics in schizophrenia.
Charney, DS; Glazer, WM; Heninger, GR; Krystal, JH; Petrakis, IL; Price, LH; Sernyak, MJ; Woods, SW, 1998
)
0.3
" The recovery of haloperidol in synthetic mixtures with parabens and pharmaceutical dosage forms is also reported."( Zero-crossing derivative spectrophotometry for the determination of haloperidol in presence of parabens.
Bouzouita, K; Kallel, M; Ouanês, S; Safta, F; Trabelsi, H, 1998
)
0.88
" Blood concentration increased in proportion to the HP dosage in all patients, and its average was significantly higher than that of the control group."( [Pharmacokinetics of haloperidol in patients on hemodialysis].
Sanga, M; Shigemura, J, 1998
)
0.62
" The aim of this study was to evaluate the degree of dopamine D2 receptor occupancy in relation to the neuroleptic dosage and to correlate the findings with the presence of extrapyramidal symptoms (EPS)."( Iodine-123-iodobenzamide SPECT assessment of dopamine D2 receptor occupancy in riperidone-treated schizophrenic patients.
Dähne, I; Dresel, S; Hahn, K; Mager, T; Scherer, J; Tatsch, K, 1998
)
0.3
" The degree of occupancy displayed an exponential dose-response relationship (r = -0."( Iodine-123-iodobenzamide SPECT assessment of dopamine D2 receptor occupancy in riperidone-treated schizophrenic patients.
Dähne, I; Dresel, S; Hahn, K; Mager, T; Scherer, J; Tatsch, K, 1998
)
0.3
"The findings suggest an exponential dose-response relationship between the daily dosage of risperidone and the dopamine D2 receptor occupancy."( Iodine-123-iodobenzamide SPECT assessment of dopamine D2 receptor occupancy in riperidone-treated schizophrenic patients.
Dähne, I; Dresel, S; Hahn, K; Mager, T; Scherer, J; Tatsch, K, 1998
)
0.3
" The results of the study indicate that the immunomodulatory effects of the neuroleptics depend mainly on dosage and experimental conditions."( Influence of neuroleptics on cytotoxic activity of macrophages in rats.
Belowski, D; Herman, ZS; Kowalski, J; Madej, A, 1998
)
0.3
"This 4-week, double-blind, randomized study was undertaken to determine the dose-response relationship of amisulpride in 319 patients with acute exacerbation of schizophrenia."( Amisulpride, and atypical antipsychotic, in the treatment of acute episodes of schizophrenia: a dose-ranging study vs. haloperidol. The Amisulpride Study Group.
Fleurot, O; Puech, A; Rein, W, 1998
)
0.51
" In contrast, increasing doses of amperozide resulted in decreasing vacuous jaw movements for this portion of the dose-response curve."( The effects of the atypical antipsychotic amperozide on vacuous jaw movements in rats: a novel dose response profile.
Moser, L; Panos, J; Parret, F; Rutell, E; Steinpreis, RE, 1998
)
0.3
") dosing of 10 mg/kg/day acrylamide produced a selective impairment of hindlimb hopping."( A force plate system for measuring low-magnitude reaction forces in small laboratory animals.
Carr, GJ; Handley, DE; Ross, JF, 1998
)
0.3
" A simulation of this dependence of clinical improvement on serum levels, mediated by the variable dose design, can be excluded because of the results of a retrospective analysis of dosing behavior."( Therapeutic window of serum haloperidol concentration in acute schizophrenia and schizoaffective disorder.
Braun, V; Meyer, FP; Neuhof, S; Ulrich, S, 1998
)
0.59
", 30 min) were administered to rats for 4 weeks in a between-groups dosing design."( Haloperidol, raclopride, and eticlopride induce microcatalepsy during operant performance in rats, but clozapine and SCH 23390 do not.
Fowler, SC; Liou, JR, 1998
)
1.74
" Sixteen patients who did not respond to the traditional antipsychotics after 2 weeks of treatment with a certain dosage of haloperidol were administered with 50 mg of sertraline for a period of 2 weeks."( Co-administration of sertraline and haloperidol.
Han, CS; Kim, SH; Lee, MS; You, YW, 1998
)
0.78
" Doses were increased weekly until the optimal therapeutic dosage was achieved."( An investigation of ethnic and gender differences in the pharmacodynamics of haloperidol.
Bean, G; Beiser, M; Zhang-Wong, J; Zipursky, RB, 1998
)
0.53
" Sulpiride increased the maximum effect afforded by different concentrations of NMDA and shifted the dose-response curve of NMDA to the left (EC50 value from 12."( Neuroleptics with differential affinities at dopamine D2 receptors and sigma receptors affect differently the N-methyl-D-aspartate-induced increase in intracellular calcium concentration: involvement of protein kinase.
Hayashi, T; Kagaya, A; Nishida, A; Shimizu, M; Su, TP; Yamawaki, S, 1999
)
0.3
"Symptoms of the autonomic nervous system were more effectively prevented by GHB as evident in the lower dosage requirement of clonidine."( [Gamma-hydroxybutyrate for treatment of alcohol withdrawal syndrome in intensive care patients. A comparison between with two symptom-oriented therapeutic concepts].
Lenzenhuber, E; Müller, C; Rommelspacher, H; Spies, C, 1999
)
0.3
"The relative affinity of metoclopramide as indicated by K(B) values was calculated in control and in haloperidol-withdrawn rats treated or not with monosialoganglioside-1 (GM1) by using dose-response curves constructed for apomorphine-induced stereotyped behavior."( Kinetic analysis of GM1 effects on haloperidol-induced dopaminergic supersensitivity.
Frussa-Filho, R; Palermo-Neto, J; Vital, MA, 1999
)
0.8
" The results indicate that at low doses haloperidol dose-dependently reduces intromission frequency, and the effect of a repeated dosage may persist several days after cessation of medication."( Effects of repeated low dose administration and withdrawal of haloperidol on sexual behaviour of male rats.
Haapalinna, A; Männistö, PT; Saano, V; Tupala, E; Viitamaa, T, 1999
)
0.81
" Assessments of attention, memory and motor control were made prior to dosing on each day, at 2, 4, 6 and 8 h after dosing on days 1 and 4, and at 24 and 48 h following the last dose."( A comparison of the effects of olanzapine, haloperidol and placebo on cognitive and psychomotor functions in healthy elderly volunteers.
Beuzen, JN; Taylor, N; Wesnes, K; Wood, A, 1999
)
0.57
" The catalepsy-reversal action of the diethylglycine-substituted peptidomimetic 5 was examined further and found to exhibit a U-shaped dose-response effect with an optimal dose of 1 microg/kg."( Modulatory effects of PLG and its peptidomimetics on haloperidol-induced catalepsy in rats.
Buckley, AT; Costain, WJ; Evans, MC; Johnson, RL; Mishra, RK, 1999
)
0.55
" Only with haloperidol (maximum 60%), risperidone (maximal 20%), and olanzapine (maximal 20%) a partial antagonism without clearcut dose-response was observed."( Inability of antipsychotics to antagonize the cueing properties of cocaine in rats.
De Haes, P; Meert, TF; van Campenhout, N, 1999
)
0.69
" We describe the case of a 41-year-old white woman with no predisposing factors who developed torsade de pointes 55 minutes after a dose of intravenous haloperidol 80 mg (total dosage 915 mg over 7 d)."( Haloperidol-induced torsade de pointes.
O'Brien, JM; Rockwood, RP; Suh, KI, 1999
)
1.94
" Haloperidol maximal effect (Emax) was less than the effect of the full agonist norepinephrine (NE), and dose-response curves for both NE in the presence of submaximal doses of haloperidol and haloperidol in the presence of Emax doses of NE showed that haloperidol behaves as a partial agonist of cerebral alpha1-adrenoceptors."( Haloperidol-mediated phosphoinositide hydrolysis via direct activation of alpha1-adrenoceptors in frontal cerebral rat cortex.
Borda, TG; Cremaschi, G; Sterin-Borda, L, 1999
)
2.66
"Antipsychotic dosing for acute mania has not been well studied."( Acute mania: haloperidol dose and augmentation with lithium or lorazepam.
Allen, MH; Charles, O; Chou, JC; Czobor, P; Trujillo, M; Tuma, I; Volavka, J; Winsberg, B, 1999
)
0.67
" Daily dosing requirements were less in the elderly for intermittent intravenous lorazepam, haloperidol, and morphine but not for midazolam (p=0."( Frequency, severity, and treatment of agitation in young versus elderly patients in the ICU.
Berthiaume, D; Fraser, GL; Prato, BS; Riker, RR; Wilkins, ML, 2000
)
0.53
"With the background of a number of meta-analyses on the optimal neuroleptic dosages [1,2] the average daily dosage for the treatment of acute schizophrenic episodes recommended in the internal treatment guidelines of our psychiatric clinic was reduced from 24 mg to 15 mg haloperidol equivalent."( ["More is less": a retrospective study of haloperidol dosages in acute schizophrenia].
Kissling, W; Kockott, G; Müller, R, 2000
)
0.75
"The evaluation of the treatment data showed that the dosing guideline was adhered to and in 1991/92 on the average actually only 15 mg haloperidol were prescribed daily in acute schizophrenic episodes."( ["More is less": a retrospective study of haloperidol dosages in acute schizophrenia].
Kissling, W; Kockott, G; Müller, R, 2000
)
0.77
" We exemplify how this dosing confounder could lead to inappropriate conclusions."( Are animal studies of antipsychotics appropriately dosed? Lessons from the bedside to the bench.
Kapur, S; Remington, G; Wadenberg, ML, 2000
)
0.31
"These results suggest that pretreatment plasma HVA could be useful for dosing antipsychotics."( Pretreatment plasma HVA and haloperidol response in acute mania.
Bebe, R; Chang, WH; Charles, O; Chou, JC; Cooper, TB; Czobor, P; Lane, HY; Stone, DL; Tuma, I, 2000
)
0.6
" Dosage regimens were flexible (amisulpride 200-800 mg/day, haloperidol 5-20 mg/day)."( Long-term safety and efficacy of amisulpride in subchronic or chronic schizophrenia. Amisulpride Study Group.
Colonna, L; Dondey-Nouvel, L; Rein, W; Saleem, P, 2000
)
0.55
" Increases in serum PRL levels are enhanced when daily dosages are administered via multiple-daily dosing of the test compound, which results in higher sustained blood levels of the test compounds."( Detection of dopaminergic modulators in a tier I screening battery for identifying endocrine-active compounds (EACs).
Cook, JC; Davis, LG; Frame, SR; O'Connor, JC,
)
0.13
" On each study day, cognitive performance was assessed prior to dosing and at 2, 4, 6, 9, 12 and 24 h after dosing with the following tests from the Cognitive Drug Research computerized assessment system: simple reaction time, digit vigilance task, choice reaction time, visual tracking, Critical Flicker Fusion, body sway, numeric working memory, immediate and delayed word recall, word recognition and self-ratings of mood and alertness."( The acute effects of amisulpride (50 mg and 200 mg) and haloperidol (2 mg) on cognitive function in healthy elderly volunteers.
Bergougnan, L; Canal, M; L'Heritier, C; Legangneux, E; McEwen, J; Miget, N; Pinquier, JL; Rosenzweig, P; Wesnes, KA, 2000
)
0.55
" A dose-response relationship was not consistently confirmed with any of the drug treatments."( The effects of olanzapine, risperidone, and haloperidol on plasma prolactin levels in patients with schizophrenia.
Breier, A; David, SR; Kinon, BJ; Taylor, CC, 2000
)
0.57
" No consistent dose-response relationship was observed, and the time course and sex-dependency of the response differed between the 3 agents."( The effects of olanzapine, risperidone, and haloperidol on plasma prolactin levels in patients with schizophrenia.
Breier, A; David, SR; Kinon, BJ; Taylor, CC, 2000
)
0.57
"The steady-state trough concentrations of haloperidol were studied to clarify the role of the characteristics of Japanese patients in estimating haloperidol dosing regimens by using routine therapeutic drug-monitoring data."( Epidemiologic investigation of the relative clearance of haloperidol by mixed-effect modeling using routine clinical pharmacokinetic data in Japanese patients.
Anai, M; Funakoshi, A; Goto, Y; Higuchi, S; Hokazono, T; Ichimaru, R; Makit, T; Matsunaga, K; Ohdo, S; Yukawa, E; Yukawa, M, 2000
)
0.82
" Correlations between drug dosage and plasma drug levels were significant for haloperidol and thioridazine, but not for lorazepam."( Relationships between psychotropic drug dosage, plasma drug concentration, and prolactin levels in nursing home residents.
Billig, N; Cohen-Mansfield, J; Lipson, S; Taylor, L; Werner, P; Woosley, R, 2000
)
0.54
" We also provide evidence of deficient NT neurotransmission as well as a left-shifted antipsychotic drug dose-response curve in isolation-reared rats."( Enhanced neurotensin neurotransmission is involved in the clinically relevant behavioral effects of antipsychotic drugs: evidence from animal models of sensorimotor gating.
Binder, EB; Kilts, CD; Kinkead, B; Nemeroff, CB; Owens, MJ, 2001
)
0.31
" Weanling male CD rats (21 days old) were dosed for 30 d by gavage with vehicle (0."( Evaluation of the male pubertal assay's ability to detect thyroid inhibitors and dopaminergic agents.
Carney, EW; Crissman, JW; Marty, MS, 2001
)
0.31
" Prolonged administration of haloperidol to mice resulted in complex I loss in frontal cortex, hippocampus, striatum and midbrain, while chronic dosing with clozapine affected only hippocampus and frontal cortex."( Protein thiol oxidation by haloperidol results in inhibition of mitochondrial complex I in brain regions: comparison with atypical antipsychotics.
Balijepalli, S; Boyd, MR; Kenchappa, RS; Ravindranath, V, 2001
)
0.9
" Following 30 sessions of training, dose-response functions were determined for HA (0."( Schedule-dependent effects of haloperidol and amphetamine: multiple-schedule task shows within-subject effects.
Brindle, NA; Caul, WF, 2001
)
0.6
" A similar dose-response relationship was determined for nifedipine, an L-type calcium channel antagonist."( Pharmacological involvement of the calcium channel blocker flunarizine in dopamine transmission at the striatum.
Armando, I; Belforte, JE; Buño, W; Magariños-Azcone, C; Pazo, JH, 2001
)
0.31
" Haloperidol blood levels may be clinically useful in identifying patients who are nonresponsive because of low drug levels and, hence, in enhancing optimal haloperidol dosing for acute mania with psychosis."( Haloperidol blood levels in acute mania with psychosis.
Chou, JC; Cooper, TB; Czobor, P; Dacpano, G; Richardson, N; Trujillo, M; Tuma, I; Volavka, J, 2001
)
2.66
" The dissociation constant (K(B)) and relative intrinsic efficacy (E(r)) for each partial agonist were calculated using a partial agonist interaction null model in which the effects of fixed concentrations of each partial agonist on the dopamine dose-response curve were evaluated."( Nonlinear analysis of partial dopamine agonist effects on cAMP in C6 glioma cells.
Abell, C; Avalos, M; Kwan, SW; Mak, C; Randall, PK; Trzeciakowski, JP; Wilcox, RE,
)
0.13
" In addition, the C57BL/6 strain exhibited a greater degree of sensitization to repeated dosing than did the other 2 strains."( Haloperiodol-induced microcatalepsy differs in CD-1, BALB/c, and C57BL/6 mice.
Fowler, SC; Vorontsova, E; Zarcone, TJ, 2001
)
0.31
" Cramping abdominal pain associated with mechanical bowel obstruction often can be managed with morphine (titrating the dosage for pain) and octreotide."( Management of common symptoms in terminally ill patients: Part II. Constipation, delirium and dyspnea.
Alexander, CS; Ross, DD, 2001
)
0.31
" The trial was divided into two periods: eight weeks during which the dosage was escalated and then fixed, and six weeks during which variable dosages were used."( Effects of clozapine, olanzapine, risperidone, and haloperidol on hostility among patients with schizophrenia.
Chakos, M; Citrome, L; Cooper, TB; Czobor, P; Lieberman, JA; Lindenmayer, JP; McEvoy, J; Sheitman, B; Volavka, J, 2001
)
0.56
" This meta-analysis provided no information about the relationship between the degree of dementia, the kind of agitation manifested, or the dosage and duration of therapy with haloperidol and response to treatment of demented patients with agitation."( Haloperidol for agitation in dementia.
Colford, J; Lonergan, E; Luxenberg, J, 2001
)
1.95
" Because of the wide focus of this meta-analysis, not enough information was provided to permit recommendations linking haloperidol treatment of agitated dementia to degree of dementia, manifestations of agitation, or dosage and duration of treatment of haloperidol."( Haloperidol for agitation in dementia.
Colford, J; Lonergan, E; Luxenberg, J, 2001
)
1.96
"336( AGE> or = 65), where CL is total body clearance (L/h), Vd is apparent volume of distribution (L), TBW is total bodyweight (kg), DOSE is daily dosage (microg/kg/day), ANTIEP = 1 for concomitant administration of antiepileptic drugs (phenobarbital, phenytoin or carbamazepine) and 0 otherwise, AGE > or = 55 = 1 for patient aged 55 years or over and 0 otherwise, and AGE > or = 65 = 1 for patient aged 65 years or over and 0 otherwise."( Population pharmacokinetics of haloperidol using routine clinical pharmacokinetic data in Japanese patients.
Anai, M; Goto, Y; Higuchi, S; Hokazono, T; Ichimaru, R; Maki, T; Matsunaga, K; Ohdo, S; Yukawa, E; Yukawa, M, 2002
)
0.6
"Application of the findings in this study to patient care may permit selection of an appropriate initial maintenance dosage to achieve target haloperidol serum concentrations, thus enabling the clinician to achieve the desired therapeutic effect."( Population pharmacokinetics of haloperidol using routine clinical pharmacokinetic data in Japanese patients.
Anai, M; Goto, Y; Higuchi, S; Hokazono, T; Ichimaru, R; Maki, T; Matsunaga, K; Ohdo, S; Yukawa, E; Yukawa, M, 2002
)
0.8
" Key assessments included the pharmacokinetics of quetiapine at steady state (area under the curve within a dosing interval [AUCtSS], maximum [CmaxSS], and minimum [CminSS] observed plasma concentrations, and oral clearance [Cl/f]), as well as the UKU Side Effect Rating Scale scores and safety evaluations."( The safety and pharmacokinetics of quetiapine when coadministered with haloperidol, risperidone, or thioridazine.
Alva, G; Arvanitis, LA; Bera, R; Potkin, SG; Thyrum, PT; Yeh, C, 2002
)
0.55
" These findings suggest that acute dystonia is affected by age factor, and that daily dosage or monitoring of drug concentration is unlikely to be a useful marker for the prediction of side-effects during bromperidol treatment."( The characteristics of side-effects of bromperidol in schizophrenic patients.
Ishida, M; Kaneko, S; Kondo, T; Mihara, K; Otani, K; Tanaka, O; Yasui-Furukori, N, 2002
)
0.31
" A dose-response relationship for IM olanzapine in the reduction of agitation was assessed by measuring the reduction in Positive and Negative Syndrome Scale Excited Component (PANSS-EC) scores 2 hours after the first injection."( A double-blind, placebo-controlled dose-response comparison of intramuscular olanzapine and haloperidol in the treatment of acute agitation in schizophrenia.
Birkett, M; Breier, A; Brook, S; David, S; Dossenbach, M; Ferchland, I; Kiesler, G; Meehan, K; Palmer, R; Sutton, V; Taylor, CC; Wright, P, 2002
)
0.53
"Olanzapine exhibited a dose-response relationship for reduction in agitation (F(1,179)= 14."( A double-blind, placebo-controlled dose-response comparison of intramuscular olanzapine and haloperidol in the treatment of acute agitation in schizophrenia.
Birkett, M; Breier, A; Brook, S; David, S; Dossenbach, M; Ferchland, I; Kiesler, G; Meehan, K; Palmer, R; Sutton, V; Taylor, CC; Wright, P, 2002
)
0.53
"0 mg per injection exhibits a dose-response relationship in the rapid treatment of acute agitation in patients with schizophrenia and demonstrates a favorable safety profile."( A double-blind, placebo-controlled dose-response comparison of intramuscular olanzapine and haloperidol in the treatment of acute agitation in schizophrenia.
Birkett, M; Breier, A; Brook, S; David, S; Dossenbach, M; Ferchland, I; Kiesler, G; Meehan, K; Palmer, R; Sutton, V; Taylor, CC; Wright, P, 2002
)
0.53
" Variations in degree of dementia, dosage and length of haloperidol treatment, and in ways of assessing response to treatment suggested caution in the interpretation of reported effects of haloperidol in the management of agitated dementia."( Haloperidol for agitation in dementia.
Colford, J; Lonergan, E; Luxenberg, J, 2002
)
2
" Using either a slower dose-titration or a high, single loading dose followed by a low maintenance dosing may have offered the possibility to obtain a good antipsychotic effect together with low incidence of EPS."( Savoxepine versus haloperidol. Reasons for a failed controlled clinical trial in patients with an acute episode of schizophrenia.
Bischoff, S; Gerebtzoff, A; Möller, HJ; Volz, HP, 2002
)
0.65
" This double-blind, randomized controlled trial, comparing flexible dosing of olanzapine (5-20 mg/day, n = 234) to haloperidol (3-15 mg/day, n = 219), consisted of a 6-week acute phase, followed by a 6-week continuation phase."( Olanzapine versus haloperidol in the treatment of acute mania: clinical outcomes, health-related quality of life and work status.
Breier, A; Edgell, ET; Gandhi, G; Haro, JM; Namjoshi, MA; Shi, L; Tohen, M; Zhang, F, 2002
)
0.86
" D2 receptor blockade, a dose-response study was employed to determine whether low doses of these atypical antipsychotics would also upregulate hippocampal BDNF mRNA in the absence of significant D2 receptor blockade."( Differential regulation of hippocampal BDNF mRNA by typical and atypical antipsychotic administration.
Ashe, P; Chlan-Fourney, J; Juorio, AV; Li, XM; Nylen, K, 2002
)
0.31
"A dose-response relationship between dopamine D(2) occupancy and acute extrapyramidal symptoms (EPS) has been well established."( The relationship between dopamine D2 receptor occupancy and the vacuous chewing movement syndrome in rats.
Kapur, S; Nobrega, JN; Remington, G; Turrone, P, 2003
)
0.32
"049) and a linear dose-response relation (P=0."( Cardiac arrest and ventricular arrhythmia in patients taking antipsychotic drugs: cohort study using administrative data.
Bilker, WB; Glasser, DB; Hennessy, S; Kimmel, SE; Knauss, JS; Margolis, DJ; Morrison, MF; Reynolds, RF; Strom, BL, 2002
)
0.31
"The present analysis investigated symptom-specific dose-response relationships of the atypical antipsychotic amisulpride (AMI) in schizophrenic patients."( Dose-related effects of amisulpride on five dimensions of psychopathology in patients with acute exacerbation of schizophrenia.
Benkert, O; Eich, FX; Müller, MJ; Puech, A; Rein, W; Wetzel, H, 2002
)
0.31
" A comparison of citalopram and fluoxetine pharmacokinetics in the same animal and at the same dosage (1 mg/kg) showed that citalopram SERT occupancy and plasma half-lives were 9 times and 14 times shorter, respectively, than those of fluoxetine and norfluoxetine."( [11C]-DASB, a tool for in vivo measurement of SSRI-induced occupancy of the serotonin transporter: PET characterization and evaluation in cats.
Ginovart, N; Houle, S; Hussey, D; Meyer, JH; Wilson, AA, 2003
)
0.32
" ChAT staining in the caudate-putamen and hippocampus was also decreased after 90 days of RISP exposure, raising the possibility of deleterious cognitive effects after exposure to this dosage for longer periods of time."( Differential effects of haloperidol, risperidone, and clozapine exposure on cholinergic markers and spatial learning performance in rats.
Evans, DR; Hill, WD; Mahadik, SP; Parikh, V; Terry, AV; Waller, JL, 2003
)
0.63
" Controlled released transdermal dosage form (TDDS) of the drug was designed for maintenance therapy."( Transdermal drug delivery system of haloperidol to overcome self-induced extrapyramidal syndrome.
Dube, R; Samanta, MK; Suresh, B, 2003
)
0.59
" Measuring rectal body temperatures, dose-response relationships were established for all compounds."( Morphine and d-amphetamine nullify each others' hypothermic effects in mice.
Baker, A; Meert, T, 2003
)
0.32
" At a lower daily dosage of HAL (<10 mg/day), the subjects with two or one CYP2D6*10 allele(s) showed significantly higher plasma concentrations of RHAL (0."( Effect of CYP2D6 genotypes on the metabolism of haloperidol in a Japanese psychiatric population.
Hirokane, G; Kawashima, Y; Morita, S; Sato, S; Shimoda, K; Someya, T; Suzuki, Y; Takahashi, S; Yokono, A, 2003
)
0.57
" We performed (1) a meta-analysis of randomized efficacy trials comparing SGAs and FGAs, (2) comparisons between SGAs, (3) a dose-response analysis of FGAs and SGAs, and (4) an analysis of the effect on efficacy of an overly high dose of an FGA comparator."( A meta-analysis of the efficacy of second-generation antipsychotics.
Chen, N; Davis, JM; Glick, ID, 2003
)
0.32
" Thus, for example, NT69L after five daily injections at a fixed dosage was as effective at reversing cocaine-induced hyperactivity as after the first injection."( Selective tolerance to the hypothermic and anticataleptic effects of a neurotensin analog that crosses the blood-brain barrier.
Boules, M; Fauq, A; McCormick, D; McMahon, B; Richelson, E; Stewart, J; Wang, R; Warrington, L; Yerbury, S, 2003
)
0.32
"Double-blind data on patients age > or =60 randomized to 5 mg/d OLZ (n=83) or 5 mg/d HAL (n=34) (Week 1) then flexibly dosed to 5-20 mg/d over six weeks, with a 48-week extension for responders, were analyzed post-hoc."( Olanzapine vs haloperidol in geriatric schizophrenia: analysis of data from a double-blind controlled trial.
Breier, A; Bymaster, FP; Dossenbach, M; Gilmore, JA; Golshan, S; Jeste, D; Kaiser, CJ; Kennedy, JS; Kinon, BJ; Maguire, GA; Sanger, T; Tollefson, G, 2003
)
0.68
"Patients were randomly assigned to receive flexibly dosed olanzapine, 5 to 20 mg/d, with prophylactic benztropine, 1 to 4 mg/d (n = 159); or haloperidol, 5 to 20 mg/d (n = 150), for 12 months."( Effectiveness and cost of olanzapine and haloperidol in the treatment of schizophrenia: a randomized controlled trial.
Allan, E; Bingham, S; Campbell, EC; Caroff, S; Collins, J; Corwin, J; Davis, L; Douyon, R; Dunn, L; Evans, D; Frecska, E; Grabowski, J; Graeber, D; Herz, L; Kwon, K; Lawson, W; Leslie, D; Liu-Mares, W; Mena, F; Perlick, D; Rosenheck, R; Sheikh, J; Smelson, D; Smith-Gamble, V; Warren, S, 2003
)
0.79
"The design consisted of 2 successive, 6-week, double-blind periods and compared flexible dosing of olanzapine (5-20 mg/d, n = 234) with haloperidol (3-15 mg/d, n = 219)."( A 12-week, double-blind comparison of olanzapine vs haloperidol in the treatment of acute mania.
Azorin, JM; Baker, RW; Breier, A; Emsley, RA; Evans, AR; Goldberg, JF; Gonzalez-Pinto Arrillaga, AM; Hardy-Bayle, MC; Lawson, WB; Namjoshi, MA; Risser, RC; Tohen, M; Vieta, E; Zhang, F, 2003
)
0.77
" A pilot dose-response study investigated an intracranial approach of topically applying endothelin-1 (ET-1) to the M2 portion of the middle cerebral artery in a small sample of marmosets for up to 6 hours (n = 2 or 3 per group)."( A new primate model of focal stroke: endothelin-1-induced middle cerebral artery occlusion and reperfusion in the common marmoset.
David, C; Elliott, H; Farnfield, B; Golder, J; Hadingham, SJ; Hunter, AJ; Parsons, AA; Roberts, JC; Virley, D; Whelan, G, 2004
)
0.32
" Haloperidol in pure form and in dosage form was assayed in this study."( Thermodynamic consideration of the charge transfer interaction of the donor: acceptor type between chloranilic acid and haloperidol.
Adikwu, MU; Akidi, FO; Attama, AA; Nnamani, PO, 2004
)
1.44
"625 mg/day) were added to a fixed dosage of haloperidol (5 mg daily)."( Conjugated estrogens as adjuvant therapy in the treatment of acute schizophrenia: a double-blind study.
Bassitt, D; Diegoli, M; Elkis, H; Gattaz, WF; Louzã, MR; Marques, AP, 2004
)
0.58
" Cox regression was used to calculate rate ratios (RRs) and 95% confidence intervals (CIs), to examine potential confounding factors, and to examine dose-response relationships."( Comparative cardiac safety of low-dose thioridazine and low-dose haloperidol.
Bilker, WB; Glasser, DB; Hennessy, S; Kimmel, SE; Knauss, JS; Margolis, DJ; Morrison, MF; Reynolds, RF; Strom, BL, 2004
)
0.56
" The mean dosage for midazolam was 18."( Use of sedation to relieve refractory symptoms in dying patients.
Blitz-Lindeque, J; Bridge, D; Cameron, D, 2004
)
0.32
" A mean therapeutic dosage for Seroquel was 316."( [Influence of long-term quetiapine (Seroquel) and haloperidol therapy on cognitive deficit in patients with paranoid schizophrenia].
Kabanov, SO; Mosolov, SN, 2004
)
0.58
"00625 mg/kg) with scopolamine shifted the dose-response curve for CLZ-appropriate responding to the left."( Discriminative stimulus properties of the atypical antipsychotic clozapine and the typical antipsychotic chlorpromazine in a three-choice drug discrimination procedure in rats.
Porter, JH; Prus, AJ; Vann, RE; Varvel, SA, 2005
)
0.33
" These results suggest that the rhythmicity of clock genes in SCN may be disturbed depending on the dosing time of Hal."( Effect of haloperidol on mPer1 gene expression in mouse suprachiasmatic nuclei.
Higuchi, S; Matsunaga, N; Ohdo, S; To, H; Viyoch, J; Yoshida, M, 2005
)
0.73
" Antipsychotic-induced laryngeal dystonia has been reported predominantly in young males, but does not correlate to the dosage or the category of the drug."( Antipsychotic drug-induced acute laryngeal dystonia: two case reports and a mini review.
Christodoulou, C; Kalaitzi, C, 2005
)
0.33
" Clinicians were instructed to target dosing at 500 mg/day of quetiapine or 200 mg of haloperidol decanoate every 4 weeks."( Long-term maintenance therapy with quetiapine versus haloperidol decanoate in patients with schizophrenia or schizoaffective disorder.
Glick, ID; Marder, SR, 2005
)
0.8
" Carbamazepine at a dosage of 800 mg daily was the most effective medication used."( Auditory hallucinations after right temporal gyri resection.
Brennan, DM; Stewart, B, 2005
)
0.33
" Initially, we established a dose-response relationship for the acute and chronic haloperidol and DOI-induced HTR."( Effects of donepezil, nicotine and haloperidol on the central serotonergic system in mice: implications for Tourette's syndrome.
Hayslett, RL; Tizabi, Y, 2005
)
0.83
" According to response, dosage was then adjusted to a maximum dosage of 20 mg daily of either drug."( Treatment response to olanzapine and haloperidol and its association with dopamine D receptor occupancy in first-episode psychosis.
Christensen, BK; Daskalakis, Z; Epstein, I; Furimsky, I; Kapur, S; Roy, P; Sanger, T; Zipursky, RB, 2005
)
0.6
" When patients were rescanned following dosage adjustment, mean D2 receptor occupancies were greater than 70% in both groups."( Treatment response to olanzapine and haloperidol and its association with dopamine D receptor occupancy in first-episode psychosis.
Christensen, BK; Daskalakis, Z; Epstein, I; Furimsky, I; Kapur, S; Roy, P; Sanger, T; Zipursky, RB, 2005
)
0.6
" Therefore, despite the potential for conversion to a hydrochloride salt form, certain nonhydrochloride salt forms may still be preferred for dosage form development due to kinetic advantages during dissolution, such as higher apparent dissolution rate of a nonhydrochloride salt before it could completely convert to the hydrochloride form."( Effect of chloride ion on dissolution of different salt forms of haloperidol, a model basic drug.
Doyle, P; Li, S; Metz, S; Royce, AE; Serajuddin, AT, 2005
)
0.57
"Patients (n=302) with bipolar I disorder (manic episode) were randomised to 12 weeks' double-blind treatment with quetiapine (flexibly dosed up to 800 mg/day), placebo, or haloperidol (up to 8 mg/day)."( Quetiapine or haloperidol as monotherapy for bipolar mania--a 12-week, double-blind, randomised, parallel-group, placebo-controlled trial.
Brecher, M; Huizar, K; McIntyre, RS; Mullen, J; Paulsson, B, 2005
)
0.88
" Patients were initiated with quetiapine to 400 mg/day over 7 days, and then flexibly dosed (300-750 mg/day) for 11 weeks."( Efficacy and tolerability of quetiapine in patients with schizophrenia who switched from haloperidol, olanzapine or risperidone.
Altman, C; de Nayer, A; Jones, AM; Larmo, I; Lindenbauer, B; Platz, T; Rittmannsberger, H; Windhager, E, 2005
)
0.55
" Some key representatives showed potent pharmacological in vivo activities after oral dosing in both the antagonism of apomorphine-induced climbing and the potentiation of 5-HTP-induced behavior in mice."( Synthesis, structure-activity relationships, and biological properties of 1-heteroaryl-4-[omega-(1H-indol-3-yl)alkyl]piperazines, novel potential antipsychotics combining potent dopamine D2 receptor antagonism with potent serotonin reuptake inhibition.
Coolen, HK; de Moes, JP; den Hartog, AP; Herremans, AH; Hesselink, MB; Keizer, HG; Kruse, CG; McCreary, AC; Niemann, LC; Plekkenpol, RH; Smid, P; Stork, B; Stroomer, CN; Tulp, MT; van Hes, R; van Stuivenberg, HH, 2005
)
0.33
" (3) Five double-blind placebo-controlled trials lasting 4 to 6 weeks showed that aripiprazole was a little more effective than placebo at daily doses of 10 mg to 30 mg, without a clear dose-response relationship."( Aripiprazole: new drug. Just another neuroleptic.
, 2005
)
0.33
" Previously, the authors demonstrated the significant dose-response relationship between abnormal liver function tests and DMF exposure and the interaction with hepatitis B virus (HBV) infection in Taiwanese workers."( Abnormal liver function associated with occupational exposure to dimethylformamide and glutathione S-transferase polymorphisms.
Chang, MJ; Cheng, TJ; Kuo, HW; Luo, JC,
)
0.13
" Results of the sensitivity analysis confirmed that the results were robust to a wide variation of different input variables (effectiveness, dosing distribution, patient status according to healthcare system)."( Long-acting risperidone compared with oral olanzapine and haloperidol depot in schizophrenia: a Belgian cost-effectiveness analysis.
Caleo, S; De Graeve, D; Lecompte, D; Mehnert, A; Miadi-Fargier, H; Mosqueda, GJ; Peuskens, J; Smet, A, 2005
)
0.57
" In addition the home cage behaviour of mice administered with the dopaminergic neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) using an acute dosing regimen was also investigated."( Further validation of LABORAS using various dopaminergic manipulations in mice including MPTP-induced nigro-striatal degeneration.
Billinton, A; Brown, M; Chapman, H; Quinn, LP; Stean, TO; Upton, N; Vidgeon-Hart, M; Virley, DJ, 2006
)
0.33
"The authors conducted a multicenter, double-blind, placebo-controlled, randomized trial of flexibly dosed quetiapine and haloperidol."( Quetiapine treatment of psychosis associated with dementia: a double-blind, randomized, placebo-controlled clinical trial.
Copenhaver, M; Katz, IR; Mintzer, JE; Schneider, L; Street, J; Tariot, PN; Williams-Hughes, C, 2006
)
0.54
" Therefore, if flupentixol's efficacy on negative symptoms is based on its interaction with 5-HT(2A) and/or D(1) receptors, it should be highly dependent on serum concentration and thus on dosage and metabolism."( Occupancy of dopamine D(1), D (2) and serotonin (2A) receptors in schizophrenic patients treated with flupentixol in comparison with risperidone and haloperidol.
Bares, R; Bartels, M; Beneke, M; Glaser, T; Machulla, HJ; Noda, S; Reimold, M; Schaefer, JE; Solbach, C; Wormstall, H, 2007
)
0.54
" When given in combination with cocaine, CJB 090 but not NGB 2904 attenuated the discriminative stimulus effects of cocaine, shifting the cocaine dose-response curve to the right."( Effects of two novel D3-selective compounds, NGB 2904 [N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-9H-fluorene-2-carboxamide] and CJB 090 [N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-4-(pyridin-2-yl)benzamide], on the reinforcing and discrimin
Claytor, R; Martelle, JL; Nader, MA; Newman, AH; Reboussin, BA; Ross, JT, 2007
)
0.34
"There is no evidence that haloperidol in low dosage has different efficacy in comparison with the atypical antipsychotics olanzapine and risperidone in the management of delirium or has a greater frequency of adverse drug effects than these drugs."( Antipsychotics for delirium.
Britton, AM; Lonergan, E; Luxenberg, J; Wyller, T, 2007
)
0.64
" However, its duration is not necessarily correlated with drug plasma levels, on which clinical dosing regimens are often based."( F15063, a potential antipsychotic with dopamine D(2)/D(3) antagonist, 5-HT(1A) agonist and D(4) partial agonist properties: (IV) duration of brain D2-like receptor occupancy and antipsychotic-like activity versus plasma concentration in mice.
Assié, MB; Auclair, A; Bardin, L; Consul-Denjean, N; Depoortère, R; Newman-Tancredi, A; Sautel, F, 2007
)
0.34
"5 and 24 h after the last dosage of chronic treatment (30 days), with haloperidol plus fluvoxamine, each drug alone, and clozapine."( Dopamine and serotonin metabolism in response to chronic administration of fluvoxamine and haloperidol combined treatment.
Chertkow, Y; Silver, H; Weinreb, O; Youdim, MB, 2007
)
0.79
" Haloperidol dose was fixed; aripiprazole was dosed at 15 mg/day for the first 4 weeks, then 30 mg/day for the following 4 weeks."( Adjunctive treatment with a dopamine partial agonist, aripiprazole, for antipsychotic-induced hyperprolactinemia: a placebo-controlled trial.
Conley, RR; Jung, DU; Kelly, DL; Liu, KH; Seo, YS; Shim, JC; Shin, JG; Shon, JH, 2007
)
1.25
" Subsequently, in order to determine whether tolerance to the activity suppressive effects of these drugs would occur in adolescents, PN40 rats were dosed and assessed for an additional nine days."( Antipsychotic-induced suppression of locomotion in juvenile, adolescent and adult rats.
Wiley, JL, 2008
)
0.35
" We treated catatonic symptoms with drugs within the upper limit of dosage and electroconvulsive therapy (ECT) to determine the maximal response."( Maximal response to electroconvulsive therapy for the treatment of catatonic symptoms.
Arai, H; Hatta, K; Miyakawa, K; Nakamura, H; Ota, T; Usui, C, 2007
)
0.34
" In treated patients, no correlation was found between NSS and daily dosage or duration of exposure of neuroleptic treatment, extrapyramidal symptoms and level of CGI-improvement."( [Neuroleptic treatment and neurological soft signs in schizophrenic patients].
Chebel, S; Gaha, L; Mandhouj, O; Mechri, A; Slama, H,
)
0.13
" The contradiction between our results and those of several previous studies may be due to the fixed plasma level dosing of imipramine refraining from concurrent psychotropic medication or limiting our patient sample to patients with mood-congruent psychotic features."( Efficacy of imipramine in psychotic versus nonpsychotic depression.
Birkenhager, TK; Bruijn, JA; Moleman, P; Mulder, PG; van den Broek, WW, 2008
)
0.35
" Haloperidol (mean dosage 4,1 mg daily) was administered to 17 patients and trifluoperazine (mean dosage 7,1 mg daily) to 14 patients."( [Prescription of traditional neuroleptics in the remission period for schizophrenic patients with excess of body mass caused by atypical antipsychotics].
Danilov, DS; Tiul'pin, IuG, 2007
)
1.25
" Neuroleptic drugs can produce severe side effects and need careful dosage and monitoring."( [Delusion in the critical patient].
Palencia-Herrejón, E; Romera, MA; Silva, JA, 2008
)
0.35
"Age, body mass index (BMI), illness duration, drug type and dosage were considered as covariates when analysing association with genetic variants as they were associated with baseline or final BPRS and CGI scores and/or extrapyramidal side effects."( Acute antipyschotic efficacy and side effects in schizophrenia: association with serotonin transporter promoter genotypes.
Dolzan, V; Kastelic, M; Koprivsek, J; Mandelli, L; Plesnicar, BK; Serretti, A, 2008
)
0.35
" Treatment was at the psychiatrist's discretion, including flexible dosing and use of concomitant therapies and medications, with assessments at 0, 3, 6, 12, 18, 24, 30, and 36 months."( Long-term antipsychotic monotherapy for schizophrenia: disease burden and comparative outcomes for patients treated with olanzapine, quetiapine, risperidone, or haloperidol monotherapy in a pan-continental observational study.
Anders, M; Dossenbach, M; Irimia, V; Kotler, M; Logozar-Perkovic, D; Lowry, AJ; Pecenak, J; Peciukaitiene, D; Smulevich, AB; Szulc, A; Treuer, T; West, TM, 2008
)
0.54
" Here, we examined the effects of acute and repeated dosing with two antipsychotics, haloperidol and clozapine, and Delta(9)-tetrahydrocannabinol [Experiments 1 and 2, respectively] in adolescent rats of both sexes that differed in shipping status (i."( To breed or not to breed? Empirical evaluation of drug effects in adolescent rats.
Evans, RL; Wiley, JL, 2009
)
0.58
"Community dwelling patients with schizophrenia were randomized to treatment with haloperidol (n=47) or ziprasidone dosed either once or twice daily (n=139)."( Reduction of functional disability with atypical antipsychotic treatment: a randomized long term comparison of ziprasidone and haloperidol.
Harvey, PD; Kremer, CM; Lombardo, I; Pappadopulos, E, 2009
)
0.79
" The preferred switch strategy was immediate discontinuation, and the preferred dosing regimen was 120 mg/day."( Efficacy and tolerability of switching to ziprasidone from olanzapine, risperidone or haloperidol: an international, multicenter study.
Akkaya, C; Alptekin, K; Brook, S; Danaci, AE; El Tallawy, H; Hafez, J; Karayal, ON; Lowe, W; Tzebelikos, E; Ucok, A, 2009
)
0.58
" Piglets subjected to hypoxia followed by asphyxic cardiac arrest were treated with saline or two dosing regimens of PPBP after resuscitation."( Sigma receptor ligand 4-phenyl-1-(4-phenylbutyl)-piperidine modulates neuronal nitric oxide synthase/postsynaptic density-95 coupling mechanisms and protects against neonatal ischemic degeneration of striatal neurons.
Carter, EL; Koehler, RC; Martin, LJ; Torbey, MT; Yang, ZJ, 2010
)
0.36
"The definition of the best combination of "when" and "how much" of haloperidol dosing during acute psychotic illness still represents a challenge."( Interaction of haloperidol plasma level and antipsychotic effect in early phases of acute psychosis treatment.
Drago, A; Giegling, I; Möller, HJ; Rujescu, D; Schäfer, M; Serretti, A, 2010
)
0.95
" The AMPH-suppressed SIP manifested again following 5-days of pretreatment with a sub-threshold dosage of AMPH (1."( Role of dopaminergic DAD1 and DAD2 receptors in the sensitization of amphetamine-suppressed schedule-induced polydipsia in rats.
Lin, PJ; Liu, YP; Tseng, CJ; Tung, CS; Wan, FJ, 2009
)
0.35
" Limited information is available regarding the dosage requirements and efficacy of neuroleptics in the palliative care setting."( Neuroleptic dose in the management of delirium in patients with advanced cancer.
Bruera, E; Bush, SH; Gallo, LE; Hui, D; Palmer, JL; Yennurajalingam, S, 2010
)
0.36
" In order to provide a dosing comparison to a therapeutically relevant endpoint, both drugs were tested against amphetamine-induced disruption of prepulse inhibition as well."( Disruption of conditioned reward association by typical and atypical antipsychotics.
Danna, CL; Elmer, GI, 2010
)
0.36
" Further investigations are warranted to identify patient characteristics and antipsychotic dosage regimens that are not associated with a greater risk of mortality in elderly patients with dementia."( Are all commonly prescribed antipsychotics associated with greater mortality in elderly male veterans with dementia?
Dysken, MW; Lederle, FA; Rector, TS; Rossom, RC, 2010
)
0.36
" Melatonin, a free radical scavenger, blocks tau hyperphosphorylation, and microtubule disorganization caused by haloperidol in a dose-response mode."( Haloperidol causes cytoskeletal collapse in N1E-115 cells through tau hyperphosphorylation induced by oxidative stress: Implications for neurodevelopment.
Benítez-King, G; Jiménez-Rubio, G; Ortíz-López, L; Ramírez-Rodríguez, G, 2010
)
2.01
" However, excessive dosing of the antipsychotic medications, in particular haloperidol, may have played an important role in accounting for the differences between aripiprazole and haloperidol in this study."( Aripiprazole versus haloperidol treatment in early-stage schizophrenia.
Girgis, RR; Lieberman, JA; Merrill, DB; Pikalov, A; Vorel, SR; Whitehead, R; You, M, 2011
)
0.92
" We found substantial differences in baseline characteristics of subjects, administered dosage and disease severity in India compared to the USA and Russia."( Impact of geographical and cultural factors on clinical trials in acute mania: lessons from a ziprasidone and haloperidol placebo-controlled study.
Lombardo, I; Mandel, FS; Pappadopulos, E; Vieta, E, 2011
)
0.58
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
" This review provides an overview of haloperidol pharmacokinetics and a comprehensive summary of the evidence for various haloperidol dosing regimens in the treatment of delirium in critically-ill patients."( Haloperidol dosing strategies in the treatment of delirium in the critically ill.
Ensom, MH; Loh, GW; Mabasa, VH; Wang, EH, 2012
)
2.09
" Administration and dosage of Trihexiphenidil (THF) was recorded."( First generation antipsychotics switch with Risperidone in the treatment of chronic schizophrenic patients.
Popović, I; Popović, V; Ravanić, D; Stanojević, A; Stojanović, M; Vladejić, S, 2011
)
0.37
" The FGA group demonstrated that extrapyramidal syndrome (EPS) worsened under an increased dosage of anti-EPS drugs."( Risperidone and olanzapine versus another first generation antipsychotic in patients with schizophrenia inadequately responsive to first generation antipsychotics.
Chan, HY; Chen, CH; Chen, JJ; Gau, SS; Hwu, HG, 2012
)
0.38
" Iloperidone 4-8, 10-16, and 20-24 mg/day (all dosed twice daily) were compared with placebo."( Efficacy of iloperidone in the short-term treatment of schizophrenia: a post hoc analysis of pooled patient data from four phase III, placebo- and active-controlled trials.
Citrome, L; Hochfeld, M; Meng, X; Stahl, SM, 2012
)
0.38
" Propensity-stratified and propensity-weighted models as well as analyses controlling for site of care and medication dosage revealed similar patterns."( Risk of mortality among individual antipsychotics in patients with dementia.
Blow, FC; Chiang, C; Cunningham, F; Kales, HC; Kim, HM; Schneider, LS; Seyfried, LS; Valenstein, M; Zivin, K, 2012
)
0.38
"Rodent models offer a tractable system to test this hypothesis, and we therefore examined the effect of chronic treatment (8 weeks) and subsequent withdrawal (8 weeks) with clinically relevant dosing of an antipsychotic (haloperidol, HAL) or lithium (Li) on brain volume using longitudinal in vivo structural MRI and confirmed the findings postmortem using unbiased stereology."( Contrasting effects of haloperidol and lithium on rodent brain structure: a magnetic resonance imaging study with postmortem confirmation.
Cooper, JD; Crum, WR; Kapur, S; Modo, M; Natesan, S; Vernon, AC; Williams, SC, 2012
)
0.87
" There was a dose-response relation for all drugs except quetiapine."( Differential risk of death in older residents in nursing homes prescribed specific antipsychotic drugs: population based cohort study.
Avorn, J; Crystal, S; Gerhard, T; Huybrechts, KF; Levin, R; Lucas, JA; Olfson, M; Schneeweiss, S, 2012
)
0.38
" A therapeutic dosage (0."( The blood concentration and organ distribution of haloperidol at therapeutic and toxic doses in severe fatty liver disease.
Ikemura, M; Inoue, H; Nakagawa, Y; Nata, M; Shinone, K, 2012
)
0.63
" The aim of the present study was to analyze on a single case basis the relationship between a sudden increase in suicidality, anxiety symptoms, medication dosing and clinician- and patient-rated akathisia."( The relationship of Akathisia with treatment emergent suicidality among patients with first-episode schizophrenia treated with haloperidol or risperidone.
Bauer, M; Doucette, S; Lewitzka, U; Meyer, S; Möller, HJ; Musil, R; Riedel, M; Schennach, R; Seemüller, F, 2012
)
0.58
" Further study is needed to determine whether these results concerning mechanism and dosage can be the basis for prevention of the development of CIS in at risk populations."( Prevention of the phencyclidine-induced impairment in novel object recognition in female rats by co-administration of lurasidone or tandospirone, a 5-HT(1A) partial agonist.
Adelekun, AE; Hannaway, KE; Horiguchi, M; Jayathilake, K; Meltzer, HY, 2012
)
0.38
" The RLAI group needed a lower dosage of biperiden compared with the control group, even though they had similar risperidone-equivalent daily dosages."( The influence of switching from haloperidol decanoate depot to risperidone long-acting injection on the clinical symptoms and cognitive function in schizophrenia.
Gen, K; Suzuki, H, 2012
)
0.66
" A lower dosage (0,1 mg/kg) of haloperidol did not affect the results of the research."( [Effect of haloperidol on changes in development of spontaneous catalepsy during subchronic injections of dopamine agonists and antagonists].
Kozlovskiĭ, VL,
)
0.81
"All trials were industry supported, with some variability in dosage of haloperidol."( Lower rate of depressive switch following antimanic treatment with second-generation antipsychotics versus haloperidol.
Capapey, J; Colom, F; Goikolea, JM; Grande, I; Sanchez-Moreno, J; Torres, I; Undurraga, J; Valentí, M; Vieta, E, 2013
)
0.84
" Pharmacokinetics and binding potential to D(2) receptor in putamen and caudate nucleus over time were analyzed using NONMEM, and simulations for the profiles of D2RO over time on various regimens of haloperidol were conducted to find the optimal dosing regimens."( Exploration of optimal dosing regimens of haloperidol, a D2 Antagonist, via modeling and simulation analysis in a D2 receptor occupancy study.
Jang, IJ; Jin, SJ; Kim, S; Kim, SE; Kim, SJ; Lee, BC; Lim, HS; Noh, YH; Park, HS, 2013
)
0.84
"This study showed that sparse D2RO measurements in steady state pharmacodynamic design after multiple dosing could reveal the possibility of treatment effect of D(2) antagonist, and could identify the potential optimal doses for later clinical studies by modeling and simulation."( Exploration of optimal dosing regimens of haloperidol, a D2 Antagonist, via modeling and simulation analysis in a D2 receptor occupancy study.
Jang, IJ; Jin, SJ; Kim, S; Kim, SE; Kim, SJ; Lee, BC; Lim, HS; Noh, YH; Park, HS, 2013
)
0.65
"In order to assess whether caffeine and theophylline have the same potency and efficacy to reverse the impairment of motor function caused by acute or chronic interruption of striatal dopamine transmission, a comparison of their dose-response relationship was made in the acute model of haloperidol-induced catalepsy, and the chronic model of unilateral lesion of the dopamine nigrostriatal pathway with 6-hydroxydopamine."( Caffeine has greater potency and efficacy than theophylline to reverse the motor impairment caused by chronic but not acute interruption of striatal dopaminergic transmission in rats.
Acuña-Lizama, MM; Alvarez-Cervera, FJ; Bata-García, JL; Góngora-Alfaro, JL, 2013
)
0.57
"9% of the total antipsychotic dosage on average."( Ten year outcomes of outpatients with schizophrenia on conventional depot antipsychotics: a systematic chart review.
Den, R; Mimura, M; Sakurai, H; Suzuki, T; Tsutsumi, C; Uchida, H; Uchida, T, 2013
)
0.39
" To test this hypothesis in a rodent model, the A2A receptor antagonists SCH 412348 (3 mg/kg), vipadenant (10 mg/kg), caffeine (30 mg/kg), or istradefylline (3 mg/kg) were chronically (19-22 days) administered to Sprague Dawley rats, and dyskinetic behaviors were scored across this chronic dosing paradigm."( A2A receptor antagonists do not induce dyskinesias in drug-naive or L-dopa sensitized rats.
Bleickardt, C; Hodgson, R; Jones, N; Mullins, D; Parker, E, 2013
)
0.39
"To determine the dosing patterns and total doses of fentanyl, lorazepam, and haloperidol according to nursing shift in a cohort of older patients in a medical intensive care unit."( Patterns of opiate, benzodiazepine, and antipsychotic drug dosing in older patients in a medical intensive care unit.
Akgün, KM; Araujo, KL; Bramley, K; Murphy, TE; Pisani, MA; Vest, MT, 2013
)
0.62
" Although dosing with fentanyl did not differ according to shift, doses of both lorazepam and haloperidol were higher during the evening shifts (4 pm to midnight) than during the day or night shifts."( Patterns of opiate, benzodiazepine, and antipsychotic drug dosing in older patients in a medical intensive care unit.
Akgün, KM; Araujo, KL; Bramley, K; Murphy, TE; Pisani, MA; Vest, MT, 2013
)
0.61
" Subsequently, the developed model was utilized to characterize an effective dosing strategy for using haloperidol as a comparator drug in future antipsychotic drug trials."( Population pharmacokinetic-pharmacodynamic modeling of haloperidol in patients with schizophrenia using positive and negative syndrome rating scale.
Danhof, M; de Greef, R; Groothuis, GM; Johnson, M; Kozielska, M; Liu, J; Mafirakureva, N; Pilla Reddy, V; Proost, JH; Rujescu, D; Vermeulen, A, 2013
)
0.85
" In case of delirium, a checklist to eliminate precipitating/ inducing factors and a protocol for standardized dosing with haloperidol was applied."( Effects of a screening and treatment protocol with haloperidol on post-cardiotomy delirium: a prospective cohort study.
Balslev Jørgensen, M; Kirkegaard, T; Lind Jørgensen, V; Schrøder Pedersen, S, 2014
)
0.86
" Microinjection of the preferential D(3) agonist 7-hydroxy-N,N-di-n-propyl-2-aminotetralin (7-OH-DPAT) into lobe 9 of the cerebellum significantly reduced spontaneous locomotor activity with a U-shaped dose-response curve."( Role of cerebellar dopamine D(3) receptors in modulating exploratory locomotion and cataleptogenicity in rats.
Andatsu, S; Kizu, T; Miyoshi, S; Ohno, Y; Sato, M; Shimizu, S; Sugiuchi, T; Tatara, A, 2014
)
0.4
" Dosing schedules are derived from expert opinion and various clinical practice guidelines as evidence-based data from palliative care settings are limited."( Treating an established episode of delirium in palliative care: expert opinion and review of the current evidence base with recommendations for future development.
Breitbart, W; Bruera, E; Bush, SH; Currow, DC; Davis, DHJ; Gagnon, B; Gagnon, PR; Hartwick, M; Kanji, S; Lawlor, PG; Meagher, D; Pereira, JL; Rabheru, K; Regnier, L; Wright, D, 2014
)
0.4
" In order to test the hypothesis that the differential blockade of the muscarinic receptor subtypes would influence their potency and efficacy to prevent EPS, here we tested four anticholinergics with varying order of affinities for the muscarinic receptor subtypes, and compared their dose-response curves to inhibit haloperidol-induced catalepsy in male rats."( The potency and efficacy of anticholinergics to inhibit haloperidol-induced catalepsy in rats correlates with their rank order of affinities for the muscarinic receptor subtypes.
Alvarez-Cervera, FJ; Bata-García, JL; Erosa-Rivero, HB; Góngora-Alfaro, JL; Heredia-López, FJ, 2014
)
0.82
" Renal dosing for topiramate, reduction in PIMs/anticholinergic burden, and substituting haloperidol for olanzapine resolved his violent behavior and CD."( Capgras delusion with violent behavior in Alzheimer dementia: case analysis with literature review.
Dawood, A; Kaufman, KR; Newman, NB, 2014
)
0.62
"Animal work on the behavioral effects of antipsychotic treatment suggests that different dosing regimens could affect drug sensitivity differently, with an intermittent treatment regimen tending to cause a sensitization effect, while a continuous treatment causing a tolerance."( Differential effects of intermittent versus continuous haloperidol treatment throughout adolescence on haloperidol sensitization and social behavior in adulthood.
Gao, J; Li, M, 2014
)
0.65
" To address this question we have investigated the cytological and functional effects of four APs: chlorpromazine (CLP), haloperidol (HAL), risperidone (RIS) and clozapine (CLZ), at concentrations typical of high therapeutic dosage on a human brain microvascular endothelial cell (HBMEC) model of the BBB."( Adverse effects of antipsychotics on micro-vascular endothelial cells of the human blood-brain barrier.
Elmorsy, E; Elsheikha, HM; Elzalabany, LM; Smith, PA, 2014
)
0.61
" For 80 patients treated with sodium valproate, the mean ± SD dosage was 1541."( Efficacy and safety of valproic acid versus haloperidol in patients with acute agitation: results of a randomized, double-blind, parallel-group trial.
Asadollahi, S; Azadbakht, A; Hatamabadi, H; Heidari, K; Mirmohseni, L; Vafaee, R; Yunesian, S, 2015
)
0.68
" It is a major determinant of half-life and dosing frequency of a drug."( Volume of Distribution in Drug Design.
Beaumont, K; Di, L; Maurer, TS; Smith, DA, 2015
)
0.42
"5 mg/kg) or MP-10 (3-30 mg/kg) did not produce cataleptic behavior when dosed alone, but co-administration of haloperidol with MP-10 (3 and 10 mg/kg) induced cataleptic behaviors."( The PDE10A inhibitor MP-10 and haloperidol produce distinct gene expression profiles in the striatum and influence cataleptic behavior in rodents.
Gentzel, RC; Hershey, J; Kandebo, M; Koser, AJ; Renger, JJ; Roberts, R; Smith, SM; Toolan, D; Uslaner, J, 2015
)
0.91
" However, precise dose-response studies have not been completed, especially in patients at high risk for PONV who require combination therapy."( Haloperidol dose combined with dexamethasone for PONV prophylaxis in high-risk patients undergoing gynecological laparoscopic surgery: a prospective, randomized, double-blind, dose-response and placebo-controlled study.
Baek, J; Joo, J; Moon, YE; Park, YG, 2015
)
1.86
"To study the impact of different semi-solid dosage form components on the leaching of Bisphenol A (BPA) and Bisphenol A diglycidyl ether (BADGE) from the epoxy resin-based inner lacquer of aluminium tubes, the tubes were filled with different matrix preparations and stored at an elevated temperature."( Matrix effect on leaching of Bisphenol A diglycidyl ether (BADGE) from epoxy resin based inner lacquer of aluminium tubes into semi-solid dosage forms.
Haverkamp, JB; Lipke, U; Lipperheide, C; Zapf, T, 2016
)
0.43
" To improve the quality of life of these patients, more knowledge and more pharmacokinetic/pharmacodynamics studies in terminally ill patients are needed to develop individualised dosing guidelines."( Pharmacokinetic considerations and recommendations in palliative care, with focus on morphine, midazolam and haloperidol.
Baar, FP; de Winter, BC; Franken, LG; Koch, BC; Mathôt, RA; Tibboel, D; van Esch, HJ; van Gelder, T; van Zuylen, L, 2016
)
0.65
"2 mg/kg/rat dosage of haloperidol provided orally to rats for 2 weeks enhanced vacuous chewing movements that escalated when the process proceeded for 5 weeks."( Co-treatment with imipramine averted haloperidol-instigated tardive dyskinesia: Association with serotonin in brain regions.
Haleem, DJ; Samad, N; Yasmin, F, 2016
)
1.02
" The haloperidol content in the finished dosage forms were determined by high-performance liquid chromatography (HPLC)."( Visualization and Non-Destructive Quantification of Inkjet-Printed Pharmaceuticals on Different Substrates Using Raman Spectroscopy and Raman Chemical Imaging.
Bar-Shalom, D; Edinger, M; Genina, N; Rantanen, J, 2017
)
0.97
" We therefore designed a population pharmacokinetic study to gain more insight into the pharmacokinetics of haloperidol in terminally ill patients and to find clinically relevant covariates that may be used in developing an individualised dosing regimen."( Population pharmacokinetics of haloperidol in terminally ill adult patients.
Baar, FPM; de Winter, BCM; Franken, LG; Koch, BCP; Masman, AD; Mathot, RAA; Tibboel, D; van Gelder, T, 2017
)
0.95
" Anesthetized adult female and male rats received either a controlled cortical impact (CCI) or sham injury and then were randomly assigned to a dosing regimen of HAL (0."( Comparable impediment of cognitive function in female and male rats subsequent to daily administration of haloperidol after traumatic brain injury.
Bondi, CO; de la Tremblaye, PB; Free, KE; Greene, AM; Kline, AE; Lajud, N, 2017
)
0.67
"Clinical studies that focused on treating schizophrenia showed that Calculus Bovis Sativus (CBS), a substitute of Calculus Bovis, when used in combination with haloperidol could significantly lower the dosage of haloperidol compared with treatment with haloperidol alone, whereas efficacy was maintained."( Investigation of the synergistic effects of haloperidol combined with Calculus Bovis Sativus in treating MK-801-induced schizophrenia in rats.
He, GF; He, GZ; Lei, K; Li, J; Li, XP; Liu, D; Liu, YN; Ren, XH; Zhang, CL, 2018
)
0.94
"As delirium in critically ill children is increasingly recognized, more children are treated with the antipsychotic drug haloperidol, while current dosing guidelines are lacking solid evidence and appear to be associated with a high risk of adverse events."( Monitoring Haloperidol Plasma Concentration and Associated Adverse Events in Critically Ill Children With Delirium: First Results of a Clinical Protocol Aimed to Monitor Efficacy and Safety.
de Wildt, SN; Ista, E; Jessurun, N; Slooff, VD; Tibboel, D; van Beusekom, BS; van den Dungen, DK, 2018
)
1.08
" These data demonstrate that hydrolysis greatly improves the sensitivity and consistency of results for patients on haloperidol therapy resulting in positivity data that strongly correlates with the dosage form administered."( Impact of β-Glucuronidase Mediated Hydrolysis on Haldol® Urinalysis.
Cummings, OT; Enders, JR; McIntire, G; Strickland, EC, 2018
)
0.69
" The duration of each adequate antipsychotic treatment at an optimal dosage was 4 weeks or more."( Predictors of remission during acute treatment of first-episode schizophrenia patients involuntarily hospitalized and treated with algorithm-based pharmacotherapy: Secondary analysis of an observational study.
Sakamoto, S; Sato, K; Takaki, M; Yamada, N; Yoshimura, B, 2019
)
0.51
" There were no differences in first-line antipsychotics, dosage of antipsychotics at time of response and adherence rates to algorithm-based pharmacotherapy between remitters and non-remitters."( Predictors of remission during acute treatment of first-episode schizophrenia patients involuntarily hospitalized and treated with algorithm-based pharmacotherapy: Secondary analysis of an observational study.
Sakamoto, S; Sato, K; Takaki, M; Yamada, N; Yoshimura, B, 2019
)
0.51
" CYP1A2 genotyping may have no clinical implications for personalized dosing of CYP1A2-metabolized antipsychotic drugs."( Impact of CYP1A2 genetic polymorphisms on pharmacokinetics of antipsychotic drugs: a systematic review and meta-analysis.
Hanprasertpong, N; Koonrungsesomboon, N; Na Takuathung, M; Teekachunhatean, S, 2019
)
0.51
"This study demonstrates a lower intubation rate in patients administered ketamine than prior literature in association with a lower weight-based dosing regimen."( Outcomes of Prehospital Chemical Sedation With Ketamine Versus Haloperidol and Benzodiazepine or Physical Restraint Only.
Castellana, A; Gross, K; O'Connor, L; O'Connor, MJ; Rebesco, M; Restuccia, M; Robinson, C,
)
0.37
" One of the heads is an extruder head of thermoplastic Fused Filament Fabrication (FFF) and the other is a dosing head, based on the Robocasting technique, designed to be assembled on the 3D printer."( Novel Technique Based on Fused Filament Fabrication (FFF) and Robocasting to Create Composite Medical Parts.
D'Amato, R; Haro, FB; Juanes, JA; Marcos, MI; Ramírez, AS, 2019
)
0.51
"The dose-response relationships of antipsychotic drugs for schizophrenia are not well defined, but such information would be important for decision making by clinicians."( Dose-Response Meta-Analysis of Antipsychotic Drugs for Acute Schizophrenia.
Crippa, A; Davis, JM; Leucht, S; Orsini, N; Patel, MX; Siafis, S, 2020
)
0.56
" Dose-response curves were constructed with random-effects dose-response meta-analyses and a spline model."( Dose-Response Meta-Analysis of Antipsychotic Drugs for Acute Schizophrenia.
Crippa, A; Davis, JM; Leucht, S; Orsini, N; Patel, MX; Siafis, S, 2020
)
0.56
" For some drugs, higher than currently licensed doses might be tested in further trials, because their dose-response curves did not plateau."( Dose-Response Meta-Analysis of Antipsychotic Drugs for Acute Schizophrenia.
Crippa, A; Davis, JM; Leucht, S; Orsini, N; Patel, MX; Siafis, S, 2020
)
0.56
" To evaluate the protocol, brain sections from mice dosed intraperitoneally with donepezil, tacrine, clozapine, haloperidol, and aripiprazole were used."( Development of an Integrated Tissue Pretreatment Protocol for Enhanced MALDI MS Imaging of Drug Distribution in the Brain.
Chen, Y; Gordon, A; Li, B; Tang, W, 2020
)
0.77
"We investigated whether 50-kHz USV playback ameliorates psychomotor deficits induced by haloperidol in a sub-chronic dosing regimen."( Playback of 50-kHz ultrasonic vocalizations overcomes psychomotor deficits induced by sub-chronic haloperidol treatment in rats.
Melo-Thomas, L; Müller, CP; Schwarting, RKW; Tonelli, LC; Wöhr, M, 2020
)
1
" Dosing recommendations however are often based on strategies used in patients with normal body habitus."( Drug dosing in the critically ill obese patient-a focus on sedation, analgesia, and delirium.
Barletta, JF; Erstad, BL, 2020
)
0.56
"Haloperidol at high dosage is associated with QTc prolongation and polymorphic ventricular arrhythmia but the effects of low-dose haloperidol remain unknown."( Should we still monitor QTc duration in frail older patients on low-dose haloperidol? A prospective observational cohort study.
Bordachar, P; Castro, E; Hazebroek, M; Körver, F; Merry, A; Ploux, S; Prinzen, F; Sipers, W; Smid, M; Strik, M; van Moorsel, F, 2020
)
2.23
" Dosing strategies, discontinuation considerations, and side effects are discussed."( The Psychopharmacology Algorithm Project at the Harvard South Shore Program: An update on management of behavioral and psychological symptoms in dementia.
Chen, A; Cloutier, A; Copeli, F; Metzger, E; Osser, DN, 2021
)
0.62
" Risperidone has weight-based dosing and a liquid dosage form available, making it a good option for use in the NICU."( Delirium in the NICU: Risk or Reality?
Liviskie, C; McPherson, C, 2021
)
0.62
" Olanzapine dosing was increased to 10 mg daily on hospital day 34 and 15 mg daily on hospital day 45."( Extrapyramidal Symptoms Induced by Treatment for Delirium: A Case Report.
Rose, MQ; Santos, CD, 2021
)
0.62
" The effects of degree of lignin depolymerization, chemical composition of lignin oligomers and dosage of ECGE on thermal and mechanical properties of the cured products were investigated."( Preparation and properties of novel bio-based epoxy resin thermosets from lignin oligomers and cardanol.
Chu, F; Huo, S; Jin, C; Kong, Z; Liu, G, 2021
)
0.62
" No significant differences were found in the rate of violent behavior and antipsychotic dosage at discharge."( Olanzapine intramuscular shows better efficacy than zuclopenthixol acetate intramuscular in reducing the need for restraint, but not in comparison to haloperidol intramuscular.
Bloemhof-Bris, E; Shelef, A; Sinai, O; Stryjer, R; Weizman, S, 2022
)
0.92
" Mean endpoint LAI dosage was 65."( An interventional pilot of customized adherence enhancement combined with long-acting injectable antipsychotic medication (CAE-L) for poorly adherent patients with chronic psychotic disorder in Tanzania.
Blixen, CE; Burant, CJ; Cassidy, KA; Kaaya, S; Lema, I; Levin, JB; Madundo, K; Magwiza, C; Mbwambo, J; Njiro, G; Sajatovic, M, 2022
)
0.72
" We aimed to fill this gap with a dose-response meta-analysis."( Antipsychotic-Induced Weight Gain: Dose-Response Meta-Analysis of Randomized Controlled Trials.
Davis, JM; Hamza, T; Leucht, S; Salanti, G; Schneider-Thoma, J; Siafis, S; Wu, H, 2022
)
0.72
" We estimated the dose-response curves by conducting random-effects dose-response meta-analyses."( Antipsychotic-Induced Weight Gain: Dose-Response Meta-Analysis of Randomized Controlled Trials.
Davis, JM; Hamza, T; Leucht, S; Salanti, G; Schneider-Thoma, J; Siafis, S; Wu, H, 2022
)
0.72
" For most drugs, dose-response curves showed an initial dose-related increase in weight which plateaued at higher doses, while for others there was no plateau and some even had bell-shaped curves, meaning less weight gain to be associated with higher doses."( Antipsychotic-Induced Weight Gain: Dose-Response Meta-Analysis of Randomized Controlled Trials.
Davis, JM; Hamza, T; Leucht, S; Salanti, G; Schneider-Thoma, J; Siafis, S; Wu, H, 2022
)
0.72
"Second-generation antipsychotics do not only differ in their propensity to produce weight gain, but also in the shapes of their dose-response curves."( Antipsychotic-Induced Weight Gain: Dose-Response Meta-Analysis of Randomized Controlled Trials.
Davis, JM; Hamza, T; Leucht, S; Salanti, G; Schneider-Thoma, J; Siafis, S; Wu, H, 2022
)
0.72
" Secondary outcomes include comparison of length of stay, utilization of restraints, and discharge outcomes between dosage groups."( Optimal Injectable Haloperidol Dose Assessment in the Older Hospitalized Inpatient.
Bhatti, H; Brenner, JM; Britton, S; Noviasky, J; Yuksel, JM, 2023
)
1.24
"Expert consensus-based clinically equivalent dose estimates and dosing recommendations can provide valuable support for the use of drugs for psychosis in clinical practice and research."( Second International Consensus Study of Antipsychotic Dosing (ICSAD-2).
Baldessarini, RJ; Gardner, DM; McAdam, MK; Murphy, AL, 2023
)
0.91
"This second International Consensus Study of Antipsychotic Dosing provides dosing equivalencies and recommendations for newer drugs for psychosis and previously reported drugs with low consensus."( Second International Consensus Study of Antipsychotic Dosing (ICSAD-2).
Baldessarini, RJ; Gardner, DM; McAdam, MK; Murphy, AL, 2023
)
0.91
"We used a two-step Delphi survey process to establish and update consensus with a broad, international sample of clinical and research experts regarding 26 drug formulations to obtain dosing recommendations (start, target range, and maximum) and estimates of clinically equivalent doses for the treatment of schizophrenia."( Second International Consensus Study of Antipsychotic Dosing (ICSAD-2).
Baldessarini, RJ; Gardner, DM; McAdam, MK; Murphy, AL, 2023
)
0.91
"As randomized, controlled, fixed, multiple-dose trials to optimize the dosing of drugs for psychosis remain rare, expert consensus remains a useful alternative for estimating clinical dosing equivalents."( Second International Consensus Study of Antipsychotic Dosing (ICSAD-2).
Baldessarini, RJ; Gardner, DM; McAdam, MK; Murphy, AL, 2023
)
0.91
"Uniformity of dosage unit (UDU) test is widely used to assess the quality, safety, and effectiveness of dosage forms in unit doses."( Measurement uncertainty for < 905 > Uniformity of Dosage Units tests using Monte Carlo and bootstrapping methods - Uncertainties arising from sampling and analytical steps.
Lourenço, FR; Martins, MT, 2024
)
1.44
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
serotonergic antagonistDrugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or serotonergic agonists.
first generation antipsychoticAntipsychotic drugs which can have different modes of action but which tend to be more likely than second generation antipsychotics to cause extrapyramidal motor control disabilities such as body rigidity or Parkinson's disease-type movements; such body movements can become permanent even after treatment has ceased.
dopaminergic antagonistA drug that binds to but does not activate dopamine receptors, thereby blocking the actions of dopamine or exogenous agonists.
antidyskinesia agentAny compound which can be used to treat or alleviate the symptoms of dyskinesia.
antiemeticA drug used to prevent nausea or vomiting. An antiemetic may act by a wide range of mechanisms: it might affect the medullary control centres (the vomiting centre and the chemoreceptive trigger zone) or affect the peripheral receptors.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (5)

ClassDescription
hydroxypiperidine
organofluorine compoundAn organofluorine compound is a compound containing at least one carbon-fluorine bond.
aromatic ketoneA ketone in which the carbonyl group is attached to an aromatic ring.
tertiary alcoholA tertiary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has three other carbon atoms attached to it.
monochlorobenzenesAny member of the class of chlorobenzenes containing a mono- or poly-substituted benzene ring in which only one substituent is chlorine.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (226)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency0.01260.003245.467312,589.2998AID2517
acetylcholinesteraseHomo sapiens (human)Potency89.35840.002541.796015,848.9004AID1347395
glp-1 receptor, partialHomo sapiens (human)Potency28.18380.01846.806014.1254AID624417
thioredoxin reductaseRattus norvegicus (Norway rat)Potency2.66790.100020.879379.4328AID488773; AID588453
15-lipoxygenase, partialHomo sapiens (human)Potency25.11890.012610.691788.5700AID887
RAR-related orphan receptor gammaMus musculus (house mouse)Potency22.60230.006038.004119,952.5996AID1159521; AID1159523
ATAD5 protein, partialHomo sapiens (human)Potency23.25840.004110.890331.5287AID493107; AID504467
Fumarate hydrataseHomo sapiens (human)Potency29.56590.00308.794948.0869AID1347053
NFKB1 protein, partialHomo sapiens (human)Potency0.28180.02827.055915.8489AID895; AID928
TDP1 proteinHomo sapiens (human)Potency23.89390.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency9.50180.000714.592883.7951AID1259369; AID1259392
ThrombopoietinHomo sapiens (human)Potency6.30960.02517.304831.6228AID917; AID918
AR proteinHomo sapiens (human)Potency36.11730.000221.22318,912.5098AID1259243; AID743036; AID743042; AID743054
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency54.48270.013326.981070.7614AID1346978
thyroid stimulating hormone receptorHomo sapiens (human)Potency39.81070.001318.074339.8107AID926
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency35.97670.001022.650876.6163AID1224838; AID1224839; AID1224893
progesterone receptorHomo sapiens (human)Potency43.27710.000417.946075.1148AID1346795
regulator of G-protein signaling 4Homo sapiens (human)Potency1.79230.531815.435837.6858AID504845
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency9.77170.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency23.15920.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency1.77830.28189.721235.4813AID2326
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency52.64300.000214.376460.0339AID720691; AID720692
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency61.13060.003041.611522,387.1992AID1159552
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency62.14720.001530.607315,848.9004AID1224841; AID1224842; AID1224848; AID1224849
farnesoid X nuclear receptorHomo sapiens (human)Potency54.94100.375827.485161.6524AID743220
pregnane X nuclear receptorHomo sapiens (human)Potency4.58150.005428.02631,258.9301AID1346982; AID720659
estrogen nuclear receptor alphaHomo sapiens (human)Potency53.69680.000229.305416,493.5996AID1259244; AID743079; AID743091
cytochrome P450 2D6Homo sapiens (human)Potency4.36490.00108.379861.1304AID1645840
polyproteinZika virusPotency29.56590.00308.794948.0869AID1347053
glucocerebrosidaseHomo sapiens (human)Potency0.79430.01268.156944.6684AID2101
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency44.21500.001024.504861.6448AID743212
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency29.87870.023723.228263.5986AID588543; AID743223
arylsulfatase AHomo sapiens (human)Potency4.25621.069113.955137.9330AID720538
caspase-3Homo sapiens (human)Potency54.48270.013326.981070.7614AID1346978
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency0.02510.035520.977089.1251AID504332
thyroid stimulating hormone receptorHomo sapiens (human)Potency68.58960.001628.015177.1139AID1259385
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency17.37390.057821.109761.2679AID1159526
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency9.05680.00207.533739.8107AID891
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency60.119823.934123.934123.9341AID1967
cytochrome P450 2C9 precursorHomo sapiens (human)Potency31.62280.00636.904339.8107AID883
D(1A) dopamine receptorHomo sapiens (human)Potency7.63860.02245.944922.3872AID488981; AID488982; AID488983
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency0.23750.01789.637444.6684AID588834
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency38.19720.000323.4451159.6830AID743065; AID743066; AID743067
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency23.28090.00378.618923.2809AID2667; AID2668
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency26.95260.000627.21521,122.0200AID651741; AID743202; AID743219
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency35.48130.00798.23321,122.0200AID2546
gemininHomo sapiens (human)Potency17.15580.004611.374133.4983AID624296; AID624297
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency28.69540.005612.367736.1254AID624032
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency4.08710.031610.279239.8107AID884; AID885
transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Potency11.22020.09120.09120.0912AID488979
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency10.21750.00106.000935.4813AID943; AID944
lethal factor (plasmid)Bacillus anthracis str. A2012Potency20.81140.020010.786931.6228AID912
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency4.08711.000012.224831.6228AID885
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency15.84890.316212.765731.6228AID881
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency61.13060.001557.789015,848.9004AID1259244
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency4.08711.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency4.08711.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency4.08711.000012.224831.6228AID885
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency61.13060.001551.739315,848.9004AID1259244
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency4.08711.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency4.08711.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency4.08711.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency4.08711.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency4.08711.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency4.08711.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency4.08711.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency22.60910.00638.235039.8107AID881; AID883
D(1A) dopamine receptorSus scrofa (pig)Potency23.28090.00378.108123.2809AID2667
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency4.08711.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency4.08711.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency4.08711.000012.224831.6228AID885
TAR DNA-binding protein 43Homo sapiens (human)Potency0.56231.778316.208135.4813AID652104
GABA theta subunitRattus norvegicus (Norway rat)Potency4.08711.000012.224831.6228AID885
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency18.83360.011917.942071.5630AID651632
Ataxin-2Homo sapiens (human)Potency18.83360.011912.222168.7989AID651632
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency4.08711.000012.224831.6228AID885
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency4.25620.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Adenylate cyclase type 1 Rattus norvegicus (Norway rat)IC50 (µMol)2.30000.14001.24672.3000AID1136419
Cocaine esteraseHomo sapiens (human)Ki0.00630.00630.98358.0000AID1272497
Solute carrier family 22 member 1 Homo sapiens (human)IC50 (µMol)141.90000.21005.553710.0000AID386625
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Transient receptor potential cation channel subfamily V member 1Rattus norvegicus (Norway rat)Ki0.00500.00010.64456.4000AID65817
Voltage-dependent L-type calcium channel subunit alpha-1CCavia porcellus (domestic guinea pig)IC50 (µMol)1.70000.02201.64228.9000AID1207187
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC50 (µMol)1.50000.00032.63119.0000AID1207187; AID1207744
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC50 (µMol)1.67650.00011.00768.7800AID625218; AID63866
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki2.13240.00000.887110.0000AID5836; AID625218
Potassium channel subfamily K member 2Homo sapiens (human)IC50 (µMol)5.50000.40003.92279.0000AID1307728
Bile salt export pumpHomo sapiens (human)IC50 (µMol)96.92000.11007.190310.0000AID1443980; AID1449628; AID1473738
Vitamin D-binding proteinRattus norvegicus (Norway rat)Ki0.00370.00210.00290.0037AID229212
Integrin beta-1Homo sapiens (human)Ki0.00390.00150.02210.0610AID448644
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC50 (µMol)1.83600.00041.877310.0000AID625207
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki1.82000.00322.28879.3160AID625207
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki4.67000.00000.690210.0000AID141100
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki4.67000.00000.79519.1201AID141100
ATP-dependent translocase ABCB1Homo sapiens (human)IC50 (µMol)5.30000.00022.318510.0000AID150618
ATP-dependent translocase ABCB1Homo sapiens (human)Ki0.20000.02002.35948.5900AID150735
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC50 (µMol)0.05400.00052.773925.1700AID141682
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki4.63060.00010.579710.0000AID141832; AID142225; AID142687; AID142719
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC50 (µMol)0.05400.00052.891925.1700AID141682
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Ki8.70650.00011.48339.1400AID142225; AID142687
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC50 (µMol)0.05400.00052.747825.1700AID141682
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)Ki8.70650.00010.68688.2600AID142225; AID142687
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)0.05500.00011.753610.0000AID5491
5-hydroxytryptamine receptor 1AHomo sapiens (human)IC50 (µMol)1.50000.00010.666410.0000AID3460
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki2.34100.00010.532610.0000AID1185959; AID1393366; AID1798075; AID342783; AID4442
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC50 (µMol)0.27850.00040.629810.0000AID4782; AID4786; AID4803; AID4812; AID4814; AID4824; AID5061; AID5703
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki0.49350.00020.667710.0000AID1185968; AID5042; AID5123; AID5218; AID5229; AID5233; AID5241; AID5246; AID5255; AID5279
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC50 (µMol)0.05400.00052.780225.1700AID141682
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)Ki8.70650.00010.66618.2600AID142225; AID142687
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC50 (µMol)3.89000.00010.99178.0000AID625155
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki3.73250.00000.72926.9183AID141100; AID625155
Alpha-2A adrenergic receptorHomo sapiens (human)IC50 (µMol)4.97300.00001.44217.3470AID625201
Alpha-2A adrenergic receptorHomo sapiens (human)Ki3.43250.00010.807410.0000AID36199; AID625201
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)2.30000.00301.17839.7724AID1136419
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)Ki10.00000.00050.35461.6000AID41748
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC50 (µMol)0.05400.00053.314249.5000AID141682
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Ki5.25420.00010.58908.2600AID142225; AID142687; AID142870; AID142943; AID142954
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC50 (µMol)5.50000.00001.403910.0000AID141053; AID141055
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki2.62330.00000.59729.1201AID141100; AID342774; AID640547
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)4.69000.00002.800510.0000AID1210069
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC50 (µMol)7.00000.00001.612910.0000AID3760
Integrin alpha-4Homo sapiens (human)Ki0.00390.00150.02210.0610AID448644
D(2) dopamine receptorHomo sapiens (human)IC50 (µMol)0.08970.00000.74728.0000AID1153309; AID1168800; AID1187745; AID1598360; AID625253; AID62573; AID62768; AID62769; AID62771; AID729692
D(2) dopamine receptorHomo sapiens (human)Ki0.06930.00000.651810.0000AID1062948; AID1063796; AID1125902; AID1142394; AID1152669; AID1184607; AID1184608; AID1185963; AID1196314; AID1249734; AID1288455; AID1380704; AID1393368; AID1458657; AID1461561; AID1461562; AID1546907; AID1570062; AID1570284; AID1601983; AID1616723; AID1664379; AID1664665; AID1667343; AID1690393; AID1691230; AID1718133; AID1756661; AID1782419; AID1798075; AID1803434; AID1823672; AID1823826; AID1878190; AID238489; AID238699; AID239052; AID254420; AID277677; AID294440; AID296886; AID298264; AID298478; AID308687; AID342777; AID346018; AID346264; AID387866; AID391273; AID391747; AID392765; AID439064; AID448410; AID45419; AID458632; AID458633; AID479242; AID492182; AID517707; AID517708; AID598815; AID605697; AID605698; AID61316; AID61612; AID61613; AID625253; AID62908; AID62909; AID62915; AID62917; AID629461; AID629462; AID63055; AID63060; AID63061; AID63064; AID63074; AID63075; AID63076; AID63087; AID63089; AID63218; AID63226; AID63387; AID63971; AID63973; AID63997; AID64000; AID64198; AID64478; AID64479; AID65814; AID65888; AID672168; AID711580
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC50 (µMol)0.14670.00040.908610.0000AID4782; AID4786; AID4803; AID4812; AID4814; AID4824; AID5061; AID5479; AID5490; AID5491
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.04830.00010.601710.0000AID1798075; AID238882; AID277974; AID410335; AID5042; AID5123; AID5218; AID5229; AID5233; AID5241; AID5246; AID5255; AID5279; AID5321; AID5324; AID5328; AID5334; AID5337; AID5522; AID5567
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.08520.00021.874210.0000AID36847; AID36849; AID36865; AID37007
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.01420.00010.949010.0000AID218673; AID298478; AID35270; AID35274; AID35285; AID36016; AID37170; AID37306; AID37449; AID37455
Alpha-2B adrenergic receptorHomo sapiens (human)IC50 (µMol)1.35400.00001.23808.1590AID625202
Alpha-2B adrenergic receptorHomo sapiens (human)Ki2.80900.00020.725710.0000AID36199; AID625202
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)Ki10.00000.00000.667310.0000AID41748
Alpha-2C adrenergic receptorHomo sapiens (human)IC50 (µMol)1.84500.00001.47257.8980AID625203
Alpha-2C adrenergic receptorHomo sapiens (human)Ki2.63400.00030.483410.0000AID36199; AID625203
DRattus norvegicus (Norway rat)IC50 (µMol)0.11030.00030.50267.7625AID34586; AID61032; AID61193; AID62868; AID62884; AID62886; AID63028
DRattus norvegicus (Norway rat)Ki0.15500.00010.610010.0000AID1478366; AID238855; AID238940; AID410331; AID61158; AID61358; AID61495; AID61498; AID61499; AID61517; AID61531; AID61670; AID61675; AID61677; AID63020; AID63365; AID63371
D(3) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00670.00030.39075.4000AID62868; AID62884; AID62886; AID63028
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki0.01510.00010.25675.8000AID1189645; AID1686279; AID259125; AID63020; AID65602; AID65609; AID65610; AID65622; AID65625; AID65753
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)3.20300.00031.38338.4000AID3669; AID37007; AID3760; AID4128; AID4136
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki1.77480.00010.739610.0000AID277973; AID37449; AID3992; AID4042; AID4334; AID4356; AID4357
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki9.60000.00000.929610.0000AID37361
D(2) dopamine receptorBos taurus (cattle)IC50 (µMol)0.13320.00100.79948.0000AID62164; AID62168; AID62445; AID62446
D(2) dopamine receptorBos taurus (cattle)Ki0.00700.00000.58366.1000AID218788; AID62337; AID62338
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki4.67000.00000.54057.7600AID141100
D(1A) dopamine receptorHomo sapiens (human)IC50 (µMol)0.05750.00031.84739.2250AID625252; AID62573
D(1A) dopamine receptorHomo sapiens (human)Ki0.09270.00010.836310.0000AID1185962; AID238490; AID342775; AID439068; AID598813; AID625252; AID63347; AID63351; AID711582
D(4) dopamine receptorHomo sapiens (human)IC50 (µMol)0.09780.00011.14239.3280AID61804; AID625255; AID62573; AID63866; AID65934; AID65935
D(4) dopamine receptorHomo sapiens (human)Ki0.01350.00000.436210.0000AID1184610; AID1456755; AID1782429; AID1823675; AID238274; AID238525; AID238778; AID238889; AID277674; AID294441; AID298480; AID342779; AID393002; AID517710; AID598817; AID605700; AID61788; AID61808; AID625255; AID629464; AID63512; AID63513; AID63514; AID63524; AID63531; AID63533; AID63534; AID63538; AID63540; AID63547; AID63549; AID63682; AID63700; AID63842; AID63849; AID64005; AID64177; AID65817; AID65950; AID65951; AID711579
D(1B) dopamine receptorHomo sapiens (human)IC50 (µMol)0.00500.00061.15468.0000AID62573
D(1B) dopamine receptorHomo sapiens (human)Ki0.10100.00030.40177.9000AID238492; AID598814; AID64187; AID711578
Adenylate cyclase type 3Rattus norvegicus (Norway rat)IC50 (µMol)2.30000.14001.24672.3000AID1136419
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki9.60000.00000.970810.0000AID37361
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki9.60000.00000.937510.0000AID37361
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.08520.00021.270410.0000AID36847; AID36849; AID36865; AID37007
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.01420.00000.575110.0000AID218673; AID298478; AID35270; AID35274; AID35285; AID36016; AID37170; AID37306; AID37449; AID37455
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC50 (µMol)1.83600.00081.541620.0000AID625207
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki3.66000.00031.465610.0000AID1185974; AID625207
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki3.00000.00030.37088.1600AID65494; AID6563
5-hydroxytryptamine receptor 3AMus musculus (house mouse)Ki10.00000.00130.23781.4300AID6022
Histamine H2 receptorHomo sapiens (human)IC50 (µMol)1.16600.02202.298710.0000AID625270
Histamine H2 receptorHomo sapiens (human)Ki1.14700.00062.197310.0000AID625270
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki0.31800.00011.20929.9700AID238940
Alpha-1D adrenergic receptorHomo sapiens (human)IC50 (µMol)0.08400.00020.75688.8970AID625200
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.02190.00000.360910.0000AID36113; AID36122; AID625200
D(1B) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00670.00030.35635.4000AID62868; AID62884; AID62886; AID63028
D(1B) dopamine receptorRattus norvegicus (Norway rat)Ki0.00170.00020.24622.0000AID238889; AID63020
Beta-3 adrenergic receptorRattus norvegicus (Norway rat)Ki10.00000.00050.33671.6000AID41748
Adenylate cyclase type 2Rattus norvegicus (Norway rat)IC50 (µMol)2.30000.14001.24672.3000AID1136419
Adenylate cyclase type 4Rattus norvegicus (Norway rat)IC50 (µMol)2.30000.14001.24672.3000AID1136419
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC50 (µMol)0.18150.00010.88018.8500AID5171; AID625192
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.12630.00000.385510.0000AID1062949; AID1185960; AID1393364; AID1823823; AID239010; AID298482; AID308685; AID342784; AID391274; AID439066; AID5127; AID5196; AID5197; AID5205; AID5363; AID625192
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC50 (µMol)6.67350.00011.03029.0000AID5686; AID625218
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki4.73670.00010.954910.0000AID308686; AID342781; AID391275; AID439070; AID5127; AID5614; AID5835; AID5836; AID5837; AID5951; AID625218
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC50 (µMol)0.50900.00051.48357.8000AID3669; AID37007
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)IC50 (µMol)0.50900.00311.73607.8000AID3669; AID37007
D(4) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00670.00030.38715.4000AID62868; AID62884; AID62886; AID63028
D(4) dopamine receptorRattus norvegicus (Norway rat)Ki0.00600.00020.18872.0000AID1185965; AID63020
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)IC50 (µMol)0.50900.00501.79627.8000AID3669; AID37007
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC50 (µMol)0.17540.00040.615610.0000AID4782; AID4786; AID4803; AID4812; AID4814; AID4824; AID5061
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.02610.00020.590910.0000AID5042; AID5123; AID5218; AID5229; AID5233; AID5241; AID5246; AID5255; AID5279
Histamine H1 receptorRattus norvegicus (Norway rat)IC50 (µMol)1.00000.00000.32271.2589AID87514
Histamine H1 receptorRattus norvegicus (Norway rat)Ki2.10000.00071.54406.5000AID87527
Sodium-dependent serotonin transporterHomo sapiens (human)IC50 (µMol)3.38600.00010.86458.7096AID625222
Sodium-dependent serotonin transporterHomo sapiens (human)Ki1.79970.00000.70488.1930AID1185975; AID342787; AID625222
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki0.03420.00000.705610.0000AID204313
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.13250.00000.14803.1800AID1798075; AID6648
C-8 sterol isomeraseSaccharomyces cerevisiae S288CKi0.00050.00000.90487.1500AID239296
Delta-type opioid receptorRattus norvegicus (Norway rat)Ki7.07000.00000.60689.2330AID149044; AID150405
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki7.07000.00000.38458.6000AID149044; AID150405
5-hydroxytryptamine receptor 2C Mus musculus (house mouse)Ki0.02650.00080.50322.8420AID5035
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki0.73660.00030.380610.0000AID1309492; AID1393367; AID298487
Kappa-type opioid receptorRattus norvegicus (Norway rat)Ki7.07000.00000.18683.9500AID149044; AID150405
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.01230.00000.272610.0000AID36113; AID36122
5-hydroxytryptamine receptor 2AMus musculus (house mouse)Ki0.02650.00080.65892.8420AID5035
Histamine H1 receptorHomo sapiens (human)IC50 (µMol)2.78100.00000.44365.1768AID625269
Histamine H1 receptorHomo sapiens (human)Ki0.47460.00000.511010.0000AID1185969; AID342782; AID625269; AID640310; AID87242
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.01230.00000.471310.0000AID36113; AID36122
Mu-type opioid receptorHomo sapiens (human)IC50 (µMol)2.44300.00010.813310.0000AID625163
Mu-type opioid receptorHomo sapiens (human)Ki4.48730.00000.419710.0000AID1558955; AID1823673; AID625163
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Ki10.00000.00030.86666.6900AID157456
D(3) dopamine receptorHomo sapiens (human)IC50 (µMol)0.00650.00011.01788.7960AID1187744; AID1598358; AID1823687; AID625254; AID62573; AID64825
D(3) dopamine receptorHomo sapiens (human)Ki0.00990.00000.602010.0000AID1125903; AID1168796; AID1184609; AID1185964; AID1249735; AID1461564; AID1546909; AID1756662; AID1782425; AID1823674; AID1878191; AID238350; AID238491; AID239150; AID239151; AID256758; AID277673; AID294442; AID298263; AID298479; AID342778; AID392764; AID410333; AID439069; AID45420; AID492183; AID517709; AID598816; AID605699; AID625254; AID629463; AID640304; AID64960; AID64962; AID64963; AID64974; AID64993; AID65127; AID65128; AID65133; AID65146; AID65280; AID65288; AID65443; AID65781; AID65785; AID65786; AID711581
Sodium channel protein type 1 subunit alphaHomo sapiens (human)IC50 (µMol)7.00000.00232.82969.0000AID1207158
Sodium channel protein type 4 subunit alphaHomo sapiens (human)IC50 (µMol)7.00000.00013.507510.0000AID1207158
Adenylate cyclase type 8Rattus norvegicus (Norway rat)IC50 (µMol)2.30000.14001.24672.3000AID1136419
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.00260.00000.20186.4240AID1184609
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC50 (µMol)2.05000.00011.18738.9125AID625217
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.66250.00030.769310.0000AID5127; AID625217
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.08520.00001.819410.0000AID36847; AID36849; AID36865; AID37007
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.01420.00000.965010.0000AID218673; AID298478; AID35270; AID35274; AID35285; AID36016; AID37170; AID37306; AID37449; AID37455
5-hydroxytryptamine receptor 2ASus scrofa (pig)Ki0.03000.03000.42700.9000AID517712
D(1A) dopamine receptorSus scrofa (pig)Ki0.00950.00051.22238.8000AID1184611
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki4.02770.00020.522910.0000AID1393365; AID342773; AID6563
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC50 (µMol)141.90002.03005.53139.9000AID386625
Cytochrome P450 2J2Homo sapiens (human)IC50 (µMol)4.69000.01202.53129.4700AID1210069
D(2) dopamine receptorChlorocebus aethiops (grivet)Ki0.00490.00480.27820.8730AID62007; AID62009
D(3) dopamine receptorChlorocebus aethiops (grivet)Ki0.00300.00301.69074.6030AID64802
Gastrin/cholecystokinin type B receptorMus musculus (house mouse)Ki0.02340.00030.01660.0940AID5123
D(2) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)0.01290.00010.54948.4000AID61326; AID61388; AID61415; AID61533; AID61566; AID62868; AID62884; AID62886; AID63028; AID64264; AID64268; AID64285; AID64295; AID64296; AID64299; AID64426; AID64434; AID64461; AID64612; AID64613
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.00230.00000.437510.0000AID1189645; AID1478367; AID1686278; AID238941; AID239086; AID277975; AID410332; AID61079; AID63020; AID63800; AID63804; AID63805; AID63809; AID63811; AID63819; AID63822; AID64645; AID65078; AID65100; AID65111; AID65239; AID65243; AID65247; AID65402; AID65425; AID65426; AID65559; AID65560; AID65562; AID65563; AID65713; AID65726; AID65884; AID65885; AID65894
AP-2 complex subunit sigmaRattus norvegicus (Norway rat)Ki0.02420.02420.02420.0242AID586709
N-acetyltransferase EisMycobacterium tuberculosis H37RvIC50 (µMol)0.39000.39001.64255.1000AID1853637
N-acetyltransferase EisMycobacterium tuberculosis H37RvKi0.39000.24000.31500.3900AID1853645
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Ki10.00000.00030.68056.6900AID157456
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Ki5.00070.00030.70716.6900AID1060809; AID157456
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Ki10.00000.00030.81966.6900AID157456
Sodium channel protein type 7 subunit alphaHomo sapiens (human)IC50 (µMol)7.00000.03603.73359.0000AID1207158
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC50 (µMol)1.50000.00032.59559.0000AID1207187; AID1207744
5-hydroxytryptamine receptor 2BMus musculus (house mouse)Ki0.02650.00080.65892.8420AID5035
Adenylate cyclase type 6Rattus norvegicus (Norway rat)IC50 (µMol)2.30000.14001.24672.3000AID1136419
Adenylate cyclase type 5Rattus norvegicus (Norway rat)IC50 (µMol)1.42500.04680.88292.3000AID1136419; AID34586
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)0.26340.00091.901410.0000AID1054122; AID1207217; AID161281; AID161283; AID1649553; AID240820; AID243151; AID243188; AID397743; AID408340; AID420668; AID576612; AID672167; AID674364; AID82355
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki0.31600.00211.840710.0000AID274128; AID410338
5-hydroxytryptamine receptor 4Homo sapiens (human)Ki0.00060.00000.443910.0000AID63997
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC50 (µMol)1.50000.00032.63119.0000AID1207187; AID1207744
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC50 (µMol)1.50000.00032.25459.6000AID1207187; AID1207744
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC50 (µMol)7.00000.00033.64849.2000AID1207158
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)Ki0.19000.00040.54906.7000AID239597
Sodium channel protein type 9 subunit alphaHomo sapiens (human)IC50 (µMol)7.00000.00602.77499.0000AID1207158
Calcitonin gene-related peptide type 1 receptorHomo sapiens (human)Ki0.00040.00000.02820.5900AID45419
Genome polyprotein Human rhinovirus sp.IC50 (µMol)140.00000.00052.98388.2000AID160788
Genome polyprotein Human rhinovirus sp.Ki0.10000.00010.01650.1000AID163467
Sigma intracellular receptor 2Homo sapiens (human)Ki0.06160.00010.83604.6005AID1467942; AID1596349; AID1655661; AID1718134; AID1744236; AID1861724
Sigma intracellular receptor 2Rattus norvegicus (Norway rat)Ki0.07210.00241.10509.3000AID1690210; AID1726850; AID1727501; AID1728290; AID1759955; AID1851837; AID1865087; AID1867872; AID1877931; AID1901078; AID1901324
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)Ki0.00480.00000.338510.0000AID1060809; AID1127303; AID1159367; AID1191388; AID1330102; AID1369086; AID1378105; AID1403514; AID1456401; AID1511007; AID1519019; AID1597397; AID1686276; AID1690209; AID1712205; AID1727502; AID1728274; AID1744232; AID1744242; AID1759953; AID1809442; AID1865086; AID1867871; AID1877932; AID1901074; AID1901323; AID317390; AID393184; AID448644; AID492183; AID538759; AID586708; AID598495; AID619547; AID675970; AID776368
Zinc finger protein 664Cavia porcellus (domestic guinea pig)Ki0.00660.00660.00660.0066AID1441551
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Ki10.00000.00030.70726.6900AID157456
Vesicular acetylcholine transporterRattus norvegicus (Norway rat)Ki0.39100.00130.56224.5230AID1506088
TransporterRattus norvegicus (Norway rat)Ki5.50000.00010.76295.5000AID342786
Cholecystokinin receptor type ACavia porcellus (domestic guinea pig)Ki0.05000.00030.13770.6310AID5255
Protease Human immunodeficiency virus 1IC50 (µMol)125.00000.00010.22487.3200AID162182
Protease Human immunodeficiency virus 1Ki50.05000.00000.04433.1000AID160616; AID160777
Adenylyl cyclase 7 Rattus norvegicus (Norway rat)IC50 (µMol)2.30000.14001.24672.3000AID1136419
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Ki10.00000.00030.70726.6900AID157456
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
DBos taurus (cattle)IC50 (µMol)0.25090.00100.47208.0000AID62445; AID62446
Sodium channel protein type 2 subunit alphaHomo sapiens (human)IC50 (µMol)7.00000.00003.740110.0000AID1207158
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC50 (µMol)0.07000.00030.70285.3660AID203852; AID203984; AID204763; AID476062; AID625223; AID751647
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.00570.00000.490110.0000AID1063782; AID1129882; AID1174258; AID1197502; AID1272497; AID1288457; AID1308619; AID1449796; AID1506085; AID1532592; AID1558961; AID1593893; AID1594271; AID1701184; AID1718132; AID1726849; AID1744234; AID1861723; AID203698; AID203702; AID203998; AID204145; AID204152; AID204153; AID204448; AID204596; AID204629; AID229212; AID239105; AID239200; AID239347; AID444005; AID625223; AID701162; AID711577; AID735278; AID751647
Transient receptor potential cation channel subfamily V member 4Rattus norvegicus (Norway rat)Ki0.00500.00500.00500.0050AID65817
Sodium channel protein type 3 subunit alphaHomo sapiens (human)IC50 (µMol)7.00000.00532.80859.0000AID1207158
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)IC50 (µMol)0.00130.00030.55704.2000AID204012; AID204615; AID204762; AID204763
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)Ki0.01480.00030.26715.0700AID152392; AID1851836; AID204304; AID204313; AID204629; AID674895; AID737906
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Ki10.00000.00030.70726.6900AID157456
Sodium channel protein type 11 subunit alphaHomo sapiens (human)IC50 (µMol)7.00000.03004.36959.0000AID1207158
Sodium channel protein type 8 subunit alphaHomo sapiens (human)IC50 (µMol)7.00000.00113.47059.0000AID1207158
Transient receptor potential cation channel subfamily V member 2Rattus norvegicus (Norway rat)Ki0.00500.00500.00500.0050AID65817
Sodium channel protein type 10 subunit alphaHomo sapiens (human)IC50 (µMol)7.00000.00803.17529.0000AID1207158
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AlbuminRattus norvegicus (Norway rat)Kd96.90001.47006.53179.3100AID1215123
Major prion proteinHomo sapiens (human)EC50 (µMol)10.00000.30004.900010.0000AID161627
HLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)Kd10.00002.50004.375010.0000AID1398702
D(2) dopamine receptorHomo sapiens (human)Kd0.00050.00000.64599.5000AID1616723
D(4) dopamine receptorHomo sapiens (human)EC50 (µMol)5.00850.00140.08892.2300AID246503; AID63858
Mu-type opioid receptorHomo sapiens (human)EC50 (µMol)10.00000.00000.32639.4000AID1558957
D(3) dopamine receptorHomo sapiens (human)Kd0.31620.00000.07480.3162AID256759
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
UDP-glucuronosyltransferase 1A9Homo sapiens (human)Km174.00005.00006.830010.0000AID1213070
ATP-dependent translocase ABCB1Homo sapiens (human)Km33.00000.01403.717210.0000AID681619
Cytochrome P450 3A4Homo sapiens (human)INH26.20001.70002.85004.0000AID711572
D(2) dopamine receptorHomo sapiens (human)Kb0.00140.00041.654910.0000AID62581
D(2) dopamine receptorHomo sapiens (human)pKi0.00910.00690.00780.0091AID63251
D(1A) dopamine receptorHomo sapiens (human)Kb0.00140.00143.667110.0000AID62581
D(4) dopamine receptorHomo sapiens (human)Kb0.00140.00143.667110.0000AID62581
D(4) dopamine receptorHomo sapiens (human)pKi0.00800.00730.00770.0080AID63699
D(1B) dopamine receptorHomo sapiens (human)Kb0.00140.00143.667110.0000AID62581
UDP-glucuronosyltransferase 1A4Homo sapiens (human)Km64.00007.00007.00007.0000AID1213067
D(3) dopamine receptorHomo sapiens (human)Kb0.00140.00141.584310.0000AID62581
D(3) dopamine receptorHomo sapiens (human)pKi0.00830.00660.00720.0083AID65437
Histamine H2 receptorCavia porcellus (domestic guinea pig)K0.50.21500.00010.40364.8000AID88009
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (776)

Processvia Protein(s)Taxonomy
prostaglandin metabolic processCocaine esteraseHomo sapiens (human)
xenobiotic metabolic processCocaine esteraseHomo sapiens (human)
catabolic processCocaine esteraseHomo sapiens (human)
xenobiotic metabolic processSolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin transportSolute carrier family 22 member 1 Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientSolute carrier family 22 member 1 Homo sapiens (human)
organic cation transportSolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transportSolute carrier family 22 member 1 Homo sapiens (human)
putrescine transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transportSolute carrier family 22 member 1 Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine transportSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transportSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 1 Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
metanephric proximal tubule developmentSolute carrier family 22 member 1 Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
monoatomic cation transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
acyl carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1A9Homo sapiens (human)
retinoic acid metabolic processUDP-glucuronosyltransferase 1A9Homo sapiens (human)
flavone metabolic processUDP-glucuronosyltransferase 1A9Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A9Homo sapiens (human)
flavonoid glucuronidationUDP-glucuronosyltransferase 1A9Homo sapiens (human)
xenobiotic glucuronidationUDP-glucuronosyltransferase 1A9Homo sapiens (human)
liver developmentUDP-glucuronosyltransferase 1A9Homo sapiens (human)
visual perceptionVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
detection of light stimulus involved in visual perceptionVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
cardiac ventricle developmentPotassium channel subfamily K member 2Homo sapiens (human)
G protein-coupled receptor signaling pathwayPotassium channel subfamily K member 2Homo sapiens (human)
memoryPotassium channel subfamily K member 2Homo sapiens (human)
response to mechanical stimulusPotassium channel subfamily K member 2Homo sapiens (human)
response to axon injuryPotassium channel subfamily K member 2Homo sapiens (human)
negative regulation of cardiac muscle cell proliferationPotassium channel subfamily K member 2Homo sapiens (human)
cellular response to hypoxiaPotassium channel subfamily K member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium channel subfamily K member 2Homo sapiens (human)
cochlea developmentPotassium channel subfamily K member 2Homo sapiens (human)
positive regulation of cellular response to hypoxiaPotassium channel subfamily K member 2Homo sapiens (human)
negative regulation of DNA biosynthetic processPotassium channel subfamily K member 2Homo sapiens (human)
stabilization of membrane potentialPotassium channel subfamily K member 2Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cellular response to copper ionMajor prion proteinHomo sapiens (human)
negative regulation of protein phosphorylationMajor prion proteinHomo sapiens (human)
intracellular copper ion homeostasisMajor prion proteinHomo sapiens (human)
response to oxidative stressMajor prion proteinHomo sapiens (human)
learning or memoryMajor prion proteinHomo sapiens (human)
long-term memoryMajor prion proteinHomo sapiens (human)
negative regulation of protein processingMajor prion proteinHomo sapiens (human)
protein destabilizationMajor prion proteinHomo sapiens (human)
negative regulation of type II interferon productionMajor prion proteinHomo sapiens (human)
negative regulation of interleukin-17 productionMajor prion proteinHomo sapiens (human)
negative regulation of interleukin-2 productionMajor prion proteinHomo sapiens (human)
negative regulation of apoptotic processMajor prion proteinHomo sapiens (human)
negative regulation of DNA-binding transcription factor activityMajor prion proteinHomo sapiens (human)
positive regulation of neuron apoptotic processMajor prion proteinHomo sapiens (human)
negative regulation of activated T cell proliferationMajor prion proteinHomo sapiens (human)
response to cadmium ionMajor prion proteinHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationMajor prion proteinHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationMajor prion proteinHomo sapiens (human)
positive regulation of calcium-mediated signalingMajor prion proteinHomo sapiens (human)
negative regulation of T cell receptor signaling pathwayMajor prion proteinHomo sapiens (human)
protein homooligomerizationMajor prion proteinHomo sapiens (human)
regulation of cell cycleMajor prion proteinHomo sapiens (human)
negative regulation of calcineurin-NFAT signaling cascadeMajor prion proteinHomo sapiens (human)
cellular response to xenobiotic stimulusMajor prion proteinHomo sapiens (human)
positive regulation of protein targeting to membraneMajor prion proteinHomo sapiens (human)
dendritic spine maintenanceMajor prion proteinHomo sapiens (human)
negative regulation of long-term synaptic potentiationMajor prion proteinHomo sapiens (human)
regulation of glutamate receptor signaling pathwayMajor prion proteinHomo sapiens (human)
positive regulation of glutamate receptor signaling pathwayMajor prion proteinHomo sapiens (human)
regulation of potassium ion transmembrane transportMajor prion proteinHomo sapiens (human)
negative regulation of amyloid-beta formationMajor prion proteinHomo sapiens (human)
negative regulation of dendritic spine maintenanceMajor prion proteinHomo sapiens (human)
negative regulation of amyloid precursor protein catabolic processMajor prion proteinHomo sapiens (human)
positive regulation of protein localization to plasma membraneMajor prion proteinHomo sapiens (human)
response to amyloid-betaMajor prion proteinHomo sapiens (human)
cellular response to amyloid-betaMajor prion proteinHomo sapiens (human)
regulation of calcium ion import across plasma membraneMajor prion proteinHomo sapiens (human)
neuron projection maintenanceMajor prion proteinHomo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
T cell mediated cytotoxicityHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
T cell mediated cytotoxicity directed against tumor cell targetHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-dependentHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
peptide antigen assembly with MHC class I protein complexHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
positive regulation of T cell cytokine productionHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
antibacterial humoral responseHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
positive regulation of type II interferon productionHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
CD8-positive, alpha-beta T cell activationHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
antigen processing and presentation of exogenous peptide antigen via MHC class IHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
defense response to Gram-positive bacteriumHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
T cell receptor signaling pathwayHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
positive regulation of CD8-positive, alpha-beta T cell proliferationHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
positive regulation of memory T cell activationHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
positive regulation of CD8-positive, alpha-beta T cell activationHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayIntegrin beta-1Homo sapiens (human)
stress fiber assemblyIntegrin beta-1Homo sapiens (human)
calcium-independent cell-matrix adhesionIntegrin beta-1Homo sapiens (human)
positive regulation of apoptotic processIntegrin beta-1Homo sapiens (human)
positive regulation of glutamate uptake involved in transmission of nerve impulseIntegrin beta-1Homo sapiens (human)
regulation of inward rectifier potassium channel activityIntegrin beta-1Homo sapiens (human)
regulation of spontaneous synaptic transmissionIntegrin beta-1Homo sapiens (human)
reactive gliosisIntegrin beta-1Homo sapiens (human)
G1/S transition of mitotic cell cycleIntegrin beta-1Homo sapiens (human)
establishment of mitotic spindle orientationIntegrin beta-1Homo sapiens (human)
in utero embryonic developmentIntegrin beta-1Homo sapiens (human)
cell migration involved in sprouting angiogenesisIntegrin beta-1Homo sapiens (human)
positive regulation of neuroblast proliferationIntegrin beta-1Homo sapiens (human)
phagocytosisIntegrin beta-1Homo sapiens (human)
cellular defense responseIntegrin beta-1Homo sapiens (human)
cell adhesionIntegrin beta-1Homo sapiens (human)
homophilic cell adhesion via plasma membrane adhesion moleculesIntegrin beta-1Homo sapiens (human)
leukocyte cell-cell adhesionIntegrin beta-1Homo sapiens (human)
cell-matrix adhesionIntegrin beta-1Homo sapiens (human)
integrin-mediated signaling pathwayIntegrin beta-1Homo sapiens (human)
neuroblast proliferationIntegrin beta-1Homo sapiens (human)
muscle organ developmentIntegrin beta-1Homo sapiens (human)
myoblast fusionIntegrin beta-1Homo sapiens (human)
germ cell migrationIntegrin beta-1Homo sapiens (human)
visual learningIntegrin beta-1Homo sapiens (human)
regulation of collagen catabolic processIntegrin beta-1Homo sapiens (human)
positive regulation of fibroblast migrationIntegrin beta-1Homo sapiens (human)
cell migrationIntegrin beta-1Homo sapiens (human)
formation of radial glial scaffoldsIntegrin beta-1Homo sapiens (human)
CD40 signaling pathwayIntegrin beta-1Homo sapiens (human)
cell projection organizationIntegrin beta-1Homo sapiens (human)
lamellipodium assemblyIntegrin beta-1Homo sapiens (human)
B cell differentiationIntegrin beta-1Homo sapiens (human)
extracellular matrix organizationIntegrin beta-1Homo sapiens (human)
positive regulation of cell migrationIntegrin beta-1Homo sapiens (human)
cell-substrate adhesionIntegrin beta-1Homo sapiens (human)
receptor internalizationIntegrin beta-1Homo sapiens (human)
cell adhesion mediated by integrinIntegrin beta-1Homo sapiens (human)
cell-cell adhesion mediated by integrinIntegrin beta-1Homo sapiens (human)
heterotypic cell-cell adhesionIntegrin beta-1Homo sapiens (human)
negative regulation of Rho protein signal transductionIntegrin beta-1Homo sapiens (human)
wound healing, spreading of epidermal cellsIntegrin beta-1Homo sapiens (human)
maintenance of blood-brain barrierIntegrin beta-1Homo sapiens (human)
positive regulation of GTPase activityIntegrin beta-1Homo sapiens (human)
sarcomere organizationIntegrin beta-1Homo sapiens (human)
myoblast differentiationIntegrin beta-1Homo sapiens (human)
negative regulation of neuron differentiationIntegrin beta-1Homo sapiens (human)
positive regulation of fibroblast growth factor receptor signaling pathwayIntegrin beta-1Homo sapiens (human)
positive regulation of angiogenesisIntegrin beta-1Homo sapiens (human)
negative regulation of vasoconstrictionIntegrin beta-1Homo sapiens (human)
symbiont entry into host cellIntegrin beta-1Homo sapiens (human)
mesodermal cell differentiationIntegrin beta-1Homo sapiens (human)
myoblast fate specificationIntegrin beta-1Homo sapiens (human)
axon extensionIntegrin beta-1Homo sapiens (human)
dendrite morphogenesisIntegrin beta-1Homo sapiens (human)
leukocyte tethering or rollingIntegrin beta-1Homo sapiens (human)
regulation of cell cycleIntegrin beta-1Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionIntegrin beta-1Homo sapiens (human)
cardiac muscle cell differentiationIntegrin beta-1Homo sapiens (human)
cardiac muscle cell myoblast differentiationIntegrin beta-1Homo sapiens (human)
cardiac cell fate specificationIntegrin beta-1Homo sapiens (human)
cellular response to low-density lipoprotein particle stimulusIntegrin beta-1Homo sapiens (human)
basement membrane organizationIntegrin beta-1Homo sapiens (human)
positive regulation of wound healingIntegrin beta-1Homo sapiens (human)
positive regulation of vascular endothelial growth factor signaling pathwayIntegrin beta-1Homo sapiens (human)
positive regulation of protein localization to plasma membraneIntegrin beta-1Homo sapiens (human)
regulation of synapse pruningIntegrin beta-1Homo sapiens (human)
negative regulation of anoikisIntegrin beta-1Homo sapiens (human)
cell-cell adhesionIntegrin beta-1Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of heart contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
response to virusMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M2Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M4Homo sapiens (human)
cell surface receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M4Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M4Homo sapiens (human)
G2/M transition of mitotic cell cycleATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic metabolic processATP-dependent translocase ABCB1Homo sapiens (human)
response to xenobiotic stimulusATP-dependent translocase ABCB1Homo sapiens (human)
phospholipid translocationATP-dependent translocase ABCB1Homo sapiens (human)
terpenoid transportATP-dependent translocase ABCB1Homo sapiens (human)
regulation of response to osmotic stressATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
transepithelial transportATP-dependent translocase ABCB1Homo sapiens (human)
stem cell proliferationATP-dependent translocase ABCB1Homo sapiens (human)
ceramide translocationATP-dependent translocase ABCB1Homo sapiens (human)
export across plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of anion channel activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
regulation of chloride transportATP-dependent translocase ABCB1Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
gamma-aminobutyric acid signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of serotonin secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of vasoconstriction5-hydroxytryptamine receptor 1AHomo sapiens (human)
exploration behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of dopamine metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of hormone secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1AHomo sapiens (human)
gastric acid secretionMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
dopamine transportMuscarinic acetylcholine receptor M5Homo sapiens (human)
transmission of nerve impulseMuscarinic acetylcholine receptor M5Homo sapiens (human)
regulation of phosphatidylinositol dephosphorylationMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M5Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M5Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
positive regulation of cytokine productionAlpha-2A adrenergic receptorHomo sapiens (human)
DNA replicationAlpha-2A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
Ras protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
Rho protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2A adrenergic receptorHomo sapiens (human)
actin cytoskeleton organizationAlpha-2A adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell migrationAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
cellular response to hormone stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2A adrenergic receptorHomo sapiens (human)
vasodilationAlpha-2A adrenergic receptorHomo sapiens (human)
glucose homeostasisAlpha-2A adrenergic receptorHomo sapiens (human)
fear responseAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of potassium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAP kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion-dependent exocytosisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2A adrenergic receptorHomo sapiens (human)
intestinal absorptionAlpha-2A adrenergic receptorHomo sapiens (human)
thermoceptionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of lipid catabolic processAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of uterine smooth muscle contractionAlpha-2A adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
phospholipase C-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of wound healingAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transmembrane transporter activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of monoatomic ion transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
neuromuscular synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M1Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M1Homo sapiens (human)
cognitionMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of postsynaptic membrane potentialMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of glial cell proliferationMuscarinic acetylcholine receptor M1Homo sapiens (human)
positive regulation of intracellular protein transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
immune response in gut-associated lymphoid tissueIntegrin alpha-4Homo sapiens (human)
cell-matrix adhesion involved in ameboidal cell migrationIntegrin alpha-4Homo sapiens (human)
leukocyte cell-cell adhesionIntegrin alpha-4Homo sapiens (human)
cell-matrix adhesionIntegrin alpha-4Homo sapiens (human)
integrin-mediated signaling pathwayIntegrin alpha-4Homo sapiens (human)
B cell differentiationIntegrin alpha-4Homo sapiens (human)
cell-cell adhesion mediated by integrinIntegrin alpha-4Homo sapiens (human)
heterotypic cell-cell adhesionIntegrin alpha-4Homo sapiens (human)
substrate adhesion-dependent cell spreadingIntegrin alpha-4Homo sapiens (human)
endodermal cell differentiationIntegrin alpha-4Homo sapiens (human)
receptor clusteringIntegrin alpha-4Homo sapiens (human)
negative regulation of vasoconstrictionIntegrin alpha-4Homo sapiens (human)
leukocyte tethering or rollingIntegrin alpha-4Homo sapiens (human)
diapedesisIntegrin alpha-4Homo sapiens (human)
axonogenesis involved in innervationIntegrin alpha-4Homo sapiens (human)
cellular response to cytokine stimulusIntegrin alpha-4Homo sapiens (human)
negative regulation of protein homodimerization activityIntegrin alpha-4Homo sapiens (human)
positive regulation of leukocyte tethering or rollingIntegrin alpha-4Homo sapiens (human)
cellular response to amyloid-betaIntegrin alpha-4Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationIntegrin alpha-4Homo sapiens (human)
neuron projection extensionIntegrin alpha-4Homo sapiens (human)
clathrin-dependent extracellular exosome endocytosisIntegrin alpha-4Homo sapiens (human)
positive regulation of endothelial cell apoptotic processIntegrin alpha-4Homo sapiens (human)
positive regulation of T cell migrationIntegrin alpha-4Homo sapiens (human)
cell-cell adhesionIntegrin alpha-4Homo sapiens (human)
cell adhesion mediated by integrinIntegrin alpha-4Homo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasisD(2) dopamine receptorHomo sapiens (human)
response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein phosphorylationD(2) dopamine receptorHomo sapiens (human)
response to amphetamineD(2) dopamine receptorHomo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressureD(2) dopamine receptorHomo sapiens (human)
regulation of heart rateD(2) dopamine receptorHomo sapiens (human)
regulation of sodium ion transportD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(2) dopamine receptorHomo sapiens (human)
positive regulation of neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
positive regulation of receptor internalizationD(2) dopamine receptorHomo sapiens (human)
autophagyD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
neuron-neuron synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
axonogenesisD(2) dopamine receptorHomo sapiens (human)
synapse assemblyD(2) dopamine receptorHomo sapiens (human)
sensory perception of smellD(2) dopamine receptorHomo sapiens (human)
long-term memoryD(2) dopamine receptorHomo sapiens (human)
grooming behaviorD(2) dopamine receptorHomo sapiens (human)
locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
adult walking behaviorD(2) dopamine receptorHomo sapiens (human)
protein localizationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell population proliferationD(2) dopamine receptorHomo sapiens (human)
associative learningD(2) dopamine receptorHomo sapiens (human)
visual learningD(2) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(2) dopamine receptorHomo sapiens (human)
response to light stimulusD(2) dopamine receptorHomo sapiens (human)
response to toxic substanceD(2) dopamine receptorHomo sapiens (human)
response to iron ionD(2) dopamine receptorHomo sapiens (human)
response to inactivityD(2) dopamine receptorHomo sapiens (human)
Wnt signaling pathwayD(2) dopamine receptorHomo sapiens (human)
striatum developmentD(2) dopamine receptorHomo sapiens (human)
orbitofrontal cortex developmentD(2) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(2) dopamine receptorHomo sapiens (human)
adenohypophysis developmentD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell migrationD(2) dopamine receptorHomo sapiens (human)
peristalsisD(2) dopamine receptorHomo sapiens (human)
auditory behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of synaptic transmission, GABAergicD(2) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(2) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
response to histamineD(2) dopamine receptorHomo sapiens (human)
response to nicotineD(2) dopamine receptorHomo sapiens (human)
positive regulation of urine volumeD(2) dopamine receptorHomo sapiens (human)
positive regulation of renal sodium excretionD(2) dopamine receptorHomo sapiens (human)
positive regulation of multicellular organism growthD(2) dopamine receptorHomo sapiens (human)
response to cocaineD(2) dopamine receptorHomo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleepD(2) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(2) dopamine receptorHomo sapiens (human)
drinking behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(2) dopamine receptorHomo sapiens (human)
response to morphineD(2) dopamine receptorHomo sapiens (human)
pigmentationD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(2) dopamine receptorHomo sapiens (human)
negative regulation of innate immune responseD(2) dopamine receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IID(2) dopamine receptorHomo sapiens (human)
negative regulation of insulin secretionD(2) dopamine receptorHomo sapiens (human)
acid secretionD(2) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(2) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(2) dopamine receptorHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityD(2) dopamine receptorHomo sapiens (human)
response to axon injuryD(2) dopamine receptorHomo sapiens (human)
branching morphogenesis of a nerveD(2) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(2) dopamine receptorHomo sapiens (human)
epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(2) dopamine receptorHomo sapiens (human)
release of sequestered calcium ion into cytosolD(2) dopamine receptorHomo sapiens (human)
dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of synapse structural plasticityD(2) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(2) dopamine receptorHomo sapiens (human)
excitatory postsynaptic potentialD(2) dopamine receptorHomo sapiens (human)
positive regulation of growth hormone secretionD(2) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeD(2) dopamine receptorHomo sapiens (human)
regulation of locomotion involved in locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
negative regulation of cellular response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor productionD(2) dopamine receptorHomo sapiens (human)
positive regulation of long-term synaptic potentiationD(2) dopamine receptorHomo sapiens (human)
hyaloid vascular plexus regressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of neuron migrationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(2) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
xenobiotic metabolic processCarbonyl reductase [NADPH] 1Homo sapiens (human)
glucocorticoid metabolic processCarbonyl reductase [NADPH] 1Homo sapiens (human)
cyclooxygenase pathwayCarbonyl reductase [NADPH] 1Homo sapiens (human)
epithelial cell differentiationCarbonyl reductase [NADPH] 1Homo sapiens (human)
vitamin K metabolic processCarbonyl reductase [NADPH] 1Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCarbonyl reductase [NADPH] 1Homo sapiens (human)
lipid metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
androgen metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 2B7Homo sapiens (human)
MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
angiogenesisAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vascular associated smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2B adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2B adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of blood pressureAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of smooth muscle contractionAlpha-2C adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2C adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2C adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2C adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2C adrenergic receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(2) dopamine receptorBos taurus (cattle)
negative regulation of prolactin secretionD(2) dopamine receptorBos taurus (cattle)
negative regulation of lactationD(2) dopamine receptorBos taurus (cattle)
positive regulation of mammary gland involutionD(2) dopamine receptorBos taurus (cattle)
hyaloid vascular plexus regressionD(2) dopamine receptorBos taurus (cattle)
calcium-mediated signalingMuscarinic acetylcholine receptor M3Homo sapiens (human)
regulation of monoatomic ion transmembrane transporter activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
synaptic transmission, cholinergicMuscarinic acetylcholine receptor M3Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M3Homo sapiens (human)
positive regulation of insulin secretionMuscarinic acetylcholine receptor M3Homo sapiens (human)
protein modification processMuscarinic acetylcholine receptor M3Homo sapiens (human)
positive regulation of smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M3Homo sapiens (human)
acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
ion channel modulating, G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
ligand-gated ion channel signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M3Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M3Homo sapiens (human)
temperature homeostasisD(1A) dopamine receptorHomo sapiens (human)
conditioned taste aversionD(1A) dopamine receptorHomo sapiens (human)
behavioral fear responseD(1A) dopamine receptorHomo sapiens (human)
regulation of protein phosphorylationD(1A) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(1A) dopamine receptorHomo sapiens (human)
response to amphetamineD(1A) dopamine receptorHomo sapiens (human)
protein import into nucleusD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
activation of adenylate cyclase activityD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
synapse assemblyD(1A) dopamine receptorHomo sapiens (human)
memoryD(1A) dopamine receptorHomo sapiens (human)
mating behaviorD(1A) dopamine receptorHomo sapiens (human)
grooming behaviorD(1A) dopamine receptorHomo sapiens (human)
adult walking behaviorD(1A) dopamine receptorHomo sapiens (human)
visual learningD(1A) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(1A) dopamine receptorHomo sapiens (human)
astrocyte developmentD(1A) dopamine receptorHomo sapiens (human)
dopamine transportD(1A) dopamine receptorHomo sapiens (human)
transmission of nerve impulseD(1A) dopamine receptorHomo sapiens (human)
neuronal action potentialD(1A) dopamine receptorHomo sapiens (human)
dentate gyrus developmentD(1A) dopamine receptorHomo sapiens (human)
striatum developmentD(1A) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(1A) dopamine receptorHomo sapiens (human)
positive regulation of cell migrationD(1A) dopamine receptorHomo sapiens (human)
peristalsisD(1A) dopamine receptorHomo sapiens (human)
operant conditioningD(1A) dopamine receptorHomo sapiens (human)
synaptic transmission, glutamatergicD(1A) dopamine receptorHomo sapiens (human)
regulation of dopamine metabolic processD(1A) dopamine receptorHomo sapiens (human)
vasodilationD(1A) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(1A) dopamine receptorHomo sapiens (human)
maternal behaviorD(1A) dopamine receptorHomo sapiens (human)
positive regulation of potassium ion transportD(1A) dopamine receptorHomo sapiens (human)
glucose importD(1A) dopamine receptorHomo sapiens (human)
habituationD(1A) dopamine receptorHomo sapiens (human)
sensitizationD(1A) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(1A) dopamine receptorHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolD(1A) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(1A) dopamine receptorHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicD(1A) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(1A) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
long-term synaptic potentiationD(1A) dopamine receptorHomo sapiens (human)
long-term synaptic depressionD(1A) dopamine receptorHomo sapiens (human)
cellular response to catecholamine stimulusD(1A) dopamine receptorHomo sapiens (human)
modification of postsynaptic structureD(1A) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(1A) dopamine receptorHomo sapiens (human)
positive regulation of neuron migrationD(1A) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
positive regulation of MAP kinase activityD(4) dopamine receptorHomo sapiens (human)
behavioral fear responseD(4) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(4) dopamine receptorHomo sapiens (human)
response to amphetamineD(4) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(4) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
adult locomotory behaviorD(4) dopamine receptorHomo sapiens (human)
positive regulation of sodium:proton antiporter activityD(4) dopamine receptorHomo sapiens (human)
positive regulation of kinase activityD(4) dopamine receptorHomo sapiens (human)
response to histamineD(4) dopamine receptorHomo sapiens (human)
social behaviorD(4) dopamine receptorHomo sapiens (human)
regulation of dopamine metabolic processD(4) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(4) dopamine receptorHomo sapiens (human)
fear responseD(4) dopamine receptorHomo sapiens (human)
regulation of circadian rhythmD(4) dopamine receptorHomo sapiens (human)
positive regulation of MAP kinase activityD(4) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(4) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(4) dopamine receptorHomo sapiens (human)
rhythmic processD(4) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(4) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(4) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(4) dopamine receptorHomo sapiens (human)
inhibitory postsynaptic potentialD(4) dopamine receptorHomo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalizationD(4) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(4) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerD(4) dopamine receptorHomo sapiens (human)
chemical synaptic transmissionD(4) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(1B) dopamine receptorHomo sapiens (human)
response to amphetamineD(1B) dopamine receptorHomo sapiens (human)
regulation of systemic arterial blood pressure by vasopressinD(1B) dopamine receptorHomo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressureD(1B) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(1B) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayD(1B) dopamine receptorHomo sapiens (human)
activation of adenylate cyclase activityD(1B) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(1B) dopamine receptorHomo sapiens (human)
chemical synaptic transmissionD(1B) dopamine receptorHomo sapiens (human)
associative learningD(1B) dopamine receptorHomo sapiens (human)
transmission of nerve impulseD(1B) dopamine receptorHomo sapiens (human)
negative regulation of NAD(P)H oxidase activityD(1B) dopamine receptorHomo sapiens (human)
wound healingD(1B) dopamine receptorHomo sapiens (human)
response to cocaineD(1B) dopamine receptorHomo sapiens (human)
positive regulation of adenylate cyclase activityD(1B) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(1B) dopamine receptorHomo sapiens (human)
regulation of female receptivityD(1B) dopamine receptorHomo sapiens (human)
sensitizationD(1B) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(1B) dopamine receptorHomo sapiens (human)
long-term synaptic depressionD(1B) dopamine receptorHomo sapiens (human)
cellular response to catecholamine stimulusD(1B) dopamine receptorHomo sapiens (human)
reactive oxygen species metabolic processD(1B) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(1B) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(1B) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(1B) dopamine receptorHomo sapiens (human)
bilirubin conjugationUDP-glucuronosyltransferase 1A4Homo sapiens (human)
heme catabolic processUDP-glucuronosyltransferase 1A4Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A4Homo sapiens (human)
vitamin D3 metabolic processUDP-glucuronosyltransferase 1A4Homo sapiens (human)
monoamine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent noradrenaline transporter Homo sapiens (human)
chemical synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent noradrenaline transporter Homo sapiens (human)
response to painSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent noradrenaline transporter Homo sapiens (human)
neuron cellular homeostasisSodium-dependent noradrenaline transporter Homo sapiens (human)
amino acid transportSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent noradrenaline transporter Homo sapiens (human)
gastric acid secretionHistamine H2 receptorHomo sapiens (human)
immune responseHistamine H2 receptorHomo sapiens (human)
positive regulation of vasoconstrictionHistamine H2 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H2 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H2 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H2 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-1D adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1D adrenergic receptorHomo sapiens (human)
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
monoamine transportSodium-dependent serotonin transporterHomo sapiens (human)
response to hypoxiaSodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transportSodium-dependent serotonin transporterHomo sapiens (human)
response to nutrientSodium-dependent serotonin transporterHomo sapiens (human)
memorySodium-dependent serotonin transporterHomo sapiens (human)
circadian rhythmSodium-dependent serotonin transporterHomo sapiens (human)
response to xenobiotic stimulusSodium-dependent serotonin transporterHomo sapiens (human)
response to toxic substanceSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of gene expressionSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of serotonin secretionSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of cerebellar granule cell precursor proliferationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of synaptic transmission, dopaminergicSodium-dependent serotonin transporterHomo sapiens (human)
response to estradiolSodium-dependent serotonin transporterHomo sapiens (human)
social behaviorSodium-dependent serotonin transporterHomo sapiens (human)
vasoconstrictionSodium-dependent serotonin transporterHomo sapiens (human)
sperm ejaculationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of neuron differentiationSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of cell cycleSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of organ growthSodium-dependent serotonin transporterHomo sapiens (human)
behavioral response to cocaineSodium-dependent serotonin transporterHomo sapiens (human)
enteric nervous system developmentSodium-dependent serotonin transporterHomo sapiens (human)
brain morphogenesisSodium-dependent serotonin transporterHomo sapiens (human)
serotonin uptakeSodium-dependent serotonin transporterHomo sapiens (human)
membrane depolarizationSodium-dependent serotonin transporterHomo sapiens (human)
platelet aggregationSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to retinoic acidSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to cGMPSodium-dependent serotonin transporterHomo sapiens (human)
regulation of thalamus sizeSodium-dependent serotonin transporterHomo sapiens (human)
conditioned place preferenceSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion transmembrane transportSodium-dependent serotonin transporterHomo sapiens (human)
amino acid transportSodium-dependent serotonin transporterHomo sapiens (human)
smooth muscle contraction5-hydroxytryptamine receptor 7Homo sapiens (human)
circadian rhythm5-hydroxytryptamine receptor 7Homo sapiens (human)
blood circulation5-hydroxytryptamine receptor 7Homo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 7Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 7Homo sapiens (human)
MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
apoptotic processAlpha-1A adrenergic receptorHomo sapiens (human)
smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
activation of phospholipase C activityAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1A adrenergic receptorHomo sapiens (human)
adult heart developmentAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of cell population proliferationAlpha-1A adrenergic receptorHomo sapiens (human)
response to xenobiotic stimulusAlpha-1A adrenergic receptorHomo sapiens (human)
response to hormoneAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of autophagyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of action potentialAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
calcium ion transport into cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
cell growth involved in cardiac muscle cell developmentAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase C signalingAlpha-1A adrenergic receptorHomo sapiens (human)
pilomotor reflexAlpha-1A adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
inflammatory responseHistamine H1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
memoryHistamine H1 receptorHomo sapiens (human)
visual learningHistamine H1 receptorHomo sapiens (human)
regulation of vascular permeabilityHistamine H1 receptorHomo sapiens (human)
positive regulation of vasoconstrictionHistamine H1 receptorHomo sapiens (human)
regulation of synaptic plasticityHistamine H1 receptorHomo sapiens (human)
cellular response to histamineHistamine H1 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H1 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1B adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of cardiac muscle contractionAlpha-1B adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1B adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMu-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
sensory perceptionMu-type opioid receptorHomo sapiens (human)
negative regulation of cell population proliferationMu-type opioid receptorHomo sapiens (human)
sensory perception of painMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
behavioral response to ethanolMu-type opioid receptorHomo sapiens (human)
positive regulation of neurogenesisMu-type opioid receptorHomo sapiens (human)
negative regulation of Wnt protein secretionMu-type opioid receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeMu-type opioid receptorHomo sapiens (human)
calcium ion transmembrane transportMu-type opioid receptorHomo sapiens (human)
cellular response to morphineMu-type opioid receptorHomo sapiens (human)
regulation of cellular response to stressMu-type opioid receptorHomo sapiens (human)
regulation of NMDA receptor activityMu-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayMu-type opioid receptorHomo sapiens (human)
response to ethanolD(3) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(3) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
learning or memoryD(3) dopamine receptorHomo sapiens (human)
learningD(3) dopamine receptorHomo sapiens (human)
locomotory behaviorD(3) dopamine receptorHomo sapiens (human)
visual learningD(3) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(3) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(3) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(3) dopamine receptorHomo sapiens (human)
response to histamineD(3) dopamine receptorHomo sapiens (human)
social behaviorD(3) dopamine receptorHomo sapiens (human)
response to cocaineD(3) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(3) dopamine receptorHomo sapiens (human)
response to morphineD(3) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(3) dopamine receptorHomo sapiens (human)
positive regulation of mitotic nuclear divisionD(3) dopamine receptorHomo sapiens (human)
acid secretionD(3) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(3) dopamine receptorHomo sapiens (human)
negative regulation of oligodendrocyte differentiationD(3) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(3) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(3) dopamine receptorHomo sapiens (human)
musculoskeletal movement, spinal reflex actionD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(3) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(3) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(3) dopamine receptorHomo sapiens (human)
positive regulation of dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(3) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(3) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(3) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(3) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(3) dopamine receptorHomo sapiens (human)
sodium ion transportSodium channel protein type 1 subunit alphaHomo sapiens (human)
adult walking behaviorSodium channel protein type 1 subunit alphaHomo sapiens (human)
determination of adult lifespanSodium channel protein type 1 subunit alphaHomo sapiens (human)
neuronal action potential propagationSodium channel protein type 1 subunit alphaHomo sapiens (human)
neuronal action potentialSodium channel protein type 1 subunit alphaHomo sapiens (human)
nerve developmentSodium channel protein type 1 subunit alphaHomo sapiens (human)
neuromuscular process controlling postureSodium channel protein type 1 subunit alphaHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of painSodium channel protein type 1 subunit alphaHomo sapiens (human)
establishment of localization in cellSodium channel protein type 1 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 1 subunit alphaHomo sapiens (human)
membrane depolarization during action potentialSodium channel protein type 1 subunit alphaHomo sapiens (human)
regulation of presynaptic membrane potentialSodium channel protein type 1 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 1 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 4 subunit alphaHomo sapiens (human)
muscle contractionSodium channel protein type 4 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 4 subunit alphaHomo sapiens (human)
regulation of skeletal muscle contraction by action potentialSodium channel protein type 4 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 4 subunit alphaHomo sapiens (human)
neural crest cell migration5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cytokine production5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of endothelial cell proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 2BHomo sapiens (human)
heart morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
cardiac muscle hypertrophy5-hydroxytryptamine receptor 2BHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
neural crest cell differentiation5-hydroxytryptamine receptor 2BHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphorylation5-hydroxytryptamine receptor 2BHomo sapiens (human)
calcium-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 2BHomo sapiens (human)
negative regulation of apoptotic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of MAP kinase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
embryonic morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of nitric-oxide synthase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell division5-hydroxytryptamine receptor 2BHomo sapiens (human)
ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2BHomo sapiens (human)
cerebral cortex cell migration5-hydroxytryptamine receptor 6Homo sapiens (human)
positive regulation of TOR signaling5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 6Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 6Homo sapiens (human)
fatty acid metabolic processCytochrome P450 2J2Homo sapiens (human)
icosanoid metabolic processCytochrome P450 2J2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2J2Homo sapiens (human)
regulation of heart contractionCytochrome P450 2J2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2J2Homo sapiens (human)
linoleic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
organic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
symbiont-mediated suppression of host defense-related programmed cell deathN-acetyltransferase EisMycobacterium tuberculosis H37Rv
osmosensory signaling pathwaySodium channel protein type 7 subunit alphaHomo sapiens (human)
response to bacteriumSodium channel protein type 7 subunit alphaHomo sapiens (human)
cellular homeostasisSodium channel protein type 7 subunit alphaHomo sapiens (human)
sodium ion homeostasisSodium channel protein type 7 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 7 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 7 subunit alphaHomo sapiens (human)
calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
sensory perception of soundVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
positive regulation of adenylate cyclase activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
positive regulation of calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion importVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
membrane depolarization during SA node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of potassium ion transmembrane transporter activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of potassium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of protein phosphorylationTAR DNA-binding protein 43Homo sapiens (human)
mRNA processingTAR DNA-binding protein 43Homo sapiens (human)
RNA splicingTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
regulation of protein stabilityTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of insulin secretionTAR DNA-binding protein 43Homo sapiens (human)
response to endoplasmic reticulum stressTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of protein import into nucleusTAR DNA-binding protein 43Homo sapiens (human)
regulation of circadian rhythmTAR DNA-binding protein 43Homo sapiens (human)
regulation of apoptotic processTAR DNA-binding protein 43Homo sapiens (human)
negative regulation by host of viral transcriptionTAR DNA-binding protein 43Homo sapiens (human)
rhythmic processTAR DNA-binding protein 43Homo sapiens (human)
regulation of cell cycleTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA destabilizationTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationTAR DNA-binding protein 43Homo sapiens (human)
nuclear inner membrane organizationTAR DNA-binding protein 43Homo sapiens (human)
amyloid fibril formationTAR DNA-binding protein 43Homo sapiens (human)
regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 4Homo sapiens (human)
maintenance of gastrointestinal epithelium5-hydroxytryptamine receptor 4Homo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 4Homo sapiens (human)
mucus secretion5-hydroxytryptamine receptor 4Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 4Homo sapiens (human)
large intestinal transit5-hydroxytryptamine receptor 4Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 4Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 4Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 4Homo sapiens (human)
skeletal system developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
extraocular skeletal muscle developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
striated muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
endoplasmic reticulum organizationVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
myoblast fusionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
neuromuscular junction developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
skeletal muscle adaptationVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
skeletal muscle fiber developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
release of sequestered calcium ion into cytosolVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
cellular response to caffeineVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
immune system developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
heart developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
embryonic forelimb morphogenesisVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
camera-type eye developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of adenylate cyclase activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transport into cytosolVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transport via high voltage-gated calcium channelVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cell communication by electrical coupling involved in cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of ventricular cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of heart rateSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac conduction system developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac ventricle developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
brainstem developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of sodium ion transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
response to denervation involved in regulation of muscle adaptationSodium channel protein type 5 subunit alphaHomo sapiens (human)
telencephalon developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
cerebellum developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
odontogenesis of dentin-containing toothSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of epithelial cell proliferationSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac muscle contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of ventricular cardiac muscle cell membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
cellular response to calcium ionSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of cardiac muscle cell contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
ventricular cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
atrial cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during Purkinje myocyte cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
AV node cell to bundle of His cell communicationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of heart rate by cardiac conductionSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of sodium ion transmembrane transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
cholesterol biosynthetic process3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
cholesterol metabolic process3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
hemopoiesis3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
cholesterol biosynthetic process via desmosterol3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
cholesterol biosynthetic process via lathosterol3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
ossification involved in bone maturation3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
sodium ion transportSodium channel protein type 9 subunit alphaHomo sapiens (human)
inflammatory responseSodium channel protein type 9 subunit alphaHomo sapiens (human)
circadian rhythmSodium channel protein type 9 subunit alphaHomo sapiens (human)
response to toxic substanceSodium channel protein type 9 subunit alphaHomo sapiens (human)
post-embryonic developmentSodium channel protein type 9 subunit alphaHomo sapiens (human)
sensory perception of painSodium channel protein type 9 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 9 subunit alphaHomo sapiens (human)
behavioral response to painSodium channel protein type 9 subunit alphaHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of painSodium channel protein type 9 subunit alphaHomo sapiens (human)
detection of mechanical stimulus involved in sensory perceptionSodium channel protein type 9 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 9 subunit alphaHomo sapiens (human)
angiogenesisCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
calcium ion transportCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
cell surface receptor signaling pathwayCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
heart developmentCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
protein transportCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
receptor internalizationCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
cellular response to sucrose stimulusCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
calcitonin gene-related peptide receptor signaling pathwayCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
adrenomedullin receptor signaling pathwayCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
vascular associated smooth muscle cell proliferationCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
regulation of cell growthSigma intracellular receptor 2Homo sapiens (human)
regulation of intracellular lipid transportSigma intracellular receptor 2Homo sapiens (human)
regulation of intracellular cholesterol transportSigma intracellular receptor 2Homo sapiens (human)
cholesterol homeostasisSigma intracellular receptor 2Homo sapiens (human)
positive regulation of wound healingSigma intracellular receptor 2Homo sapiens (human)
positive regulation of lipoprotein transportSigma intracellular receptor 2Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
synaptic transmission, dopaminergicDBos taurus (cattle)
vasodilationDBos taurus (cattle)
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
sodium ion transportSodium channel protein type 2 subunit alphaHomo sapiens (human)
nervous system developmentSodium channel protein type 2 subunit alphaHomo sapiens (human)
intrinsic apoptotic signaling pathway in response to osmotic stressSodium channel protein type 2 subunit alphaHomo sapiens (human)
neuron apoptotic processSodium channel protein type 2 subunit alphaHomo sapiens (human)
memorySodium channel protein type 2 subunit alphaHomo sapiens (human)
determination of adult lifespanSodium channel protein type 2 subunit alphaHomo sapiens (human)
neuronal action potentialSodium channel protein type 2 subunit alphaHomo sapiens (human)
dentate gyrus developmentSodium channel protein type 2 subunit alphaHomo sapiens (human)
nerve developmentSodium channel protein type 2 subunit alphaHomo sapiens (human)
myelinationSodium channel protein type 2 subunit alphaHomo sapiens (human)
cellular response to hypoxiaSodium channel protein type 2 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 2 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 2 subunit alphaHomo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
lipid transportSigma non-opioid intracellular receptor 1Homo sapiens (human)
nervous system developmentSigma non-opioid intracellular receptor 1Homo sapiens (human)
G protein-coupled opioid receptor signaling pathwaySigma non-opioid intracellular receptor 1Homo sapiens (human)
regulation of neuron apoptotic processSigma non-opioid intracellular receptor 1Homo sapiens (human)
protein homotrimerizationSigma non-opioid intracellular receptor 1Homo sapiens (human)
sodium ion transportSodium channel protein type 3 subunit alphaHomo sapiens (human)
behavioral response to painSodium channel protein type 3 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 3 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 3 subunit alphaHomo sapiens (human)
thigmotaxisSodium channel protein type 11 subunit alphaHomo sapiens (human)
acute inflammatory responseSodium channel protein type 11 subunit alphaHomo sapiens (human)
chronic inflammatory responseSodium channel protein type 11 subunit alphaHomo sapiens (human)
axonogenesisSodium channel protein type 11 subunit alphaHomo sapiens (human)
circadian rhythmSodium channel protein type 11 subunit alphaHomo sapiens (human)
response to heatSodium channel protein type 11 subunit alphaHomo sapiens (human)
response to xenobiotic stimulusSodium channel protein type 11 subunit alphaHomo sapiens (human)
response to toxic substanceSodium channel protein type 11 subunit alphaHomo sapiens (human)
response to high light intensitySodium channel protein type 11 subunit alphaHomo sapiens (human)
protein kinase A signalingSodium channel protein type 11 subunit alphaHomo sapiens (human)
response to auditory stimulusSodium channel protein type 11 subunit alphaHomo sapiens (human)
neuronal action potentialSodium channel protein type 11 subunit alphaHomo sapiens (human)
sensory perception of painSodium channel protein type 11 subunit alphaHomo sapiens (human)
response to prostaglandin ESodium channel protein type 11 subunit alphaHomo sapiens (human)
thermosensory behaviorSodium channel protein type 11 subunit alphaHomo sapiens (human)
mast cell degranulationSodium channel protein type 11 subunit alphaHomo sapiens (human)
cell motilitySodium channel protein type 11 subunit alphaHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of painSodium channel protein type 11 subunit alphaHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of painSodium channel protein type 11 subunit alphaHomo sapiens (human)
reflexSodium channel protein type 11 subunit alphaHomo sapiens (human)
micturitionSodium channel protein type 11 subunit alphaHomo sapiens (human)
skeletal muscle organ developmentSodium channel protein type 11 subunit alphaHomo sapiens (human)
artery developmentSodium channel protein type 11 subunit alphaHomo sapiens (human)
behavioral response to acetic acid induced painSodium channel protein type 11 subunit alphaHomo sapiens (human)
behavioral response to formalin induced painSodium channel protein type 11 subunit alphaHomo sapiens (human)
cellular response to coldSodium channel protein type 11 subunit alphaHomo sapiens (human)
calcium ion transmembrane transportSodium channel protein type 11 subunit alphaHomo sapiens (human)
response to nitric oxideSodium channel protein type 11 subunit alphaHomo sapiens (human)
membrane depolarization during action potentialSodium channel protein type 11 subunit alphaHomo sapiens (human)
action potential initiationSodium channel protein type 11 subunit alphaHomo sapiens (human)
sensory perception of itchSodium channel protein type 11 subunit alphaHomo sapiens (human)
calcitonin gene-related peptide receptor signaling pathwaySodium channel protein type 11 subunit alphaHomo sapiens (human)
small intestine smooth muscle contractionSodium channel protein type 11 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 11 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 11 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 8 subunit alphaHomo sapiens (human)
nervous system developmentSodium channel protein type 8 subunit alphaHomo sapiens (human)
peripheral nervous system developmentSodium channel protein type 8 subunit alphaHomo sapiens (human)
neuronal action potentialSodium channel protein type 8 subunit alphaHomo sapiens (human)
optic nerve developmentSodium channel protein type 8 subunit alphaHomo sapiens (human)
myelinationSodium channel protein type 8 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 8 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 8 subunit alphaHomo sapiens (human)
regulation of heart rateSodium channel protein type 10 subunit alphaHomo sapiens (human)
sensory perceptionSodium channel protein type 10 subunit alphaHomo sapiens (human)
regulation of monoatomic ion transmembrane transportSodium channel protein type 10 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 10 subunit alphaHomo sapiens (human)
odontogenesis of dentin-containing toothSodium channel protein type 10 subunit alphaHomo sapiens (human)
regulation of cardiac muscle contractionSodium channel protein type 10 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane depolarizationSodium channel protein type 10 subunit alphaHomo sapiens (human)
membrane depolarization during action potentialSodium channel protein type 10 subunit alphaHomo sapiens (human)
AV node cell action potentialSodium channel protein type 10 subunit alphaHomo sapiens (human)
bundle of His cell action potentialSodium channel protein type 10 subunit alphaHomo sapiens (human)
regulation of presynaptic membrane potentialSodium channel protein type 10 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 10 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (244)

Processvia Protein(s)Taxonomy
methylumbelliferyl-acetate deacetylase activityCocaine esteraseHomo sapiens (human)
carboxylesterase activityCocaine esteraseHomo sapiens (human)
carboxylic ester hydrolase activityCocaine esteraseHomo sapiens (human)
acetylcholine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
dopamine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
secondary active organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
identical protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A9Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A9Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A9Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A9Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A9Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
outward rectifier potassium channel activityPotassium channel subfamily K member 2Homo sapiens (human)
potassium ion leak channel activityPotassium channel subfamily K member 2Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
type 8 metabotropic glutamate receptor bindingMajor prion proteinHomo sapiens (human)
amyloid-beta bindingMajor prion proteinHomo sapiens (human)
protease bindingMajor prion proteinHomo sapiens (human)
copper ion bindingMajor prion proteinHomo sapiens (human)
protein bindingMajor prion proteinHomo sapiens (human)
lamin bindingMajor prion proteinHomo sapiens (human)
glycosaminoglycan bindingMajor prion proteinHomo sapiens (human)
microtubule bindingMajor prion proteinHomo sapiens (human)
tubulin bindingMajor prion proteinHomo sapiens (human)
aspartic-type endopeptidase inhibitor activityMajor prion proteinHomo sapiens (human)
type 5 metabotropic glutamate receptor bindingMajor prion proteinHomo sapiens (human)
signaling receptor activityMajor prion proteinHomo sapiens (human)
identical protein bindingMajor prion proteinHomo sapiens (human)
ATP-dependent protein bindingMajor prion proteinHomo sapiens (human)
transmembrane transporter bindingMajor prion proteinHomo sapiens (human)
protein-containing complex bindingMajor prion proteinHomo sapiens (human)
protein-folding chaperone bindingMajor prion proteinHomo sapiens (human)
molecular adaptor activityMajor prion proteinHomo sapiens (human)
molecular function activator activityMajor prion proteinHomo sapiens (human)
molecular condensate scaffold activityMajor prion proteinHomo sapiens (human)
cupric ion bindingMajor prion proteinHomo sapiens (human)
cuprous ion bindingMajor prion proteinHomo sapiens (human)
RNA bindingHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
beta-2-microglobulin bindingHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
T cell receptor bindingHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
CD8 receptor bindingHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
TAP complex bindingHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
C-X3-C chemokine bindingIntegrin beta-1Homo sapiens (human)
magnesium ion bindingIntegrin beta-1Homo sapiens (human)
virus receptor activityIntegrin beta-1Homo sapiens (human)
fibronectin bindingIntegrin beta-1Homo sapiens (human)
protease bindingIntegrin beta-1Homo sapiens (human)
actin bindingIntegrin beta-1Homo sapiens (human)
integrin bindingIntegrin beta-1Homo sapiens (human)
calcium ion bindingIntegrin beta-1Homo sapiens (human)
protein bindingIntegrin beta-1Homo sapiens (human)
coreceptor activityIntegrin beta-1Homo sapiens (human)
protein-containing complex bindingIntegrin beta-1Homo sapiens (human)
cadherin bindingIntegrin beta-1Homo sapiens (human)
protein heterodimerization activityIntegrin beta-1Homo sapiens (human)
cell adhesion molecule bindingIntegrin beta-1Homo sapiens (human)
collagen binding involved in cell-matrix adhesionIntegrin beta-1Homo sapiens (human)
integrin binding involved in cell-matrix adhesionIntegrin beta-1Homo sapiens (human)
protein tyrosine kinase bindingIntegrin beta-1Homo sapiens (human)
protein kinase bindingIntegrin beta-1Homo sapiens (human)
laminin bindingIntegrin beta-1Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
arrestin family protein bindingMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M4Homo sapiens (human)
protein bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATP bindingATP-dependent translocase ABCB1Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
efflux transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ATP hydrolysis activityATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ubiquitin protein ligase bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylcholine floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylethanolamine flippase activityATP-dependent translocase ABCB1Homo sapiens (human)
ceramide floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
receptor-receptor interaction5-hydroxytryptamine receptor 1AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein kinase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-1B adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-2C adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
thioesterase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
heterotrimeric G-protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
norepinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2A adrenergic receptorHomo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
C-X3-C chemokine bindingIntegrin alpha-4Homo sapiens (human)
fibronectin bindingIntegrin alpha-4Homo sapiens (human)
integrin bindingIntegrin alpha-4Homo sapiens (human)
protein bindingIntegrin alpha-4Homo sapiens (human)
coreceptor activityIntegrin alpha-4Homo sapiens (human)
metal ion bindingIntegrin alpha-4Homo sapiens (human)
cell adhesion molecule bindingIntegrin alpha-4Homo sapiens (human)
protein antigen bindingIntegrin alpha-4Homo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(2) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(2) dopamine receptorHomo sapiens (human)
protein bindingD(2) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(2) dopamine receptorHomo sapiens (human)
dopamine bindingD(2) dopamine receptorHomo sapiens (human)
ionotropic glutamate receptor bindingD(2) dopamine receptorHomo sapiens (human)
identical protein bindingD(2) dopamine receptorHomo sapiens (human)
heterocyclic compound bindingD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(2) dopamine receptorHomo sapiens (human)
carbonyl reductase (NADPH) activityCarbonyl reductase [NADPH] 1Homo sapiens (human)
alcohol dehydrogenase (NADP+) activityCarbonyl reductase [NADPH] 1Homo sapiens (human)
oxidoreductase activity, acting on the CH-OH group of donors, NAD or NADP as acceptorCarbonyl reductase [NADPH] 1Homo sapiens (human)
oxidoreductase activity, acting on NAD(P)H, quinone or similar compound as acceptorCarbonyl reductase [NADPH] 1Homo sapiens (human)
15-hydroxyprostaglandin-D dehydrogenase (NADP+) activityCarbonyl reductase [NADPH] 1Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NADP+) activityCarbonyl reductase [NADPH] 1Homo sapiens (human)
prostaglandin-E2 9-reductase activityCarbonyl reductase [NADPH] 1Homo sapiens (human)
S-nitrosoglutathione reductase (NADPH) activityCarbonyl reductase [NADPH] 1Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 2B7Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 2B7Homo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2B adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2B adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2B adrenergic receptorHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2C adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingAlpha-2C adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2C adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2C adrenergic receptorHomo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
signaling receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
acetylcholine bindingMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via GsD(1A) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(1A) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(1A) dopamine receptorHomo sapiens (human)
protein bindingD(1A) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(1A) dopamine receptorHomo sapiens (human)
dopamine bindingD(1A) dopamine receptorHomo sapiens (human)
arrestin family protein bindingD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(1A) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(4) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(4) dopamine receptorHomo sapiens (human)
protein bindingD(4) dopamine receptorHomo sapiens (human)
potassium channel regulator activityD(4) dopamine receptorHomo sapiens (human)
SH3 domain bindingD(4) dopamine receptorHomo sapiens (human)
dopamine bindingD(4) dopamine receptorHomo sapiens (human)
identical protein bindingD(4) dopamine receptorHomo sapiens (human)
metal ion bindingD(4) dopamine receptorHomo sapiens (human)
epinephrine bindingD(4) dopamine receptorHomo sapiens (human)
norepinephrine bindingD(4) dopamine receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityD(4) dopamine receptorHomo sapiens (human)
neurotransmitter receptor activityD(4) dopamine receptorHomo sapiens (human)
serotonin bindingD(4) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via GsD(1B) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(1B) dopamine receptorHomo sapiens (human)
protein bindingD(1B) dopamine receptorHomo sapiens (human)
dopamine bindingD(1B) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(1B) dopamine receptorHomo sapiens (human)
adenylate cyclase activityAdenylate cyclase type 3Rattus norvegicus (Norway rat)
retinoic acid bindingUDP-glucuronosyltransferase 1A4Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A4Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A4Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A4Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A4Homo sapiens (human)
actin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
protein bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
alpha-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
metal ion bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
beta-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
histamine receptor activityHistamine H2 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H2 receptorHomo sapiens (human)
neurotransmitter receptor activityHistamine H2 receptorHomo sapiens (human)
protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
identical protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1D adrenergic receptorHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
integrin bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoatomic cation channel activitySodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
serotonin:sodium:chloride symporter activitySodium-dependent serotonin transporterHomo sapiens (human)
protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
antiporter activitySodium-dependent serotonin transporterHomo sapiens (human)
syntaxin-1 bindingSodium-dependent serotonin transporterHomo sapiens (human)
cocaine bindingSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion bindingSodium-dependent serotonin transporterHomo sapiens (human)
identical protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
nitric-oxide synthase bindingSodium-dependent serotonin transporterHomo sapiens (human)
actin filament bindingSodium-dependent serotonin transporterHomo sapiens (human)
serotonin bindingSodium-dependent serotonin transporterHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 7Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 7Homo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorHomo sapiens (human)
histamine receptor activityHistamine H1 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H1 receptorHomo sapiens (human)
neurotransmitter receptor activityHistamine H1 receptorHomo sapiens (human)
protein bindingAlpha-1B adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1B adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1B adrenergic receptorHomo sapiens (human)
G-protein alpha-subunit bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled receptor activityMu-type opioid receptorHomo sapiens (human)
beta-endorphin receptor activityMu-type opioid receptorHomo sapiens (human)
voltage-gated calcium channel activityMu-type opioid receptorHomo sapiens (human)
protein bindingMu-type opioid receptorHomo sapiens (human)
morphine receptor activityMu-type opioid receptorHomo sapiens (human)
G-protein beta-subunit bindingMu-type opioid receptorHomo sapiens (human)
neuropeptide bindingMu-type opioid receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(3) dopamine receptorHomo sapiens (human)
protein bindingD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(3) dopamine receptorHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 1 subunit alphaHomo sapiens (human)
voltage-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialSodium channel protein type 1 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 4 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 4 subunit alphaHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
G-protein alpha-subunit binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
GTPase activator activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
histamine receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
protein binding5-hydroxytryptamine receptor 6Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
monooxygenase activityCytochrome P450 2J2Homo sapiens (human)
iron ion bindingCytochrome P450 2J2Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
isomerase activityCytochrome P450 2J2Homo sapiens (human)
linoleic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
hydroperoxy icosatetraenoate isomerase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 5,6-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
heme bindingCytochrome P450 2J2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2J2Homo sapiens (human)
N-acetyltransferase activityN-acetyltransferase EisMycobacterium tuberculosis H37Rv
sodium channel activitySodium channel protein type 7 subunit alphaHomo sapiens (human)
transmembrane transporter bindingSodium channel protein type 7 subunit alphaHomo sapiens (human)
osmolarity-sensing monoatomic cation channel activitySodium channel protein type 7 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 7 subunit alphaHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
ankyrin bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
alpha-actinin bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activity involved SA node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
double-stranded DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingTAR DNA-binding protein 43Homo sapiens (human)
mRNA 3'-UTR bindingTAR DNA-binding protein 43Homo sapiens (human)
protein bindingTAR DNA-binding protein 43Homo sapiens (human)
lipid bindingTAR DNA-binding protein 43Homo sapiens (human)
identical protein bindingTAR DNA-binding protein 43Homo sapiens (human)
pre-mRNA intronic bindingTAR DNA-binding protein 43Homo sapiens (human)
molecular condensate scaffold activityTAR DNA-binding protein 43Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 4Homo sapiens (human)
protein binding5-hydroxytryptamine receptor 4Homo sapiens (human)
serotonin receptor activity5-hydroxytryptamine receptor 4Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 4Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calmodulin bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
small molecule bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
molecular function activator activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calmodulin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
alpha-actinin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 5 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
calmodulin bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
fibroblast growth factor bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
enzyme bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
protein kinase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
protein domain specific bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
ankyrin bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
ubiquitin protein ligase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
transmembrane transporter bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
nitric-oxide synthase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in Purkinje myocyte action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
scaffold protein bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
C-8 sterol isomerase activity3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
steroid delta-isomerase activity3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
protein binding3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
identical protein binding3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
cholestenol delta-isomerase activity3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 9 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 9 subunit alphaHomo sapiens (human)
adrenomedullin receptor activityCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
calcitonin gene-related peptide receptor activityCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
G protein-coupled receptor activityCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
calcitonin receptor activityCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
protein bindingCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
adrenomedullin bindingCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
protein bindingSigma intracellular receptor 2Homo sapiens (human)
oxysterol bindingSigma intracellular receptor 2Homo sapiens (human)
cholesterol bindingSigma intracellular receptor 2Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 2 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 2 subunit alphaHomo sapiens (human)
calmodulin bindingSodium channel protein type 2 subunit alphaHomo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
G protein-coupled opioid receptor activitySigma non-opioid intracellular receptor 1Homo sapiens (human)
protein bindingSigma non-opioid intracellular receptor 1Homo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 3 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 11 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 8 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 8 subunit alphaHomo sapiens (human)
ATP bindingSodium channel protein type 8 subunit alphaHomo sapiens (human)
sodium ion bindingSodium channel protein type 8 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 10 subunit alphaHomo sapiens (human)
transmembrane transporter bindingSodium channel protein type 10 subunit alphaHomo sapiens (human)
voltage-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialSodium channel protein type 10 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (162)

Processvia Protein(s)Taxonomy
endoplasmic reticulumCocaine esteraseHomo sapiens (human)
endoplasmic reticulum lumenCocaine esteraseHomo sapiens (human)
intracellular membrane-bounded organelleCocaine esteraseHomo sapiens (human)
plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
membraneSolute carrier family 22 member 1 Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
lateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
presynapseSolute carrier family 22 member 1 Homo sapiens (human)
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A9Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A9Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A9Homo sapiens (human)
photoreceptor outer segmentVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
membraneVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
perikaryonVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
endoplasmic reticulum membranePotassium channel subfamily K member 2Homo sapiens (human)
plasma membranePotassium channel subfamily K member 2Homo sapiens (human)
cell surfacePotassium channel subfamily K member 2Homo sapiens (human)
apical plasma membranePotassium channel subfamily K member 2Homo sapiens (human)
neuronal cell bodyPotassium channel subfamily K member 2Homo sapiens (human)
calyx of HeldPotassium channel subfamily K member 2Homo sapiens (human)
astrocyte projectionPotassium channel subfamily K member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium channel subfamily K member 2Homo sapiens (human)
plasma membranePotassium channel subfamily K member 2Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
dendriteMajor prion proteinHomo sapiens (human)
cytoplasmMajor prion proteinHomo sapiens (human)
endoplasmic reticulumMajor prion proteinHomo sapiens (human)
Golgi apparatusMajor prion proteinHomo sapiens (human)
cytosolMajor prion proteinHomo sapiens (human)
plasma membraneMajor prion proteinHomo sapiens (human)
external side of plasma membraneMajor prion proteinHomo sapiens (human)
cell surfaceMajor prion proteinHomo sapiens (human)
postsynaptic densityMajor prion proteinHomo sapiens (human)
inclusion bodyMajor prion proteinHomo sapiens (human)
extrinsic component of membraneMajor prion proteinHomo sapiens (human)
nuclear membraneMajor prion proteinHomo sapiens (human)
terminal boutonMajor prion proteinHomo sapiens (human)
intracellular membrane-bounded organelleMajor prion proteinHomo sapiens (human)
membrane raftMajor prion proteinHomo sapiens (human)
extracellular exosomeMajor prion proteinHomo sapiens (human)
postsynapseMajor prion proteinHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
endoplasmic reticulum membraneHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
Golgi medial cisternaHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
endoplasmic reticulum exit siteHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
MHC class I peptide loading complexHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)
focal adhesionIntegrin beta-1Homo sapiens (human)
ruffle membraneIntegrin beta-1Homo sapiens (human)
ruffleIntegrin beta-1Homo sapiens (human)
cytoplasmIntegrin beta-1Homo sapiens (human)
plasma membraneIntegrin beta-1Homo sapiens (human)
focal adhesionIntegrin beta-1Homo sapiens (human)
external side of plasma membraneIntegrin beta-1Homo sapiens (human)
cell surfaceIntegrin beta-1Homo sapiens (human)
endosome membraneIntegrin beta-1Homo sapiens (human)
intercalated discIntegrin beta-1Homo sapiens (human)
membraneIntegrin beta-1Homo sapiens (human)
lamellipodiumIntegrin beta-1Homo sapiens (human)
filopodiumIntegrin beta-1Homo sapiens (human)
neuromuscular junctionIntegrin beta-1Homo sapiens (human)
cleavage furrowIntegrin beta-1Homo sapiens (human)
ruffle membraneIntegrin beta-1Homo sapiens (human)
integrin alpha1-beta1 complexIntegrin beta-1Homo sapiens (human)
integrin alpha2-beta1 complexIntegrin beta-1Homo sapiens (human)
integrin alpha4-beta1 complexIntegrin beta-1Homo sapiens (human)
integrin alpha5-beta1 complexIntegrin beta-1Homo sapiens (human)
integrin alpha6-beta1 complexIntegrin beta-1Homo sapiens (human)
integrin alpha9-beta1 complexIntegrin beta-1Homo sapiens (human)
integrin alpha10-beta1 complexIntegrin beta-1Homo sapiens (human)
integrin alphav-beta1 complexIntegrin beta-1Homo sapiens (human)
myelin sheath abaxonal regionIntegrin beta-1Homo sapiens (human)
sarcolemmaIntegrin beta-1Homo sapiens (human)
melanosomeIntegrin beta-1Homo sapiens (human)
dendritic spineIntegrin beta-1Homo sapiens (human)
membrane raftIntegrin beta-1Homo sapiens (human)
perinuclear region of cytoplasmIntegrin beta-1Homo sapiens (human)
recycling endosomeIntegrin beta-1Homo sapiens (human)
extracellular exosomeIntegrin beta-1Homo sapiens (human)
synaptic membraneIntegrin beta-1Homo sapiens (human)
glial cell projectionIntegrin beta-1Homo sapiens (human)
Schaffer collateral - CA1 synapseIntegrin beta-1Homo sapiens (human)
cerebellar climbing fiber to Purkinje cell synapseIntegrin beta-1Homo sapiens (human)
integrin alpha3-beta1 complexIntegrin beta-1Homo sapiens (human)
integrin alpha7-beta1 complexIntegrin beta-1Homo sapiens (human)
integrin alpha8-beta1 complexIntegrin beta-1Homo sapiens (human)
integrin alpha11-beta1 complexIntegrin beta-1Homo sapiens (human)
receptor complexIntegrin beta-1Homo sapiens (human)
focal adhesionIntegrin beta-1Homo sapiens (human)
synapseIntegrin beta-1Homo sapiens (human)
integrin complexIntegrin beta-1Homo sapiens (human)
cell surfaceIntegrin beta-1Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
clathrin-coated endocytic vesicle membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
asymmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
symmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
neuronal cell bodyMuscarinic acetylcholine receptor M2Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M2Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M4Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M4Homo sapiens (human)
cytoplasmATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cell surfaceATP-dependent translocase ABCB1Homo sapiens (human)
membraneATP-dependent translocase ABCB1Homo sapiens (human)
apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
extracellular exosomeATP-dependent translocase ABCB1Homo sapiens (human)
external side of apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M5Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M5Homo sapiens (human)
cytoplasmAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
basolateral plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
neuronal cell bodyAlpha-2A adrenergic receptorHomo sapiens (human)
axon terminusAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic active zone membraneAlpha-2A adrenergic receptorHomo sapiens (human)
dopaminergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
postsynaptic density membraneAlpha-2A adrenergic receptorHomo sapiens (human)
glutamatergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
GABA-ergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
receptor complexAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M1Homo sapiens (human)
Schaffer collateral - CA1 synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic density membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M1Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
plasma membraneIntegrin alpha-4Homo sapiens (human)
focal adhesionIntegrin alpha-4Homo sapiens (human)
cell surfaceIntegrin alpha-4Homo sapiens (human)
membraneIntegrin alpha-4Homo sapiens (human)
growth coneIntegrin alpha-4Homo sapiens (human)
integrin alpha4-beta1 complexIntegrin alpha-4Homo sapiens (human)
integrin alpha4-beta7 complexIntegrin alpha-4Homo sapiens (human)
neuronal cell bodyIntegrin alpha-4Homo sapiens (human)
extracellular exosomeIntegrin alpha-4Homo sapiens (human)
integrin complexIntegrin alpha-4Homo sapiens (human)
external side of plasma membraneIntegrin alpha-4Homo sapiens (human)
Golgi membraneD(2) dopamine receptorHomo sapiens (human)
acrosomal vesicleD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
ciliumD(2) dopamine receptorHomo sapiens (human)
lateral plasma membraneD(2) dopamine receptorHomo sapiens (human)
endocytic vesicleD(2) dopamine receptorHomo sapiens (human)
axonD(2) dopamine receptorHomo sapiens (human)
dendriteD(2) dopamine receptorHomo sapiens (human)
synaptic vesicle membraneD(2) dopamine receptorHomo sapiens (human)
sperm flagellumD(2) dopamine receptorHomo sapiens (human)
dendritic spineD(2) dopamine receptorHomo sapiens (human)
perikaryonD(2) dopamine receptorHomo sapiens (human)
axon terminusD(2) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(2) dopamine receptorHomo sapiens (human)
ciliary membraneD(2) dopamine receptorHomo sapiens (human)
non-motile ciliumD(2) dopamine receptorHomo sapiens (human)
dopaminergic synapseD(2) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(2) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(2) dopamine receptorHomo sapiens (human)
presynaptic membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
cytosolCarbonyl reductase [NADPH] 1Homo sapiens (human)
extracellular exosomeCarbonyl reductase [NADPH] 1Homo sapiens (human)
extracellular vesicleCarbonyl reductase [NADPH] 1Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 2B7Homo sapiens (human)
membraneUDP-glucuronosyltransferase 2B7Homo sapiens (human)
cytosolAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cell surfaceAlpha-2B adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
cytoplasmAlpha-2C adrenergic receptorHomo sapiens (human)
endosomeAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
Golgi membraneD(2) dopamine receptorBos taurus (cattle)
endoplasmic reticulum membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
basal plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
basolateral plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M3Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M3Homo sapiens (human)
nucleusD(1A) dopamine receptorHomo sapiens (human)
endoplasmic reticulum membraneD(1A) dopamine receptorHomo sapiens (human)
plasma membraneD(1A) dopamine receptorHomo sapiens (human)
ciliumD(1A) dopamine receptorHomo sapiens (human)
presynaptic membraneD(1A) dopamine receptorHomo sapiens (human)
dendritic spineD(1A) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(1A) dopamine receptorHomo sapiens (human)
ciliary membraneD(1A) dopamine receptorHomo sapiens (human)
non-motile ciliumD(1A) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(1A) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(1A) dopamine receptorHomo sapiens (human)
plasma membraneD(1A) dopamine receptorHomo sapiens (human)
centrosomeD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(4) dopamine receptorHomo sapiens (human)
membraneD(4) dopamine receptorHomo sapiens (human)
postsynapseD(4) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(4) dopamine receptorHomo sapiens (human)
dendriteD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(1B) dopamine receptorHomo sapiens (human)
ciliumD(1B) dopamine receptorHomo sapiens (human)
brush border membraneD(1B) dopamine receptorHomo sapiens (human)
synapseD(1B) dopamine receptorHomo sapiens (human)
ciliary membraneD(1B) dopamine receptorHomo sapiens (human)
non-motile ciliumD(1B) dopamine receptorHomo sapiens (human)
plasma membraneD(1B) dopamine receptorHomo sapiens (human)
plasma membraneAdenylate cyclase type 3Rattus norvegicus (Norway rat)
endoplasmic reticulumUDP-glucuronosyltransferase 1A4Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A4Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A4Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
cell surfaceSodium-dependent noradrenaline transporter Homo sapiens (human)
membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
presynaptic membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
axonSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneHistamine H2 receptorHomo sapiens (human)
synapseHistamine H2 receptorHomo sapiens (human)
plasma membraneHistamine H2 receptorHomo sapiens (human)
dendriteHistamine H2 receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
focal adhesionSodium-dependent serotonin transporterHomo sapiens (human)
endosome membraneSodium-dependent serotonin transporterHomo sapiens (human)
endomembrane systemSodium-dependent serotonin transporterHomo sapiens (human)
presynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
membrane raftSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
postsynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
serotonergic synapseSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
neuron projectionSodium-dependent serotonin transporterHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
trans-Golgi network membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
synapse5-hydroxytryptamine receptor 7Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 7Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
nucleusAlpha-1A adrenergic receptorHomo sapiens (human)
nucleoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
caveolaAlpha-1A adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolHistamine H1 receptorHomo sapiens (human)
plasma membraneHistamine H1 receptorHomo sapiens (human)
synapseHistamine H1 receptorHomo sapiens (human)
dendriteHistamine H1 receptorHomo sapiens (human)
plasma membraneHistamine H1 receptorHomo sapiens (human)
nucleusAlpha-1B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
caveolaAlpha-1B adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
endosomeMu-type opioid receptorHomo sapiens (human)
endoplasmic reticulumMu-type opioid receptorHomo sapiens (human)
Golgi apparatusMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
axonMu-type opioid receptorHomo sapiens (human)
dendriteMu-type opioid receptorHomo sapiens (human)
perikaryonMu-type opioid receptorHomo sapiens (human)
synapseMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
neuron projectionMu-type opioid receptorHomo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
synapseD(3) dopamine receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
plasma membraneSodium channel protein type 1 subunit alphaHomo sapiens (human)
nucleoplasmSodium channel protein type 1 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 1 subunit alphaHomo sapiens (human)
intercalated discSodium channel protein type 1 subunit alphaHomo sapiens (human)
nuclear bodySodium channel protein type 1 subunit alphaHomo sapiens (human)
Z discSodium channel protein type 1 subunit alphaHomo sapiens (human)
T-tubuleSodium channel protein type 1 subunit alphaHomo sapiens (human)
node of RanvierSodium channel protein type 1 subunit alphaHomo sapiens (human)
neuronal cell bodySodium channel protein type 1 subunit alphaHomo sapiens (human)
axon initial segmentSodium channel protein type 1 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 1 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 4 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 4 subunit alphaHomo sapiens (human)
plasma membraneAdenylate cyclase type 8Rattus norvegicus (Norway rat)
nucleoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
cilium5-hydroxytryptamine receptor 6Homo sapiens (human)
synapse5-hydroxytryptamine receptor 6Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 6Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2J2Homo sapiens (human)
extracellular exosomeCytochrome P450 2J2Homo sapiens (human)
cytoplasmCytochrome P450 2J2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2J2Homo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membraneAP-2 complex subunit sigmaRattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
cytosolN-acetyltransferase EisMycobacterium tuberculosis H37Rv
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
plasma membraneSodium channel protein type 7 subunit alphaHomo sapiens (human)
glial cell projectionSodium channel protein type 7 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 7 subunit alphaHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
Z discVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
intracellular non-membrane-bounded organelleTAR DNA-binding protein 43Homo sapiens (human)
nucleusTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
perichromatin fibrilsTAR DNA-binding protein 43Homo sapiens (human)
mitochondrionTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmic stress granuleTAR DNA-binding protein 43Homo sapiens (human)
nuclear speckTAR DNA-binding protein 43Homo sapiens (human)
interchromatin granuleTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
chromatinTAR DNA-binding protein 43Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 4Homo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 4Homo sapiens (human)
endosome5-hydroxytryptamine receptor 4Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 4Homo sapiens (human)
membrane5-hydroxytryptamine receptor 4Homo sapiens (human)
synapse5-hydroxytryptamine receptor 4Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 4Homo sapiens (human)
cytoplasmVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
sarcoplasmic reticulumVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
T-tubuleVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
I bandVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
cytoplasmVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic densityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
Z discVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
dendriteVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
perikaryonVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic density membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
caveolaSodium channel protein type 5 subunit alphaHomo sapiens (human)
nucleoplasmSodium channel protein type 5 subunit alphaHomo sapiens (human)
nucleolusSodium channel protein type 5 subunit alphaHomo sapiens (human)
endoplasmic reticulumSodium channel protein type 5 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
caveolaSodium channel protein type 5 subunit alphaHomo sapiens (human)
cell surfaceSodium channel protein type 5 subunit alphaHomo sapiens (human)
intercalated discSodium channel protein type 5 subunit alphaHomo sapiens (human)
membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
lateral plasma membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
Z discSodium channel protein type 5 subunit alphaHomo sapiens (human)
T-tubuleSodium channel protein type 5 subunit alphaHomo sapiens (human)
sarcolemmaSodium channel protein type 5 subunit alphaHomo sapiens (human)
perinuclear region of cytoplasmSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 5 subunit alphaHomo sapiens (human)
nuclear envelope3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
endoplasmic reticulum3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
endoplasmic reticulum membrane3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
cytoplasmic vesicle3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
nuclear membrane3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
endoplasmic reticulum3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
plasma membraneSodium channel protein type 9 subunit alphaHomo sapiens (human)
axonSodium channel protein type 9 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 9 subunit alphaHomo sapiens (human)
plasma membraneCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
cytoplasmCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
lysosomeCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
endosomeCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
endoplasmic reticulumCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
plasma membraneCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
adrenomedullin receptor complexCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
CGRP receptor complexCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
plasma membraneCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
endoplasmic reticulumSigma intracellular receptor 2Homo sapiens (human)
lysosomeSigma intracellular receptor 2Homo sapiens (human)
endoplasmic reticulumSigma intracellular receptor 2Homo sapiens (human)
rough endoplasmic reticulumSigma intracellular receptor 2Homo sapiens (human)
plasma membraneSigma intracellular receptor 2Homo sapiens (human)
rough endoplasmic reticulum membraneSigma intracellular receptor 2Homo sapiens (human)
nuclear membraneSigma intracellular receptor 2Homo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
endoplasmic reticulum membraneDBos taurus (cattle)
dendritic spineDBos taurus (cattle)
ciliary membraneDBos taurus (cattle)
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
plasma membraneSodium channel protein type 2 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 2 subunit alphaHomo sapiens (human)
intercalated discSodium channel protein type 2 subunit alphaHomo sapiens (human)
T-tubuleSodium channel protein type 2 subunit alphaHomo sapiens (human)
axonSodium channel protein type 2 subunit alphaHomo sapiens (human)
node of RanvierSodium channel protein type 2 subunit alphaHomo sapiens (human)
paranode region of axonSodium channel protein type 2 subunit alphaHomo sapiens (human)
presynaptic membraneSodium channel protein type 2 subunit alphaHomo sapiens (human)
glutamatergic synapseSodium channel protein type 2 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 2 subunit alphaHomo sapiens (human)
membraneSodium channel protein type 2 subunit alphaHomo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
nuclear envelopeSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear inner membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear outer membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulum membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
lipid dropletSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytosolSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic densitySigma non-opioid intracellular receptor 1Homo sapiens (human)
membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
growth coneSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytoplasmic vesicleSigma non-opioid intracellular receptor 1Homo sapiens (human)
anchoring junctionSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic density membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
sarcoplasmSodium channel protein type 3 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 3 subunit alphaHomo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
plasma membraneSodium channel protein type 11 subunit alphaHomo sapiens (human)
axonSodium channel protein type 11 subunit alphaHomo sapiens (human)
neuronal cell bodySodium channel protein type 11 subunit alphaHomo sapiens (human)
axonal growth coneSodium channel protein type 11 subunit alphaHomo sapiens (human)
C-fiberSodium channel protein type 11 subunit alphaHomo sapiens (human)
extracellular exosomeSodium channel protein type 11 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 11 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 8 subunit alphaHomo sapiens (human)
membraneSodium channel protein type 8 subunit alphaHomo sapiens (human)
Z discSodium channel protein type 8 subunit alphaHomo sapiens (human)
cell junctionSodium channel protein type 8 subunit alphaHomo sapiens (human)
axonSodium channel protein type 8 subunit alphaHomo sapiens (human)
cytoplasmic vesicleSodium channel protein type 8 subunit alphaHomo sapiens (human)
node of RanvierSodium channel protein type 8 subunit alphaHomo sapiens (human)
axon initial segmentSodium channel protein type 8 subunit alphaHomo sapiens (human)
presynaptic active zone membraneSodium channel protein type 8 subunit alphaHomo sapiens (human)
parallel fiber to Purkinje cell synapseSodium channel protein type 8 subunit alphaHomo sapiens (human)
postsynaptic density membraneSodium channel protein type 8 subunit alphaHomo sapiens (human)
glutamatergic synapseSodium channel protein type 8 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 8 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 10 subunit alphaHomo sapiens (human)
axonSodium channel protein type 10 subunit alphaHomo sapiens (human)
presynaptic membraneSodium channel protein type 10 subunit alphaHomo sapiens (human)
extracellular exosomeSodium channel protein type 10 subunit alphaHomo sapiens (human)
glutamatergic synapseSodium channel protein type 10 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 10 subunit alphaHomo sapiens (human)
clathrin complexSodium channel protein type 10 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (2272)

Assay IDTitleYearJournalArticle
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1645848NCATS Kinetic Aqueous Solubility Profiling2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1508591NCATS Rat Liver Microsome Stability Profiling2020Scientific reports, 11-26, Volume: 10, Issue:1
Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
AID1508612NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Highly predictive and interpretable models for PAMPA permeability.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID414524Hypothermic activity in Sprague-Dawley rat assessed as decrease in core body temperature at 5 mg/kg, ip at time of maximal body temperature decrease2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Comparison of N-terminal modifications on neurotensin(8-13) analogues correlates peptide stability but not binding affinity with in vivo efficacy.
AID1213026Drug metabolism assessed as human liver microsomes assessed as O-glucuronide measured per mg of protein at 25 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID63637Ratio of Ki(uM) of D2 receptor to the Ki(uM) of 5-hydroxytryptamine 2 receptor1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia.
AID203982Displacement of [3H]DTG from sigma opioid receptor of homogenized guinea pig whole brain1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
Radiosynthesis of sigma receptor ligands for positron emission tomography: 11C- and 18F-labeled guanidines.
AID176235Inhibitory activity in apomorphine antagonism test at a dose of 20 mg/kg, sc1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study.
AID232561Ratio of ED50 for inhibition of catalepsy induction to stereotypy induction1981Journal of medicinal chemistry, Oct, Volume: 24, Issue:10
Synthesis and neuroleptic activity of benzamides. Cis-N-(1-benzyl-2-methylpyrrolidin-3-yl)-5-chloro-2-methoxy-4-(methylamino)benzamide and related compounds.
AID239296Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening.
AID177633Compound was evaluated in vivo for antagonist activity against apomorphine induced behavioral syndrome such as Hyperactivity in rat after intraperitoneal administration; activity value ranges from 0.27-0.351985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Potential neuroleptic agents. 3. Chemistry and antidopaminergic properties of substituted 6-methoxysalicylamides.
AID1185976Antipsychotic activity in ip dosed Swiss-Webster mouse assessed as inhibition of APO-induced climbing behavior after 30 mins2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Further evaluation of the tropane analogs of haloperidol.
AID1409514Therapeutic index, ratio of ED50 for catalepsy in Kunming mouse to ED50 for MK-801-induced hyperactivity in Kunming mouse2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID298492Displacement of [3H]prazosin from adrenergic alpha1 receptor in rat cerebral cortex2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID5035Binding affinity against 5-hydroxytryptamine 2 receptor from rat cortical synaptosomal membrane using radioligand [3H]ketanserin.1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bridged gamma-carbolines and derivatives possessing selective and combined affinity for 5-HT2 and D2 receptors.
AID62338Evaluated for binding towards Dopamine receptor D2 using [3H]-spiperone as radioligand, in cloned mammalian receptors expressed in CHO-K1 cells1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID232553Ratio of ED50 for antagonism of apomorphine induced stereotypy to ED50 for antagonism of apomorphine induced climbing1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents.
AID410137Inhibition of dopamine D2 receptor-mediated apomorphine-induced cage climbing behavior in Swiss albino mouse at 1 mg/kg, ip2008Bioorganic & medicinal chemistry letters, 12-01, Volume: 18, Issue:23
Synthesis and preliminary pharmacological evaluation of N-2-(4-(4-(2-substitutedthiazol-4-yl) piperazin-1-yl)-2-oxoethyl)acetamides as novel atypical antipsychotic agents.
AID4334Affinity against the 5-hydroxytryptamine receptor 1A using [3H]WB-4101.1995Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21
N-aryl-N'-benzylpiperazines as potential antipsychotic agents.
AID410535Toxicity in sc dosed NMRI mouse assessed as cataleptogenic potential administered 30 mins prior to testing measured every 15 mins for 60 mins by horizontal bar test2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
AID28236Unbound fraction (tissues)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1336363Displacement of [3H]DTG from sigma receptor in human Jurkat cells measured after 120 mins by scintillation counting method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
AID1853686Cytotoxicity against human HEK293 cells assessed as reduction in cell viability at 200 uM incubated for 24 hrs by resazurin assay2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from
AID1213088Drug metabolism assessed as human liver microsomes assessed as velocity of N-glucuronidation at 100 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID63700Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test2003Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21
The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+.
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
AID1318840Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes after 120 mins by scintillation counting method2016European journal of medicinal chemistry, Oct-04, Volume: 121Computer-assisted design, synthesis, binding and cytotoxicity assessments of new 1-(4-(aryl(methyl)amino)butyl)-heterocyclic sigma 1 ligands.
AID298485Displacement of [3H]mesulergine from 5HT2C receptor expressed in CHO cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID139070Antagonism of apomorphine in reserpinized mice when a dose of 0.3 micro mol/kg is administered intraperitoneally1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 1. Synthesis and structure-activity relationships of 2,3,3a,4,5,9b-hexahydro-1H-benz[e]indole derivatives.
AID64296Inhibition of [3H]methylspiperone binding to rat striatal membrane Dopamine receptor D21998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID1169871Antipsychotic-like activity in sc dosed NMRI mouse assessed as reduction in PCP-induced locomotor activity dosed 15 to 30 mins before administration of methamphetamine measured for 60 mins2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.
AID255170Ratio of inhibitory concentration against rat opioid receptor sigma 2 and guinea pig opioid sigma 12005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective sigma1 ligands. Part 1.
AID61669Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.2000Journal of medicinal chemistry, Feb-24, Volume: 43, Issue:4
Binding and preliminary evaluation of 5-hydroxy- and 10-hydroxy-2,3, 12,12a-tetrahydro-1H-[1]benzoxepino[2,3,4-ij]isoquinolines as dopamine receptor ligands.
AID63234Selectivity is the ratio of binding affinities for human Dopamine receptor D2 to that of Dopamine receptor D32002Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
Design and synthesis of a piperazinylalkylisoxazole library for subtype selective dopamine receptor ligands.
AID1686281Cytotoxicity in HREC assessed as reduction in cell viability incubated for 48 hrs by MTT assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1060809Displacement of [3H]-(+)-pentazocine from guinea pig brain sigma1 receptor after 150 mins by scintillation counting analysis2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
From NMDA receptor antagonists to discovery of selective σ₂ receptor ligands.
AID705726Displacement of [3H](+)-pentazocine from Sigma1 receptor in rat brain homogenate2012Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
New positron emission tomography (PET) radioligand for imaging σ-1 receptors in living subjects.
AID1335651Therapeutic index, ratio of ED50 for induction of catalepsy in po dosed Chinese Kun Ming mouse to ED50 for inhibition of apomorphine-induced climbing behavior in po dosed Chinese Kun Ming mouse2016European journal of medicinal chemistry, Nov-29, Volume: 124Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.
AID3460Affinity towards 5-hydroxytryptamine 1A receptor in membranes from bovine hippocampus using [3H]OH-DPAT1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.
AID576612Inhibition of human ERG2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model.
AID301906Induction of catalepsy in Mill Hill hooded rat at 1 mg/kg after 30-180 min2007Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
Two new phenylpiperazines with atypical antipsychotic potential.
AID5483Binding affinity towards 5-hydroxytryptamine 2A receptor from rat frontal cortex using [3H]ketanserin as radioligand1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID239052Inhibition of [3H]-spiperone binding to human Dopamine receptor D22005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
AID1853687Cytotoxicity against human A549 cells assessed as reduction in cell viability at 50 to 200 uM incubated for 24 hrs by resazurin assay2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from
AID298489Displacement of [3H]paraxetine from human 5HT transporter expressed in HEK293 cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID194380Effect of compound (0.2 mg/kg ip) on the concentration of HVA in rat mesolimbic region1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID3760In vitro binding affinity was measured on serotonergic 5-hydroxytryptamine 1A receptor by displacement of [3H]- tetralin1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents.
AID203697Binding affinity towards sigma 1 receptor was determined in guinea pig brain membrane using [3H](+)-pentazocine as radioligand1994Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2
A new approach to the design of sigma-2-selective ligands: synthesis and evaluation of N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1- pyrrolidinyl)ethylamine-related polyamines at sigma-1 and sigma-2 receptor subtypes.
AID298032Acid dissociation constant, pKa of the compound2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery.
AID342788Blockade of apomorphine-induced climbing stereotypy in Swiss Webster mouse after 30 mins2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1511009Selectivity ratio of Ki for sigma1 receptor in guinea pig brain membranes to Ki for sigma2 receptor in rat liver membranes2019European journal of medicinal chemistry, Oct-15, Volume: 180Discovery of new potent dual sigma receptor/GluN2b ligands with antioxidant property as neuroprotective agents.
AID177491Effect on half-maximal decrease of DOPA formation in rat limbic regions; In active (no significant effect at 1.4 pmol/kg ip)1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
C1- and C3-methyl-substituted derivatives of 7-hydroxy-2-(di-n-propylamino)tetralin: activities at central dopamine receptors.
AID224647Area under curve(AUC) value of Dopamine level after second treatment(7.4 umol/kg) in dialysates collected from rat striatum2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID4061Compound was evaluated for its binding affinity with 5-hydroxytryptamine 1A receptor using membranes prepared from rat cerebral cortex1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Orally active benzamide antipsychotic agents with affinity for dopamine D2, serotonin 5-HT1A, and adrenergic alpha1 receptors.
AID1210015Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID176734Dose (administered orally) inhibiting apomorphine-induced stereotypy in rats1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID280704Increase in apoptosis in albino Wistar rat primary 14 DIV astroglial cells at 25 uM after 24 hrs by TUNEL assay relative to control2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Novel sigma receptor ligands: synthesis and biological profile.
AID243274Binding affinity towards dopamine receptor D3 was determined2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
The role of QSAR in dopamine interactions.
AID203686Compound tested for binding affinity towards sigma 1 receptor in quinea pig brain membranes using [3H](+)-pentazocine as the radioligand.1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Synthesis and quantitative structure-activity relationships of N-(1-benzylpiperidin-4-yl)phenylacetamides and related analogues as potent and selective sigma1 receptor ligands.
AID1221963Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1256682Neurotoxicity in Chinese Kun Ming mouse assessed as locomotor activity by measuring total distance traveled at 0.1 mg/kg, po administered 1 hr before test measured for 10 mins (Rvb = 13415.6 +/- 9555.8 millimeter)2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
AID239200Inhibitory constant against sigma receptor type 2 using 3 nM [3H]ditolylguanidine2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands.
AID629462Displacement of [3H]spiperone from human DRD2 short receptor expressed in chinese hamster CHO cells by radioligand binding assay2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Development of a bivalent dopamine D₂ receptor agonist.
AID1901323Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane by competitive radioligand receptor binding assay
AID280721Activity at sigma 2 receptor in rat astroglial cells2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Novel sigma receptor ligands: synthesis and biological profile.
AID128984Anticonvulsant activity against electroshock-induced convulsions, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID1664665Displacement of [3H]-N-Methylspiperone from human dopamine D2 receptor expressed in stable fibroblast cells incubated for 90 mins by microbeta counting method2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Structural manipulation of aporphines via C10 nitrogenation leads to the identification of new 5-HT
AID578855Displacement of [3H]-(+)-pentazocine from Sigma1-receptor in guinea pig brain membrane2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Effect of structural modification in the amine portion of substituted aminobutyl-benzamides as ligands for binding σ1 and σ2 receptors.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1744232Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes incubated for 1 hr by liquid scintillation counting method2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management.
AID298490Displacement of [3H]pirenzepine from human M1 receptor expressed in CHO cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID1144199Acute toxicity in ip dosed Swiss-Webster mouse assessed as ataxia administered as single dose after 72 hrs1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Synthesis and biological actions of 2-substituted quinolizidines.
AID63811Displacement of [3H]NPA from rat brain Dopamine receptor D21996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID1462754Displacement of [3H]-(+)-MK-801 from PCP binding site of NMDA receptor in pig brain cortex at 1 uM2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Replacement of benzylic hydroxy group by vinyl or hydroxymethyl moiety at the 3-benzazepine scaffold retaining GluN2B affinity.
AID397743Inhibition of human ERG channel2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Side chain flexibilities in the human ether-a-go-go related gene potassium channel (hERG) together with matched-pair binding studies suggest a new binding mode for channel blockers.
AID61675Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID393359Displacement of [3H](+)-pentazocine from sigma 1 receptor in rat liver membrane2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Substituted benzo[d]oxazol-2(3H)-one derivatives with preference for the sigma1 binding site.
AID1213033Drug metabolism assessed as recombinant human UGT1A9 assessed as O-glucuronidation at 25 to 200 uM incubated for 60 mins by LC-MS/MS analysis in presence of 10 uM hecogenin relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID130873Inhibition against apomorphine-induced climbing, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID178710Compound was tested for the antagonistic activity against amphetamine-induced stereotypy in rats; (5 mg/kg administered ip 5 hr after the test compound)1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Neuroleptic activity of chiral trans-hexahydro-gamma-carbolines.
AID23095Ratio of pKi of 5-HT2A receptor to that of D2 receptor2000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.
AID36122The compound was tested against Alpha-1 adrenergic receptor for percent displacement of radioligand at 10e-6 M1999Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.
AID1197504Selectivity ratio of Ki for sigma2 receptor in human Jurkat cells to Ki for sigma1 receptor human Jurkat cells2015European journal of medicinal chemistry, Mar-06, Volume: 92Synthesis and pharmacological evaluation of benzannulated derivatives as potent and selective sigma-1 protein ligands.
AID1596351Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
AID1318841Displacement of [3H]-DTG from sigma2 receptor in rat liver membranes after 120 mins by scintillation counting method2016European journal of medicinal chemistry, Oct-04, Volume: 121Computer-assisted design, synthesis, binding and cytotoxicity assessments of new 1-(4-(aryl(methyl)amino)butyl)-heterocyclic sigma 1 ligands.
AID1650560Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membranes incubated for 120 mins in the presence of sigma1 receptor ligand (+)-pentazocine by scintillation counting method2020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Thiophene bioisosteres of GluN2B selective NMDA receptor antagonists: Synthesis and pharmacological evaluation of [7]annuleno[b]thiophen-6-amines.
AID1335648Inhibition of MK-801 induced hyperactivity in po dosed Chinese Kun Ming mouse administered for 60 mins followed by MK-801 challenge and measured for 90 mins2016European journal of medicinal chemistry, Nov-29, Volume: 124Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.
AID266791Reduction of icv dosed 1 ug 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]-pyridine-induced penile erection in Sprague-Dawley rat at 1 mg/kg, ip2006Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13
2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist.
AID185004Compound is tested for concomitant ability to antagonize the locomotor activity induced by Di-Pr-5,6-ADTN1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.
AID1461563Displacement of [3H]spiperone from human D2short receptor L2.64C mutant expressed in HEK293T cell membranes by radioligand binding assay2017Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19
Potent haloperidol derivatives covalently binding to the dopamine D2 receptor.
AID1215944Intrinsic clearance in human intestinal S9 fraction at 50 to 1000 nM after 60 mins by HPLC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Significance of reductive metabolism in human intestine and quantitative prediction of intestinal first-pass metabolism by cytosolic reductive enzymes.
AID1280525Cataleptic activity in ip dosed C57BL/6J mouse measured after 60 mins2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.
AID176663Suppression of conditioned avoidance behavior in rats following p.o. administration.1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2.
AID410334Displacement of [3H]8OH-DPAT from 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus by scintillation spectrometry2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
AID5233Binding affinity for 5-hydroxytryptamine 2 receptor from striata of male Wistar rats by displacement of [3H]ketanserin2000Bioorganic & medicinal chemistry letters, Mar-06, Volume: 10, Issue:5
N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]cyclohexanecarboxamides as selective 5-HT1A receptor agonists.
AID1782419Displacement of [3H]-N-methylspiperone from D2 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
2-Phenylcyclopropylmethylamine Derivatives as Dopamine D
AID392049Cardiotoxicity in Dunkin-Hartley guinea pig assessed as maximal QTc prolongation time at 10 mg/kg, iv administered as 3 fold cumulative doses measured every 10 seconds at end of every 20 mins follow up period of individual dose by ECG2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Identification of "toxicophoric" features for predicting drug-induced QT interval prolongation.
AID65753Binding affinity towards baculovirus expressed rat dopamine D3 receptors1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects.
AID1204344Displacement of [3H]N-methylspiperone from human recombinant dopamine D2 receptor expressed in CHOK1 cells assessed as total radioligand binding at 1.66 x 10'-7 M incubated for 60 mins by microbeta plate reader based method2015European journal of medicinal chemistry, Jun-05, Volume: 97Structure-activity relationships and molecular studies of novel arylpiperazinylalkyl purine-2,4-diones and purine-2,4,8-triones with antidepressant and anxiolytic-like activity.
AID1215953Drug metabolism in human intestinal cytosol at 200 nM after 60 mins in presence of ondansetron2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Significance of reductive metabolism in human intestine and quantitative prediction of intestinal first-pass metabolism by cytosolic reductive enzymes.
AID1782429Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
2-Phenylcyclopropylmethylamine Derivatives as Dopamine D
AID711571Half life in human liver microsomes2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID178706Compound was tested for the antagonistic activity against amphetamine-induced stereotypy in rats; (5 mg/kg administered ip 24 hr after the test compound)1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Neuroleptic activity of chiral trans-hexahydro-gamma-carbolines.
AID1129880Displacement of [3H]-DTG from sigma-2 receptor in rat liver homogenates after 120 mins by scintillation counting analysis in presence of (+)-pentazocine2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
Synthesis, pharmacological evaluation, and σ1 receptor interaction analysis of hydroxyethyl substituted piperazines.
AID540226Clearance in monkey after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID64299In vitro binding affinity for Dopamine D2 receptor of rat using [3H]YM-09151 as radioligand2002Journal of medicinal chemistry, Oct-10, Volume: 45, Issue:21
Synthesis and pharmacological evaluation of 1-[(1,2-diphenyl-1H-4-imidazolyl)methyl]-4-phenylpiperazines with clozapine-like mixed activities at dopamine D(2), serotonin, and GABA(A) receptors.
AID591693Induction of apoptosis in human HEK293 cells expressing sigma receptor assessed as late apoptotic cells using annexin V/propidium iodide staining at 5 uM after 24 hrs by flow cytometry (Rvb = 99.76%)2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Structure-activity study to develop cationic lipid-conjugated haloperidol derivatives as a new class of anticancer therapeutics.
AID65884Displacement of [3H]-Spiperone from Dopamine receptor D2 in rat striatum1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2.
AID1813189Ratio of Ki for displacement of [3H]-(+)-pentazocine from sigma-1 receptor to Ki for displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes in presence of phenytoin2021European journal of medicinal chemistry, Dec-15, Volume: 226Optimization of bifunctional piperidinamide derivatives as σ
AID1309493Lipophilicity, log P of the compound2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores.
AID1213065Drug metabolism assessed as human liver microsomes assessed as O-glucuronidation measured per mg of protein at 10 to 400 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID113114Antagonism of apomorphine-induced climbing in mice when administered intraperitoneally 60 min prior to apomorphine (1 mg/kg)1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
AID1213034Drug metabolism assessed as recombinant human UGT2B7 assessed as O-glucuronidation at 25 to 200 uM incubated for 60 mins by LC-MS/MS analysis in presence of 10 uM hecogenin2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1318843Selectivity ratio of Ki for sigma2 receptor in rat liver membranes to Ki for sigma1 receptor in guinea pig brain cortex membranes2016European journal of medicinal chemistry, Oct-04, Volume: 121Computer-assisted design, synthesis, binding and cytotoxicity assessments of new 1-(4-(aryl(methyl)amino)butyl)-heterocyclic sigma 1 ligands.
AID203998Inhibition of [3H]DTG binding to Sigma opioid receptor1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
Binding of substituted and conformationally restricted derivatives of N-(3-phenyl-n-propyl)-1-phenyl-2-aminopropane at sigma-receptors.
AID131875Effective dose required for inhibition of apomorphine(sc, 2.5 mg/kg ) induced stereotypy in mice on ip administration2001Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10
Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic?
AID1724119Induction of catalepsy in po dosed mouse by vertical grid and elevated bar test2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID63226Ability to displace [3H]spiperone from human dopamine receptor D2 stably expressed in CHO cells.1997Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15
4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor.
AID729709Antagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Asymmetric total synthesis and identification of tetrahydroprotoberberine derivatives as new antipsychotic agents possessing a dopamine D(1), D(2) and serotonin 5-HT(1A) multi-action profile.
AID65128Displacement of [3H]raclopride from Dopamine receptor D31996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Novel (R)-2-amino-5-fluorotetralins: dopaminergic antagonists and inverse agonists.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1215951Drug metabolism in human intestinal cytosol at 200 nM after 60 mins in presence of flufenamic acid2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Significance of reductive metabolism in human intestine and quantitative prediction of intestinal first-pass metabolism by cytosolic reductive enzymes.
AID675970Displacement of [3H]-(+)pentazocine from guinea pig brain sigma 1-type opioid receptor after 120 mins by scintillation counting analysis2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Thiophene bioisosteres of spirocyclic σ receptor ligands: relationships between substitution pattern and σ receptor affinity.
AID298486Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID29139Calculated dissociation constant (pKa, calculated with ACD/pKa)2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID3992Binding affinity measured at the 5-hydroxytryptamine 1A receptor by the inhibition of [3H]8-OH-DPAT binding to rat cortex using unlabeled buspirone for nonspecific binding.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID458634Selectivity ratio of Ki for human dopamine D2 receptor at low affinity state to Ki for human dopamine D2 receptor at high affinity state2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
AID5558Compound was tested for the Binding affinity against rat frontal cortex 5-hydroxytryptamine 2A receptor by Radio ligand [3H]ketanserin binding assay.1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.
AID596434Biodistribution in haloperidol-pretreated ICR mouse heart at 1 mg/kg, iv pretreated 5 mins before haloperidol challenge measured after 60 mins postinjection (Rvb = 1.72 +/- 0.31 %ID/g)2011Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9
Synthesis and biological evaluation of novel 4-benzylpiperazine ligands for sigma-1 receptor imaging.
AID65814Binding affinity towards Dopamine type 2 receptor was determined by displacement assays using [3H]-YM 09151 as the competitive ligand2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 2: asymmetric synthesis and biological evaluation.
AID711583Apparent permeability across human Caco2 cells2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID128987Anticonvulsant activity against tryptamine-induced convulsions, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID186042Locomotor activity in male Wistar rats after a dose of 0.003 uM/kg, 30 min before 1 mg/kg of apomorphine administration1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.
AID605698Displacement of [3H]spiperone from human D2short receptor expressed in CHO cells2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Bivalent dopamine D2 receptor ligands: synthesis and binding properties.
AID229002Compound was measured for the inhibition of [3H]ketanserin binding to rat frontal cortex membrane (5-HT2A receptor)1998Bioorganic & medicinal chemistry letters, Dec-15, Volume: 8, Issue:24
Butyrophenone analogues in the carbazole series: synthesis and determination of affinities at D2 and 5-HT2A receptors.
AID1309492Displacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting method2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores.
AID169806Compound was assessed for its ability to block a conditioned avoidance response; Dose administered perorally is 1.25 mg/kg; 51-75%block1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
4-Piperazinyl-10H-thieno[2,3-b][1,5]benzodiazepines as potential neuroleptics.
AID62581Dopamine receptor antagonist activity in the superfused rabbit ear artery preparation1981Journal of medicinal chemistry, Jun, Volume: 24, Issue:6
Synthesis and evaluation of novel alkylpiperazines as potential dopamine antagonists.
AID224649Area under curve(AUC) value of DOPAC level after total treatment in dialysates collected from rat striatum.2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID65950Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID701945Displacement of [3H]di-o-tolylguanidine from Sigma 2 receptor in rat liver membrane after 120 mins by scintillation counting2012Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
Pd-catalyzed direct C-H bond functionalization of spirocyclic σ1 ligands: generation of a pharmacophore model and analysis of the reverse binding mode by docking into a 3D homology model of the σ1 receptor.
AID1393522Reversal of PCP-induced cognitive impairment in Sprague-Dawley rat assessed as reduction in time spent exploring novel object over familiar object at 0.05 mg/kg, ip pretreated for 60 mins followed by PCP addition by novel object recognition assay
AID781329pKa (acid-base dissociation constant) as determined by other workers2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID203851Relative binding to sigma-2 and sigma-1 type receptors, ratio of Ki1994Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2
A new approach to the design of sigma-2-selective ligands: synthesis and evaluation of N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1- pyrrolidinyl)ethylamine-related polyamines at sigma-1 and sigma-2 receptor subtypes.
AID1185966Displacement of [3H]SCH23390 from human dopamine D5 receptor by liquid scintillation counting2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Further evaluation of the tropane analogs of haloperidol.
AID1213058Drug metabolism assessed as human liver microsomes assessed as retention time at 100 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1185973Displacement of [3H]GBR12935 from human dopamine transporter by liquid scintillation counting2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Further evaluation of the tropane analogs of haloperidol.
AID177902Inhibition of firing rates of dopaminergic neurons in the substantia nigra pars compacta by intravenous injection in rats1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 1. Synthesis and structure-activity relationships of 2,3,3a,4,5,9b-hexahydro-1H-benz[e]indole derivatives.
AID64985Binding affinity measured at the Dopamine receptor D3 by the inhibition of [3H]YM-09151-2 binding to human recombinant CCL 1.3 cells using unlabeled 7-OH-DPAT for nonspecific binding; ND = 'Not determined'1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID598812Displacement of [3H]DTG from sigma 2 receptor in rat brain homogenate2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Molecular hybridization of 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecane-3-ol with sigma (σ) receptor ligands modulates off-target activity and subtype selectivity.
AID1060807Selectivity ratio of Ki for guinea pig brain sigma1 receptor to Ki for guinea pig brain sigma2 receptor2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
From NMDA receptor antagonists to discovery of selective σ₂ receptor ligands.
AID178321Compound was tested for anti-dopamine activity in vivo by its ability to inhibit apomorphine induced stereotypy in rat1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Potential neuroleptic agents. 4. Chemistry, behavioral pharmacology, and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides.
AID308688Ratio of pKi for human 5HT2A receptor to pKi for human D2 receptor2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics.
AID36912Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta2003Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2
New arylpiperazine derivatives with high affinity for alpha1A, D2 and 5-HT2A receptors.
AID1546907Displacement of [3H]spiperone from human D2S receptor expressed in CHO-K1 cells by radioligand competitive binding analysis
AID161281Inhibition of human Potassium channel HERG expressed in mammalian cells2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
AID596438Biodistribution in haloperidol-pretreated ICR mouse kidney at 1 mg/kg, iv pretreated 5 mins before haloperidol challenge measured after 60 mins postinjection (Rvb = 8.18 +/- 0.13 %ID/g)2011Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9
Synthesis and biological evaluation of novel 4-benzylpiperazine ligands for sigma-1 receptor imaging.
AID65559Evaluated for binding towards Dopamine receptor D2 using [3H]N-0437 as radioligand from rat striatal membrane1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1462132Displacement of [3H]-DTG from sigma2 receptor in rat liver membranes after 120 mins by liquid scintillation counting2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Chiral-pool synthesis of 1,2,4-trisubstituted 1,4-diazepanes as novel σ
AID62590Ability to displace the Dopamine receptor agonist DiPr-5,6-ADTN from rat striatal binding sites in vivo at a dose of 2.7 uM/kg by subcutaneous administration1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID1314060Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 2 hrs by scintillation counting2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Oxa-Pictet-Spengler reaction as key step in the synthesis of novel σ receptor ligands with 2-benzopyran structure.
AID138929Antagonism of apomorphine for 10-20 minutes in reserpinized mice when a dose of 2.7 micro mol/kg is administered intraperitoneally1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives.
AID112952Compound was tested for inhibition of norepinephrine lethality in mouse when administered perorally1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.
AID65562Inhibition of [3H]spiperone binding to rat striatal membrane Dopamine receptor D21990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds.
AID1478368Selectivity index, ratio of Ki for sigma2 receptor in guinea pig brain membrane to Ki for sigma2 receptor in guinea pig brain membrane2018Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
(+)-Methyl (1R,2S)-2-{[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]methyl}-1-phenylcyclopropanecarboxylate [(+)-MR200] Derivatives as Potent and Selective Sigma Receptor Ligands: Stereochemistry and Pharmacological Properties.
AID235773Therapeutic ratio by Peroral dose of administration (quotient ED50 catalepsy/ED50 climbing)1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID63237Inhibition of [35 S] GTP gamma S binding to cell membranes expressing Dopamine receptor D21996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Novel (R)-2-amino-5-fluorotetralins: dopaminergic antagonists and inverse agonists.
AID1123526Neuroleptic activity in Wistar HLA rat assessed as inhibition of methamphetamine-induced stereotyped behavior at 0.1 mg/kg, ip administered 20 mins before methamphetamine challenge measured every 30 mins for 3 hrs followed by every 1 hr for further 3 hrs1979Journal of medicinal chemistry, Jun, Volume: 22, Issue:6
Synthesis of 2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole derivatives and their central nervous system activities.
AID342784Binding affinity to human cloned 5HT2A receptor2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID517708Displacement of [3H]Spiperone from human dopamine D2 short receptor expressed in CHO cells2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Bioisosteric replacement leading to biologically active [2.2]paracyclophanes with altered binding profiles for aminergic G-protein-coupled receptors.
AID1210074Inhibition of CYP1A2 in human liver microsomes using phenacetin substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID395325Lipophilicity, log P by microemulsion electrokinetic chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID129968Compound was evaluated for inhibition of apomorphine-induced climbing in mouse after peroral administration.1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia.
AID1330100Displacement of [3H]DAMGO from human MOR expressed in HEK cells after 90 mins by microbeta scintillation counting method2016Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
AID729710Agonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Asymmetric total synthesis and identification of tetrahydroprotoberberine derivatives as new antipsychotic agents possessing a dopamine D(1), D(2) and serotonin 5-HT(1A) multi-action profile.
AID176324In vivo blocking of apomorphine induced stereotypies following 1 mg/kg i.p. in rats after 60 min.1982Journal of medicinal chemistry, Nov, Volume: 25, Issue:11
Potential neuroleptic agents. 2,6-Dialkoxybenzamide derivatives with potent dopamine receptor blocking activities.
AID592132Induction of apoptosis in against african green monkey COS1 cells expressing sigma receptor assessed as late apoptotic cells using annexin V/propidium iodide staining at 5 uM after 24 hrs by flow cytometry (Rvb = 0.04%)2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Structure-activity study to develop cationic lipid-conjugated haloperidol derivatives as a new class of anticancer therapeutics.
AID1123528Neuroleptic activity in Wistar HLA rat assessed as inhibition of methamphetamine-induced stereotyped behavior at 0.5 mg/kg, ip administered 20 mins before methamphetamine challenge measured every 30 mins for 3 hrs followed by every 1 hr for further 3 hrs1979Journal of medicinal chemistry, Jun, Volume: 22, Issue:6
Synthesis of 2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole derivatives and their central nervous system activities.
AID1409611AUC (cytotoxicity %) of compound against Vero E6 cells by MTT assay.2020Nature, 07, Volume: 583, Issue:7816
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID138782Antagonism of apomorphine for 0-10 minutes in reserpinized mice when a dose of 0.3 micro mol/kg is administered intraperitoneally1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives.
AID1616727Agonist activity at SNAP-tagged human D2LR expressed in Flp-In CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation at 10 uM measured after 10 mins in presence of coelenterazine by BRET assay relative to control
AID303620Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Synthesis of bicyclic sigma receptor ligands with cytotoxic activity.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID387868Selectivity ratio of Ki for human dopamine D2S receptor to Ki for human dopamine D4.2 receptor2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Synthesis of 1-arylpiperazyl-2-phenylcyclopropanes designed as antidopaminergic agents: cyclopropane-based conformationally restricted analogs of haloperidol.
AID1308619Displacement of [3H](+)-Pentazocine from sigma 1 receptor in human RPMI8226 cell membranes2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity?
AID1636357Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID593483Displacement of [3H]-Spiperone from human dopamine D2L receptor expressed in CHO cells at 4 times IC50 for 5 mins measured after 60 mins by topcount scintillation counting2011Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
Molecular properties affecting fast dissociation from the D2 receptor.
AID418675Cytotoxicity against human RT4 cells after 96 hrs by crystal violet staining2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Dancing of the second aromatic residue around the 6,8-diazabicyclo[3.2.2]nonane framework: influence on sigma receptor affinity and cytotoxicity.
AID37376In vitro binding affinity towards alpha-2 adrenergic receptor in rat frontal cortex homogenate using of [3H]clonidine as radioligand2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.
AID61517Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID1532592Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in human Jurkat cell membranes after 2 hrs by liquid scintillation counting method2019European journal of medicinal chemistry, Jan-15, Volume: 162Novel multitarget-directed ligands targeting acetylcholinesterase and σ
AID65271Compound was evaluated for in vitro binding affinity towards Dopamine receptor D2 in rat striatum using [3H]- spiperone as radioligand1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia.
AID65610Binding affinity towards Dopamine receptor D3 of rat using [3H]spiroperidol as radioligand2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands.
AID131362Effect on Ataxia in mouse following i.p. administration.1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
N6-(2,2-diphenylethyl)adenosine, a novel adenosine receptor agonist with antipsychotic-like activity.
AID177946Antagonistic activity against amphetamine-induced stereotypy, after 1 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID194372Effect of compound (0.2 mg/kg ip) on the concentration of DA in rat mesolimbic region1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID177488Effect on Sidman conditioned avoidance in rat.1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
N6-(2,2-diphenylethyl)adenosine, a novel adenosine receptor agonist with antipsychotic-like activity.
AID598814Displacement of [3H]SCH233930 from human D5 receptor expressed in HEK cells2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Molecular hybridization of 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecane-3-ol with sigma (σ) receptor ligands modulates off-target activity and subtype selectivity.
AID176780In vivo DOPA accumulation in reserpine pretreated rat striatum system after 1.4 umol/kg ip; I denotes inactive1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID64426In vitro binding affinity was measured by displacement of [3H]- raclopride from D2 receptor isolated from the striata of male Dawley rats1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents.
AID218788Binding affinity towards dopamine receptor D2 was determined by displacement of [3H]spiroperidol from bovine nucleus caudate membranes.1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Synthesis and neuroleptic activity of a series of 1-[1-(benzo-1,4-dioxan-2-ylmethyl)-4-piperidinyl]benzim idazolone derivatives.
AID177492Effect on half-maximal decrease of DOPA formation in rat striatal regions1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
C1- and C3-methyl-substituted derivatives of 7-hydroxy-2-(di-n-propylamino)tetralin: activities at central dopamine receptors.
AID203699Inhibition of [3H]pentazocine binding to sigma-1 sites in guinea pig brain membranes1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
(+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties.
AID330538Orexigenic activity in H1RKO mouse2007Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9
From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase.
AID5334Serotonergic activity of the compound.2000Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17
GRid-INdependent descriptors (GRIND): a novel class of alignment-independent three-dimensional molecular descriptors.
AID586709Displacement of [3H]-DTG from rat sigma2 receptor by liquid scintillation counting2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Synthesis and pharmacological evaluation of fluorine-containing D₃ dopamine receptor ligands.
AID1213068Drug metabolism assessed as recombinant human UGT1A4 assessed as O-glucuronidation measured per mg of protein at 10 to 400 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1686283Cytotoxicity in HREC assessed as reduction in cell viability incubated for 96 hrs by MTT assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells.
AID1215936Unbound intrinsic clearance in human liver microsomes at 50 to 1000 nM after 30 to 60 mins by HPLC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Significance of reductive metabolism in human intestine and quantitative prediction of intestinal first-pass metabolism by cytosolic reductive enzymes.
AID1369086Displacement of [3H]-(+)-Pentazocine from sigma 1 receptor in guinea pig brain cortex membranes after 120 mins by scintillation counting analysis2018Bioorganic & medicinal chemistry, 01-15, Volume: 26, Issue:2
2-Methyltetrahydro-3-benzazepin-1-ols - The missing link in SAR of GluN2B selective NMDA receptor antagonists.
AID65785Binding affinity towards human Dopamine receptor D32004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Selective optimization of side activities: another way for drug discovery.
AID204012Inhibitory activity against Sigma opioid receptor1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
Binding of substituted and conformationally restricted derivatives of N-(3-phenyl-n-propyl)-1-phenyl-2-aminopropane at sigma-receptors.
AID317395Ratio of Ki for sigma2 receptor in Hartley guinea pig brain to Ki for sigma1 receptor in Hartley guinea pig brain2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Synthesis and structure-activity relationships of N-(3-phenylpropyl)-N'-benzylpiperazines: Potent ligands for sigma1 and sigma2 receptors.
AID177479Effect on Ataxia(ATX) in rat was measured as ED50 by perorally administration of compound.1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
N6-(2,2-diphenylethyl)adenosine, a novel adenosine receptor agonist with antipsychotic-like activity.
AID1335652Therapeutic index, ratio of ED50 for induction of catalepsy in po dosed Chinese Kun Ming mouse to ED50 for inhibition of MK-801 induced hyperactivity in po dosed Chinese Kun Ming mouse2016European journal of medicinal chemistry, Nov-29, Volume: 124Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.
AID226426In vitro binding affinity for D2 receptor compared to that of 5-HT2 receptor2001Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10
Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic?
AID176744Dose inhibiting conditioned avoidance response in rats after oral administration1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID63534Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 091511997Journal of medicinal chemistry, Jan-03, Volume: 40, Issue:1
2-Phenyl-4(5)-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]imidazole. A highly selective antagonist at cloned human D4 receptors.
AID711577Inhibition of sigma 1 receptor2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID204153Sigma opioid receptor type 1 affinity in guinea pig brain by employing [3H](+)-pentazocine as radioligand.2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.
AID177887Inhibition of apomorphine-induced stereotypy in rats.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID303626Growth inhibition of human A427 cells at 20 uM after 96 hrs relative to control2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Synthesis of bicyclic sigma receptor ligands with cytotoxic activity.
AID5279In vitro 5-hydroxytryptamine 2 receptor affinity by using [3H]-Spiperone as the radioligand in rat cortical tissue.1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Antipsychotic activity of substituted gamma-carbolines.
AID439069Displacement of [3H]spiperone from human dopamine D3 receptor2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.
AID1053286Fraction unbound in rat brain homogenate at 5 uM after 4 hrs equilibrium dialysis method2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Design, synthesis and discovery of picomolar selective α4β2 nicotinic acetylcholine receptor ligands.
AID131419Potentiation against pentobarbital-induced sleeping, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID592113Induction of apoptosis in human MCF7 cells expressing sigma receptor assessed as viable cells using annexin V/propidium iodide staining at 5 uM after 24 hrs by flow cytometry (Rvb = 97.33%)2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Structure-activity study to develop cationic lipid-conjugated haloperidol derivatives as a new class of anticancer therapeutics.
AID705396Antipsychotic activity in sc dosed rat prepulse inhibition model2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID592133Induction of apoptosis in against african green monkey COS1 cells expressing sigma receptor assessed as early apoptotic cells using annexin V/propidium iodide staining at 5 uM after 24 hrs by flow cytometry (Rvb = 0.06%)2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Structure-activity study to develop cationic lipid-conjugated haloperidol derivatives as a new class of anticancer therapeutics.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID194374Effect of compound (0.2 mg/kg ip) on the concentration of DOPAC in rat frontal cortex1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID592131Induction of apoptosis in against african green monkey COS1 cells expressing sigma receptor assessed as viable cells using annexin V/propidium iodide staining at 5 uM after 24 hrs by flow cytometry (Rvb = 99.82%)2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Structure-activity study to develop cationic lipid-conjugated haloperidol derivatives as a new class of anticancer therapeutics.
AID87516Inhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranes1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.
AID266790Reduction of sc dosed 20 ug/kg 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]-pyridine-induced penile erection in Sprague-Dawley rat at 1 mg/kg, ip2006Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13
2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist.
AID254420In vitro inhibitory constant against [3H]spiperone binding to human dopamine D2 receptor expressed in CHO cells2005Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
Synthesis, structure-activity relationships, and biological properties of 1-heteroaryl-4-[omega-(1H-indol-3-yl)alkyl]piperazines, novel potential antipsychotics combining potent dopamine D2 receptor antagonism with potent serotonin reuptake inhibition.
AID1487359Antagonist activity at human D2L receptor expressed in CHO cell membranes assessed as residence time after 15 mins by liquid scintillation counting method2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID438612Selectivity ratio of Ki for sigma 2 receptor in rat liver membrane to Ki for sigma 1 receptor in guinea pig brain membrane2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Evaluation of spirocyclic 3-(3-fluoropropyl)-2-benzofurans as sigma1 receptor ligands for neuroimaging with positron emission tomography.
AID5837In vitro affinity against serotonin (5-hydroxytryptamine 2C) receptor2000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.
AID298491Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1506086Displacement of (+)-[3H]pentazocine from sigma1 receptor in rat brain membranes after 60 mins by liquid scintillation counting method2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.
AID238940Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies.
AID61358Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D12003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
AID391277Ratio of pKi for human cloned 5HT2A receptor to pKi for human cloned dopamine D2 receptor2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Synthesis, binding affinity, and molecular docking analysis of new benzofuranone derivatives as potential antipsychotics.
AID229516Ratio of IC50 value against dopamine receptor D2 to that of 5-hydroxytryptamine 3 receptor.1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID1552399Displacement of [3H]-(+)pentazocine from sigma-1 receptor in guinea pig brain membranes after 120 mins by scintillation counting method2019Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16
Modification of the 4-phenylbutyl side chain of potent 3-benzazepine-based GluN2B receptor antagonists.
AID64187Compound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assay1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.
AID61620Inhibition of [35S]GTP-gamma-S, binding to cell membranes expressing dopamine D2A receptor at 100 uM dopamine1999Bioorganic & medicinal chemistry letters, Aug-02, Volume: 9, Issue:15
Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor.
AID63531Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor.
AID776367Displacement of [3H]DTG from sigma-2 receptor in rat liver membrane after 120 mins by scintillation counting2013European journal of medicinal chemistry, Nov, Volume: 69New combination of pharmacophoric elements of potent σ₁ ligands: design, synthesis and σ receptor affinity of aminoethyl substituted tetrahydrobenzothiophenes.
AID1809442Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 150 mins by microbeta scintillation counting method2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Haloperidol Metabolite II Valproate Ester (
AID195772Tested for locomotor activity by measuring accumulated counts/30 min in reserpine-non-pretreated rats1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
C1- and C3-methyl-substituted derivatives of 7-hydroxy-2-(di-n-propylamino)tetralin: activities at central dopamine receptors.
AID63061Binding affinity towards human Dopamine receptor D2 using [3H]spiroperidol as radioligand2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands.
AID672150Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining relative to acetylcholine2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Hit-to-lead investigation of a series of novel combined dopamine D2 and muscarinic M1 receptor ligands with putative antipsychotic and pro-cognitive potential.
AID437143Inhibition of haloperidol-induced catalepsy in Swiss albino mouse assessed as time elapsed until release of forepaw from bar at 100 mg/kg, po administered 30 min prior to haloperidol challenge measured after 60 mins by bar test2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
Synthesis of some urea and thiourea derivatives of 3-phenyl/ethyl-2-thioxo-2,3-dihydrothiazolo[4,5-d]pyrimidine and their antagonistic effects on haloperidol-induced catalepsy and oxidative stress in mice.
AID65564In vitro Dopamine receptor D2 affinity by using [3H]-Spiperone as the radioligand in rat limbic system at 1 uM concentration of compound1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Antipsychotic activity of substituted gamma-carbolines.
AID64271Binding affinity towards Dopamine receptor D2 of rat corpus striatum using [3H]spiperone as radioligand1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID190978Effect on dopamine agonist-induced rotation in unilaterally 6-OH-DA-lesioned rat at 0.1 mg/kg, ip; Compound 35 was injected subcutaneously at 75 mg/kg1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Troponoids. 6. Troponylpiperazines: a new class of dopamine agonists.
AID346018Displacement of [3H]spiroperidol from human cloned dopaminergic D2 receptor expressed in rat C6 cells2008Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
2-[(3-Methoxyphenylethyl)phenoxy]-based ABCB1 inhibitors: effect of different basic side-chains on their biological properties.
AID133854Anticonvulsant activity against pentylenetetrazole-induced convulsions, after 1 hour of peroral administration in mouse at a dose of 20 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID1853647Inhibition of Mycobacterium tuberculosis AAC(3')-IV at 200 uM using NEO as substrate in presence of Acetyl-CoA by UV-Vis spectroscopy analysis2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from
AID303621Displacement of [3H]ditolylguanidine from sigma 2 receptor in rat liver membrane2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Synthesis of bicyclic sigma receptor ligands with cytotoxic activity.
AID303628Growth inhibition of human MCF7 cells at 20 uM after 96 hrs relative to control2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Synthesis of bicyclic sigma receptor ligands with cytotoxic activity.
AID1215124Binding affinity to Wistar rat brain lipid assessed as percentage unbound by TRANSIL assay2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID1232316Volume of distribution at steady state in mouse2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Volume of Distribution in Drug Design.
AID65888Tested for affinity against cloned mammalian dopamine autoreceptor (DA) D2 receptors expressed in CHO-K1 cells using [3H]spiperone as radioligand1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.
AID171875Antipsychotic efficacy of compound at intraperitoneal dose of 0.5 mg/kg on 6.8 (A10 units) dopamine neurons in the mesolimbic region of rat1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID1768730Relative lipophilicity of the compound in methanol assessed as retardation factor by reversed-phase TLC analysis2021Bioorganic & medicinal chemistry letters, 10-01, Volume: 49Estimation of the lipophilicity of purine-2,6-dione-based TRPA1 antagonists and PDE4/7 inhibitors with analgesic activity.
AID629460Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Development of a bivalent dopamine D₂ receptor agonist.
AID63351Compound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assay1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.
AID1636440Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID1409510Antipsychotic activity in po dosed Kunming mouse assessed as reduction in MK-801-induced hyperactivity pretreated for 60 mins followed by MK-801 challenge measured for 90 mins2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID1853648Inhibition of Mycobacterium tuberculosis AAC(2')-Ic at 200 uM using NEO as substrate in presence of Acetyl-CoA by UV-Vis spectroscopy analysis2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from
AID619350Displacement of [3H]di-o-tolylguanidine from sigma 2 receptor in rat brain membrane after 120 mins2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Synthesis and pharmacological evaluation of indole-based sigma receptor ligands.
AID1853690Cytotoxicity against mouse J774.A1 cells assessed as reduction in cell viability at 100 uM incubated for 24 hrs by resazurin assay2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from
AID177732Inhibition against conditioned avoidance response, after 5 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID367547Selectivity ratio, Ki for sigma 1 receptor in guinea pig brain homogenates to Ki for sigma 2 receptor in rat liver homogenates2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
New N-substituted 9-azabicyclo[3.3.1]nonan-3alpha-yl phenylcarbamate analogs as sigma2 receptor ligands: synthesis, in vitro characterization, and evaluation as PET imaging and chemosensitization agents.
AID230925Binding affinities for sigma-1 and sigma 2 receptors, ratio of IC501995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
AID592124Induction of apoptosis in human MCF7 cells expressing sigma receptor assessed as late apoptotic cells using annexin V/propidium iodide staining at 5 uM after 24 hrs by flow cytometry (Rvb = 1.48%)2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Structure-activity study to develop cationic lipid-conjugated haloperidol derivatives as a new class of anticancer therapeutics.
AID1782425Displacement of [3H]-SCH23390 from D3 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
2-Phenylcyclopropylmethylamine Derivatives as Dopamine D
AID176063Effect on the synthesis rates of dopamine in the rat ventral limbic brain region at 2.7 micro mol/kg.1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives.
AID1853668Synergistic antibacterial activity against Mycobacterium smegmatis mc2 155 assessed as fold reduction in MIC value at 8 ug/ml in presence of clarithromycin by checkerboard assay2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from
AID1686276Displacement of [3H]-pentazocine from sigma1 receptor in guinea pig brain membranes by scintillation counting2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells.
AID1136360Neuroleptic activity in squirrel monkey assessed as inhibition of Sidman avoidance at 0.75 mg/kg, po measured for 4 hrs1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 4. Central nervous system depressants.
AID549676Displacement of [3H]ditolylguanidine from sigma2 receptor in rat liver membrane by scintillation counting2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Synthesis, pharmacological activity and structure affinity relationships of spirocyclic σ(1) receptor ligands with a (2-fluoroethyl) residue in 3-position.
AID1191390Selectivity ratio of Ki for rat liver sigma2 receptor to Ki for guinea pig brain cortex sigma1 receptor2015European journal of medicinal chemistry, Jan-27, Volume: 90Improving selectivity preserving affinity: new piperidine-4-carboxamide derivatives as effective sigma-1-ligands.
AID156976Compound was tested for its affinity towards PCP receptor in rat brain membrane [3H]MK-801 as radioligand; ND = not determined1991Journal of medicinal chemistry, Dec, Volume: 34, Issue:12
Novel 1-phenylpiperazine and 4-phenylpiperidine derivatives as high-affinity sigma ligands.
AID1185963Displacement of [3H]N-methylspiperone from human dopamine D2 receptor by liquid scintillation counting2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Further evaluation of the tropane analogs of haloperidol.
AID180526The compound was tested for its ability to induced catalepsy in rats1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents.
AID1129882Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in human RPMI8226 cell membranes after 120 mins by scintillation counting analysis2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
Synthesis, pharmacological evaluation, and σ1 receptor interaction analysis of hydroxyethyl substituted piperazines.
AID65951Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors.
AID1292381Terminal half life in psychotic patient (9 patients) at 3.5 +/- 1.2 mg, iv by reversed phase HPLC method1987Psychopharmacology, , Volume: 91, Issue:4
Pharmacokinetics of haloperidol in psychotic patients.
AID1215125Percentage unbound in solid supported porcine brain membrane vesicles at 5 uM using four compound cocktail after 5 hrs by TRANSIL assay2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID410335Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat cortex by scintillation spectrometry2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
AID1144198Acute toxicity in ip dosed Swiss-Webster mouse assessed as tremor administered as single dose after 72 hrs1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Synthesis and biological actions of 2-substituted quinolizidines.
AID1393368Displacement of [3H]-raclopride from human D2LR expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
AID179827Tested for the inhibition of locomotor activity in rats intraperitoneally; value ranges from 0.21-0.3 mg/Kg1994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
The discovery and structure-activity relationships of 1,2,3,6-tetrahydro-4-phenyl-1-[(arylcyclohexenyl)alkyl]pyridines. Dopamine autoreceptor agonists and potential antipsychotic agents.
AID1292382Terminal phase volume of distribution at steady state in psychotic patient (9 patients) at 3.5 +/- 1.2 mg, iv by reversed phase HPLC method1987Psychopharmacology, , Volume: 91, Issue:4
Pharmacokinetics of haloperidol in psychotic patients.
AID1209973Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID226337Binding affinity for sigma 1 opioid receptor, measured on guinea pig brain membranes using [3H]- (+)-pentazocine as radioligand2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
Synthesis and structure-activity relationships of N-(1-benzylpiperidin-4-yl)arylacetamide analogues as potent sigma1 receptor ligands.
AID62444Inhibition of binding of 5 nM [3H]dopamine to dopamine receptor by 50%1981Journal of medicinal chemistry, Sep, Volume: 24, Issue:9
Synthesis and evaluation of 1,2,3,4-tetrahydro[1]benzothieno[2,3-h]isoquinolines as dopamine antagonists.
AID1144217Depression of spontaneous motor activity in Swiss-Webster mouse at 5 mg/kg, ip by photocell cage test relative to control1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Synthesis and biological actions of 2-substituted quinolizidines.
AID1169867Antipsychotic-like activity in sc dosed NMRI mouse assessed as reduction in MK801-induced locomotor activity dosed 15 to 30 mins before administration of MK801 measured for 60 mins2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.
AID592134Induction of apoptosis in human HEK293 cells expressing sigma receptor assessed as viable cells using annexin V/propidium iodide staining at 5 uM after 24 hrs by flow cytometry (Rvb = 99.76%)2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Structure-activity study to develop cationic lipid-conjugated haloperidol derivatives as a new class of anticancer therapeutics.
AID418670Displacement of [3H]1,3-ditolylguanine from sigma 2 receptor in rat liver membrane by solid scintillation analysis2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Dancing of the second aromatic residue around the 6,8-diazabicyclo[3.2.2]nonane framework: influence on sigma receptor affinity and cytotoxicity.
AID234393ratio between ED50 values of DA receptor antagonist activity and catalepsy.1998Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5
Novel antipsychotic agents with dopamine autoreceptor agonist properties: synthesis and pharmacology of 7-[4-(4-phenyl-1-piperazinyl)butoxy]-3,4-dihydro-2(1H)-quinolinone derivatives.
AID1221962Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1292383Volume of distribution at steady state in psychotic patient (9 patients) at 3.5 +/- 1.2 mg, iv by reversed phase HPLC method1987Psychopharmacology, , Volume: 91, Issue:4
Pharmacokinetics of haloperidol in psychotic patients.
AID391475Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Thiophene bioisosteres of spirocyclic sigma receptor ligands. 1. N-substituted spiro[piperidine-4,4'-thieno[3,2-c]pyrans].
AID1177035Intrinsic agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of a forskolin-dependent whole cell adenylyl cyclase activity after 20 mins relative to quinpirole2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Synthesis, pharmacological evaluation and molecular modeling studies of triazole containing dopamine D3 receptor ligands.
AID239010Inhibition of [125I]R91150 binding to human 5-hydroxytryptamine 2A receptor2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
AID180901The dose required to reduce the number of apomorphine induced rotation by 50% in rats with monolateral lesion of nigrostriatal tracts1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Combined analgesic/neuroleptic activity in N-butyrophenone prodine-like compounds.
AID5708Inhibition of [3H]mesulergine binding to 5-hydroxytryptamine 2C receptor in rat brain membranes1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.
AID242945Ratio of dopamine receptor D2 long and D4 ki values2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID116898Lethal dose in mice after perorla administration1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
10-Piperazinyl-4H-theino[3,2-b][1,5]- and -[3,4-b][1,5]benzodiazepines as potential neuroleptics.
AID1744233Displacement of [3H]-DTG from sigma-2 receptor in guinea pig brain membrane incubated for 1 hr by liquid scintillation counting method2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management.
AID1169869Antipsychotic-like activity in sc dosed NMRI mouse assessed as reduction in methamphetamine-induced locomotor activity dosed 15 to 30 mins before administration of methamphetamine measured for 60 mins2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.
AID395328Lipophilicity, log P of the compound2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID711574Half life in rat liver microsomes2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID176225Inhibition of apomorphine-induced stereotypy in rats via peroral route1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.
AID642496Displacement of [3H]-1,3-di(o-tolyl)guanidine from sigma 2 receptor in rat liver homogenates in the presence of (+)-pentazocine2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis, radiofluorination and pharmacological evaluation of a fluoromethyl spirocyclic PET tracer for central σ1 receptors and comparison with fluoroalkyl homologs.
AID549675Selectivity ratio of Ki for guinea pig sigma1 receptor to Ki rat sigma2 receptor2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Synthesis, pharmacological activity and structure affinity relationships of spirocyclic σ(1) receptor ligands with a (2-fluoroethyl) residue in 3-position.
AID1867871Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes measured after 120 mins by scintillation counting method2022European journal of medicinal chemistry, Jul-05, Volume: 237Synthesis and biological evaluation of conformationally restricted GluN2B ligands derived from eliprodil.
AID1285664Displacement of [3H]DTG from sigma receptor in human jurkat cells2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
AID184035In vivo activity administered intraperitoneally was determined by social interaction of rat at 5.0 uM1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID1744236Displacement of [3H]-DTG from sigma-2 receptor in human Jurkat cell membrane incubated for 1 hr by liquid scintillation counting method2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID181424Tested for the amphetamine induced stereotyped behavior in rats after oral administration1993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system.
AID1308623Growth inhibition of human A427 cells incubated for 96 hrs by crystal violet assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity?
AID711573Clearance in human liver microsomes2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID5018Effective dose through peroral route for in vivo inhibition against 5-hydroxytryptamine 2 receptor in male CF-1 mice by using radioligand [3H]ketanserin1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bridged gamma-carbolines and derivatives possessing selective and combined affinity for 5-HT2 and D2 receptors.
AID1213074Drug metabolism assessed as recombinant human UGT2B7 assessed as O-glucuronidation at 10 to 400 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID298264Displacement of [3H]spiroperidol from human cloned dopamine D2L receptor2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
4-[omega-[4-arylpiperazin-1-yl]alkoxy]phenyl)imidazo[1,2-a]pyridine derivatives: fluorescent high-affinity dopamine D3 receptor ligands as potential probes for receptor visualization.
AID177108ED50 value for catalepsy indicates the dose required to produce a 50% of maximum catalepsy score. parentheses value indicate 95% confidence limit.1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Pyrrole mannich bases as potential antipsychotic agents.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1168800Antagonist activity at D2 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of quinpirole2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Design, synthesis and evaluation of benzo[a]thieno[3,2-g]quinolizines as novel l-SPD derivatives possessing dopamine D1, D2 and serotonin 5-HT1A multiple action profiles.
AID382243Binding affinity to adrenergic alpha1 receptor2008Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9
Recent advances in selective alpha1-adrenoreceptor antagonists as antihypertensive agents.
AID26304Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID259127Selectivity ratio for dopamine D2-like receptor over dopamine D3 receptor2006Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2
Design of novel hexahydropyrazinoquinolines as potent and selective dopamine D3 receptor ligands with improved solubility.
AID130897Inhibition of locomotor activity in mouse after intraperitoneal administration1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines.
AID203984In vitro binding affinity measured on sigma opioid receptor using [3H]DTG as radioligand1995Journal of medicinal chemistry, Mar-17, Volume: 38, Issue:6
High affinity and selectivity on 5-HT1A receptor of 1-aryl-4-[1-tetralin)alkyl]piperazines. 2.
AID5491Binding affinity towards 5-hydroxytryptamine 2A receptor binding site using [3H]ketanserin. 1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
AID63371Binding affinity against dopamine receptor D11994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study.
AID1616722Displacement of PPHT-red from SNAP-tagged human D2LR expressed in CHOK1 cell membranes assessed as dissociation half-life by TR-FRET assay
AID1861724Binding affinity to sigma 2 receptor (unknown origin) assessed as inhibition constant by radioligand binding assay2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.
AID1433418Displacement of [3H]-PTZ from sigma1 receptor in guinea pig brain membranes after 150 mins in presence of DPH solvent by liquid scintillation counting method
AID277985Antagonist activity against rat D2 receptor assessed effect on quinelorane-stimulated [35S]GTP-gamma-S binding2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.
AID701946Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting2012Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
Pd-catalyzed direct C-H bond functionalization of spirocyclic σ1 ligands: generation of a pharmacophore model and analysis of the reverse binding mode by docking into a 3D homology model of the σ1 receptor.
AID176662Suppression of conditioned avoidance behavior in rats after ip administration1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2.
AID65894Tested for binding affinity towards rat striatal D2 receptor using [3H]spiperone as radioligand1994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
The discovery and structure-activity relationships of 1,2,3,6-tetrahydro-4-phenyl-1-[(arylcyclohexenyl)alkyl]pyridines. Dopamine autoreceptor agonists and potential antipsychotic agents.
AID1861725Selectivity index, ratio of Ki for sigma 1 receptor (unknown origin) to Ki for sigma 2 receptor (unknown origin)2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.
AID223305Effective dose administered in apomorphine induced climbing test in mice (in vivo)value in parentheses represents 95% confidence limit2000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.
AID1598360Antagonist activity at recombinant human D2 receptor expressed in CHOK1 cells assessed as inhibition of quinpirole-induced beta arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and measured after 90 mins by coelenterazine-bas
AID23695Partition coefficient (logP)1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID63682Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.1997Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15
4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor.
AID180551The compound was tested in vivo for induction of catalepsy in rat after ip administration1999Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID37370Half-maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor in rat frontal cortex homogenate2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID1853639Potentiation of kanamycin-induced antibacterial activity against Mycobacterium tuberculosis K204 assessed as kanamycin MIC incubated for 1 day followed by kanamycin addition for 6 days and by Alamar blue assay2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from
AID256758Displacement of [3H]spiroperidol from cloned human dopamine receptor D3 in CHO cell membrane2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
First structure-activity relationship study on dopamine D3 receptor agents with N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamide structure.
AID1144202Depression of forced motor activity in Swiss-Webster mouse at 10 mg/kg, ip after 30 mins by rotarod test relative to control1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Synthesis and biological actions of 2-substituted quinolizidines.
AID194523Effect of compound on (0.2 mg/kg ip) the concentration of 5-HIAA in rat mesolimbic region1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID37455Affinity for alpha-1 adrenergic receptor1998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.
AID458650Reduction in amphetamine-induced locomotor activity in Sprague-Dawley rat striatum at 1 umol/kg, sc relative to control2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
AID1441553Displacement of [3H]-DTG from sigma 2 receptor in rat liver membranes after 120 mins by scintillation counting2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective κ-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo.
AID1409509Antipsychotic activity in po dosed Kunming mouse assessed as reduction in apomorphine-induced climbing pretreated for 30 mins followed by apomorphine injection measured at 10 to 30 mins post dose2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID1213036Drug metabolism assessed as recombinant human UGT1A1 assessed as O-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID176331Inhibition of d-amphetamine induced stereotypy in rats; i.p. treatment 1 hr before amphetamine.1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Neuroleptics from the 4a,9b-cis- and 4a,9b-trans-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole series. 2.
AID524791Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1409613Selectivity ratio: ratio of AUC (viral infection %) of SARS-CoV-2 in the Vero E6 cell line compared to AUC (cytotoxicity %) of compound against Vero E6 cells by MTT assay.2020Nature, 07, Volume: 583, Issue:7816
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID724161Displacement of (+)-[3H]pentazocine from sigma1 receptor in rat brain membranes2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Synthesis and biological evaluation of ¹⁸F labeled fluoro-oligo-ethoxylated 4-benzylpiperazine derivatives for sigma-1 receptor imaging.
AID517711Displacement of [3H]WAY-100635 from 5-HT1A receptor in pig cerebral cortex homogenates2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Bioisosteric replacement leading to biologically active [2.2]paracyclophanes with altered binding profiles for aminergic G-protein-coupled receptors.
AID444008Antagonist activity at sigma2 receptor in guinea pig ileum longitudinal muscle assessed as inhibition of 5-HT-induced contractions2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane.
AID1686280Cytotoxicity in HREC assessed as reduction in cell viability incubated for 24 hrs by MTT assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells.
AID224650Area under curve(AUC) value of Dopamine level after total treatment in dialysates collected from rat striatum.2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID1210071Inhibition of CYP3A4 in human liver microsomes using testosterone substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID176807Suppression of conditioned avoidance behavior in rats when administered intraperitoneally 60 min before measurement1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
AID3699The binding affinity was measured on serotonin 5-hydroxytryptamine 1 receptor in rat brain tissue1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Pyrrole mannich bases as potential antipsychotic agents.
AID1878192Ratio of Ki for binding affinity to D2S (unknown origin) to Ki for binding affinity to D3R (unknown origin)
AID566433Displacement radioligand form dopamine D3 receptor in rat olfactory tubercle by liquid scintillation counting2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Antiproliferative activity of phenylbutyrate ester of haloperidol metabolite II [(±)-MRJF4] in prostate cancer cells.
AID65563Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID203698Compound was tested for its binding affinity towards sigma 1 receptor using [3H](+)-pentazocine from guinea pig brain1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand.
AID170279Locomotor activity after reserpine pretreatment in rat; Not Tested1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Novel dopamine receptor agonists and antagonists with preferential action on autoreceptors.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1213083Drug metabolism assessed as human liver microsomes assessed as O-glucuronide measured at 100 uM by LC-MS/MS analysis in presence of 10 uM gemfibrozil relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID113687Inhibition of head twitches-induced by 2,5-dimethoxy-4-iodoamphetamine in mice.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID63028Ability to inhibit [3H]haloperidol binding to dopamine receptor in rat striatal homogenate1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents.
AID130864In vivo the ability to antagonize the apomorphine induced climbing response in mice1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents.
AID1441551Displacement of [3H]-(+)-pentazocine from sigma1-type opioid receptor in guinea pig cortex membranes after 120 mins by solid scintillation counting2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective κ-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo.
AID1478365Displacement of [3H]-(+)-DTG from sigma2 receptor in guinea pig brain membrane after 120 mins by liquid scintillation counting method2018Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
(+)-Methyl (1R,2S)-2-{[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]methyl}-1-phenylcyclopropanecarboxylate [(+)-MR200] Derivatives as Potent and Selective Sigma Receptor Ligands: Stereochemistry and Pharmacological Properties.
AID1213092Drug metabolism assessed as recombinant human UGT1A9 assessed as O-glucuronidation at 25 to 200 uM incubated for 60 mins by LC-MS/MS analysis in presence of 10 uM niflumic acid relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID131873Effective dose required for inhibition of apomorphine(sc, 2.5 mg/kg ) induced climbing in mice on ip administration2001Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10
Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic?
AID1213045Drug metabolism assessed as Sprague-Dawley rat liver microsomes assessed as velocity of O-glucuronidation at 100 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID138928Antagonism of apomorphine for 10-20 minutes in reserpinized mice when a dose of 2.7 micro mol/kg is administered intraperitoneally1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 1. Synthesis and structure-activity relationships of 2,3,3a,4,5,9b-hexahydro-1H-benz[e]indole derivatives.
AID141682The compound was tested for inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents.
AID128163Activity of inclined screen in mouse, after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID204443Ability to displace [3H](+)-pentazocine at sigma receptor in guinea pig brain membrane was determined1993Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16
Synthesis and evaluation of conformationally restricted N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylamines at sigma receptors. 2. Piperazines, bicyclic amines, bridged bicyclic amines, and miscellaneous compounds.
AID737843Selectivity ratio of Ki for sigma 2 receptor in rat liver membranes to Ki for sigma 1 receptor in guinea pig brain membranes2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Improvement of σ1 receptor affinity by late-stage C-H-bond arylation of spirocyclic lactones.
AID1213049Drug metabolism assessed as recombinant human UGT1A7 assessed as N-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID138757Ability to stimulate dopaminergic systems by effect on locomotor activity in reserpinized mice when a dose of 0.3 micro mol/kg is administered intraperitoneally1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives.
AID1146537Inhibition of apomorphine-induced stereotyped behavior in po dosed albino Wistar rat administered 2 hrs before apomorphine challenge measured after 20 mins1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
AID204596Binding affinity against sigma receptor of MCF cells1994Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12
Synthesis and characterization of [125I]-N-(N-benzylpiperidin-4-yl)-4- iodobenzamide, a new sigma receptor radiopharmaceutical: high-affinity binding to MCF-7 breast tumor cells.
AID1782426Displacement of [3H]-LSD from 5HT1A receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
2-Phenylcyclopropylmethylamine Derivatives as Dopamine D
AID1207187Inhibition of voltage-gated L-type Ca channel (species unknown)2011Cardiovascular research, Jul-01, Volume: 91, Issue:1
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID5197Binding affinity towards human serotonin 5-hydroxytryptamine 2A receptor2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Selective optimization of side activities: another way for drug discovery.
AID1135932Neuroleptic activity in ip dosed ICR-DUB mouse assessed as survival administered 3 days prior to d-amphetamine challenge measured after 24 hrs1978Journal of medicinal chemistry, Jan, Volume: 21, Issue:1
(1-(3-(Phenothiazin-10-yl)propyl)-4-piperidinyl)phenylmethanones, a novel class of long-acting neuroleptic agents.
AID1545633Displacement of [3H]N-methylspiperone from human recombinant D2 receptor expressed in HEK293 cells at 10'-6 M incubated for 60 mins by microbeta2 scintillation counter relative to control2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Novel multitarget 5-arylidenehydantoins with arylpiperazinealkyl fragment: Pharmacological evaluation and investigation of cytotoxicity and metabolic stability.
AID1209974Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID177958Antagonistic activity administered intraperitoneally on head twitches induced by 5- HTP1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID184992Compound is evaluated for locomotor activity in nonhabituated rats at 1.3 micro mol/kg of subcuteneous dose1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.
AID35274Evaluated for binding affinity against alpha-1 adrenergic receptor2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
A rapid computational method for lead evolution: description and application to alpha(1)-adrenergic antagonists.
AID65935In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.1998Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24
N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide: a potent and selective dopamine D4 ligand.
AID437147Inhibition of haloperidol-induced catalepsy in Swiss albino mouse assessed as time elapsed until release of forepaw from bar at 100 mg/kg, po administered 30 min prior to haloperidol challenge measured after 150 mins by bar test2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
Synthesis of some urea and thiourea derivatives of 3-phenyl/ethyl-2-thioxo-2,3-dihydrothiazolo[4,5-d]pyrimidine and their antagonistic effects on haloperidol-induced catalepsy and oxidative stress in mice.
AID595907Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 150 mins2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Novel potent and selective σ ligands: evaluation of their agonist and antagonist properties.
AID566274Inhibition of rat sigma receptor2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: de
AID176476Catalepsy interval defined as the time required for both fore limbs to be removed from the bar when administered intraperitoneally1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds.
AID63971Binding affinity for dopamine receptor D2 determined using [3H]spiperone2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.
AID1308625Growth inhibition of human 5637 cells incubated for 96 hrs by crystal violet assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity?
AID457705Toxicity in CF1 mouse assessed as induction of catalepsy by measuring time spent on elevated wood bar at 4 mg/kg, po after 90 mins (Rvb = 2.4 +/- 2.6 sec)2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors.
AID1063796Displacement of [3H]N-Methylspiperone from dopamine D2 receptor (unknown origin)2014Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.
AID1726851Selectivity index, ratio of Ki for human sigma1 receptor expressed in HEK293 cell membrane to Ki for sigma2 receptor in SPRD rat liver membrane
AID1409608AUC (viral infection %) for SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells).2020Nature, 07, Volume: 583, Issue:7816
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID1433420Displacement of [3H]-PTZ from sigma1 receptor in guinea pig brain membranes after 150 mins in presence of 1 mM DPH by liquid scintillation counting method
AID1213052Drug metabolism assessed as recombinant human UGT1A10 assessed as N-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID63822In vitro ability to displace [3H]spiperone binding from dopamine receptor D2 in rat striatal membrane.1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical an
AID255057Inhibitory concentration against opioid receptor sigma 1 of guinea pig cerebral cortex using [3H](+)-pentazocine upon incubation for 150 minutes at 22 degree C2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective sigma1 ligands. Part 1.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID605699Displacement of [3H]spiperone from human D3 receptor expressed in CHO cells2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Bivalent dopamine D2 receptor ligands: synthesis and binding properties.
AID1598358Antagonist activity at recombinant human D3 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta arrestin2 recruitment preincubated for 30 mins followed by dopamine addition and measured after 90 mins by coelenterazine-based b
AID598811Displacement of [3H](+)-pentazocine from sigma 1 receptor in rat brain homogenate2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Molecular hybridization of 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecane-3-ol with sigma (σ) receptor ligands modulates off-target activity and subtype selectivity.
AID1136364Non-specific toxicity in ip dosed Wistar rat assessed as inhibition of amphetamine-induced circling administered 60 mins prior to amphetamine challenge1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 4. Central nervous system depressants.
AID63819Inhibition of [3H]-spiperone 23390 binding to dopamine receptor D2 rat striatal membrane1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
Synthesis and atypical antipsychotic profile of some 2-(2-piperidinoethyl)benzocycloalkanones as analogues of butyrophenone.
AID112671In vivo inhibition of apomorphine-induced climbing response in mice.1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Effect of linking bridge modifications on the antipsychotic profile of some phthalimide and isoindolinone derivatives.
AID61612Displacement of [3H]quinpirole from human dopamine D2A receptors expressed in LtK cells1999Bioorganic & medicinal chemistry letters, Aug-02, Volume: 9, Issue:15
Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor.
AID439066Displacement of [3H]ketanserin from human cloned 5HT2A receptor2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.
AID138786Antagonism of apomorphine for 0-10 minutes in reserpinized mice when a dose of 2.7 micro mol/kg is administered intraperitoneally1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives.
AID1728290Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membrane incubated for 120 mins by liquid scintillation counting method relative to control2021European journal of medicinal chemistry, Jan-15, Volume: 210Novel σ
AID1207744Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits2013Scientific reports, , Volume: 3MICE models: superior to the HERG model in predicting Torsade de Pointes.
AID223306Effective dose administered in catalepsy test in mice(in vivo) value in parentheses represents 95% confidence limit2000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.
AID218673Binding affinity towards alpha-1 adrenergic receptor1987Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.
AID298031Lipophilicity, log D at pH7.42007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery.
AID64930Displacement of [3H]spiperone (0.5 nM) from rat corpus striatum dopamine D2 receptor2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
AID218805Binding affinity towards alpha-2 adrenergic receptor at 1.0 uM concentration1987Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.
AID1213025Drug metabolism assessed as recombinant human UGT2B7 assessed as O-glucuronidation measured as inhibition constant at 10 to 400 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID681116TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing MDCKII cells2002The Journal of pharmacology and experimental therapeutics, Dec, Volume: 303, Issue:3
Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs.
AID1215935Unbound intrinsic clearance in human intestinal microsomes at 50 to 1000 nM after 30 to 60 mins by HPLC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Significance of reductive metabolism in human intestine and quantitative prediction of intestinal first-pass metabolism by cytosolic reductive enzymes.
AID231459Ratio between D2 receptor and 5-HT2 receptor binding affinities.1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Examination of the D2/5-HT2 affinity ratios of resolved 5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indoles: an enantioselective approach toward the design of potential atypical antipsychotics.
AID298483Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID1594272Displacement of [3H]-DTG from sigma2 receptor in guinea pig brain membranes after 120 mins in presence of sigma1 antagonist (+)-SKF10047 by microbeta scintillation counting method2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Discovery of a novel class of potent and selective tetrahydroindazole-based sigma-1 receptor ligands.
AID62884Displacement of [3H]spiroperidol from Dopamine receptor of rat striatum membrane1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems.
AID63218In vitro binding affinity towards Dopamine receptor D2 in human using [3H]-spiperone as radioligand2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.
AID36730Its affinity towards alpha-1 receptor using [3H]WB-4101 as radioligand in whole brain minus cerebellum1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents.
AID1532588Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes at 1 uM after 60 mins relative to control2019European journal of medicinal chemistry, Jan-15, Volume: 162Novel multitarget-directed ligands targeting acetylcholinesterase and σ
AID410532Antipsychotic activity in NMRI mouse assessed as reduction in phencyclidine-induced locomotor activity administered 30 mins prior to testing measured for 60 mins2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
AID323226Displacement of [3H]ditolylguanidine from sigma 2 opioid receptor in rat liver2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Synthesis and structure-affinity relationships of novel spirocyclic sigma receptor ligands with furopyrazole structure.
AID342778Binding affinity to human cloned dopamine D3 receptor2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID1393364Displacement of [3H]-ketanserin from human 5-HT2AR expressed in CHO-K1 cell membranes after 1.5 hrs by microbeta counting method
AID63524Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID705722Displacement of [3H]di-o-tolylguanidine from Sigma2 receptor in rat liver homogenate2012Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
New positron emission tomography (PET) radioligand for imaging σ-1 receptors in living subjects.
AID224644Area under curve(AUC) value of Dopamine level after first treatment (0.74 umol/kg) in dialysates collected from rat striatum.2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID711578Inhibition of human dopamine D5 receptor2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID711581Inhibition of human dopamine D3 receptor2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID1135931Neuroleptic activity in ip dosed ICR-DUB mouse assessed as survival administered 2 days prior to d-amphetamine challenge measured after 24 hrs1978Journal of medicinal chemistry, Jan, Volume: 21, Issue:1
(1-(3-(Phenothiazin-10-yl)propyl)-4-piperidinyl)phenylmethanones, a novel class of long-acting neuroleptic agents.
AID259123Displacement of [3H]SCH 23390 from rat caudate putamen dopamine D1-like receptor2006Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2
Design of novel hexahydropyrazinoquinolines as potent and selective dopamine D3 receptor ligands with improved solubility.
AID1211294Unbound fraction in plasma (unknown origin) at pH 7.4 after 6 hrs by equilibrium dialysis method in presence of 5% CO22011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID112955Compound was tested for inhibition of spontaneous motor activity in mouse when administered perorally1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.
AID36137In vitro binding affinity towards alpha-1 adrenergic receptor by using [3H]-prazosin in rat brain cortex membranes.2000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
A structure-affinity relationship study on derivatives of N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a high-affinity and selective D(4) receptor ligand.
AID37441Binding affinity was evaluated against Alpha-1 adrenergic receptor on rat cortex using [3H]prazosin as radioligand; ND = Not determined1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists.
AID1213069Intrinsic clearance in recombinant human UGT1A4 measured per mg of protein at 10 to 400 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID61619Inhibition of [35S]GTP-gamma-S, binding to cell membranes expressing dopamine D2A receptors at 100 uM1999Bioorganic & medicinal chemistry letters, Aug-02, Volume: 9, Issue:15
Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor.
AID1144195Acute toxicity in ip dosed Swiss-Webster mouse administered as single dose after 7 days1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Synthesis and biological actions of 2-substituted quinolizidines.
AID1300374Toxicity in Kun Ming mouse assessed as reduction in spontaneous locomotor activity by measuring total distance traveled at 1 mg/kg, po administered 30 mins prior to testing measured after 30 to 120 mins (Rvb = 24881.4 +/- 9545.8 mm)2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Synthesis and Biological Evaluation of Novel σ1 Receptor Ligands for Treating Neuropathic Pain: 6-Hydroxypyridazinones.
AID415888Displacement of [3H]ditolylguanidine from sigma 2 receptor in rat liver membrane by liquid scintillation analyzer2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
1,4-Diazepanes derived from (S)-serine--homopiperazines with improved sigma(1) (sigma) receptor affinity and selectivity.
AID65790Selectivity ratio against Dopamine receptor D3 to Dopamine receptor D12002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID1782428Displacement of [3H]-LSD from 5HT2C receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
2-Phenylcyclopropylmethylamine Derivatives as Dopamine D
AID205147Tested for inhibition of conditioned avoidance in squirrel monkeys; value ranges from 0.4-0.6 mg/Kg1994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
The discovery and structure-activity relationships of 1,2,3,6-tetrahydro-4-phenyl-1-[(arylcyclohexenyl)alkyl]pyridines. Dopamine autoreceptor agonists and potential antipsychotic agents.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1411896Half life in po dosed human plasma2018MedChemComm, May-01, Volume: 9, Issue:5
Schizophrenia: synthetic strategies and recent advances in drug design.
AID177947Antagonistic activity against amphetamine-induced stereotypy, after 5 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID1211297Drug recovery in plasma (unknown origin)2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID1409609Cytotoxicity of compound against Vero E6 cells by MTT assay.2020Nature, 07, Volume: 583, Issue:7816
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID1213071Drug metabolism assessed as recombinant human UGT1A9 assessed as O-glucuronidation measured per mg of protein at 10 to 400 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID492182Displacement of [125I]ABN from human dopamine D2 long receptor expressed in HEK293 cells after 60 mins by gamma counting2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Synthesis and characterization of selective dopamine D2 receptor antagonists. 2. Azaindole, benzofuran, and benzothiophene analogs of L-741,626.
AID1062947Selectivity ratio of pKi for human 5-HT2A receptor to pKi for human D2 receptor2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis and biological evaluation of a series of aminoalkyl-tetralones and tetralols as dual dopamine/serotonin ligands.
AID196821Compound was evaluated for the pA2 values against Dopamine (DA)-induced contraction of isolated rat vas deferens.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Synthesis and antidopaminergic activity of some 3-(aminomethyl)tetralones as analogues of butyrophenone.
AID492646Antipsychotic activity in NMRI mouse assessed as increase of PCP-induced locomotor activity at 3 mg/kg, ip administered 30 mins prior to testing measured for 60 mins2010Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors.
AID133191Tested for physostigmine lethality at a dose of 5 mg/kg after oral administration in mice1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems.
AID1853637Inhibition of Mycobacterium tuberculosis Eis assessed as Eis-mediated kanamycin acetylation preincubated for 10 mins followed by substrate addition and measured for 2 to 5 mins using acetyl-CoA as substrate in presence of kanamycin by UV-Vis spectroscopy 2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from
AID592116Cytotoxicity against human MDA-MB-231 cells expressing sigma receptor at 0.5 to 50 uM after 48 hrs by MTT assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Structure-activity study to develop cationic lipid-conjugated haloperidol derivatives as a new class of anticancer therapeutics.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID160798The irreversibility of the inactivation reaction of HIV-2 PR was assessed; NI =No detectable reversible reaction1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Haloperidol-based irreversible inhibitors of the HIV-1 and HIV-2 proteases.
AID1809445Antiproliferative activity against VEGF-A stimulated human retinal endothelial cell assessed as reduction in cell viability measured after 48 hrs by MTT assay2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Haloperidol Metabolite II Valproate Ester (
AID255169Selectivity against opioid receptor sigma 2 to that of opioid receptor sigma 12005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective sigma1 ligands. Part 2.
AID64479In vitro binding affinity towards Dopamine receptor D2L, using [3H]spiroperidol radioligand in Sf9 baculovirus expression.2000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
A structure-affinity relationship study on derivatives of N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a high-affinity and selective D(4) receptor ligand.
AID141053Inhibition of binding of 1.0 nM [3H]pirenzepine to cloned human Muscarinic acetylcholine receptor M1 expressed in membranes from CHO-K1 cells1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID63060Binding affinity towards human Dopamine receptor D22004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Selective optimization of side activities: another way for drug discovery.
AID1128477Inhibition of conditioned avoidance response in Sprague-Dawley rat model at 2 mg/kg, po after 2 hrs by electric foot shock test2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.
AID1144197Acute toxicity in ip dosed Swiss-Webster mouse assessed as death administered as single dose after 72 hrs1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Synthesis and biological actions of 2-substituted quinolizidines.
AID142719Binding affinity was measured against muscarinic (M1) receptor in rat using [3H]pirenzepine as radioligand1994Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.
AID1578087Brain to plasma partition coefficient, Kp of the compound in rat2019European journal of medicinal chemistry, Nov-15, Volume: 182Practical approaches to evaluating and optimizing brain exposure in early drug discovery.
AID1409511Induction of catalepsy in po dosed Kunming mouse measured after 60 secs2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID142225Binding affinity towards Muscarinic acetylcholine receptor in rat was determined1987Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.
AID277978Normalizing effect on methylphenidate-induced behaviours in ip dosed rat after 30 min2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.
AID1153309Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Functionally selective dopamine D₂, D₃ receptor partial agonists.
AID1215949Metabolic stability in human intestinal cytosol at 200 nM after 60 mins in presence of menadione2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Significance of reductive metabolism in human intestine and quantitative prediction of intestinal first-pass metabolism by cytosolic reductive enzymes.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1288455Displacement of [3H]N-methylspiperone from human dopamine D2 receptor by PDSP assay2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Tetrahydroprotoberberine alkaloids with dopamine and σ receptor affinity.
AID229213Tested for [3H](+)-pentazocine binding to sigma-1 receptor in guinea pig brain membrane1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID45980Compound was evaluated for the inhibition of [3H]haloperidol binding in calf brain homogenates1981Journal of medicinal chemistry, Jun, Volume: 24, Issue:6
Synthesis and evaluation of novel alkylpiperazines as potential dopamine antagonists.
AID715356Toxicity in rat assessed as increase in prolactin level up to 1.5 mg/kg, po2012Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID1147993Reduction in apomorphine-induced sterotypic climbing in Swiss-Webster mouse at 0.1 mg/kg, ip administered 30 mins prior to apomorphine-challenge measured after 5 mins1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
2,5-Bis(3,4-dimethoxybenzyl)cyclopentylamine, a peripheral dopamine blocking agent.
AID1409513Therapeutic index, ratio of ED50 for catalepsy in Kunming mouse to ED50 for apomorphine-induced climbing in Kunming mouse2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID1127305Selectivity ratio of Ki for sigma 2 receptor in Dunkin Hartley guinea pig membrane to Ki for sigma 1 receptor in Dunkin Hartley guinea pig membrane2014European journal of medicinal chemistry, May-22, Volume: 79Synthesis and biological evaluation of a novel sigma-1 receptor antagonist based on 3,4-dihydro-2(1H)-quinolinone scaffold as a potential analgesic.
AID45592Compound was tested for stimulation of mitogenesis in CHO.hD3 cells in a dose dependent manner1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists.
AID183724Inhibitory activity in apomorphine antagonism test at a dose of 20 mg/kg, sc1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1221958Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID61566Compound was tested for its binding affinity towards Dopamine receptor D2 by using [3H]domperidone as radioligand1991Journal of medicinal chemistry, Dec, Volume: 34, Issue:12
Novel 1-phenylpiperazine and 4-phenylpiperidine derivatives as high-affinity sigma ligands.
AID1756661Displacement of [3H]N-methylspiperone from human D2L receptor expressed in HEK293T cells co-expressing CRE-Luc incubated for 60 mins by microbeta scintillation counting method2021European journal of medicinal chemistry, Mar-15, Volume: 214Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the H
AID1191391Displacement of [3H]MK801 from pig brain cortex NMDA receptor PCP binding site at 1 uM by scintillation analyzer2015European journal of medicinal chemistry, Jan-27, Volume: 90Improving selectivity preserving affinity: new piperidine-4-carboxamide derivatives as effective sigma-1-ligands.
AID63064Binding affinity on human Dopamine receptor D2 expressed in CHO cells using radioligand [3H]-YM 091511997Journal of medicinal chemistry, Jan-03, Volume: 40, Issue:1
2-Phenyl-4(5)-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]imidazole. A highly selective antagonist at cloned human D4 receptors.
AID64295In vitro binding affinity at Dopamine receptor D2 in rat by displacing [3H]- spiperone from rat striatal membrane1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Potential neuroleptic agents. 3. Chemistry and antidopaminergic properties of substituted 6-methoxysalicylamides.
AID65494Inhibitory constant towards reuptake of [125I]-12 from dopamine transporter in rat striatal membranes1994Journal of medicinal chemistry, May-13, Volume: 37, Issue:10
Synthesis and characterization of radioiodinated N-(3-iodopropen-1-yl)-2 beta-carbomethoxy-3 beta-(4-chlorophenyl)tropanes: potential dopamine reuptake site imaging agents.
AID1690209Displacement of [3H]-(+)-pentazocine from Sigma1 receptor in guinea pig cortex membranes incubated for 120 mins by scintillation counting method
AID1144205Depression of forced motor activity in Swiss-Webster mouse at 5 mg/kg, ip after 30 mins by rotarod test relative to control1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Synthesis and biological actions of 2-substituted quinolizidines.
AID1415571Displacement of [3H](+)-Pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis2017MedChemComm, May-01, Volume: 8, Issue:5
Do GluN2B subunit containing NMDA receptors tolerate a fluorine atom in the phenylalkyl side chain?
AID640310Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting2012Bioorganic & medicinal chemistry, Feb-01, Volume: 20, Issue:3
Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.
AID1215963Activity of recombinant carbonyl reductase (unknown origin)2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Significance of reductive metabolism in human intestine and quantitative prediction of intestinal first-pass metabolism by cytosolic reductive enzymes.
AID1297660Displacement of [3H]DTG from sigma2 receptor in rat liver homogenate incubated for 120 mins by solid scintillation counting analysis2016European journal of medicinal chemistry, Jun-30, Volume: 116Benzimidazolone bioisosteres of potent GluN2B selective NMDA receptor antagonists.
AID1185978Toxicity in ip dosed Sprague-Dawley rat assessed as catalepsy by crossed-legs position test2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Further evaluation of the tropane analogs of haloperidol.
AID439064Displacement of [3H]spiperone from human cloned dopamine D2 receptor2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.
AID448644Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain after 180 mins by scintillation counting2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Synthesis of sigma receptor ligands with unsymmetrical spiro connection of the piperidine moiety.
AID63800Compound was evaluated for its affinity (pKi) to inhibit [3H]spiperone binding to the Dopamine receptor D21991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Synthesis and antidopaminergic activity of some 3-(aminomethyl)tetralones as analogues of butyrophenone.
AID161627Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells2003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Antimalarial drug quinacrine binds to C-terminal helix of cellular prion protein.
AID1136138Ratio of MED for inhibition of amphetamine-induced stereotyped-behavior in ip dosed Sprague-Dawley rat to ED50 for suppression of conditioned avoidance response in ip dosed Sprague-Dawley rat1978Journal of medicinal chemistry, Jul, Volume: 21, Issue:7
Neuroleptics related to butaclamol. Synthesis and some psychopharmacological effects of a series of 3-aryl analogues.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID63347Binding affinity towards human Dopamine receptor D12004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Selective optimization of side activities: another way for drug discovery.
AID5218Ability to inhibit [3H]spiperone binding to 5-hydroxytryptamine 2 receptor determined in rat1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
AID1809444Antiproliferative activity against VEGF-A stimulated human retinal endothelial cell assessed as reduction in cell viability measured after 24 hrs by MTT assay2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Haloperidol Metabolite II Valproate Ester (
AID1215962Activity of carbonyl reductase in liver cytosol (unknown origin) assessed as enzyme-mediated drug metabolism2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Significance of reductive metabolism in human intestine and quantitative prediction of intestinal first-pass metabolism by cytosolic reductive enzymes.
AID1300373Toxicity in Kun Ming mouse assessed as reduction in spontaneous locomotor activity by measuring total distance traveled at 0.3 mg/kg, po administered 30 mins prior to testing measured after 30 to 120 mins (Rvb = 24881.4 +/- 9545.8 mm)2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Synthesis and Biological Evaluation of Novel σ1 Receptor Ligands for Treating Neuropathic Pain: 6-Hydroxypyridazinones.
AID317390Displacement of [3H](+)-PTZ from sigma1 receptor in Hartley guinea pig brain2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Synthesis and structure-activity relationships of N-(3-phenylpropyl)-N'-benzylpiperazines: Potent ligands for sigma1 and sigma2 receptors.
AID1704752Therapeutic index, ratio of ED50 for toxicity in po dosed Kunming mouse assessed as catalepsy to ED50 for antipsychotic activity in Kunming mouse assessed as inhibition of MK801-induced locomotor activity
AID3756In vitro binding affinity for serotonin 5-hydroxytryptamine 1A receptor fof rat cerebral cortex using [3H]8-OH-DPAT as radioligand2002Journal of medicinal chemistry, Oct-10, Volume: 45, Issue:21
Synthesis and pharmacological evaluation of 1-[(1,2-diphenyl-1H-4-imidazolyl)methyl]-4-phenylpiperazines with clozapine-like mixed activities at dopamine D(2), serotonin, and GABA(A) receptors.
AID211852Acute toxicity on male outbred albino mice upon intraperitoneal administration1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
Design of N-acylprolyltyrosine "tripeptoid" analogues of neurotensin as potential atypical antipsychotic agents.
AID184659Compound was evaluated for the inhibition of haloperidol induced catalepsy behavior in rats after sc administration; Inactive1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents.
AID492187Displacement of [3H]DTG from sigma 2 receptor in rat liver homogenates after 1 hr by liquid scintillation counting2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Synthesis and characterization of selective dopamine D2 receptor antagonists. 2. Azaindole, benzofuran, and benzothiophene analogs of L-741,626.
AID750622Toxicity in po dosed mouse assessed as induction of catalepsy2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID113543Induction of catalepsy in mice1998Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5
Novel antipsychotic agents with dopamine autoreceptor agonist properties: synthesis and pharmacology of 7-[4-(4-phenyl-1-piperazinyl)butoxy]-3,4-dihydro-2(1H)-quinolinone derivatives.
AID1861729Cytotoxicity against ER/PR-negative HER2-positive human SK-BR-3 cells harbouring wild type p53 assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based assay2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.
AID49738Compound at a dose of 100 ug/kg was evaluated for the reversal of the inhibition of nerve stimulation using the cat cardioaccelerator nerve preparation; Reversed inhibition1986Journal of medicinal chemistry, Dec, Volume: 29, Issue:12
p-Dimethoxy-substituted trans-octahydrobenzo[f]- and -[g]quinolines: synthesis and assessment of dopaminergic agonist effects.
AID4053Compound was evaluated for in vitro binding affinity towards 5-hydroxytryptamine 1A receptor in rat hippocampus using [3H]8-OH-DPAT as radioligand1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia.
AID62736Affinity for Dopamine receptors in the rat striatum using [3H]spiroperidol displacement.1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Neuroleptics from the 4a,9b-cis- and 4a,9b-trans-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole series. 2.
AID150735High affinity constant at binding site of human P-Glycoprotein (P-gp) in two-affinity model2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID1393470Therapeutic index, ratio of MED for sedation in ip dosed Sprague-Dawley rat to MED for antipsychotic activity in ip dosed Sprague-Dawley rat assessed as reduction in PCP-induced hyper-locomotion
AID1308624Growth inhibition of human LCLC-103H cells incubated for 96 hrs by crystal violet assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity?
AID234273Selectivity is determined by the ratio of Ki for rat sigma 2 receptor to that of guinea pig sigma-1 receptor2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
Synthesis and structure-activity relationships of N-(1-benzylpiperidin-4-yl)arylacetamide analogues as potent sigma1 receptor ligands.
AID1063782Displacement of [3H](+)Pentazocine from sigma 1 receptor (unknown origin)2014Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.
AID420668Inhibition of human ERG in MCF7 cells2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.
AID171010Change in rectal temperature induced by DiPr-5,6-ADTN at a dose of 2.7 umol/kg of compound by subcutaneous administration1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID204304Ability to displace [3H]ditolylguanidine in the presence of 100 nM (+)-pentazocine from Sigma opioid receptor type 2 of rat liver2002Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22
Novel sigma receptor ligands. Part 2. SAR of spiro[[2]benzopyran-1,4'-piperidines] and spiro[[2]benzofuran-1,4'-piperidines] with carbon substituents in position 3.
AID176231Effective peroral dose for inhibition of conditioned avoidance response in rats1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.
AID298478Displacement of [3H]spiperone from human dopamine D2 receptor short form expressed in CHO cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID177826Effective dose against DOPA accumulation in rat brain striatal region after reserpine pretreatment by subcutaneous administration; No significant effect at 0.5 mg/kg intraperitoneal administration1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Novel dopamine receptor agonists and antagonists with preferential action on autoreceptors.
AID243273Binding affinity towards dopamine receptor D2 was determined2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
The role of QSAR in dopamine interactions.
AID63055Binding affinity towards cloned human Dopamine receptor D2 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor.
AID592127Induction of apoptosis in mouse B16F10 cells expressing sigma receptor assessed as viable cells using annexin V/propidium iodide staining at 5 uM after 24 hrs by flow cytometry (Rvb = 98.30%)2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Structure-activity study to develop cationic lipid-conjugated haloperidol derivatives as a new class of anticancer therapeutics.
AID1701184Displacement of [3H]-(+)-pentazocine from human sigma1 receptor expressed in HEK293 cell membranes incubated for 120 mins by liquid scintillation counting method2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
EST64454: a Highly Soluble σ
AID5321Binding affinity towards 5-hydroxytryptamine 2A receptor using [3H]ketanserin2003Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2
New arylpiperazine derivatives with high affinity for alpha1A, D2 and 5-HT2A receptors.
AID177506In vivo inhibition of apomorphine induced stereotypy in rat by the compound administered intraperitoneally1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID64601Neuroleptic activity in terms of [3H]spiroperidol binding in rat striatal membrane to Dopamine receptor D21991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Common stereospecificity of opioid and dopamine systems for N-butyrophenone prodine-like compounds.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID65239Binding affinity towards Dopamine receptor D21987Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.
AID33271Compound was evaluated In vitro for its activity by binding to Alpha adrenergic receptor in the rat brain using [3H]prazosin as radioligand.1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents.
AID170883Percentage change in Total activity (anti psychotic) when compound administered at a doe of 0.05 mg/kg ip in rats1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID1071721Therapeutic index, ratio of ED50 for induction of catalepsy to ED50 for antipsychotic activity in po dosed Kunming mouse assessed as reversal of apomorphine-induced cage climbing response2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics.
AID1185977Toxicity in ip dosed Sprague-Dawley rat assessed as catalepsy by Bar test2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Further evaluation of the tropane analogs of haloperidol.
AID342777Binding affinity to human cloned dopamine D2 receptor2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID303625Growth inhibition of human RT4 cells at 20 uM after 96 hrs relative to control2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Synthesis of bicyclic sigma receptor ligands with cytotoxic activity.
AID233472Hill coefficient for [3H]-Raclopride binding for high and low affinity binding to dopamine D2 receptor1999Bioorganic & medicinal chemistry letters, Aug-02, Volume: 9, Issue:15
Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor.
AID113686Inhibition of grooming-induced by SKF 38393 in mice.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID492634Antipsychotic activity in ip dosed NMRI mouse assessed as reduction in spontaneous exploratory locomotor activity administered 30 mins prior to testing measured for 60 mins2010Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors.
AID1213087Drug metabolism assessed as human liver microsomes assessed as velocity of O-glucuronidation at 100 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID63849Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone 1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID444007Selectivity for human sigma1 receptor over rat sigma2 receptor2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane.
AID1461564Displacement of [3H]spiperone from human D3 receptor expressed in CHO cell membranes by radioligand binding assay2017Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19
Potent haloperidol derivatives covalently binding to the dopamine D2 receptor.
AID113139Compound was tested in vivo for its ability to antagonize apomorphine-induced climbing response in mice upon intraperitoneal administration1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
Design of N-acylprolyltyrosine "tripeptoid" analogues of neurotensin as potential atypical antipsychotic agents.
AID177487Effect on Motor activity(MA) in rat was measured as ED50 by perorally administration of compound.1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
N6-(2,2-diphenylethyl)adenosine, a novel adenosine receptor agonist with antipsychotic-like activity.
AID5123In vitro binding affinity against rat 5-hydroxytryptamine 2 receptor.1993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study.
AID481104Displacement of [3H](+)-pentazocine from sigma1 receptor in guinea pig brain membrane2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID130133Neuroleptic activity in vivo by ability to antagonise climbing in apomorphine dosed mice after intraperitoneal administration.1985Journal of medicinal chemistry, Jun, Volume: 28, Issue:6
Synthesis and neuroleptic activity of 3-(1-substituted-4-piperidinyl)-1,2-benzisoxazoles.
AID87531In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.
AID1146536Inhibition of methamphetamine-induced stereotyped behavior in po dosed albino Wistar rat administered 2 hrs before methamphetamine challenge measured up to 3 hrs1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
AID457707Toxicity in CF1 mouse assessed as induction of motor impairment by measuring permanence time at 4 mg/kg, po by rotarod test (Rvb = 241.4 +/- 18.0 sec)2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors.
AID112818Compound was tested for inhibition of Apomorphine induced climbing in Mice1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.
AID1249734Displacement of [3H]spiperone from human dopamine D2L receptor expressed in CHO cells2015ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
Multicomponent Synthesis and Biological Evaluation of a Piperazine-Based Dopamine Receptor Ligand Library.
AID131420Potentiation against pentobarbital-induced sleeping, after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID317391Displacement of [3H]DTG from sigma2 receptor in Hartley guinea pig brain2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Synthesis and structure-activity relationships of N-(3-phenylpropyl)-N'-benzylpiperazines: Potent ligands for sigma1 and sigma2 receptors.
AID61151Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID1292386Serum clearance in psychotic patient (9 patients) at 3.5 +/- 1.2 mg, iv by reversed phase HPLC method based model-dependent approach analysis1987Psychopharmacology, , Volume: 91, Issue:4
Pharmacokinetics of haloperidol in psychotic patients.
AID65885Affinity against the dopamine receptor D2 using [3H]spiperinone.1995Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21
N-aryl-N'-benzylpiperazines as potential antipsychotic agents.
AID113351In vivo effective dose for inhibition of apomorphine-induced climbing in mice after intraperitoneal administration at a dose 20 mg/kg1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents.
AID22293Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID218670The compound was tested for inhibition of [3H]WB-4101 binding to alpha-1 adrenergic receptor of rat frontal cortex1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID197732Cataleptogenic activity was evaluated for the compound as the 50% effective dose required to induce cataleptic effect in rats1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Synthesis and neuroleptic activity of a series of 1-[1-(benzo-1,4-dioxan-2-ylmethyl)-4-piperidinyl]benzim idazolone derivatives.
AID578857Selectivity ratio, ratio of Ki for pig sigma1 receptor to Ki for pig sigma2 receptor2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Effect of structural modification in the amine portion of substituted aminobutyl-benzamides as ligands for binding σ1 and σ2 receptors.
AID178517Inhibition of conditioned avoidance response (CAR)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.
AID418677Cytotoxicity against human LCLC-103H cells after 96 hrs by crystal violet staining2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Dancing of the second aromatic residue around the 6,8-diazabicyclo[3.2.2]nonane framework: influence on sigma receptor affinity and cytotoxicity.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1638285Displacement of [3H]-DTG from sigma2 receptor in rat brain membranes after 120 mins in presence of (+)-pentazocine by radioligand binding assay
AID342773Binding affinity to human cloned 5HT6 receptor2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID5485Inhibition of [3H]ketanserin binding to rat frontal cortex membrane 5-hydroxytryptamine 2A receptor1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID1129883Displacement of [3H]-DTG from sigma-2 receptor in human RT4 cell membranes after 120 mins by scintillation counting analysis in presence of (+)-pentazocine2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
Synthesis, pharmacological evaluation, and σ1 receptor interaction analysis of hydroxyethyl substituted piperazines.
AID150405Compound was tested for its binding affinity towards Opioid receptors in rat membranes in the presence of [3H]naloxone1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
(+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties.
AID729692Antagonist activity at dopamine D2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Asymmetric total synthesis and identification of tetrahydroprotoberberine derivatives as new antipsychotic agents possessing a dopamine D(1), D(2) and serotonin 5-HT(1A) multi-action profile.
AID1308628Growth inhibition of human MCF7 cells incubated for 96 hrs by crystal violet assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity?
AID566432Displacement radioligand form dopamine D2 receptor in rat striatum by liquid scintillation counting2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Antiproliferative activity of phenylbutyrate ester of haloperidol metabolite II [(±)-MRJF4] in prostate cancer cells.
AID194525Effect of compound on (0.2 mg/kg ip) the concentration of 5-HT in rat mesolimbic region1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID592115Cytotoxicity against human MCF7 cells expressing sigma receptor at 0.5 to 50 uM after 48 hrs by MTT assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Structure-activity study to develop cationic lipid-conjugated haloperidol derivatives as a new class of anticancer therapeutics.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID194522Effect of compound on (0.2 mg/kg ip) the concentration of 5-HIAA in rat frontal cortex1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID152392Inhibitory activity against Opioid receptor sigma 1 isolated from whole rat membranes using [3H](+)-pentazocine as radioligand1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives.
AID36026Binding affinity against alpha-1 adrenergic receptor in rat brain using [3H]- WB-41011986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents.
AID274502Blockade of ABT-670-induced erctogenic activity in rat at 1 umol/kg, ip2006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction.
AID1184607Displacement of [3H]spiperone from human D2long receptor stably expressed in CHO cell membranes by competitive binding assay2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
Synthesis and binding profile of haloperidol-based bivalent ligands targeting dopamine D(2)-like receptors.
AID524792Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID346274Displacement of [3H](+)-pentazocine from opioid sigma1 receptor in guinea pig brain homogenate2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Relationships between the structure of 6-allyl-6,8-diazabicyclo[3.2.2]nonane derivatives and their sigma receptor affinity and cytotoxic activity.
AID141100Binding affinity towards human muscarinic receptor2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Selective optimization of side activities: another way for drug discovery.
AID63956Binding affinity was evaluated against Dopamine receptor D2 on rat striatum using [3H]spiperone as radioligand; ND = Not determined1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists.
AID1262302Displacement of [3H]DTG from sigma2 receptor in rat liver membranes by scintillation counting analysis2015Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
Benzo[7]annulene-based GluN2B selective NMDA receptor antagonists: Surprising effect of a nitro group in 2-position.
AID598496Displacement of [3H]-1,3-di(o-tolyl)guanidine from sigma 2 receptor in rat liver by scintillation analyzer2011Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10
Design, synthesis and pharmacological evaluation of spirocyclic σ(1) receptor ligands with exocyclic amino moiety (increased distance 1).
AID595908Displacement of [3H]DTG from sigma 2 receptor in guinea pig brain membranes after 120 mins2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Novel potent and selective σ ligands: evaluation of their agonist and antagonist properties.
AID65300Inhibition of [35 S] GTP gamma S binding to cell membranes expressing Dopamine receptor D31996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Novel (R)-2-amino-5-fluorotetralins: dopaminergic antagonists and inverse agonists.
AID763638Antipsychotic activity in CF1 mouse assessed as prevention of apomorphine-induced climbing behaviour at 0.5 mg/kg, po administered 30 mins prior apomorphine challenge measured 5 to 30 mins post challenge2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579.
AID1574666Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membranes after 120 mins by scintillation counting method2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Development of Novel Quinoxaline-Based κ-Opioid Receptor Agonists for the Treatment of Neuroinflammation.
AID37449Binding affinity towards alpha-1 adrenergic receptor using [3H]prazosin as radioligand.1995Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21
N-aryl-N'-benzylpiperazines as potential antipsychotic agents.
AID1744242Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes incubated for 1 hr in presence of 250 uM phenytoin liquid scintillation counting method2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management.
AID177879Inhibition of Sidman avoidance in rats after peroral administration1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines.
AID64625Inhibitory activity against methyl-phenidate-induced gnawing at dopamine receptor D2 in rat1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Characterization of potent and selective antagonists at postsynaptic 5-HT1A receptors in a series of N4-substituted arylpiperazines.
AID1823826Displacement of [3H]-methylspiperone from human D2 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
AID231522Ratio of binding affinity towards 5-HT2 to D2 receptor was measured1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study.
AID1213059Drug metabolism assessed as human liver microsomes assessed as N-glucuronide retention time at 100 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID196014Compound was evaluated in paw test for the hindlimb retraction at effective dose of 5 (mg/kg)2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors.
AID28233Fraction ionized (pH 7.4)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID61808Binding affinity towards human dopamine-4.2 receptor2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Selective optimization of side activities: another way for drug discovery.
AID1136350Neuroleptic activity in ip dosed Long-Evans rat assessed as inhibition of pole-climb avoidance1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 4. Central nervous system depressants.
AID186043Locomotor activity in male Wistar rats after a dose of 0.03 uM/kg, 30 min before 1 mg/kg of apomorphine administration1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.
AID204938Binding affinity for sigma-2 receptor measured on rat liver membranes using [3H]DTG as radioligand in the presence of (+)-pentazocine2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Synthesis and structure-activity relationships of naphthamides as dopamine D3 receptor ligands.
AID436796Selectivity for Wistar rat dopamine D2 receptor over Wistar rat dopamine D1 receptor2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Tetrahydroisoquinolines as dopaminergic ligands: 1-Butyl-7-chloro-6-hydroxy-tetrahydroisoquinoline, a new compound with antidepressant-like activity in mice.
AID1292387Terminal phase volume of distribution at steady state in psychotic patient (9 patients) at 3.5 +/- 1.2 mg, iv by reversed phase HPLC method based model-dependent approach analysis1987Psychopharmacology, , Volume: 91, Issue:4
Pharmacokinetics of haloperidol in psychotic patients.
AID737904Selectivity ratio of Ki for rat liver sigma2 receptor to rat brain sigma1 receptor2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Synthesis and evaluation of novel (18)F-labeled spirocyclic piperidine derivatives as σ1 receptor ligands for positron emission tomography imaging.
AID176767In vivo DOPA accumulation in non pre-treated rat striatal system following s.c. administration.1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID592129Induction of apoptosis in mouse B16F10 cells expressing sigma receptor assessed as early apoptotic cells using annexin V/propidium iodide staining at 5 uM after 24 hrs by flow cytometry (Rvb = 0.92%)2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Structure-activity study to develop cationic lipid-conjugated haloperidol derivatives as a new class of anticancer therapeutics.
AID351591Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane by solid scintillation analysis2009Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10
Synthesis of spirocyclic sigma1 receptor ligands as potential PET radiotracers, structure-affinity relationships and in vitro metabolic stability.
AID177742Activity to evoke catalepsy, after 5 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID231528Ratio of binding affinity towards D2 to muscarinic receptor (M) was measured1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study.
AID750620Therapeutic Index, ratio of ED50 for catalepsy in mouse to ED50 for antipsychotic activity in po dosed mouse assessed as reduction in apomorphine-induced climbing behavior2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID177489Effect on half-maximal decrease of DOPA formation in rat limbic regions1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
C1- and C3-methyl-substituted derivatives of 7-hydroxy-2-(di-n-propylamino)tetralin: activities at central dopamine receptors.
AID194376Effect of compound (0.2 mg/kg ip) on the concentration of DOPAC in rat striatum1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID228678Delta ED50 value by peroral administration (ED50 catalepsy-ED50 Climbing)1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID642495Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain homogenates after 180 mins by solid scintillation counting2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis, radiofluorination and pharmacological evaluation of a fluoromethyl spirocyclic PET tracer for central σ1 receptors and comparison with fluoroalkyl homologs.
AID1187744Antagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay2014Journal of medicinal chemistry, Aug-28, Volume: 57, Issue:16
Design, synthesis, and structure-activity relationship studies of a series of [4-(4-carboxamidobutyl)]-1-arylpiperazines: insights into structural features contributing to dopamine D3 versus D2 receptor subtype selectivity.
AID1300810Selectivity ratio of Ki for Sigma1 receptor in Dunkin Hartley guinea pig brain membrane to Ki for Sigma2 receptor in Sprague-Dawley rat liver membrane2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
One-pot synthesis and sigma receptor binding studies of novel spirocyclic-2,6-diketopiperazine derivatives.
AID4042Binding affinity was determined against 5-hydroxytryptamine 1A receptor using [3H]WB-41011995Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21
Piperazinylalkyl heterocycles as potential antipsychotic agents.
AID176327Body weight gain, after 2 hour period of conditioned feeding in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID194370Effect of compound (0.2 mg/kg ip) on the concentration of 5-HT in rat striatum1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID3656In vitro affinity towards 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand in hippocampus1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents.
AID1184608Displacement of [3H]spiperone from human D2short receptor stably expressed in CHO cell membranes by competitive binding assay2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
Synthesis and binding profile of haloperidol-based bivalent ligands targeting dopamine D(2)-like receptors.
AID1174074Displacement of [3H]DTG from sigma2 receptor in rat liver membranes after 180 mins by scintillation counting method2014Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23
Synthesis, GluN2B affinity and selectivity of benzo[7]annulen-7-amines.
AID1809449Antiangiogenic activity against VEGF-A stimulated Human endothelial cell assessed as cell proliferation measured after 72 hrs by crystal violet assay2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Haloperidol Metabolite II Valproate Ester (
AID4067Compound was tested for the Binding affinity against rat hippocampal 5-hydroxytryptamine 1A receptor by Radio ligand [3H]8-OH-DPAT binding assay.1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.
AID1062949Displacement of [3H]ketanserin from human 5-HT2A receptor2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis and biological evaluation of a series of aminoalkyl-tetralones and tetralols as dual dopamine/serotonin ligands.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID173003Blockade of uptake of the radiotracer in posterior cortex of rat1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Halogenated 4-(phenoxymethyl)piperidines as potential radiolabeled probes for sigma-1 receptors: in vivo evaluation of [123I]-1-(iodopropen-2-yl)-4-[(4-cyanophenoxy)methyl]pip eri dine.
AID665430Inhibition of human ERG expressed in CHO cells assessed as remaining activity at 10 uM by fluorescence-based assay2012European journal of medicinal chemistry, Jul, Volume: 53Microwave assisted synthesis of spirocyclic pyrrolidines -σ1 receptor ligands with modified benzene-N-distance.
AID177227Compound was evaluated for intracranial self-stimulation in rat after intraperitoneal administration.1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia.
AID190980Effect on dopamine agonist-induced rotation in unilaterally 6-OH-DA-lesioned rat at 0.5 mg/kg, ip; Compound 35 was injected subcutaneously at 75 mg/kg1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Troponoids. 6. Troponylpiperazines: a new class of dopamine agonists.
AID3669Binding affinity towards 5-hydroxytryptamine 1 receptor was measured using radioligand ([3H]5-HT) binding assay1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.
AID1308616Displacement of [3H]-di-o-tolylguanidine from sigma 2 receptor in rat liver membranes after 120 mins by scintillation counting analysis2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity?
AID386625Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID131366Effect on skeletal muscle tone, after 5 hour of peroral administration in mouse at dose 20 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID437145Inhibition of haloperidol-induced catalepsy in Swiss albino mouse assessed as time elapsed until release of forepaw from bar at 100 mg/kg, po administered 30 min prior to haloperidol challenge measured after 90 mins by bar test2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
Synthesis of some urea and thiourea derivatives of 3-phenyl/ethyl-2-thioxo-2,3-dihydrothiazolo[4,5-d]pyrimidine and their antagonistic effects on haloperidol-induced catalepsy and oxidative stress in mice.
AID239105Inhibitory constant against sigma receptor type 1 using 3 nM [3H]pentazocine2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands.
AID1756662Displacement of [3H]N-methylspiperone from human D3 receptor expressed in HEK293T cells co-expressing CRE-Luc incubated for 60 mins by microbeta scintillation counting method2021European journal of medicinal chemistry, Mar-15, Volume: 214Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the H
AID178680Antipsychotic activity determined in vivo by inhibition of amphetamine induced locomotor behavior in rats by the po administration.1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents.
AID1467942Displacement of [3H]-DTG from sigma 2 receptor (unknown origin) after 120 mins by liquid scintillation counting method2017Journal of medicinal chemistry, 12-14, Volume: 60, Issue:23
Novel Sigma Receptor Ligand-Nitric Oxide Photodonors: Molecular Hybrids for Double-Targeted Antiproliferative Effect.
AID173706Percent decrease on dopamine agonist-induced rotation in unilaterally 6-OH-DA-lesioned rat at 0.5 mg/kg1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Troponoids. 6. Troponylpiperazines: a new class of dopamine agonists.
AID243151Inhibitory concentration against potassium channel HERG2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors.
AID131054Inhibitory activity against tremorine-induced tremors, after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID4670Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.
AID1125905Ratio of Ki for human D3 receptor expressed in HEK293 cell membrane to Ki for human D2L receptor expressed in HEK cell membrane2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery, optimization, and characterization of novel D2 dopamine receptor selective antagonists.
AID45420Displacement of [3H]-spiperone from CHO-K1 cell membranes expressing human dopamine 3 receptors1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID63973Binding affinity for Dopamine receptor D2 by displacement of [3H]-spiperone2000Bioorganic & medicinal chemistry letters, Mar-06, Volume: 10, Issue:5
N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]cyclohexanecarboxamides as selective 5-HT1A receptor agonists.
AID1127303Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in Dunkin Hartley guinea pig membrane after 180 mins by liquid scintillation counting analysis2014European journal of medicinal chemistry, May-22, Volume: 79Synthesis and biological evaluation of a novel sigma-1 receptor antagonist based on 3,4-dihydro-2(1H)-quinolinone scaffold as a potential analgesic.
AID448643Displacement of [3H]di-o-tolylguanidine from sigma 2 receptor in rat liver after 180 mins by scintillation counting2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Synthesis of sigma receptor ligands with unsymmetrical spiro connection of the piperidine moiety.
AID26362Ionization constant (pKa)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID751711Displacement of [3H]Haloperidol from sigma 1 receptor in human jurkat cells at 10 uM after 4 hrs relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
AID1213063Drug metabolism assessed as recombinant human UGT1A4 assessed as velocity of N-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1187745Antagonist activity against human D2LR expressed in CHOK1 cells assessed as inhibition of pergolide-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay2014Journal of medicinal chemistry, Aug-28, Volume: 57, Issue:16
Design, synthesis, and structure-activity relationship studies of a series of [4-(4-carboxamidobutyl)]-1-arylpiperazines: insights into structural features contributing to dopamine D3 versus D2 receptor subtype selectivity.
AID65565In vitro Dopamine receptor D2 affinity by using [3H]spiperone as the radioligand in rat limbic system at 1 uM concentration of compound; value may range from 0.7 to 3.51987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Antipsychotic activity of substituted gamma-carbolines.
AID1213084Drug metabolism assessed as human liver microsomes assessed as O-glucuronide measured at 200 uM by LC-MS/MS analysis in presence of 10 uM gemfibrozil relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID177816Compound was evaluated in vivo its antagonist activity against apomorphine induced behavioral syndrome such as Stereotypy in rat after intraperitoneal administration1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Potential neuroleptic agents. 3. Chemistry and antidopaminergic properties of substituted 6-methoxysalicylamides.
AID5567In vitro binding affinity at serotonin 5-hydroxytryptamine 2A receptor in rat cortical membrane2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors.
AID259126Selectivity ratio for dopamine D1-like receptor over dopamine D3 receptor2006Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2
Design of novel hexahydropyrazinoquinolines as potent and selective dopamine D3 receptor ligands with improved solubility.
AID750619Therapeutic Index, ratio of ED50 for catalepsy in mouse to ED50 for antipsychotic activity in po dosed mouse assessed as reduction in MK-801-induced hyperactivity2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID750623Antipsychotic activity in po dosed mouse assessed as reduction in MK-801-induced hyperactivity administered for 30 mins prior to MK-801-challenge measured after 90 mins2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID64435In vivo binding affinity against dopamine (D2) receptor in rat caudate-putamen tissue using [3H]nemonapride as radioligand2003Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22
Synthesis and affinity of a possible byproduct of electrophilic radiolabeling of [123I]IBZM.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID131045Inhibition of spontaneous motor activity, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID1690393Displacement of [3H]-methylspiperone from recombinant human D2 receptor expressed in CHOK1 cell membranes measured after 60 mins by microbeta counting method2020European journal of medicinal chemistry, Apr-01, Volume: 191Multifunctional 6-fluoro-3-[3-(pyrrolidin-1-yl)propyl]-1,2-benzoxazoles targeting behavioral and psychological symptoms of dementia (BPSD).
AID61623Binding affinity to the dopamine receptor D2L in rat brain membranes1999Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.
AID128818Antagonistic activity against amphetamine-induced hypermotility, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID204763Binding affinity towards sigma receptor binding site 1 using [3H](+)-pentazocine1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
AID1308626Growth inhibition of human RT4 cells incubated for 96 hrs by crystal violet assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity?
AID65560Binding towards Dopamine receptor D2 using [3H]spiperone from rat striatal membrane1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID458644Reduction in spontaneous locomotor activity in Sprague-Dawley rat striatum at 1 umol/kg, sc relative to control2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
AID1136419Inhibition of dopamine-sensitive rat brain adenylyl cyclase activity assessed as cAMP level1978Journal of medicinal chemistry, Sep, Volume: 21, Issue:9
Synthesis and biological evaluation of some 2-amino-4-aryl-3H-1,5-benzodiazepine analogues of clozapine.
AID547622Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.
AID238882Inhibition of [3H]ketanserin binding to rat 5-hydroxytryptamine 2A receptor2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies.
AID674896Displacement of [3H]DTG from sigma2 receptor in Sprague-Dawley rat liver membrane after 90 mins by liquid scintillation counting in presence of pentazocine2012Bioorganic & medicinal chemistry, Aug-15, Volume: 20, Issue:16
Syntheses and in vitro evaluation of decalinvesamicol analogues as potential imaging probes for vesicular acetylcholine transporter (VAChT).
AID1724115Antipsychotic activity in po dosed mouse assessed as suppression of apomorphine-induced climbing behaviour2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID63233Ratio of binding affinity for D2 and D4 dopamine receptors2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species.
AID128670Antagonism of apomorphine-induced climbing behavior in mice after ip administration1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2.
AID177951Antagonistic activity against apomorphine-induced stereotypy, after 5 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID1213089Drug metabolism assessed as recombinant human UGT1A4 assessed as O-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1330102Displacement of [3H]pentazocine from guinea pig sigma1 receptor measured after 90 mins by microbeta scintillation counting method2016Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
AID133857Anticonvulsant activity against pentylenetetrazole-induced convulsions, after 1 hour of peroral administration in mouse at a dose of 9.4 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID177731Inhibition against conditioned avoidance response, after 1 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID1256683Neurotoxicity in Chinese Kun Ming mouse assessed as locomotor activity by measuring total distance traveled at 0.3 mg/kg, po administered 1 hr before test measured for 10 mins (Rvb = 13415.6 +/- 9555.8 millimeter)2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
AID776366Selectivity ratio of Ki for sigma-2 receptor in rat liver membrane to Ki for sigma-1 receptor in guinea pig brain cortex membrane2013European journal of medicinal chemistry, Nov, Volume: 69New combination of pharmacophoric elements of potent σ₁ ligands: design, synthesis and σ receptor affinity of aminoethyl substituted tetrahydrobenzothiophenes.
AID62769Binding affinity towards human Dopamine receptor D21999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID62908Ability to displace [3H]spiperone from human cloned Dopamine receptor D2 expressed in CHO K-1 cells in vitro.1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents.
AID180185The compound was evaluated for the conditioned avoidance response data (CAR) in rat intra peritoneally1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects.
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID1759955Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membrane by solid scintillation counting method
AID132128Tested in vivo for their ability to antagonize the apomorphine induced stereotypy response in mice1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents.
AID243275Binding affinity towards dopamine receptor D4 was determined2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
The role of QSAR in dopamine interactions.
AID1823674Displacement of [3H]-N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
AID1712207Selectivity ratio of Ki for displacement of [3H]-DTG from sigma2 receptor in guinea pig brain membrane to Ki for displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane2016Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14
New bifunctional antioxidant/σ1 agonist ligands: Preliminary chemico-physical and biological evaluation.
AID1213073Drug metabolism assessed as recombinant human UGT1A9 assessed as O-glucuronidation measured as inhibition constant at 10 to 400 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1558961Displacement of [3H]-(+)-pentazocine from human sigma-1 receptor expressed in HEK293 membranes incubated for 120 mins by liquid scintillation counting method2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual μ-Opioid Receptor Agonists and σ
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID62009Displacement of [3H]YM-09151 from recombinant African green monkey Dopamine receptor D21995Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
2-Phenyl-4-(aminomethyl)imidazoles as potential antipsychotic agents. Synthesis and dopamine D2 receptor binding.
AID1393369Selectivity index, ratio of pKi for 5-HT2AR to pKi for human D2LR
AID1693538Antipsychotic activity in ip dosed Swiss Webster mouse assessed as inhibition of apomorphine-induced climbing behaviour pretreated with compound for 30 mins followed by APO challenge and measured after 15 to 20 mins2021Bioorganic & medicinal chemistry, 01-15, Volume: 30A study of the structure-affinity relationship in SYA16263; is a D
AID1185663Displacement of [3H]-DTG from sigma-2 receptor in rat liver membrane in presence of (+)-pentazocine2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted κ-opioid receptor agonists.
AID177498In vivo inhibition of amphetamine induced stereotypy in rat by the compound administered intraperitoneally1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID1211293Unbound fraction in plasma (unknown origin) under normal atmospheric condition at pH 7.22 after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID1853691Cytotoxicity against mouse J774.A1 cells assessed as reduction in cell viability at 50 uM incubated for 24 hrs by resazurin assay2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from
AID458635Activity at dopamine D2L receptor expressed in HEK293 cells coexpressing Galphaqi5 assessed as maximal efficacy relative to control2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
AID635314Displacement of [125I]IAF from sigma 1 receptor in human RT4 cells at 10 uM after 30 mins preincubation by photoaffinity labeling experiment2011Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24
Electron-donating para-methoxy converts a benzamide-isoquinoline derivative into a highly Sigma-2 receptor selective ligand.
AID4804Binding affinity against serotonin-2 receptor in rat brain using [3H]spiroperidol1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents.
AID61193Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1221965Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID63514Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
(Aryloxy)alkylamines as selective human dopamine D4 receptor antagonists: potential antipsychotic agents.
AID205268Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID180915The inhibitory effect on the continuous avoidance was expressed as the dose to increase the number of electroshocks by 60% of the rats1981Journal of medicinal chemistry, Oct, Volume: 24, Issue:10
Synthesis and neuroleptic activity of benzamides. Cis-N-(1-benzyl-2-methylpyrrolidin-3-yl)-5-chloro-2-methoxy-4-(methylamino)benzamide and related compounds.
AID1823687Antagonist activity at human dopamine D3 opioid receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BR
AID323225Displacement of [3H](+)-pentazocine from sigma 1 opioid receptor in guinea pig brain membrane2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Synthesis and structure-affinity relationships of novel spirocyclic sigma receptor ligands with furopyrazole structure.
AID547804Selectivity window, ratio of EC50 for BESM cells to EC50 for Trypanosoma cruzi amastigotes infected in BESM cells2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.
AID1191389Displacement of [3H]DTG from rat liver sigma2 receptor by scintillation analyzer2015European journal of medicinal chemistry, Jan-27, Volume: 90Improving selectivity preserving affinity: new piperidine-4-carboxamide derivatives as effective sigma-1-ligands.
AID1667343Binding affinity to human D2 receptor2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Identification of C10 nitrogen-containing aporphines with dopamine D
AID751847Binding affinity to human sigma receptor by radioligand displacement assay2013European journal of medicinal chemistry, May, Volume: 63Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
AID134417Lethal dose in mice after perorla administration1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
4-Piperazinyl-10H-thieno[2,3-b][1,5]benzodiazepines as potential neuroleptics.
AID724160Selectivity index, ratio of Ki for sigma2 receptor in rat liver membranes to Ki for sigma1 receptor in rat brain membranes2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Synthesis and biological evaluation of ¹⁸F labeled fluoro-oligo-ethoxylated 4-benzylpiperazine derivatives for sigma-1 receptor imaging.
AID1213050Drug metabolism assessed as recombinant human UGT1A8 assessed as N-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID61616Inhibition of [35S]GTP-gamma-S, binding to cell membranes expressing dopamine D2A receptor at 1 uM dopamine1999Bioorganic & medicinal chemistry letters, Aug-02, Volume: 9, Issue:15
Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor.
AID177251Compound was evaluated for pole-climb avoidance in rat after peroral administration.1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia.
AID3730Binding affinity towards serotonin 5-HT1A receptor was determined in rat hippocampus using [3H]8-OH-DPAT as ligand1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID277974Displacement of [3H]ketanserin from rat cortex 5HT2A receptor2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.
AID1809447Antiangiogenic activity against VEGF-A stimulated human retinal endothelial cell assessed as cell proliferation measured after 24 hrs by crystal violet assay2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Haloperidol Metabolite II Valproate Ester (
AID184995Compound is evaluated for locomotor activity in nonpretreated habituated rats at 1.6 micro mol/kg of subcuteneous dose1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1136415Antipsychotic activity in mouse assessed as protection against amphetamine-induced lethality at 50 mg/kg, ip treated 30 mins before amphetamine challenge1978Journal of medicinal chemistry, Sep, Volume: 21, Issue:9
Synthesis and biological evaluation of some 2-amino-4-aryl-3H-1,5-benzodiazepine analogues of clozapine.
AID238778In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.42004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand.
AID61617Inhibition of [35S]GTP-gamma-S, binding to cell membranes expressing dopamine D2A receptors at 10 uM1999Bioorganic & medicinal chemistry letters, Aug-02, Volume: 9, Issue:15
Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor.
AID619547Displacement of (+)-[3H]pentazocine from guinea pig brain sigma 1 receptor after 180 mins by scintillation counting2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Combination of two pharmacophoric systems: synthesis and pharmacological evaluation of spirocyclic pyranopyrazoles with high σ₁ receptor affinity.
AID63692Selectivity is the ratio of binding affinities for human Dopamine receptor D4 to that of Dopamine receptor D32002Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
Design and synthesis of a piperazinylalkylisoxazole library for subtype selective dopamine receptor ligands.
AID135326BBB penetration classification2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
Predicting blood-brain barrier permeation from three-dimensional molecular structure.
AID5053Compound was tested for the inhibition of quipazine induced head twitches in rats1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles.
AID753962Displacement of [3H]DTG from sigma2 receptor in Sprague-Dawley rat liver membrane after 150 mins by liquid scintillation counting analysis2013European journal of medicinal chemistry, Jun, Volume: 64Synthesis and receptor binding studies of novel 4,4-disubstituted arylalkyl/arylalkylsulfonyl piperazine and piperidine-based derivatives as a new class of σ1 ligands.
AID1300372Toxicity in Kun Ming mouse assessed as reduction in spontaneous locomotor activity by measuring total distance traveled at 0.1 mg/kg, po administered 30 mins prior to testing measured after 30 to 120 mins (Rvb = 24881.4 +/- 9545.8 mm)2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Synthesis and Biological Evaluation of Novel σ1 Receptor Ligands for Treating Neuropathic Pain: 6-Hydroxypyridazinones.
AID170896Percentage change in chronic single unit sampling when compound given at a dose of 0.5 mg/kg ip in rats (Expt-2)1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID391274Displacement of [3H]ketanserin from human cloned 5HT2A receptor2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Synthesis, binding affinity, and molecular docking analysis of new benzofuranone derivatives as potential antipsychotics.
AID61670Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D11991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Synthesis and antidopaminergic activity of some 3-(aminomethyl)tetralones as analogues of butyrophenone.
AID729708Agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Asymmetric total synthesis and identification of tetrahydroprotoberberine derivatives as new antipsychotic agents possessing a dopamine D(1), D(2) and serotonin 5-HT(1A) multi-action profile.
AID1125902Displacement of [3H]methylspiperone from human D2L receptor expressed in HEK cell membrane after 90 mins by scintillation counting analysis2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery, optimization, and characterization of novel D2 dopamine receptor selective antagonists.
AID113189In vivo antipsychotic activity measured by the inhibition of apomorphine-induced climbing behavior in mice after 30 min po administration.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID205267Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID176733Dose (administered orally) inhibiting amphetamine-induced locomotor behavior in rats1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID142500In vitro inhibition of [3H]-Oxo-Mas binding to M1 and M4 receptors in rat brain homogenate; Not tested.1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Muscarinic agonists with antipsychotic-like activity: structure-activity relationships of 1,2,5-thiadiazole analogues with functional dopamine antagonist activity.
AID5330Inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor rat frontal cortex membrane1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
Synthesis and atypical antipsychotic profile of some 2-(2-piperidinoethyl)benzocycloalkanones as analogues of butyrophenone.
AID750624Antipsychotic activity in po dosed mouse assessed as reduction in apomorphine-induced climbing behavior administered for 30 mins prior to apomorphine-challenge measured at 10 to 30 mins post-dose2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID129967Compound was evaluated for inhibition of apomorphine-induced climbing in mouse after intraperitoneal administration.1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia.
AID1213066Intrinsic clearance in human liver microsomes measured per mg of protein at 10 to 400 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1704747Antipsychotic activity in Kunming mouse assessed as inhibition of apomorphine-induced climbing behavior administered orally 30 mins prior to apomorphine challenge and measured for 10 to 30 mins
AID61495Binding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligand1994Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.
AID64645Binding affinity for dopamine receptor D2 long expressed in Sf9 cells using [125I]IABN radioligand2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Synthesis and structure-activity relationships of naphthamides as dopamine D3 receptor ligands.
AID5205In vitro binding affinity towards 5-hydroxytryptamine 2A receptor in human using [3H]ketanserin as radioligand2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.
AID1215120Binding affinity to Wistar rat brain lipid by TRANSIL assay2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID64000In vitro binding affinity for Dopamine receptor D22001Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10
Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic?
AID5490Inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor from rat brain1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.
AID36016Displacement of [3H]prazosin from rat brain Alpha-1 adrenergic receptor1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID1125903Displacement of [3H]methylspiperone from human D3 receptor expressed in HEK293 cell membrane after 90 mins by scintillation counting analysis2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Discovery, optimization, and characterization of novel D2 dopamine receptor selective antagonists.
AID1782424Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
2-Phenylcyclopropylmethylamine Derivatives as Dopamine D
AID243422log (1/Km) value for human liver microsome cytochrome P450 3A42005Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
Modeling K(m) values using electrotopological state: substrates for cytochrome P450 3A4-mediated metabolism.
AID36199Binding affinity towards human alpha-2 adrenergic receptor2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Selective optimization of side activities: another way for drug discovery.
AID1853655Antibacterial activity against Mycobacterium tuberculosis mc2 6230 with Eis C-14T mutation assessed as inhibition of bacterial growth incubated upto 3 weeks hrs by resazurin dye based double-dilution method2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from
AID596432Biodistribution in haloperidol-pretreated ICR mouse blood at 1 mg/kg, iv pretreated 5 mins before haloperidol challenge measured after 60 mins postinjection (Rvb = 1.32 +/- 0.41 %ID/g)2011Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9
Synthesis and biological evaluation of novel 4-benzylpiperazine ligands for sigma-1 receptor imaging.
AID1213044Drug metabolism assessed as recombinant human UGT2B17 assessed as O-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1478364Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane after 150 mins by liquid scintillation counting method2018Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
(+)-Methyl (1R,2S)-2-{[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]methyl}-1-phenylcyclopropanecarboxylate [(+)-MR200] Derivatives as Potent and Selective Sigma Receptor Ligands: Stereochemistry and Pharmacological Properties.
AID277668Selectivity for dopamine D3 over dopamine D22007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.
AID672167Inhibition of human ERG expressed in CHO cells after 30 mins by Rb+ flux assay2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Hit-to-lead investigation of a series of novel combined dopamine D2 and muscarinic M1 receptor ligands with putative antipsychotic and pro-cognitive potential.
AID1169865Effect on spontaneous exploratory locomotor activity in sc dosed NMRI mouse measured for 30 mins with activity counts each 5 mins2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.
AID64993Binding affinity towards cloned human Dopamine receptor D3 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor.
AID131722Effective dose for inhibition of norepinephrine induced lethality in mouse1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.
AID342787Binding affinity to human SERT2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID160788In vitro inhibition of recombinant HIV-2 protease expressed in Escherichia coli strain X901994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Haloperidol-based irreversible inhibitors of the HIV-1 and HIV-2 proteases.
AID37475Compound was evaluated for its binding affinity with Alpha-1 adrenergic receptor using membranes prepared from rat cerebral cortex1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Orally active benzamide antipsychotic agents with affinity for dopamine D2, serotonin 5-HT1A, and adrenergic alpha1 receptors.
AID1292378Hepatic extraction ratio in psychotic patient (9 patients) at 3.5 +/- 1.2 mg, iv by reversed phase HPLC method1987Psychopharmacology, , Volume: 91, Issue:4
Pharmacokinetics of haloperidol in psychotic patients.
AID1136362Non-specific toxicity in po dosed Beagle dog assessed as inhibition of apomorphine hydrochloride-induced emesis1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 4. Central nervous system depressants.
AID1389776Reversal of methamphetamine-induced hyperlocomotion in ICR mouse at 0.3 mg/kg, po pretreated 60 mins post habituation followed by methamphetamine injection after 60 mins measured for 150 mins2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Design and synthesis of 1-(1-benzothiophen-7-yl)-1H-pyrazole, a novel series of G protein-coupled receptor 52 (GPR52) agonists.
AID232558Ratio of ED50 for induction of catalepsy to ED50 for antagonism of apomorphine induced climbing1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents.
AID205033Binding affinity against serotonin-1 receptor in rat brain using [3H]5-HT1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents.
AID1853645Competitive inhibition of Mycobacterium tuberculosis Eis assessed as reduction in Eis-mediated kanamycin acetylation preincubated for 10 mins followed by substrate addition and measured for 2 to 5 mins using acetyl-CoA as substrate in presence of kanamyci2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from
AID204014Binding affinity of compound towards sigma receptor using [3H]DTG (4 nM) ligand in hippocampus rat was determined1997Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands.
AID5061Affinity for 5-hydroxytryptamine 2 receptor binding sites by its ability to displace [3H]spiperone from rat frontal cortex.1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID1213090Drug metabolism assessed as recombinant human UGT1A4 assessed as N-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID5381Selectivity ratio towards 5-hydroxytryptamine 2A receptor to Dopamine receptor D2 (5-HT2A/D2 )2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID418679Cytotoxicity against human MCF7 cells after 96 hrs by crystal violet staining2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Dancing of the second aromatic residue around the 6,8-diazabicyclo[3.2.2]nonane framework: influence on sigma receptor affinity and cytotoxicity.
AID62915Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D2 in CHO cells2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.
AID603955In-vivo blood to lung partition coefficients of the compound, logP(lung) in rat2008European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
Air to lung partition coefficients for volatile organic compounds and blood to lung partition coefficients for volatile organic compounds and drugs.
AID1690210Displacement of [3H]DTG from sigma 2 receptor in rat liver membranes incubated for 120 mins by scintillation counting method
AID5703Binding affinity towards 5-HT2C receptor from rat using [3H]mesulergine as radioligand1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID578856Displacement of [3H]ditolylguanidine from sigma2 receptor in guinea pig brain membrane2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Effect of structural modification in the amine portion of substituted aminobutyl-benzamides as ligands for binding σ1 and σ2 receptors.
AID61415Binding affinity towards Dopamine receptor D2 was determined in rat striatal homogenate using [3H]- spiperone as radioligand1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID1335650Induction of catalepsy in po dosed Chinese Kun Ming mouse assessed as increase in unwanted extrapyramidal motor disturbances measured for 60 seconds2016European journal of medicinal chemistry, Nov-29, Volume: 124Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.
AID27370Lethal dose after peroral administration in mouse1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.
AID5836In vitro ability to displace [3H]mesulergine binding from 5-hydroxytryptamine 2C receptor from bovine choroid plexus.1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical an
AID592683Apparent permeability from basolateral side to apical side of human Caco2 cells by LC/MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID751647Displacement of [3H]Haloperidol from sigma 1 receptor in human jurkat cells after 4 hrs2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
AID176339Compound was tested in vivo for its ability to induce catalepsy in rats upon intraperitoneal administration1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
Design of N-acylprolyltyrosine "tripeptoid" analogues of neurotensin as potential atypical antipsychotic agents.
AID181191Antagonism of SKF 10047 -induced hypermotility (% vs controls) dose(mg/Kg po) = 21998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.
AID1283242Decrease in lanosterol levels in mouse Neuro2a cells by LC-MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts.
AID28235Unbound fraction (plasma)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID229628Selectivity ratio for serotonin 5-HT2A to that of dopamine D2 receptors2004Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics.
AID5614Binding affinity towards human serotonin 5-hydroxytryptamine 2C receptor2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Selective optimization of side activities: another way for drug discovery.
AID190819Total activity (anti psychotic) when compound administered at a doe of 0.125 mg/kg ip in rats1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID176371Conditioned avoidance response activity was determined by the ability to block the conditioned avoidance of a foot shock (ip)1995Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21
N-aryl-N'-benzylpiperazines as potential antipsychotic agents.
AID1664379Displacement of [3H]N-methylspiperone from dopamine D2 receptor (unknown origin)2020Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
Synthesis and dopamine receptor pharmacological evaluations on ring C ortho halogenated 1-phenylbenzazepines.
AID320558Displacement of [3H]DTG from sigma 2 receptor in rat liver membrane2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Tritium radiolabelling of PB28, a potent sigma-2 receptor ligand: pharmacokinetic and pharmacodynamic characterization.
AID178197Effective dose in blocking conditioned avoidance responding (CAR) in the rat when administered intraperitoneally1989Journal of medicinal chemistry, May, Volume: 32, Issue:5
Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy.
AID1213061Drug metabolism assessed as recombinant human UGT2B7 assessed as velocity of O-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID231370Ratio representing inhibitory activity against spontaneous locomotor behavior to inhibitory activity against amphetamine-induced stereotypy in rats1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID171691Catalytic action on male Wistar rats after subcutaneous administration of 0.3 mg/kg dose of compound1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.
AID63074Displacement of the radioligand [3H]spiperone from the cloned human Dopamine receptor D2 long expressed in CHO cells2002Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
Design and synthesis of a piperazinylalkylisoxazole library for subtype selective dopamine receptor ligands.
AID1262301Displacement of [3H]-(+)-Pentazocine from sigma1 receptor in guniea pig brain cortex membranes by scintillation counting analysis2015Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
Benzo[7]annulene-based GluN2B selective NMDA receptor antagonists: Surprising effect of a nitro group in 2-position.
AID36849Binding affinity towards alpha-1 adrenergic receptor from rat brain membranes using [3H]prazosin as radioligand1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID205150The compound was tested for its ability to induced catalepsy in squirrel monkeys1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents.
AID1393474Toxicity in ip dosed Sprague-Dawley rat assessed as induction of catalepsy measured every 30 mins up to 240 mins by bar test
AID1136346Neuroleptic activity in ip dosed Sprague-Dawley rat assessed as inhibition of Sidman avoidance measured for 4 to 6 hrs1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 4. Central nervous system depressants.
AID131206Contractile activity in skeletal muscles, after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID1272498Binding affinity to sigma-2 receptor (unknown origin) by radioligand displacement assay2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Role of the phenolic OH moiety of GluN2B-selective NMDA antagonists with 3-benzazepine scaffold.
AID1744243Ratio of Ki for displacement of [3H]-(+)-pentazocine from sigma-1 receptor to Ki for displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes in presence of phenytoin2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management.
AID1593893Displacement of [3H]-Pentazocine from sigma 1 receptor (unknown origin) expressed in HEK293T cell membranes2019Bioorganic & medicinal chemistry, 06-15, Volume: 27, Issue:12
New analogs of SYA013 as sigma-2 ligands with anticancer activity.
AID346278Displacement of [3H]MK-801 from NMDA receptor in pig brain cortex at 1 uM2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Relationships between the structure of 6-allyl-6,8-diazabicyclo[3.2.2]nonane derivatives and their sigma receptor affinity and cytotoxic activity.
AID5569In vitro binding affinity towards 5-hydroxytryptamine 2A receptor in rat tissue homogenate using [3H]ketanserin as radioligand2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.
AID1128476Toxicity in rat step-down latency model assessed as frank catalepsy at 30 mg/kg2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.
AID1292385Serum clearance in psychotic patient (9 patients) at 3.5 +/- 1.2 mg, iv by reversed phase HPLC method based model-independent approach analysis1987Psychopharmacology, , Volume: 91, Issue:4
Pharmacokinetics of haloperidol in psychotic patients.
AID62445Inhibition of [3H]dopamine binding to Dopamine receptor in calf caudate nuclei.1980Journal of medicinal chemistry, Sep, Volume: 23, Issue:9
Synthesis of 8-aryltetrahydroisoquinolines as dopamine antagonists and evaluation for potential neuroleptic activity.
AID1272497Binding affinity to sigma-1 receptor (unknown origin) by radioligand displacement assay2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Role of the phenolic OH moiety of GluN2B-selective NMDA antagonists with 3-benzazepine scaffold.
AID65733In vitro binding affinity towards Dopamine receptor D2 in rat tissue homogenate using [3H]-spiperone as radioligand2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.
AID3736Binding affinity to 5-hydroxytryptamine 1A receptor in the rat brain using [3H]8-hydroxy-2-(di-n-propylamine)tetralin as radioligand.1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents.
AID3688Affinity for 5-hydroxytryptamine 1 receptor1998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.
AID342779Binding affinity to human cloned dopamine D4 receptor2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID1762064Antipsychotic activity in po dosed mouse assessed as suppression of apomorphine-induced climbing behaviour2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID61375Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID238274Binding affinity for Dopamine receptor D42005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.
AID672166Intrinsic clearance in human liver microsomes at 1 uM after 60 mins2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Hit-to-lead investigation of a series of novel combined dopamine D2 and muscarinic M1 receptor ligands with putative antipsychotic and pro-cognitive potential.
AID321565Displacement of [3H]DTG from opioid sigma2 receptor in rat brain homogenate2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Conversion of a highly selective sigma-1 receptor-ligand to sigma-2 receptor preferring ligands with anticocaine activity.
AID1184611Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
Synthesis and binding profile of haloperidol-based bivalent ligands targeting dopamine D(2)-like receptors.
AID1877932Displacement of [3H]-(+)-pentazocine from Dunkin-Hartley guinea pig brain cortex Sigma 1 receptor incubated for 150 mins by liquid scintillation counting analysis2022European journal of medicinal chemistry, Feb-15, Volume: 230Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation.
AID1461567Selectivity index, ratio of Ki for human dopamine D4.4 receptor expressed in CHO cell membranes to Ki for human D2short receptor expressed in CHO cell membranes2017Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19
Potent haloperidol derivatives covalently binding to the dopamine D2 receptor.
AID1558958Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation at 10 uM incubated for 45 mins by HTRF assay2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual μ-Opioid Receptor Agonists and σ
AID194524Effect of compound on (0.2 mg/kg ip) the concentration of 5-HT in rat frontal cortex1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID737844Displacement of [3H]-di-o-tolylguanidine from sigma 2 receptor in rat liver membranes after 120 mins by scintillation counting analysis2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Improvement of σ1 receptor affinity by late-stage C-H-bond arylation of spirocyclic lactones.
AID175752Effect on DOPA accumulation level at an intraperitoneal dose of 0.5 mg/kg in rat1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Dopamine autoreceptor agonists as potential antipsychotics. 2. (Aminoalkoxy)-4H-1-benzopyran-4-ones.
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID1215121Fraction unbound in Wistar rat brain homogenate at 5 uM after 5 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID231369Ratio representing inhibitory activity against catalepsy to inhibitory activity against amphetamine-induced locomotor behavior in rats1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID1215943Metabolic stability in human intestinal S9 fraction assessed as compound remaining at 50 to 1000 nM after 60 mins by HPLC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Significance of reductive metabolism in human intestine and quantitative prediction of intestinal first-pass metabolism by cytosolic reductive enzymes.
AID194371Effect of compound (0.2 mg/kg ip) on the concentration of DA in rat frontal cortex1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID1197503Displacement of [3H]DTG from sigma 1 receptor in human Jurkat cells after 60 mins by liquid scintillation counting analysis in presence of pentazocine2015European journal of medicinal chemistry, Mar-06, Volume: 92Synthesis and pharmacological evaluation of benzannulated derivatives as potent and selective sigma-1 protein ligands.
AID1210072Inhibition of CYP2C9 in human liver microsomes using tolbutamide substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID1409614Overall antiviral activity against SARS-CoV-2 (isolate France/IDF0372/2020) in the Vero E6 cell line at 48 h based on three assays 1) detection of viral RNA by qRT-PCR (targeting the N-gene), 2) plaque assay using lysate 3 days after addition of compound 2020Nature, 07, Volume: 583, Issue:7816
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID298494Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID61236Compound was tested in vivo for induction of catalepsy against dopamine receptor D2 in rats1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles.
AID1456401Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membrane incubated for 120 mins measured for 5 mins by scintillation counting method
AID238889In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.42004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand.
AID1213078Drug metabolism assessed as recombinant human UGT1A9 assessed as O-glucuronidation at 25 to 200 uM incubated for 60 mins by LC-MS/MS analysis in presence of 10 uM gemfibrozil relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID5013Compound was tested for its binding affinity towards 5-hydroxytryptamine 2 receptor using [3H]ketanserin from guinea pig frontal cortex1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1546912Displacement of [3H]spiperone from human D4.2 receptor expressed in CHO-K1 cells at 10 uM by radioligand competitive binding analysis relative to control
AID1762087Therapeutic index, ratio of ED50 for induction of catalepsy in po dosed mouse to ED50 for antipsychotic activity in po dosed mouse assessed as reduction in MK-801-induced hyperlocomotor activity2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID63387Cataleptogenic effect against cloned human Dopamine receptor D2 in male Sprague-Dawley rats in a bar test2003Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21
The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+.
AID176499Compound is measured for inhibition of catalepsy in rat by peroral administration of compound1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID177716Induction of catalepsy in nonfasted male Sprague-Dawley rats (dose that produced catalepsy in 50% of the animals)1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Buspirone analogues. 1. Structure-activity relationships in a series of N-aryl- and heteroarylpiperazine derivatives.
AID1415568Displacement of [3H]-(+)-MK-801 from PCP binding site of NMDA receptor in pig brain cortex membranes after 90 mins by scintillation counting method2017MedChemComm, May-01, Volume: 8, Issue:5
Do GluN2B subunit containing NMDA receptors tolerate a fluorine atom in the phenylalkyl side chain?
AID63797In vitro by displacement of [3H]raclopride from Dopamine receptor D2 on rat striatal membrane1997Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation.
AID598813Displacement of [3H]SCH233930 from human D1 receptor expressed in HEK cells2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Molecular hybridization of 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecane-3-ol with sigma (σ) receptor ligands modulates off-target activity and subtype selectivity.
AID63512Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.
AID724159Displacement of [3H]ditolyguanidine from sigma2 receptor in rat liver membranes2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Synthesis and biological evaluation of ¹⁸F labeled fluoro-oligo-ethoxylated 4-benzylpiperazine derivatives for sigma-1 receptor imaging.
AID63027Binding affinity against dopamine receptor in rat striatal membrane using [3H]haloperidol1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents.
AID439067Ratio of pKi for human cloned dopamine D2 receptor to pKi for human cloned 5HT2A receptor2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.
AID540223Volume of distribution at steady state in rat after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID277677Binding affinity to dopamine D22007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.
AID142954Compound was tested for the binding affinity against rat heart Muscarinic acetylcholine receptor M2 by quinuclidinyl binding assay.1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.
AID1613973Inhibition of OST-tagged DGKalpha (unknown origin) expressed in MDCK cell homogenates assessed as residual activity at 100 uM using DAG as substrate measured after 5 mins in presence of [gamma-32P]ATP by TLC analysis relative to control2019European journal of medicinal chemistry, Feb-15, Volume: 164Identification of a novel DGKα inhibitor for XLP-1 therapy by virtual screening.
AID318421Toxicity in NSA mouse assessed as reduction of locomotor activity2007Proceedings of the National Academy of Sciences of the United States of America, May-08, Volume: 104, Issue:19
Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators.
AID598816Displacement of [3H]N-methylspiperone from human D3 receptor expressed in HEK cells2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Molecular hybridization of 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecane-3-ol with sigma (σ) receptor ligands modulates off-target activity and subtype selectivity.
AID204771Binding affinity towards Sigma receptor type 2 in whole rat brain homogenates except cerebellum using radioligand ([3H]DTG) binding assay.1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines.
AID238490Binding affinity for human recombinant dopamine receptor D12004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 receptor selectivity.
AID141055Inhibitory binding of [3H]pirenzepine to human Muscarinic acetylcholine receptor M1 in membranes from CHO-K1 cells1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.
AID1063780Displacement of [3H]DTG from sigma 2 receptor (unknown origin)2014Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.
AID176749Dose required to induce 50% maximum catalepsy in rat1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics.
AID8002Observed volume of distribution2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID566430Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membrane after 150 mins by liquid scintillation counting2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Antiproliferative activity of phenylbutyrate ester of haloperidol metabolite II [(±)-MRJF4] in prostate cancer cells.
AID1213077Drug metabolism assessed as recombinant human UGT2B7 assessed as O-glucuronidation at 25 to 200 uM incubated for 60 mins by LC-MS/MS analysis in presence of 10 uM gemfibrozil relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID717111Displacement of [3H]DTG from sigma 2 receptor in rat PC12 cell membrane after 2 hrs by scintillation counting2012Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
Synthesis of N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamides as new selective ligands for sigma receptors.
AID176093Effect on the synthesis rates of serotonin in the rat ventral limbic brain region at 2.7 micro mol/kg1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 1. Synthesis and structure-activity relationships of 2,3,3a,4,5,9b-hexahydro-1H-benz[e]indole derivatives.
AID438610Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane after 180 mins by scintillation counting2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Evaluation of spirocyclic 3-(3-fluoropropyl)-2-benzofurans as sigma1 receptor ligands for neuroimaging with positron emission tomography.
AID1318842Antagonist activity at sigma1 receptor in human SH-SY5Y cells assessed as cytotoxic effect by measuring inhibition of cell viability at 50 uM after 48 hrs by MTT assay relative to NE-1002016European journal of medicinal chemistry, Oct-04, Volume: 121Computer-assisted design, synthesis, binding and cytotoxicity assessments of new 1-(4-(aryl(methyl)amino)butyl)-heterocyclic sigma 1 ligands.
AID5326Half-maximal inhibition of [3H]- Ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID1601980Displacement of [3H]-ketanserin from recombinant human 5HT2A receptor expressed in HEK293 cells measured after 1.5 hrs by microbeta scintillation counting analysis2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT
AID1222793Dissociation constant, pKa of the compound2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Which metabolites circulate?
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID64434In vitro inhibitory concentration against radioligand [3H]spiperone binding to rat striatal dopamine receptor D21992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.
AID437144Inhibition of haloperidol-induced catalepsy in Swiss albino mouse assessed as time elapsed until release of forepaw from bar at 100 mg/kg, po administered 30 min prior to haloperidol challenge measured after 30 mins by bar test2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
Synthesis of some urea and thiourea derivatives of 3-phenyl/ethyl-2-thioxo-2,3-dihydrothiazolo[4,5-d]pyrimidine and their antagonistic effects on haloperidol-induced catalepsy and oxidative stress in mice.
AID5196Binding affinity towards human 5-HT2A receptor in BEK cells1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID1213028Drug metabolism assessed as human liver microsomes assessed as O-glucuronide measured per mg of protein at 200 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1638286Selectivity ratio of Ki for sigma1 receptor in rat brain membranes to Ki for sigma2 receptor in rat brain membranes
AID5289In vitro binding affinity towards 5-hydroxytryptamine 2 receptor in rat striatal membranes by [3H]ketanserin displacement.1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Examination of the D2/5-HT2 affinity ratios of resolved 5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indoles: an enantioselective approach toward the design of potential atypical antipsychotics.
AID6563Binding affinity towards human 5-hydroxytryptamine 6 receptor2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
AID180347The compound was tested (after peroral administration) for its ability to induce catalepsy in rats1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents.
AID1901324Displacement of [3H]di-O-tolylguanidine from sigma 2 receptor in rat liver membrane by competitive radioligand receptor binding assay
AID619550Displacement of (+)-[3H]MK-801 from pig NMDA receptor PCP binding site at 1 uM2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Combination of two pharmacophoric systems: synthesis and pharmacological evaluation of spirocyclic pyranopyrazoles with high σ₁ receptor affinity.
AID1616723Displacement of PPHT-red from SNAP-tagged human D2LR expressed in CHOK1 cell membranes by TR-FRET assay
AID131248Neuroleptic activity determined by its inhibitory effect on apomorphine-induced climbing behavior in mice by intraperitoneal administration in experiment 2 Range is 0.05-0.171987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Synthesis and neuroleptic activity of a series of 1-[1-(benzo-1,4-dioxan-2-ylmethyl)-4-piperidinyl]benzim idazolone derivatives.
AID1865086Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane measured after 120 mins by scintillation counting method
AID1724117Antipsychotic activity in po dosed mouse assessed as reduction in MK-801-induced hyperlocomotor activity2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID229188Inhibition of specific binding of [3H]3-PPP to sigma binding site in Guinea pig brain membranes1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites.
AID457704Toxicity in CF1 mouse assessed as induction of catalepsy by measuring time spent on elevated wood bar at 4 mg/kg, po after 60 mins (Rvb = 2.7 +/- 2.9 sec)2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors.
AID239150Inhibition of [125I]iodosulpiride binding to human Dopamine receptor D32005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
AID160777Binding affinity to HIV-1 protease1994Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12
Three-dimensional pharmacophores from binding data.
AID170115Compound was evaluated for its ability to block conditioned avoidance response (CAR) in rats; Dose administered perorally is 1.25 mg/kg; 51-75% block1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
10-Piperazinyl-4H-theino[3,2-b][1,5]- and -[3,4-b][1,5]benzodiazepines as potential neuroleptics.
AID61547Compound was evaluated In vitro for its activity by binding to Dopamine receptor D2 in the rat brain using [3H]NPA as radioligand.1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents.
AID1853651Antibacterial activity against Mycobacterium intracellulare ATCC 13950 assessed as inhibition of bacterial growth incubated upto 3 weeks hrs by resazurin dye based double-dilution method2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from
AID204313Sigma opioid receptor type 2 affinity in rat liver by employing [3H]ditolylguanidine as radioligand2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.
AID5560Half-maximal inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID277987Activity at human D2 receptor expressed in Xenopus oocytes2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.
AID64613Binding affinity towards Dopamine receptor D2 binding site using [3H]spiroperidol.1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
AID1179609Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain cortex membranes2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Pyridine analogues of spirocyclic σ₁ receptor ligands.
AID540224Clearance in dog after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID243188Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state2005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
A two-state homology model of the hERG K+ channel: application to ligand binding.
AID82355K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.12002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers.
AID1213035Drug metabolism assessed as recombinant human UGT2B7 assessed as O-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1378105Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes after 120 mins by microbeta scintillation counting method2017European journal of medicinal chemistry, Sep-29, Volume: 138Deconstruction - reconstruction approach to analyze the essential structural elements of tetrahydro-3-benzazepine-based antagonists of GluN2B subunit containing NMDA receptors.
AID5042Binding affinity against serotonin 5-hydroxytryptamine 2 receptor1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study.
AID62446Inhibition of [3H]haloperidol binding to Dopamine receptor in calf caudate nuclei.1980Journal of medicinal chemistry, Sep, Volume: 23, Issue:9
Synthesis of 8-aryltetrahydroisoquinolines as dopamine antagonists and evaluation for potential neuroleptic activity.
AID113716Inhibition of the GBL-induced increase in DOPA accumulation in mice(DA auto receptor agonist activity); IA = inactive1998Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5
Novel antipsychotic agents with dopamine autoreceptor agonist properties: synthesis and pharmacology of 7-[4-(4-phenyl-1-piperazinyl)butoxy]-3,4-dihydro-2(1H)-quinolinone derivatives.
AID65426Compound was tested for its binding affinity towards Dopamine receptor D2 using [3H]spiperone from rat striatum1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand.
AID112713Tested for the apomorphine climbing behavior in mice after oral administration1993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system.
AID65905Binding affinity towards dopamine D2 receptors in rat brain synaptosomal preparations1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects.
AID176413Evaluated in vitro for antipsychotic activity (hyperactivity) for the block of apomorphine induced response after ip administration 60 min prior to apomorphine (1 mg/kg sc)1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds.
AID65622In vitro binding affinity towards Dopamine receptor D3 in Sf9 cell membranes using [3H]7-OH-DPAT as radioligand2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.
AID64461Inhibitory binding of [3H]spiperone to Dopamine receptor D2 in membranes from rat corpus striatum1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.
AID36454Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.
AID221060Inhibition of apomorphine-induced climbing behavior in mice, after Intraperitoneal administration1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics.
AID1467943Selectivity ratio of Ki for sigma 1 receptor in guinea pig brain membranes to Ki for sigma 2 receptor (unknown origin)2017Journal of medicinal chemistry, 12-14, Volume: 60, Issue:23
Novel Sigma Receptor Ligand-Nitric Oxide Photodonors: Molecular Hybrids for Double-Targeted Antiproliferative Effect.
AID65100Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.
AID1546909Displacement of [3H]spiperone from human D3 receptor expressed in CHO-K1 cells by radioligand competitive binding analysis
AID1185661Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain cortex membranes2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted κ-opioid receptor agonists.
AID346275Displacement of [3H]ditolylguanine from opioid sigma2 receptor in rat liver homogenate in presence of (+)-pentazocine2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Relationships between the structure of 6-allyl-6,8-diazabicyclo[3.2.2]nonane derivatives and their sigma receptor affinity and cytotoxic activity.
AID229631Selectivity ratio for serotonin 5-HT2C to that of serotonin 5-HT2A receptors2004Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics.
AID3746Compound was measured for affinity at 5-hydroxytryptamine 1A receptor labeled with [3H]8-OH-DPAT radioligand in hippocampus tissue1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID391275Displacement of [3H]mesulergine from human cloned 5HT2C receptor2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Synthesis, binding affinity, and molecular docking analysis of new benzofuranone derivatives as potential antipsychotics.
AID184626Compound was tested for its acute toxicity in rat after ip administration1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Potential neuroleptic agents. 4. Chemistry, behavioral pharmacology, and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides.
AID427337Displacement of [3H](+)-pentazocine from sigma1 receptor in rat liver membrane by liquid scintillation counting2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Synthesis, biological evaluation, and three-dimensional in silico pharmacophore model for sigma(1) receptor ligands based on a series of substituted benzo[d]oxazol-2(3H)-one derivatives.
AID64177In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.2000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
A structure-affinity relationship study on derivatives of N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a high-affinity and selective D(4) receptor ligand.
AID233354The lipophilicity was measured in an octanol/water system at pH 7.4.2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Radioiodinated N-(2-diethylaminoethyl)benzamide derivatives with high melanoma uptake: structure-affinity relationships, metabolic fate, and intracellular localization.
AID64264Compound was tested for the inhibition of [3H]spiperone binding to dopamine receptor D21992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles.
AID524795Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID701944Selectivity ratio of Ki for sigma 1 receptor in guinea pig membrane to Ki for sigma 2 receptor in rat liver membrane2012Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
Pd-catalyzed direct C-H bond functionalization of spirocyclic σ1 ligands: generation of a pharmacophore model and analysis of the reverse binding mode by docking into a 3D homology model of the σ1 receptor.
AID1159368Displacement of (+)-DTG from sigma2 receptor in rat liver membrane by scintillation counting analysis2014European journal of medicinal chemistry, Aug-18, Volume: 83Identification, pharmacological evaluation and binding mode analysis of novel chromene and chromane based σ1 receptor ligands.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1159370Selectivity ratio of Ki for guinea pig sigma1 receptor to Ki for rat sigma2 receptor2014European journal of medicinal chemistry, Aug-18, Volume: 83Identification, pharmacological evaluation and binding mode analysis of novel chromene and chromane based σ1 receptor ligands.
AID1221956Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID63538Displacement of [3H]-YM 09151 from human Dopamine receptor D41995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
1-Phenyl-3-(aminomethyl)pyrroles as potential antipsychotic agents. Synthesis and dopamine receptor binding.
AID1213067Drug metabolism assessed as recombinant human UGT1A4 assessed as O-glucuronidation at 10 to 400 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1506087Displacement of [3H]DTG from sigma2 receptor in rat liver membranes after 60 mins by liquid scintillation counting method2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.
AID231161Ratio of the sigma-2 receptor versus sigma-1 receptor1993Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
Synthesis and binding characteristics of potential SPECT imaging agents for sigma-1 and sigma-2 binding sites.
AID61618Inhibition of [35S]GTP-gamma-S, binding to cell membranes expressing dopamine D2A receptors at 10 uM1999Bioorganic & medicinal chemistry letters, Aug-02, Volume: 9, Issue:15
Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor.
AID711582Inhibition of human dopamine D1 receptor2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID1596350Selectivity ratio of Ki for sigma2 receptor (unknown origin) to Ki for sigma1 receptor in guinea pig brain cortex membranes
AID176943Dose which blocks the hypothermic effect of apomorphine by 50% against Sprague-Dawley rats when administered intraperitoneally1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds.
AID51566Minimal effective dose required for signs of EPS in cebus monkeys1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents.
AID298479Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID88009Displacement of [3H](-)-trans-H2-PAT from histamine H2 PAT binding site by competition binding assay.1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Synthesis, evaluation, and comparative molecular field analysis of 1-phenyl-3-amino-1,2,3,4-tetrahydronaphthalenes as ligands for histamine H(1) receptors.
AID1185965Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Further evaluation of the tropane analogs of haloperidol.
AID665422Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver after 180 mins by solid scintillation counting in the presence of (+)-pentazocine2012European journal of medicinal chemistry, Jul, Volume: 53Microwave assisted synthesis of spirocyclic pyrrolidines -σ1 receptor ligands with modified benzene-N-distance.
AID204762Compound was evaluated for the binding affinity towards Sigma receptor type 1 using radioligand ([3H]-(+)- Pentazocine) binding assay.1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines.
AID1288458Displacement of [3H]DTG from human sigma2 receptor by PDSP assay2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Tetrahydroprotoberberine alkaloids with dopamine and σ receptor affinity.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID1174259Displacement of [3H]-DTG from human sigma 2 receptor in human Jurkat cell membranes incubated for 1 hr by liquid scintillation counting2015European journal of medicinal chemistry, Jan-07, Volume: 89Carboline- and phenothiazine-derivated heterocycles as potent SIGMA-1 protein ligands.
AID1861726Binding affinity to MOR (unknown origin) assessed as inhibition constant by radioligand binding assay2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.
AID175170Compound was tested for its affect on the accumulation of the dopamine metabolite homovanillic acid (HAV) in the rat striatum at 1 mg/kg dose after peroral administration1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents.
AID1552400Displacement of [3H]-Di-o-tolylguanidine from sigma-2 receptor in rat liver membranes after 120 mins by scintillation counting method2019Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16
Modification of the 4-phenylbutyl side chain of potent 3-benzazepine-based GluN2B receptor antagonists.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID711572Inhibition of CYP3A42011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID1221960Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID176087Effect on the synthesis rates of serotonin in the rat ventral limbic brain region 2.7 micro mol/kg.1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives.
AID5328Displacement of [3H]-ketanserin from rat brain 5-hydroxytryptamine 2A receptor1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID112526In vivo analgesic activity in mice after subcutaneous administration by hot plate assay method.1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Combined analgesic/neuroleptic activity in N-butyrophenone prodine-like compounds.
AID181661Binding affinity against rat striatal membranes using [3H]spiroperidol as the radioligand after 2 hours of conditioned feeding1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID62771In vitro binding affinity at human cloned Dopamine receptor D2 by [3H]spiroperidol displacement.1998Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24
N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide: a potent and selective dopamine D4 ligand.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID173704Percent decrease on dopamine agonist-induced rotation in unilaterally 6-OH-DA-lesioned rat at 0.1 mg/kg1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Troponoids. 6. Troponylpiperazines: a new class of dopamine agonists.
AID1686282Cytotoxicity in HREC assessed as reduction in cell viability incubated for 72 hrs by MTT assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells.
AID1393468Antipsychotic activity in ip dosed Sprague-Dawley rat assessed as reduction in PCP-induced hyper-locomotion pretreated for 60 mins followed by PCP addition measured for 30 mins starting 15 min after rat reintroduction to auto-tracks
AID1297659Displacement of [3H]-(+)-Pentazocine from sigma1 receptor in guinea pig brain homogenate incubated for 120 mins by solid scintillation counting analysis2016European journal of medicinal chemistry, Jun-30, Volume: 116Benzimidazolone bioisosteres of potent GluN2B selective NMDA receptor antagonists.
AID63795Binding affinity towards Dopamine receptor D2 in rat frontal striatum using [3H]spiperone2003Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2
New arylpiperazine derivatives with high affinity for alpha1A, D2 and 5-HT2A receptors.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID61326Compound was tested in vitro for its affinity towards rat striatal Dopamine receptor D2 labeled with [3H]- spiperone1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.
AID35436The compound was tested for its binding affinity towards alpha-1 adrenergic receptor by displacing [3H]WB-4101 radioligand in rat cerebral cortexc1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Pyrrole mannich bases as potential antipsychotic agents.
AID171952compound was evaluated for its ability to produce catalepsy activity in rats1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
10-Piperazinyl-4H-theino[3,2-b][1,5]- and -[3,4-b][1,5]benzodiazepines as potential neuroleptics.
AID629463Displacement of [3H]spiperone from human dopamine D3 receptor expressed in chinese hamster CHO cells by radioligand binding assay2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Development of a bivalent dopamine D₂ receptor agonist.
AID61562Compound was measured for affinity at dopamine receptor D2 labeled with [3H]spiroperidol radioligand in striatum tissue1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID1365723Solubility of compound in Middlebrook 7H9 broth media at pH 6.4 at 200 uM after 90 mins by UV-VIS spectrophotometric method2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
The antitubercular activity of various nitro(triazole/imidazole)-based compounds.
AID175174Compound was tested for serum prolactin assay method in rats at 1 mg/kg dose after peroral administration1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents.
AID141155Binding affinity measured at the Muscarinic acetylcholine receptor by the inhibition of [3H]pyrilamine binding to guinea pig cerebellum using unlabeled Triprolidine for nonspecific binding; Not determined; ND = 'Not determined'1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID681619TP_TRANSPORTER: ATP hydrolysis in membranes from MDR1-expressing insect cells2002Life sciences, May-31, Volume: 71, Issue:2
In vitro P-glycoprotein affinity for atypical and conventional antipsychotics.
AID591692Induction of apoptosis in human HEK293 cells expressing sigma receptor assessed as necrotic cells using annexin V/propidium iodide staining at 5 uM after 24 hrs by flow cytometry (Rvb = 0.06%)2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Structure-activity study to develop cationic lipid-conjugated haloperidol derivatives as a new class of anticancer therapeutics.
AID1054122Inhibition of human ERG2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Polypharmacology - foe or friend?
AID110213Ability to inhibit apomorphine-induced climbing behavior in mice.1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID492645Antipsychotic activity in NMRI mouse assessed as increase of PCP-induced locomotor activity at 10 mg/kg, ip administered 30 mins prior to testing measured for 60 mins2010Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors.
AID1213056Drug metabolism assessed as recombinant human UGT2B17 assessed as N-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID131046Inhibition of spontaneous motor activity, after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID176802In vivo activity administered intraperitoneally was determined by induction of catalepsy in rat1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID184656Compound was evaluated for the inhibition of apomorphine induced stereotypy behavior in rats after sc administration.1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents.
AID1409607IC50 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells).2020Nature, 07, Volume: 583, Issue:7816
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID675977Selectivity index, ratio of Ki for guinea pig brain sigma1 receptor to Ki for rat liver sigma2 receptor2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Thiophene bioisosteres of spirocyclic σ receptor ligands: relationships between substitution pattern and σ receptor affinity.
AID65425Inhibition of [3H]spiroperidol binding to Dopamine receptor D2 of rat striatal membranes1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
(+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties.
AID753963Displacement of [3H](+)pentazocine from sigma1 receptor in Dunkin Hartley guinea pig brain membrane after 120 mins by liquid scintillation counting analysis2013European journal of medicinal chemistry, Jun, Volume: 64Synthesis and receptor binding studies of novel 4,4-disubstituted arylalkyl/arylalkylsulfonyl piperazine and piperidine-based derivatives as a new class of σ1 ligands.
AID63412Effective dose through peroral route for in vivo inhibition against dopamine receptor D2 in male CF-1 mice by using radioligand [3H]raclopride1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bridged gamma-carbolines and derivatives possessing selective and combined affinity for 5-HT2 and D2 receptors.
AID37361Compound was tested for the binding affinity against rat cortical Alpha-2 adrenergic receptor by Radio ligand ([3H]Rx-821002) binding assay1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.
AID467613Volume of distribution at steady state in human2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID114076post-synaptic dopamine autoreceptor antagonist activity evaluated by inhibition of the apomorphine-induced stereotyped behavior in mice.1998Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5
Novel antipsychotic agents with dopamine autoreceptor agonist properties: synthesis and pharmacology of 7-[4-(4-phenyl-1-piperazinyl)butoxy]-3,4-dihydro-2(1H)-quinolinone derivatives.
AID1393365Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID141838In vitro binding affinity towards M1 receptor of rat frontal cortex homogenate by using radioligand [3H]QNB2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.
AID1210069Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID1213024Intrinsic clearance in recombinant human UGT2B7 measured per mg of protein at 10 to 400 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1655192Displacement of [3H]-Di-o-tolylguanidine from sigma-2 receptor in rat liver membranes after 120 mins by scintillation counting method2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Synthesis, Cytotoxicity Evaluation, and Computational Insights of Novel 1,4-Diazepane-Based Sigma Ligands.
AID62168Affinity towards Dopamine receptor D2 in membranes from bovine striatum using [3H]raclopride1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.
AID204764Ratio of the binding affinities against Sigma receptor type 1 and Sigma receptor type 21995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines.
AID1420180Cytotoxicity against human SH-SY5Y cells at 50 uM after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
New piperidine-based derivatives as sigma receptor ligands. Synthesis and pharmacological evaluation.
AID242944Ratio of dopamine receptor D2 long and D3 ki values2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.
AID321564Displacement of [3H](+)-pentazocine from opioid sigma1 receptor in rat brain homogenate2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Conversion of a highly selective sigma-1 receptor-ligand to sigma-2 receptor preferring ligands with anticocaine activity.
AID35428Binding affinity towards alpha-1 adrenergic receptors in rat brain synaptosomal preparations1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects.
AID1461561Displacement of [3H]spiperone from human D2long receptor expressed in CHO cell membranes by radioligand binding assay2017Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19
Potent haloperidol derivatives covalently binding to the dopamine D2 receptor.
AID1546911Displacement of [3H]spiperone from human D4.2 receptor expressed in CHO-K1 cells by radioligand competitive binding analysis
AID203830Inhibition of [3H]DTG binding to sigma-2 sites of guinea pig brain membranes1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
(+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1532590Inhibition of human erythrocytes AChE at 1 uM using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 1 min time interval for 10 mins by Ellman's method relative to control2019European journal of medicinal chemistry, Jan-15, Volume: 162Novel multitarget-directed ligands targeting acetylcholinesterase and σ
AID392048Cardiotoxicity in iv dosed Dunkin-Hartley guinea pig assessed as drug level required to evoke 50 ms QTc prolongation administered as 3 fold cumulative doses measured every 10 seconds at end of every 20 mins follow up period of individual dose by ECG2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Identification of "toxicophoric" features for predicting drug-induced QT interval prolongation.
AID592114Induction of apoptosis in human MCF7 cells expressing sigma receptor assessed as necrotic cells using annexin V/propidium iodide staining at 5 uM after 24 hrs by flow cytometry (Rvb = 0.27%)2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Structure-activity study to develop cationic lipid-conjugated haloperidol derivatives as a new class of anticancer therapeutics.
AID1215939Unbound intrinsic clearance in human intestinal S9 fraction at 50 to 1000 nM after 30 to 60 mins by HPLC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Significance of reductive metabolism in human intestine and quantitative prediction of intestinal first-pass metabolism by cytosolic reductive enzymes.
AID64612Displacement of [3H]spiroperidol from D2 dopamine receptor1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
Synthesis of 2-piperazinylbenzothiazole and 2-piperazinylbenzoxazole derivatives with 5-HT3 antagonist and 5-HT4 agonist properties.
AID646280Antipsychotic activity in CD1 mouse assessed as inhibition of MK-801-induced hyperactivity measuring number of crossings measured every 5 mins for 1 hr2012Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
Quinoline- and isoquinoline-sulfonamide derivatives of LCAP as potent CNS multi-receptor-5-HT1A/5-HT2A/5-HT7 and D2/D3/D4-agents: the synthesis and pharmacological evaluation.
AID763632Antipsychotic activity in CF1 mouse assessed as prevention of ketamine-induced hyperlocomotion at 0.01 mg/kg, po administered 30 mins prior ketamine challenge measured for 20 mins post challenge2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579.
AID1136368Non-specific toxicity in sc dosed Wistar rat assessed as inhibition of apomorphine hydrochloride-induced stereotypy administered 1 hr prior to apomorphine hydrochloride challenge measured after 5 to 20 mins1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 4. Central nervous system depressants.
AID640304Displacement of [3H]N-methylspiperone from human dopamine D3 receptor by liquid scintillation counting2012Bioorganic & medicinal chemistry, Feb-01, Volume: 20, Issue:3
Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.
AID1393469Toxicity in ip dosed Sprague-Dawley rat assessed as sedation pretreated for 60 mins followed by PCP addition measured for 30 mins starting 15 min after rat reintroduction to auto-tracks
AID204290Ratio of binding affinity towards Sigma opioid receptor type 1 versus Sigma opioid receptor type 22002Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22
Novel sigma receptor ligands. Part 2. SAR of spiro[[2]benzopyran-1,4'-piperidines] and spiro[[2]benzofuran-1,4'-piperidines] with carbon substituents in position 3.
AID410339Sedative activity in NMRI mouse assessed as reduction in spontaneous locomotor activity administered 30 mins prior to testing2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
AID705398Antipsychotic activity in sc dosed rat assessed as decrease in phencyclidine-induced locomotor activity2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID112953Compound was tested for inhibition of physostigmine lethality in mouse when administered perorally1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.
AID387867Displacement of [3H]YM-09151-2 from human dopamine D4.2 receptor in membrane suspensions by liquid scintillation counter2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Synthesis of 1-arylpiperazyl-2-phenylcyclopropanes designed as antidopaminergic agents: cyclopropane-based conformationally restricted analogs of haloperidol.
AID492186Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain homogenates after 1 hr by liquid scintillation counting2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Synthesis and characterization of selective dopamine D2 receptor antagonists. 2. Azaindole, benzofuran, and benzothiophene analogs of L-741,626.
AID1123512Neuroleptic activity in Wistar HLA rat assessed as inhibition of methamphetamine-induced stereotyped behavior at 1 mg/kg, ip administered 20 mins before methamphetamine challenge measured every 30 mins for 3 hrs followed by every 1 hr for further 3 hrs1979Journal of medicinal chemistry, Jun, Volume: 22, Issue:6
Synthesis of 2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole derivatives and their central nervous system activities.
AID717103Selectivity ratio of Ki for sigma 2 receptor in rat PC12 cell membrane to Ki for sigma 1 receptor in rat brain membrane2012Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
Synthesis of N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamides as new selective ligands for sigma receptors.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID182041In vivo inhibition of apomorphine-mediated stereotypy in rats administered subcutaneously at 0.6 mg/kg expressed as percent inhibition1993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study.
AID675971Displacement of [3H]-di-o-tolyguanidine from rat liver sigma 2 receptor after 180 mins by scintillation counting analysis2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Thiophene bioisosteres of spirocyclic σ receptor ligands: relationships between substitution pattern and σ receptor affinity.
AID1686278Displacement of [3H]-spiperone from DRD2 in rat striatum by scintillation counting2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells.
AID1185974Displacement of [3H]Nisoxetine from human Norepinephrine transporter by liquid scintillation counting2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Further evaluation of the tropane analogs of haloperidol.
AID239151Inhibition of [3H]7-OH-DPAT binding to Dopamine D3 receptor expressed in Sf9 cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies.
AID65402Compound was evaluated for its binding affinity with Dopamine receptor D2 using membranes prepared from rat striatum1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Orally active benzamide antipsychotic agents with affinity for dopamine D2, serotonin 5-HT1A, and adrenergic alpha1 receptors.
AID1578090Unbound brain-to-plasma concentration ratio in rat2019European journal of medicinal chemistry, Nov-15, Volume: 182Practical approaches to evaluating and optimizing brain exposure in early drug discovery.
AID705725Displacement of [3H]di-o-tolylguanidine from Sigma2 receptor in rat brain homogenate2012Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
New positron emission tomography (PET) radioligand for imaging σ-1 receptors in living subjects.
AID194375Effect of compound (0.2 mg/kg ip) on the concentration of DOPAC in rat mesolimbic region1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID176251Intracranial self stimulation in rat was determined after 1 hr of intraperitoneal administration of the compound1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID1718132Binding affinity to sigma-1 receptor (unknown origin)2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.
AID41473Binding affinity against beta-2 adrenergic receptor in rat brain using [3H]DHA1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents.
AID490176Anticonvulsant activity in rat assessed as protection against maximal electric shock-induced seizures at 0.5 mL, ip2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
Synthesis and antipsychotic and anticonvulsant activity of some new substituted oxa/thiadiazolylazetidinonyl/thiazolidinonylcarbazoles.
AID1330104Selectivity ratio of Ki for sigma2 receptor in rat PC12 cells to Ki for guinea pig sigma1 receptor2016Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
AID61499Affinity for Dopamine receptor D11998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.
AID65713Displacement of [3H]NPA from rat brain Dopamine receptor D21996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID231654Binding ratio of -log Ki between D2 and D1 receptors1993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study.
AID1655661Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor (unknown origin) incubated for 1 hr in presence of (+)SKF10047 by liquid scintillation counting method
AID203829Binding affinity towards sigma 2 receptor using [3H]DTG in the presence of 200 nM (+)-NANM from guinea pig brain1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand.
AID1712205Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane incubated for 150 mins by liquid scintillation counting method2016Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14
New bifunctional antioxidant/σ1 agonist ligands: Preliminary chemico-physical and biological evaluation.
AID1532591Inhibition of human erythrocytes AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 1 min time interval for 10 mins by Ellman's method2019European journal of medicinal chemistry, Jan-15, Volume: 162Novel multitarget-directed ligands targeting acetylcholinesterase and σ
AID665421Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane after 180 mins by solid scintillation counting2012European journal of medicinal chemistry, Jul, Volume: 53Microwave assisted synthesis of spirocyclic pyrrolidines -σ1 receptor ligands with modified benzene-N-distance.
AID203852The compound was tested for affinity towards sigma-3 receptor1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
Conformational analysis, pharmacophore identification, and comparative molecular field analysis of ligands for the neuromodulatory sigma 3 receptor.
AID1478367Displacement of [3H]-spiperone from dopamine D2 receptor in rat strriatum after 15 mins by liquid scintillation counting method2018Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
(+)-Methyl (1R,2S)-2-{[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]methyl}-1-phenylcyclopropanecarboxylate [(+)-MR200] Derivatives as Potent and Selective Sigma Receptor Ligands: Stereochemistry and Pharmacological Properties.
AID1768729Lipophilicity, logP of compound by shake flask method2021Bioorganic & medicinal chemistry letters, 10-01, Volume: 49Estimation of the lipophilicity of purine-2,6-dione-based TRPA1 antagonists and PDE4/7 inhibitors with analgesic activity.
AID517707Displacement of [3H]Spiperone from human dopamine D2 long receptor expressed in CHO cells2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Bioisosteric replacement leading to biologically active [2.2]paracyclophanes with altered binding profiles for aminergic G-protein-coupled receptors.
AID87530Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID194381Effect of compound (0.2 mg/kg ip) on the concentration of HVA in rat striatum1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID1546910Displacement of [3H]spiperone from human D3 receptor expressed in CHO-K1 cells at 10 uM by radioligand competitive binding analysis relative to control
AID5012Inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2 receptor of guinea pig frontal cortex membranes1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
(+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties.
AID49739Compound at a dose of 50 ug/kg was evaluated for the reversal of the inhibition of nerve stimulation using the cat cardioaccelerator nerve preparation; Reversed inhibition1986Journal of medicinal chemistry, Dec, Volume: 29, Issue:12
p-Dimethoxy-substituted trans-octahydrobenzo[f]- and -[g]quinolines: synthesis and assessment of dopaminergic agonist effects.
AID1616720Displacement of PPHT-red from SNAP-tagged human D2LR expressed in CHOK1 cell membranes assessed as association rate constant by TR-FRET assay
AID1153310Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay relative to qunipirole2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Functionally selective dopamine D₂, D₃ receptor partial agonists.
AID63804Affinity against Dopamine receptor D22000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.
AID1136084Ratio of IC50 for displacement of [3H]-DA from dopamine receptor in calf caudate membranes to IC50 for displacement of [3H]-HALO from dopamine receptor in calf caudate membranes1978Journal of medicinal chemistry, Apr, Volume: 21, Issue:4
5-Chloro-2-phenyl-1-benzo[b]thiophene-3-alkanimines, potential antipsychotic agents.
AID238855Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D12005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
AID255071Inhibitory activity against opioid sigma 2 receptor in rat cerebral cortex using [3H]DTG (+300 nM (+)pentazocine) as radio ligand at pH 7.5 for 120 min at 22 degree C2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective sigma1 ligands. Part 2.
AID61788In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.1998Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7
Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist.
AID1136359Neuroleptic activity in squirrel monkey assessed as inhibition of Sidman avoidance at 1 mg/kg, po measured for 4 hrs1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 4. Central nervous system depressants.
AID177555Ability to block apomorphine-induced stereotypy in rats.1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID1221982Fraction absorbed in human2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID109889Tail suspension test in mice, dose(mg/Kg ip) = 4;duration of immobility(% vs controls)1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.
AID204461Binding affinity measured at the sigma receptor by the inhibition of [3H]-3-PPP binding to guinea pig cerebellum using unlabeled 3-PPP for nonspecific binding.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID367546Displacement of [3H]RHM-1 from sigma 2-type opioid receptor in rat liver homogenates2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
New N-substituted 9-azabicyclo[3.3.1]nonan-3alpha-yl phenylcarbamate analogs as sigma2 receptor ligands: synthesis, in vitro characterization, and evaluation as PET imaging and chemosensitization agents.
AID196012Compound was evaluated in paw test for the forelimb retraction at effective dose of 20 (mg/kg)2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors.
AID1146534Neuroleptic activity in po dosed STD-ddY mouse assessed as protection against methamphetamine-induced toxicity administered 1 hr before methamphetamine challenge measured after 24 hrs1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
AID280701Increase in TG-2 expression in albino Wistar rat primary 14 DIV astroglial cell at 25 uM after 24 hrs by CLSM analysis2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Novel sigma receptor ligands: synthesis and biological profile.
AID367548Partition coefficient, log P of the compound2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
New N-substituted 9-azabicyclo[3.3.1]nonan-3alpha-yl phenylcarbamate analogs as sigma2 receptor ligands: synthesis, in vitro characterization, and evaluation as PET imaging and chemosensitization agents.
AID62746Intrinsic activity relative to quinpirole in the reversal of forskolin-stimulated cAMP accumulation in cells transfected with the human DA D2 receptor1994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
The discovery and structure-activity relationships of 1,2,3,6-tetrahydro-4-phenyl-1-[(arylcyclohexenyl)alkyl]pyridines. Dopamine autoreceptor agonists and potential antipsychotic agents.
AID62465Ratio of IC50 evaluated by using [3H]DA to [3H]-HP1981Journal of medicinal chemistry, Sep, Volume: 24, Issue:9
Synthesis and evaluation of 1,2,3,4-tetrahydro[1]benzothieno[2,3-h]isoquinolines as dopamine antagonists.
AID1129361Unbound fraction in HEK293 cell homogenate at 0.1 uM by equilibrium dialysis based UPLC-MS/MS analysis2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
A high-throughput cell-based method to predict the unbound drug fraction in the brain.
AID176254Intraperitoneal effective dose required for inhibition of apomorphine-induced stereotypy in rat1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID1403515Displacement of [3H]-di-o-tolylguanidine from sigma-2 receptor in rat liver membranes incubated for 120 mins measured for 5 mins by scintillation counting method
AID178541Compound was tested for its ability to induce catalepsy in rats.1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.
AID1129878Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain cortex membranes after 120 mins by scintillation counting analysis2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
Synthesis, pharmacological evaluation, and σ1 receptor interaction analysis of hydroxyethyl substituted piperazines.
AID5331Inhibitory constant on 5-hydroxytryptamine 2A receptor of Rat frontal cortex2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
New serotonin 5-HT(2A), 5-HT(2B), and 5-HT(2C) receptor antagonists: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo and heterocycloalkanones.
AID178179Inhibition of conditioned avoidance response in rat following s.c. administration.1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Muscarinic agonists with antipsychotic-like activity: structure-activity relationships of 1,2,5-thiadiazole analogues with functional dopamine antagonist activity.
AID148465Ability to inhibit the specific binding of [3H]- dihydromorphine to opiate receptors in rat brain membrane preparation by 50%1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Combined analgesic/neuroleptic activity in N-butyrophenone prodine-like compounds.
AID61046Compound was tested in vivo for methyl phenidate-induced gnawing behavior antagonistic activity against dopamine receptor D2 in mice1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles.
AID131589Suppression of aggressive behavior, after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID4786Binding affinity towards 5-hydroxytryptamine 2 receptor measured using radioligand ([3H]spiperone) binding assay1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.
AID194379Effect of compound (0.2 mg/kg ip) on the concentration of HVA in rat frontal cortex1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID540222Clearance in rat after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1184609Displacement of [3H]spiperone from human D3 receptor stably expressed in CHO cell membranes by competitive binding assay2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
Synthesis and binding profile of haloperidol-based bivalent ligands targeting dopamine D(2)-like receptors.
AID226334The Binding affinity was evaluated using [3H]DTG -(+)-Dextrallorphan] in rat liver1993Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
Synthesis and binding characteristics of potential SPECT imaging agents for sigma-1 and sigma-2 binding sites.
AID1256684Neurotoxicity in Chinese Kun Ming mouse assessed as locomotor activity by measuring total distance traveled at 1 mg/kg, po administered 1 hr before test measured for 10 mins (Rvb = 13415.6 +/- 9555.8 millimeter)2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
AID1136369Non-specific toxicity in ip dosed Wistar rat assessed as inhibition of d-amphetamine sulfate-induced stereotypy administered 1 hr prior to d-amphetamine sulfate challenge measured after 55 to 65 mins1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 4. Central nervous system depressants.
AID717217Displacement of [3H](+)-pentazocine from sigma 1 receptor in rat brain membrane after 2.5 hrs by scintillation counting2012Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
Synthesis of N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamides as new selective ligands for sigma receptors.
AID1411898Half life in im dosed human plasma2018MedChemComm, May-01, Volume: 9, Issue:5
Schizophrenia: synthetic strategies and recent advances in drug design.
AID298493Displacement of [3H]RX 821002 from adrenergic alpha-2 receptor in rat cerebral cortex2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID308686Displacement of [3H]mesulergine human cloned serotonin 5HT2C receptor2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics.
AID135365Inhibitory activity against tremorine-induced tremors, after 1 hour of peroral administration in mouse at dose 20 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID1853650Antibacterial activity against Mycobacterium abscessus ATCC 19977 assessed as inhibition of bacterial growth incubated upto 3 weeks hrs by resazurin dye based double-dilution method2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from
AID224648Area under curve(AUC) value of HVA level after second treatment(7.4 umol/kg) in dialysates collected from rat striatum.2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID1213038Drug metabolism assessed as recombinant human UGT1A6 assessed as O-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID640547Displacement of [3H]QNB from human M1 receptor by liquid scintillation counting2012Bioorganic & medicinal chemistry, Feb-01, Volume: 20, Issue:3
Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.
AID180891The dosage at which 50% of the animals were cataleptic was measured after (ip) administration in male Sprague-Dawley rats1982Journal of medicinal chemistry, Nov, Volume: 25, Issue:11
Potential neuroleptic agents. 2,6-Dialkoxybenzamide derivatives with potent dopamine receptor blocking activities.
AID458632Displacement of [3H]spiperone from human dopamine D2 receptor at low affinity state expressed in HEK293 cells2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
AID1877931Displacement of [3H]-DTG from Sprague-Dawley rat liver Sigma 2 receptor incubated for 120 mins in presence of [3H]-(+)-pentazocine by liquid scintillation counting analysis2022European journal of medicinal chemistry, Feb-15, Volume: 230Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation.
AID205174The compound was tested for inhibition of sidman avoidance in squirrel monkeys1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents.
AID298488Displacement of [3H]BLR-43694 from human 5HT3 receptor expressed in HEK293 cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID408340Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Support vector machines classification of hERG liabilities based on atom types.
AID1213064Drug metabolism assessed as human liver microsomes assessed as O-glucuronidation at 10 to 400 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID274128Displacement of [3H]Astemizole from hERG expressed in HEK293 cells at 10 uM2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Ureas with histamine H3-antagonist receptor activity--a new scaffold discovered by lead-hopping from cinnamic acid amides.
AID1853667Synergistic antibacterial activity against Mycobacterium smegmatis mc2 155 assessed as fold reduction in MIC value at 8 ug/ml in presence of spectinomycin by checkerboard assay2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from
AID1127647Displacement of [3H]progesterone from sigma-1 opioid receptor in porcine liver microsome membranes2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
The σ2 receptor: a novel protein for the imaging and treatment of cancer.
AID1179611Selectivity ratio of Ki for sigma 2 receptor in rat liver membranes to Ki for sigma 1 receptor in guinea pig brain cortex membranes2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Pyridine analogues of spirocyclic σ₁ receptor ligands.
AID415887Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane by liquid scintillation analyzer2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
1,4-Diazepanes derived from (S)-serine--homopiperazines with improved sigma(1) (sigma) receptor affinity and selectivity.
AID1597397Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes incubated for 120 mins by scintillation counting method
AID34586Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Combined analgesic/neuroleptic activity in N-butyrophenone prodine-like compounds.
AID1136083Displacement of [3H]-HALO from dopamine receptor in calf caudate membranes after 10 mins by liquid scintillation counting analysis1978Journal of medicinal chemistry, Apr, Volume: 21, Issue:4
5-Chloro-2-phenyl-1-benzo[b]thiophene-3-alkanimines, potential antipsychotic agents.
AID427338Displacement of [3H]DTG from sigma2 receptor in rat liver membrane by liquid scintillation counting2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Synthesis, biological evaluation, and three-dimensional in silico pharmacophore model for sigma(1) receptor ligands based on a series of substituted benzo[d]oxazol-2(3H)-one derivatives.
AID184872Minimum effective dose observed in rat catalepsy experiments2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.
AID65609Binding affinity to rat Dopamine receptor D3 expressed in CHO cells was determined using [125 I] iodosulpride as radioligand1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.
AID113872Intraperitoneal effective dose required for inhibition of apomorphine-induced climbing in mice1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID1330103Displacement of [3H]DTG from sigma2 receptor in rat PC12 cells measured after 90 mins by microbeta scintillation counting method2016Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
AID204152Inhibition of [3H]- pentazocine binding against alpha-1 from guinea pig brain1999Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25
A series of 6- and 7-piperazinyl- and -piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent.
AID62768Binding affinity to dopamine receptor D2 cloned from human, using [3H]- YM09151 as competitive ligand2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.
AID203688Compound was evaluated for its in vitro competition binding studies using sigma-ligand (0.05-10000 nM) - [3H](+)-pentazocine (sigma1 receptor) in guinea pig brain membranes1998Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
Substituted halogenated arylsulfonamides: a new class of sigma receptor binding tumor imaging agents.
AID65767Half-maximal inhibition of [3H]7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID1596348Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membranes incubated for 150 mins by scintillation counting method
AID1378106Displacement of [3H]DTG from sigma2 receptor in rat liver membranes after 120 mins by microbeta scintillation counting method2017European journal of medicinal chemistry, Sep-29, Volume: 138Deconstruction - reconstruction approach to analyze the essential structural elements of tetrahydro-3-benzazepine-based antagonists of GluN2B subunit containing NMDA receptors.
AID142504The ability to displace [3H]QNB from Muscarinic acetylcholine receptor in rat brain membrane was determined1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems.
AID194369Effect of compound (0.2 mg/kg ip) on the concentration of 5-HIAA in rat striatum1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID674895Displacement of (+)-[3H]pentazocine from sigma1 receptor in Sprague-Dawley rat cerebral membrane after 90 mins by liquid scintillation counting2012Bioorganic & medicinal chemistry, Aug-15, Volume: 20, Issue:16
Syntheses and in vitro evaluation of decalinvesamicol analogues as potential imaging probes for vesicular acetylcholine transporter (VAChT).
AID63540Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells2002Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
Design and synthesis of a piperazinylalkylisoxazole library for subtype selective dopamine receptor ligands.
AID1411897Half life in iv dosed human plasma2018MedChemComm, May-01, Volume: 9, Issue:5
Schizophrenia: synthetic strategies and recent advances in drug design.
AID395327Dissociation constant, pKa by capillary electrophoresis2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID62573The IC50 value was reported as apparent, since [3H]NCA was purported to be irreversible. Result indicates the mean of two separate experiments, each performed in triplicate.1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
Aporphines. 58. N-(2-chloroethyl) [8,9-2H]norapomorphine, an irreversible ligand for dopamine receptors: synthesis and application.
AID1330101Displacement of [3H]U69593 from KOR (unknown origin) expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method2016Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
AID5686Affinity towards 5-hydroxytryptamine 2C receptor in membranes from pig choroid plexus using [3H]N-methyl-mesulergine1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.
AID1292384Blood clearance in psychotic patient (9 patients) at 3.5 +/- 1.2 mg, iv by reversed phase HPLC method1987Psychopharmacology, , Volume: 91, Issue:4
Pharmacokinetics of haloperidol in psychotic patients.
AID168344Social interaction of rats was determined after 1 hr of intraperitoneal administration at 0.25 mg/kg1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID256759Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assay2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
First structure-activity relationship study on dopamine D3 receptor agents with N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamide structure.
AID62723Ability to inhibit the binding of [3H]spiroperidol in rat striatal tissue1985Journal of medicinal chemistry, Jun, Volume: 28, Issue:6
Synthesis and neuroleptic activity of 3-(1-substituted-4-piperidinyl)-1,2-benzisoxazoles.
AID65245Binding affinity towards dopamine receptor D2 in rat striatal membranes2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines.
AID448641Selectivity ratio of Ki for guinea pig brain sigma 1 receptor to Ki for rat liver sigma 2 receptor2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Synthesis of sigma receptor ligands with unsymmetrical spiro connection of the piperidine moiety.
AID1686304Suppression of VEGF-A-induced angiogenesis in HREC assessed as reduction of the ramification number at 5 uM incubated for 24 hrs by Matrigel based tube formation assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells.
AID194526Effect of compound on (0.2 mg/kg ip) the concentration of DOPAC/DA in rat frontal cortex1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID1878191Binding affinity to dopamine D3 receptor (unknown origin) by radioligand displacement assay
AID1213076Drug metabolism assessed as recombinant human UGT2B7 assessed as O-glucuronidation at 25 to 200 uM incubated for 60 mins by LC-MS/MS analysis in presence of 10 uM niflumic acid relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1593895Selectivity index, ratio of Ki for displacement of [3H]-Pentazocine from sigma 1 receptor (unknown origin) expressed in HEK293T cell membranes to KI for displacement of [3H]-DTG from sigma 2 receptor (unknown origin) expressed in HEK293T cell membranes2019Bioorganic & medicinal chemistry, 06-15, Volume: 27, Issue:12
New analogs of SYA013 as sigma-2 ligands with anticancer activity.
AID437146Inhibition of haloperidol-induced catalepsy in Swiss albino mouse assessed as time elapsed until release of forepaw from bar at 100 mg/kg, po administered 30 min prior to haloperidol challenge measured after 120 mins by bar test2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
Synthesis of some urea and thiourea derivatives of 3-phenyl/ethyl-2-thioxo-2,3-dihydrothiazolo[4,5-d]pyrimidine and their antagonistic effects on haloperidol-induced catalepsy and oxidative stress in mice.
AID395324Lipophilicity, log D at pH 7.4 by liquid chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID1655193Displacement of [3H]ifenprodil from GluN2B (unknown origin) expressed in mouse L(tk-) cell membranes co-expressing GluN1a incubated for 120 mins by scintillation counting method2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Synthesis, Cytotoxicity Evaluation, and Computational Insights of Novel 1,4-Diazepane-Based Sigma Ligands.
AID112508In vivo Antipsychotic activity was quantified by induction of catalepsy in mice1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical an
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID591694Induction of apoptosis in human HEK293 cells expressing sigma receptor assessed as early apoptotic cells using annexin V/propidium iodide staining at 5 uM after 24 hrs by flow cytometry (Rvb = 99.76%)2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Structure-activity study to develop cationic lipid-conjugated haloperidol derivatives as a new class of anticancer therapeutics.
AID171689Catalytic action on male Wistar rats after subcutaneous administration of 0.003 mg/kg dose of compound1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.
AID173680Locomotor activity after no pretreatment in rat at high-dose region expressed as percent of saline control1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Novel dopamine receptor agonists and antagonists with preferential action on autoreceptors.
AID131214Lethal dose in mice by administered the compound intraperitoneally1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID1461568Selectivity index, ratio of Ki for human D2short receptor expressed in CHO cell membranes to Ki for human D2short receptor L2.64C mutant expressed in HEK293T cell membranes2017Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19
Potent haloperidol derivatives covalently binding to the dopamine D2 receptor.
AID204448Inhibitory activity against sigma receptor isolated from guinea pig brain cortex membrane using [3H]DTG as radioligand1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives.
AID605696Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Bivalent dopamine D2 receptor ligands: synthesis and binding properties.
AID1462756Displacement of [3H]-di-o-tolylguanidine from sigma 2 receptor in rat liver membranes after 120 mins by scintillation counting analysis2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Replacement of benzylic hydroxy group by vinyl or hydroxymethyl moiety at the 3-benzazepine scaffold retaining GluN2B affinity.
AID35270Compound was tested for the binding affinity against rat cortical Alpha-1 adrenergic receptor by radioligand [3H]prazosin binding assay.1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.
AID238941Inhibition of [3H]spiperone binding to rat dopamine D2 receptor2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies.
AID1215946Intrinsic clearance in human intestinal S9 fraction at 50 to 1000 nM after 60 mins by HPLC-MS/MS analysis in presence of NADH2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Significance of reductive metabolism in human intestine and quantitative prediction of intestinal first-pass metabolism by cytosolic reductive enzymes.
AID62337Binding towards Dopamine receptor D2 expressed in CHO-K1 cells using [3H]U-861701993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID227559Relative binding affinity for dopamine D2 and alpha receptors1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID1853652Antibacterial activity against Mycobacterium avium ATCC 25921 assessed as inhibition of bacterial growth incubated upto 3 weeks hrs by resazurin dye based double-dilution method2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from
AID196117effects on Sidman Avoidance performance in rats, number of shocks (absolute change from control), p<0.001, dose(mg/Kg po) =11998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.
AID476062Displacement of [3H](+)-pentazocine from sigma 1 opioid receptor in human Jurkat cells by scintillation counting2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Sigma-1 ligands: Tic-hydantoin as a key pharmacophore.
AID1211298Dissociation constant, pKa of the compound2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID665423Selectivity ratio of Ki for rat sigma 2 receptor to Ki for guinea pig sigma1 receptor2012European journal of medicinal chemistry, Jul, Volume: 53Microwave assisted synthesis of spirocyclic pyrrolidines -σ1 receptor ligands with modified benzene-N-distance.
AID37306Binding affinity was tested on Alpha-1 adrenergic receptor using radioligand [3H](+)-pentazocine binding assay.1996Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
Novel potent sigma 1 ligands: N-[omega-(tetralin-1-yl)alkyl]piperidine derivatives.
AID63549In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1638284Displacement of [3H](+)-pentazocine from sigma1 receptor in rat brain membranes after 120 mins by radioligand binding assay
AID1369084Displacement of [3H]-DTG from sigma 2 receptor in rat liver membranes after 120 mins by scintillation counting analysis2018Bioorganic & medicinal chemistry, 01-15, Volume: 26, Issue:2
2-Methyltetrahydro-3-benzazepin-1-ols - The missing link in SAR of GluN2B selective NMDA receptor antagonists.
AID1867872Displacement of [3H]-DTG from sigma 2 receptor in rat liver membrane measured after 120 mins by microbeta counting analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Synthesis and biological evaluation of conformationally restricted GluN2B ligands derived from eliprodil.
AID476061Selectivity ratio of IC50 for sigma 2 opioid receptor in rat cerebral cortex membrane to IC50 for sigma 1 opioid receptor in human Jurkat cells2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Sigma-1 ligands: Tic-hydantoin as a key pharmacophore.
AID63499Antagonistic activity against apomorphine-induced emesis, after 5 hour of peroral administration in dogs1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID1292388Ratio of steady state drug level in blood to plasma in psychotic patient at 3.5 +/- 1.2 mg, iv by reversed phase HPLC method1987Psychopharmacology, , Volume: 91, Issue:4
Pharmacokinetics of haloperidol in psychotic patients.
AID29925Volume of distribution in man (IV dose)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID308685Displacement of [3H]ketanserin human cloned serotonin 5HT2A receptor2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics.
AID1215128Ratio, ratio of fraction unbound in solid supported porcine brain membrane vesicles at 5 uM dosed as discrete compounds after 5 hrs by TRANSIL assay to fraction unbound in solid supported porcine brain membrane vesicles at 5 uM using four compound cocktai2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID1865087Displacement of [3H]DTG from sigma 2 receptor in rat liver membranes measured after 120 mins by scintillation counting method
AID176414Evaluated in vitro for antipsychotic activity (stereotypies) for the block of apomorphine induced response after ip administration 60 min prior to apomorphine (1 mg/kg sc)1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds.
AID301872Blockade of conditioned avoidance response in ip dosed rat2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
Rational design, synthesis and evaluation of (6aR( *),11bS( *))-1-(4-fluorophenyl)-4-{7-[4-(4-fluorophenyl)-4-oxobutyl]1,2,3,4,6,6a,7,11b,12,12a(RS)-decahydropyrazino[2',1':6,1]pyrido[3,4-b]indol-2-yl}-butan-1-one as a potential neuroleptic agent.
AID63533Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands.
AID131051Inhibitory activity against tremorine-induced salivation, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID549678Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane by scintillation counting2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Synthesis, pharmacological activity and structure affinity relationships of spirocyclic σ(1) receptor ligands with a (2-fluoroethyl) residue in 3-position.
AID277984Ratio of ED50 for catalepsy induction to ED50 for normalization in ip dosed rat2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.
AID178395Effective dose for ethanol potentiation in rats1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.
AID448410Displacement of [3H]spiperone from D2 receptor2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Tetrahydrocarbazole-based serotonin reuptake inhibitor/dopamine D2 partial agonists for the potential treatment of schizophrenia.
AID1704750Toxicity in po dosed Kunming mouse assessed as catalepsy
AID1185964Displacement of [3H]N-methylspiperone from human dopamine D3 receptor by liquid scintillation counting2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Further evaluation of the tropane analogs of haloperidol.
AID65786Binding towards Dopamine receptor D3 expressed in CHO-K1 cells using [3H]spiperone 1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID1861728Binding affinity to KOR (unknown origin) assessed as inhibition constant by radioligand binding assay2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.
AID1061889Displacement of [3H]BTX-B from neuronal voltage-gated sodium channel in rat cerebral cortex synaptoneurosomes after 60 mins by scintillation counting2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
A highly predictive 3D-QSAR model for binding to the voltage-gated sodium channel: design of potent new ligands.
AID4782Binding affinity towards serotonin 5-HT2 receptor was determined in rat cortex using [3H]spiperone as ligand1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID140974In vitro binding affinity against Muscarinic acetylcholine receptors in rat brain.1993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study.
AID177809Compound was evaluated in vivo for its antipsychotic activity for inhibition of apomorphine-induced stereotypy in rat1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents.
AID367545Displacement of [3H](+)-pentazocine from sigma 1-type opioid receptor in guinea pig brain homogenates2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
New N-substituted 9-azabicyclo[3.3.1]nonan-3alpha-yl phenylcarbamate analogs as sigma2 receptor ligands: synthesis, in vitro characterization, and evaluation as PET imaging and chemosensitization agents.
AID237685Lipophilicity determined as logarithm of the partition coefficient in the alkane/water system2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Calculating virtual log P in the alkane/water system (log P(N)(alk)) and its derived parameters deltalog P(N)(oct-alk) and log D(pH)(alk).
AID229212Binding affinity was evaluated against sigma-1 binding site in guinea pig, using [3H]- -(+)- Pentazocine1993Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
Synthesis and binding characteristics of potential SPECT imaging agents for sigma-1 and sigma-2 binding sites.
AID160632The irreversibility of the inactivation reaction of HIV-1 PR was assessed; NI =No detectable reversible reaction1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Haloperidol-based irreversible inhibitors of the HIV-1 and HIV-2 proteases.
AID392764Displacement of [3H]N-methylspiperone from human dopamine D3 receptor by liquid scintillation counting2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups.
AID196771In vivo accumulation of L-DOPA was measured in striatum of rats1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID180162Antipsychotic activity at a dose 10 times the ED50 value for CAR block for production of catalepsy in the rat (following i.p. dosing)1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Pyrrole mannich bases as potential antipsychotic agents.
AID737845Displacement of [3H](+)-Pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Improvement of σ1 receptor affinity by late-stage C-H-bond arylation of spirocyclic lactones.
AID5561In vitro ability to displace [3H]ketanserin from 5-hydroxytryptamine 2A receptor in rat brain.1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID4128Inhibitory concentration against binding of 5-hydroxytryptamine 1A receptor from striata of male Wistar rats by displacement of [3H]8-OH-DPAT2000Bioorganic & medicinal chemistry letters, Mar-06, Volume: 10, Issue:5
N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]cyclohexanecarboxamides as selective 5-HT1A receptor agonists.
AID41748Compound was tested for the binding affinity against rat cortical Beta adrenergic receptor by Radio ligand [3H]dihydroalprenolol binding assay.1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.
AID64963Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in CHO cells1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors.
AID1292377Terminal phase volume of distribution at steady state in psychotic patient (9 patients) at 3.5 +/- 1.2 mg, iv by reversed phase HPLC method based model-independent approach analysis1987Psychopharmacology, , Volume: 91, Issue:4
Pharmacokinetics of haloperidol in psychotic patients.
AID1146540Ratio of ED50 for po dosed albino Wistar rat assessed as induction of catalepsy to ED50 for apomorphine-induced stereotyped behavior in po dosed albino Wistar rat1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
AID295928Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane2007European journal of medicinal chemistry, Oct, Volume: 42, Issue:10
Synthesis of bridged piperazines with sigma receptor affinity.
AID131872Effective dose required for inhibition of DOI-induced head-twitches in mice on ip administration2001Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10
Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic?
AID4814Inhibition of [3H]ketanserin binding at 5-hydroxytryptamine 2 receptor from rat frontal cortex.1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Effect of linking bridge modifications on the antipsychotic profile of some phthalimide and isoindolinone derivatives.
AID592125Induction of apoptosis in human MCF7 cells expressing sigma receptor assessed as early apoptotic cells using annexin V/propidium iodide staining at 5 uM after 24 hrs by flow cytometry (Rvb = 0.92%)2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Structure-activity study to develop cationic lipid-conjugated haloperidol derivatives as a new class of anticancer therapeutics.
AID190818Total activity (anti psychotic) when compound administered at a doe of 0.05 mg/kg ip in rats1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID37001Inhibition of [3H]prazosin binding to Alpha-1 adrenergic receptor in rat brain membranes1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.
AID230953Ratio of binding to dopamine D2A low/D2A high receptors1999Bioorganic & medicinal chemistry letters, Aug-02, Volume: 9, Issue:15
Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor.
AID1210070Inhibition of CYP2D6 in human liver microsomes using bufuralol substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID701162Displacement of [3H](+)pentazocine from human sigma 1 receptor transfected in HEK293 cell membranes after 120 mins by scintillation counter2012Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862).
AID160616Binding affinity for HIV-1 protease1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
HIV protease: a novel chemotherapeutic target for AIDS.
AID342780Ratio of Ki for human cloned dopamine D2 receptor to Ki for human cloned dopamine D4 receptor2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID1213043Drug metabolism assessed as recombinant human UGT2B15 assessed as O-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID171690Catalytic action on male Wistar rats after subcutaneous administration of 0.03 mg/kg dose of compound1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.
AID1456402Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membrane incubated for 120 mins measured for 5 mins by scintillation counting method
AID1724116Antipsychotic activity in po dosed mouse assessed as suppression in DOI-induced head twitching response2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID1726849Displacement of [3H]pentazocine from human sigma 1 receptor expressed in HEK293 cell membrane incubated for 2 hrs by liquid scintillation counting method
AID1411895Protein binding in human plasma2018MedChemComm, May-01, Volume: 9, Issue:5
Schizophrenia: synthetic strategies and recent advances in drug design.
AID311934Dissociation constant, pKa of the compound2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID1901074Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane measured by competitive radioligand receptor binding assay2022European journal of medicinal chemistry, Feb-15, Volume: 230Synthesis of 8-aminomorphans with high KOR affinity.
AID62887Ability to inhibit [3H]haloperidol binding to dopamine receptor in rat striatal homogenate at a dose of 10E-8 M1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents.
AID1210014Inhibition of recombinant CYP2J2 (unknown origin)-mediated astemizole O-demethylation assessed as remaining activity at 30 uM after 5 mins by LC-MS/MS analysis relative to control2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID294442Displacement of [3H]YM-09151-2 from human cloned dopamine D3 receptor expressed in CHO cells2007European journal of medicinal chemistry, Jul, Volume: 42, Issue:7
Asymmetric synthesis of chiral piperazinylpropylisoxazoline ligands for dopamine receptors.
AID1853638Potentiation of kanamycin-induced antibacterial activity against Mycobacterium tuberculosis H37Rv assessed as kanamycin MIC incubated for 1 day followed by kanamycin addition for 6 days and by Alamar blue assay2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from
AID655088Neurotoxicity in rat assessed as decrease in spontaneous locomotory activity at 1 umol/kg, ip after 30 mins2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Synthesis and evaluation of 2-amido-3-carboxamide thiophene CB₂ receptor agonists for pain management.
AID540229Volume of distribution at steady state in human after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1686279Displacement of [3H]-7-OH-DPAT from DRD3 in rat olfactory tubercle by scintillation counting2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells.
AID128162Activity of inclined screen in mouse, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID5484In vitro binding affinity for serotonin 5-hydroxytryptamine 2A receptor of rat cerebral cortex using [3H]ketanserin as radioligand2002Journal of medicinal chemistry, Oct-10, Volume: 45, Issue:21
Synthesis and pharmacological evaluation of 1-[(1,2-diphenyl-1H-4-imidazolyl)methyl]-4-phenylpiperazines with clozapine-like mixed activities at dopamine D(2), serotonin, and GABA(A) receptors.
AID1213053Drug metabolism assessed as recombinant human UGT2B4 assessed as N-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID640311Displacement of [3H]clonidine from human Alpha-2C receptor by liquid scintillation counting2012Bioorganic & medicinal chemistry, Feb-01, Volume: 20, Issue:3
Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.
AID204791Binding affinity for sigma-1 receptor measured on guinea pig brain membranes using [3H](+)-pentazocine as radioligand2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Synthesis and structure-activity relationships of naphthamides as dopamine D3 receptor ligands.
AID130877Inhibition against apomorphine-induced turning, after 1 hr of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID21263Permeability coefficient reported (Expressed as Permeability coefficient x 10 e 4 cm/s)1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Computation of brain-blood partitioning of organic solutes via free energy calculations.
AID1292393Unbound fraction in human serum1987Psychopharmacology, , Volume: 91, Issue:4
Pharmacokinetics of haloperidol in psychotic patients.
AID65111Binding affinity was measured against dopamine (D2) receptor in rat using [3H]spiperone as radioligand1994Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.
AID169953Compound was assessed for its ability to produce catalepsy in rats; Dose administered perorally is 1.25 mg/kg; Group score is 16-301980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
4-Piperazinyl-10H-thieno[2,3-b][1,5]benzodiazepines as potential neuroleptics.
AID712770Displacement of [3H]pentazocine from sigma 1 receptor in rat brain membrane after 2.5 hrs by microbeta scintillation counting analysis2012ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12
From α4β2 Nicotinic Ligands to the Discovery of σ1 Receptor Ligands: Pharmacophore Analysis and Rational Design.
AID173682Locomotor activity after no pretreatment in rat at low-dose region expressed as percent of saline control1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Novel dopamine receptor agonists and antagonists with preferential action on autoreceptors.
AID255035Inhibitory concentration against opioid receptor sigma 2 of rat cerebral cortex using [3H]DTG upon incubation for 120 minutes at 22 degree C2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective sigma1 ligands. Part 1.
AID1213041Drug metabolism assessed as recombinant human UGT1A10 assessed as O-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID176333Inhibition of d-amphetamine induced stereotypy in rats; i.p. treatment 24 hr before amphetamine.1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Neuroleptics from the 4a,9b-cis- and 4a,9b-trans-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole series. 2.
AID1570284Displacement of [3H]Spiperone from human D2S receptor expressed in CHOK1 cell membranes measured after 120 mins
AID128985Anticonvulsant activity against electroshock-induced convulsions, after 5 hours of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID178319Compound was tested for anti-dopamine activity in vivo by its ability to inhibit apomorphine induced hyperactivity in rat1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Potential neuroleptic agents. 4. Chemistry, behavioral pharmacology, and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides.
AID711584Dissociation constant, pKa of the compound2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID178537Compound was tested for inhibition of spontaneous motor activity in rat when administered perorally1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.
AID203833Affinity at sigma-2 site by inhibition of [3H]1,3-di(2-tolyl)guanidine (DTG) binding in guinea pig brain.1994Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.
AID1144248Reduction in body temperature in Wistar rat at 1 to 6 mg/kg, ip relative to control1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Synthesis and biological actions of 2-substituted quinolizidines.
AID233510Ratio between pKi values of D1 and D2 receptors1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
Synthesis and atypical antipsychotic profile of some 2-(2-piperidinoethyl)benzocycloalkanones as analogues of butyrophenone.
AID63238Inhibition of [35 S] GTP gamma S binding to cell membranes expressing Dopamine receptor D2 with dopamine1996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Novel (R)-2-amino-5-fluorotetralins: dopaminergic antagonists and inverse agonists.
AID128819Antagonistic activity against amphetamine-induced hypermotility, after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID65619Half-maximal inhibition of [3H]-7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID170155Effect of locomotor activity in reserpine pretreated rats at the dose of 25.0uM/Kg, sc ip after count of 30 minute1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
Synthesis and pharmacology of the enantiomers of cis-7-hydroxy-3-methyl-2-(dipropylamino)tetralin.
AID61531Tested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligand1994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
The discovery and structure-activity relationships of 1,2,3,6-tetrahydro-4-phenyl-1-[(arylcyclohexenyl)alkyl]pyridines. Dopamine autoreceptor agonists and potential antipsychotic agents.
AID540228Clearance in human after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID517712Displacement of [3H]Ketanserin from 5-HT2 receptor in pig cortex membranes2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Bioisosteric replacement leading to biologically active [2.2]paracyclophanes with altered binding profiles for aminergic G-protein-coupled receptors.
AID238491Binding affinity for human recombinant dopamine receptor D32004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 receptor selectivity.
AID680297TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: 0.5 uM, Haloperidol: 80 uM) in MDR1-expressing NIH-3T3 cells2004Biochemical and biophysical research communications, Mar-19, Volume: 315, Issue:4
Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies.
AID1184610Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
Synthesis and binding profile of haloperidol-based bivalent ligands targeting dopamine D(2)-like receptors.
AID218904In vitro affinity towards D2 receptor using [3H]spiroperidol as radioligand in striatum1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents.
AID5127In vitro binding affinity for 5-hydroxytryptamine 2 receptor2001Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10
Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic?
AID1308627Growth inhibition of human DAN-G cells incubated for 96 hrs by crystal violet assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity?
AID238525Binding affinity for human recombinant dopamine receptor D4.22004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 receptor selectivity.
AID178399Effective dose for motor incoordination in rats was determined by rotarod method1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.
AID451850Dopaminergic activity in apomorphine-induced Wistar rat assessed as licking count at 0.5 mg/kg, iv treated 15 mins before apomorphine challenge measured after 10 mins for 60 mins by behavioral study2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Synthesis and dopaminergic activity of some E-3-(piperidin-1-yl)-1-(4-substituted phenyl)prop-2-en-1-one derivatives.
AID1060808Displacement of [3H]DTG from guinea pig brain sigma2 receptor after 120 mins by scintillation counting analysis in presence of SKF10,0472014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
From NMDA receptor antagonists to discovery of selective σ₂ receptor ligands.
AID1174260Selectivity index, ratio of Ki for human sigma 2 receptor in human Jurkat cell membranes to Ki for human sigma 1 receptor in human Jurkat cell membranes2015European journal of medicinal chemistry, Jan-07, Volume: 89Carboline- and phenothiazine-derivated heterocycles as potent SIGMA-1 protein ligands.
AID269018Inhibition of (E)-1-(4-chlorophenyl)-3-(4-pyridin-2-ylpiperazin-1-yl)propan-1-one O-methyloxime-induced erectogenic effect in Wistar rat at 1 umol/kg, ip2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
1-aryl-3-(4-pyridine-2-ylpiperazin-1-yl)propan-1-one oximes as potent dopamine D4 receptor agonists for the treatment of erectile dysfunction.
AID1213091Drug metabolism assessed as recombinant human UGT1A9 assessed as O-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1570062Displacement of [3H]-raclopride from human D2 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT
AID5241Binding affinity towards 5-hydroxytryptamine 2 receptor1987Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.
AID1762065Antipsychotic activity in po dosed mouse assessed as reduction in MK-801-induced hyperlocomotor activity2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID298481Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID203837Selectivity for sigma 2 receptor and sigma 1 receptor from guinea pig brain was evaluated1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand.
AID444005Displacement of [3H](+)-pentazocine from sigma1 receptor in human Jurkat cell membrane2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane.
AID1594271Displacement of [3H]-(+)-pentazocine from recombinant human sigma1 receptor expressed in HEK293 cell membranes after 120 mins by microbeta scintillation counting method2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Discovery of a novel class of potent and selective tetrahydroindazole-based sigma-1 receptor ligands.
AID227558In vitro ability to displace [3H]ketanserin from 5-hydroxytryptamine 2A receptor in rat brain.1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID596435Biodistribution in haloperidol-pretreated ICR mouse liver at 1 mg/kg, iv pretreated 5 mins before haloperidol challenge measured after 60 mins postinjection (Rvb = 5.73 +/- 0.95 %ID/g)2011Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9
Synthesis and biological evaluation of novel 4-benzylpiperazine ligands for sigma-1 receptor imaging.
AID37170Ability to inhibit [3H]WB-4101 binding to alpha-1 adrenergic receptor was determined in rat1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
AID414525Hypothermic activity in Sprague-Dawley rat assessed as decrease in core body temperature at 5 mg/kg, ip measured up to 150 mins2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Comparison of N-terminal modifications on neurotensin(8-13) analogues correlates peptide stability but not binding affinity with in vivo efficacy.
AID177895Inhibition of conditioned avoidance response (CAR) in fasted male Sprague-Dawley rats.1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Buspirone analogues. 1. Structure-activity relationships in a series of N-aryl- and heteroarylpiperazine derivatives.
AID1185962Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Further evaluation of the tropane analogs of haloperidol.
AID169630Evaluated for biochemical levels of DOPAC in nonpretreated habituated rats for subcuteneous dose of 100 micro mol/kg in rat striatum1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.
AID112509In vivo Antipsychotic activity was quantified by inhibition of apomorphine-induced climbing(CL 95%) by mice1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical an
AID131247Neuroleptic activity determined by its inhibitory effect on apomorphine-induced climbing behavior in mice by intraperitoneal administration in experiment 1 Range is 0.04-0.091987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Synthesis and neuroleptic activity of a series of 1-[1-(benzo-1,4-dioxan-2-ylmethyl)-4-piperidinyl]benzim idazolone derivatives.
AID781326pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID176500Inhibition of catalepsy in rat by subcutaneous administration of compound1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID418674Cytotoxicity against human 5637 cells after 96 hrs by crystal violet staining2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Dancing of the second aromatic residue around the 6,8-diazabicyclo[3.2.2]nonane framework: influence on sigma receptor affinity and cytotoxicity.
AID45419Displacement of [3H]spiperone from CHO-K1 cell membranes expressing human dopamine receptor D21993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID203842Binding affinity towards sigma 2 receptor was determined in rat liver membrane using [3H]DTG as radioligand in presence of dextrallorphan1994Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2
A new approach to the design of sigma-2-selective ligands: synthesis and evaluation of N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1- pyrrolidinyl)ethylamine-related polyamines at sigma-1 and sigma-2 receptor subtypes.
AID1144222Depression of spontaneous motor activity in Swiss-Webster mouse at 2.5 mg/kg, ip by photocell cage test relative to control1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Synthesis and biological actions of 2-substituted quinolizidines.
AID342774Binding affinity to human cloned muscarinic M1 receptor2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID457703Toxicity in CF1 mouse assessed as induction of catalepsy by measuring time spent on elevated wood bar at 4 mg/kg, po after 30 mins (Rvb = 1.8 +/- 1.1 sec)2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors.
AID5229Binding affinity determined in radioreceptor binding assay by using [3H]ketanserin radioligand against 5-hydroxytryptamine 2 receptor1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Pyrrole mannich bases as potential antipsychotic agents.
AID131363Effect on Motor activity in mouse following i.p. administration.1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
N6-(2,2-diphenylethyl)adenosine, a novel adenosine receptor agonist with antipsychotic-like activity.
AID35638Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding; ND = 'Not determined'1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID540227Volume of distribution at steady state in monkey after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID303630Growth inhibition of human MCF7 cells after 96 hrs2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Synthesis of bicyclic sigma receptor ligands with cytotoxic activity.
AID61521In vitro binding affinity against Dopamine receptor D1 in rat striatal tissue1993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study.
AID63858Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay2003Bioorganic & medicinal chemistry letters, Sep-01, Volume: 13, Issue:17
1H-Pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes: a unique structural class of dopamine D4 selective ligands.
AID320561Displacement of [3H]PB28 from sigma 2 receptor in rat liver membrane2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Tritium radiolabelling of PB28, a potent sigma-2 receptor ligand: pharmacokinetic and pharmacodynamic characterization.
AID196822Compound was evaluated for the pA2 values against Norepinephrine (NE)-induced contraction of isolated rat vas deferens1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Synthesis and antidopaminergic activity of some 3-(aminomethyl)tetralones as analogues of butyrophenone.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID177725Induction of catalepsy in rats when administered intraperitoneally 4 hr prior to measurement to groups of 9 animals. value is based on at least three dose levels(40% of animals showed catalepsy)1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
AID224651Area under curve(AUC) value of HVA level after total treatment in dialysates collected from rat striatum.2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID6648Binding affinity towards rat 5-hydroxytryptamine 7 receptor2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
AID226638Hill coefficient value.1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Synthesis of (R,S)-2'-trans-7-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'- propenyl)-amino]tetralin (trans-7-OH-PIPAT): a new D3 dopamine receptor ligand.
AID150736Fraction of high affinity at binding site of human P-Glycoprotein (P-gp) in two-affinity model2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID162182In vitro inhibition of recombinant HIV-1 protease expressed in Escherichia coli strain D12101994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Haloperidol-based irreversible inhibitors of the HIV-1 and HIV-2 proteases.
AID672168Displacement of [3H]raclopride from human D2L receptor expressed in CHO cells after 60 mins by scintillation proximity assay2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Hit-to-lead investigation of a series of novel combined dopamine D2 and muscarinic M1 receptor ligands with putative antipsychotic and pro-cognitive potential.
AID1461565Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand binding assay2017Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19
Potent haloperidol derivatives covalently binding to the dopamine D2 receptor.
AID303624Growth inhibition of human 5637 cells at 20 uM after 96 hrs relative to control2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Synthesis of bicyclic sigma receptor ligands with cytotoxic activity.
AID277674Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane2007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.
AID1772561Aqueous solubility of compound in PBS buffer at 200 uM at pH 7.4 incubated for 2 hrs2021European journal of medicinal chemistry, Nov-05, Volume: 223Non-carboxylic acid inhibitors of aldose reductase based on N-substituted thiazolidinedione derivatives.
AID1545634Displacement of [3H]N-methylspiperone from human recombinant D2 receptor expressed in HEK293 cells at 10'-7 M incubated for 60 mins by microbeta2 scintillation counter relative to control2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Novel multitarget 5-arylidenehydantoins with arylpiperazinealkyl fragment: Pharmacological evaluation and investigation of cytotoxicity and metabolic stability.
AID61388Affinity for dopamine receptor D2 binding sites by its ability to displace [3H]spiperone from rat striatum.1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID108860Relative CNS activity of compound was measured in mice (+++ =for activity in > 6 assays)1980Journal of medicinal chemistry, Sep, Volume: 23, Issue:9
Synthesis of 8-aryltetrahydroisoquinolines as dopamine antagonists and evaluation for potential neuroleptic activity.
AID1215123Binding affinity to Wistar rat serum albumin2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID36847In vitro affinity for cortical alpha-1 adrenergic receptor labelled with [3H]WB-41011986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.
AID294443Selectivity for human dopamine D3 receptor over human dopamine D2 receptor2007European journal of medicinal chemistry, Jul, Volume: 42, Issue:7
Asymmetric synthesis of chiral piperazinylpropylisoxazoline ligands for dopamine receptors.
AID1168795Displacement of [3H]Spiperone from D3 receptor (unknown origin) transfected in HEK293T cells at 10 uM after 50 mins by liquid scintillation counting analysis2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Design, synthesis and evaluation of benzo[a]thieno[3,2-g]quinolizines as novel l-SPD derivatives possessing dopamine D1, D2 and serotonin 5-HT1A multiple action profiles.
AID1292379Plasma concentration in psychotic patient1987Psychopharmacology, , Volume: 91, Issue:4
Pharmacokinetics of haloperidol in psychotic patients.
AID181088compound was tested for antipsychotic activity by conditioned avoidance response(CAR) assay in rats with a pretreatment period of 60 min upon peroral administration. Values in brackets indicates 95% confidence limits for ED501998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Orally active benzamide antipsychotic agents with affinity for dopamine D2, serotonin 5-HT1A, and adrenergic alpha1 receptors.
AID439068Displacement of [3H]SCH23390 from human dopamine D1 receptor2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.
AID715355Toxicity in rat assessed as induction of catalepsy up to 1.5 mg/kg, po2012Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
AID204629Binding affinity was measured on Sigma receptor type 1 with guinea pig membranes and [3H]- pentazocine as ligand.2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Radioiodinated N-(2-diethylaminoethyl)benzamide derivatives with high melanoma uptake: structure-affinity relationships, metabolic fate, and intracellular localization.
AID177907Inhibition of firing rates of serotonergic neurons in the dorsal raphe nucleus by intravenous injection in rats1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives.
AID139071Antagonism of apomorphine in reserpinized mice when a dose of 0.3 micro mol/kg is administered intraperitoneally1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives.
AID233508Ratio between pKi values of 5-HT2A and D1 receptors1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
Synthesis and atypical antipsychotic profile of some 2-(2-piperidinoethyl)benzocycloalkanones as analogues of butyrophenone.
AID176195Effective dose to induce catalepsy in 50% of the rats1981Journal of medicinal chemistry, Oct, Volume: 24, Issue:10
Synthesis and neuroleptic activity of benzamides. Cis-N-(1-benzyl-2-methylpyrrolidin-3-yl)-5-chloro-2-methoxy-4-(methylamino)benzamide and related compounds.
AID61399Affinity towards Dopamine receptor D2 was evaluated in rat striatal membrane using [3H]spiperone as radioligand1996Journal of medicinal chemistry, Dec-06, Volume: 39, Issue:25
Structure-activity relationship studies on the 5-HT(1A) receptor affinity of 1-phenyl-4-[omega-(alpha- or beta-tetralinyl)alkyl]piperazines. 4.
AID63251Displacement of [3H]spiperone from human Dopamine receptor D22004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species.
AID64478In vitro binding affinity at human cloned Dopamine receptor D2L expressed in Sf9 cell membranes2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors.
AID149044Binding affinity was measured against opioid receptor in rat using [3H]naloxone as radioligand1994Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID176178Compound was tested in vivo for its ability to antagonize extrapolatory behavior impairment induced by DOPA in rats upon intraperitoneal administration1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
Design of N-acylprolyltyrosine "tripeptoid" analogues of neurotensin as potential atypical antipsychotic agents.
AID61032Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand1991Journal of medicinal chemistry, Dec, Volume: 34, Issue:12
Novel 1-phenylpiperazine and 4-phenylpiperidine derivatives as high-affinity sigma ligands.
AID1601982Displacement of [3H]-5-CT from recombinant human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT
AID781330pKa (acid-base dissociation constant) as determined by potentiometric titration2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID781328pKa (acid-base dissociation constant) as determined by Luan ref: Pharm. Res. 20052014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID711575Clearance in rat liver microsomes2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID1596349Displacement of [3H]-DTG from sigma2 receptor (unknown origin) incubated for 120 mins by scintillation counting method
AID63089In vitro binding affinity at human cloned dopamine receptor D2 (long) stably expressed in CHO cells by [3H]spiperone displacement.2003Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3
SLV310, a novel, potential antipsychotic, combining potent dopamine D2 receptor antagonism with serotonin reuptake inhibition.
AID1691230Antagonist activity at D2 receptor (unknown origin)2020European journal of medicinal chemistry, May-01, Volume: 193Discovery of aryl-piperidine derivatives as potential antipsychotic agents using molecular hybridization strategy.
AID711580Inhibition of human dopamine D2 receptor2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID629464Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Development of a bivalent dopamine D₂ receptor agonist.
AID1636356Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID232153Ratio of 5-HT2A receptor to that of dopamine 2 (D2) receptor in rat tissue homogenate2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.
AID5255Compound was evaluated for in vitro binding affinity towards 5-hydroxytryptamine 2 receptor in rat cortex using [3H]- spiperone as radioligand1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia.
AID1519019Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes incubated for 120 mins by solid scintillation counting method
AID36713Binding affinity to alpha-1 adrenergic receptor from rat brain homogenate, using [3H]- prazosin as the competitive ligand2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.
AID176062Effect on the synthesis rates of dopamine in the rat ventral limbic brain region at 2.7 micro mol/kg1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 1. Synthesis and structure-activity relationships of 2,3,3a,4,5,9b-hexahydro-1H-benz[e]indole derivatives.
AID169395Locomotory activity was determined in non pretreated rats at a dose of 2.7 umol/kg by subcutaneous administration1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID203702The compound was evaluated for affinity at sigma-1 site by inhibition of [3H](+)-pentazocine (PENT) binding in guinea pig brain.1994Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.
AID1462129Displacement of [3H]-pentazocine from sigma1 receptor in guinea pig brain membranes after 120 mins by liquid scintillation counting2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Chiral-pool synthesis of 1,2,4-trisubstituted 1,4-diazepanes as novel σ
AID1185960Displacement of [3H]Ketanserin from human 5-HT2A receptor by liquid scintillation counting2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Further evaluation of the tropane analogs of haloperidol.
AID298482Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID226576In vitro binding affinity for D2 receptor compared to that of D4 receptor2001Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10
Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic?
AID1215955Apparent permeability of the compound at 50 uM at pH 7.4 after 240 mins by PAMPA2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Significance of reductive metabolism in human intestine and quantitative prediction of intestinal first-pass metabolism by cytosolic reductive enzymes.
AID228343Relative binding to dopamine D2 and D4 receptor, ratio of Ki1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents.
AID130711In vivo inhibition of the apomorphine-induced climbing behavior in mice2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.
AID1762066Induction of catalepsy in po dosed mouse by Horizontal grid and elevated bar test2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID65602Binding affinity for dopamine receptor D3 expressed in Sf9 cells using [125I]IABN the radioligand.2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Synthesis and structure-activity relationships of naphthamides as dopamine D3 receptor ligands.
AID420669Lipophilicity, log D at pH 7.02009European journal of medicinal chemistry, May, Volume: 44, Issue:5
GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.
AID169616Compound is evaluated DOPA accumulation in nonhabituated rats for (1.3 micro mol/kg) subcuteneous dose in rat striatum1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.
AID176762In vivo DOPA accumulation in non pre-treated rat limbic system following s.c. administration.1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID1185972Displacement of [3H]QNB from human muscarinic M3 receptor by liquid scintillation counting2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Further evaluation of the tropane analogs of haloperidol.
AID138760Ability to stimulate dopaminergic systems by effect on locomotor activity in reserpinized mice when a dose of 2.7 micro mol/kg is administered intraperitoneally1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 1. Synthesis and structure-activity relationships of 2,3,3a,4,5,9b-hexahydro-1H-benz[e]indole derivatives.
AID592130Induction of apoptosis in against african green monkey COS1 cells expressing sigma receptor assessed as necrotic cells using annexin V/propidium iodide staining at 5 uM after 24 hrs by flow cytometry (Rvb = 0.08%)2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Structure-activity study to develop cationic lipid-conjugated haloperidol derivatives as a new class of anticancer therapeutics.
AID1558957Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual μ-Opioid Receptor Agonists and σ
AID112272Inhibition of apomorphine induced climbing affects in mice by administering the compound subcutaneously in mice1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID176335Inhibition of d-amphetamine induced stereotypy in rats; i.p. treatment 5 hr before amphetamine.1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Neuroleptics from the 4a,9b-cis- and 4a,9b-trans-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole series. 2.
AID705397Antipsychotic activity in sc dosed rat assessed as decrease in amphetamine-induced spontaneous locomotor activity2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID705399Antipsychotic activity in sc dosed rat assessed as decrease in spontaneous locomotor activity2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID1207248Effective free therapeutic plasma concentration (EFTPC): the concentration of unbound compund in the blood plasma at therapeutic dose (mean of range)2011Cardiovascular research, Jul-01, Volume: 91, Issue:1
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID1071722Toxicity in po dosed Kunming mouse assessed as induction of catalepsy2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics.
AID1185975Displacement of [3H]Citalopram from human Serotonin transporter by liquid scintillation counting2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Further evaluation of the tropane analogs of haloperidol.
AID131052Inhibitory activity against tremorine-induced salivation, after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID87527Compound was tested for the binding affinity against rat cortical H1 receptor by Radio ligand [3H]pyrilamine binding assay.1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.
AID1292389Drug lag time in psychotic patient (9 patients) at 2.9 +/- 1.2 mg, po by reversed phase HPLC method1987Psychopharmacology, , Volume: 91, Issue:4
Pharmacokinetics of haloperidol in psychotic patients.
AID1215940Unbound intrinsic clearance in human liver S9 fraction at 50 to 1000 nM after 30 to 60 mins by HPLC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Significance of reductive metabolism in human intestine and quantitative prediction of intestinal first-pass metabolism by cytosolic reductive enzymes.
AID1616721Displacement of PPHT-red from SNAP-tagged human D2LR expressed in CHOK1 cell membranes assessed as dissociation rate constant by TR-FRET assay
AID592682Apparent permeability from apical to basolateral side of human Caco2 cells after 2 hrs by LC/MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID134514Contractile activity in skeletal muscles, after 1 hour of peroral administration in mouse at dose 30 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID132101Tested for the inhibition of locomotor activity in mice intraperitoneally; value ranges from 0.2-0.5 mg/Kg1994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
The discovery and structure-activity relationships of 1,2,3,6-tetrahydro-4-phenyl-1-[(arylcyclohexenyl)alkyl]pyridines. Dopamine autoreceptor agonists and potential antipsychotic agents.
AID35191Binding affinity towards alpha-2 adrenergic receptors in rat brain synaptosomal preparations1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects.
AID35276Inhibition of [3H]-prazosin binding to Alpha-1 adrenergic receptor in rat frontal cortex homogenate2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID1308615Displacement of [3H](+)-Pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity?
AID63020In vitro ability to displace [3H]spiroperidol from rat dopamine receptor1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
2-Amino-6-chloro-4-(N-methylpiperazino)pyrimidines, inhibitors of spiroperidol binding.
AID1144230Depression of motor activity in Wistar rat at 1 to 6 mg/kg, ip1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Synthesis and biological actions of 2-substituted quinolizidines.
AID178385Effective dose for apomorphine induced circling behavior was determined in rats after subcutaneous administration of the compound1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Common stereospecificity of opioid and dopamine systems for N-butyrophenone prodine-like compounds.
AID169650Compound is tested for its ability to displace Di-Pr-5,6-ADTN at 0.25 umol/kg subcutaneous dose from rat striatal binding sites in vivo1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.
AID642497Selectivity ratio of Ki for sigma 2 receptor in rat liver homogenates to sigma 1 receptor in guinea pig brain homogenates2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis, radiofluorination and pharmacological evaluation of a fluoromethyl spirocyclic PET tracer for central σ1 receptors and comparison with fluoroalkyl homologs.
AID393360Displacement of [3H]DTG from sigma 2 receptor in rat liver membrane2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Substituted benzo[d]oxazol-2(3H)-one derivatives with preference for the sigma1 binding site.
AID61316In vitro binding affinity against human D2 dopamine receptor in CHO cells by [3H]spiperone displacement.1998Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7
Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist.
AID176965In vivo activity was measured by the intracranial self stimulation in rat1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID702710Neurotoxicity in sc dosed C57BL/6 mouse assessed as induction of catalepsy measured at 0.5 to 1 hr2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Imidazopyridazinones as novel PDE7 inhibitors: SAR and in vivo studies in Parkinson's disease model.
AID595982Selectivity ratio of Ki for sigma 1 receptor in guinea pig brain membranes to Ki for sigma 2 receptor in guinea pig brain membranes2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Novel potent and selective σ ligands: evaluation of their agonist and antagonist properties.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID64931Ability to inhibit the [3H]spiperone binding to striatum Dopamine receptor D2 was determined in rat1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
AID5522Binding affinity measured at the 5-hydroxytryptamine 2A receptor by the inhibition of [3H]ketanserin binding to rat cortex using unlabeled mianserin for nonspecific binding.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID342783Binding affinity to human cloned 5HT1A receptor2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID167992Effective dose for reversal of trifluoperazine-induced catalepsy in rats; I=Inactive (ED50 mg/Kg)1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.
AID1142394Displacement of [3H]spiperone from human D2 receptor transfected in HEK cells2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Shuttle-cargo fusion molecules of transport peptides and the hD2/3 receptor antagonist fallypride: a feasible approach to preserve ligand-receptor binding?
AID145105Binding affinity was measured against N-methyl-D-aspartate (NMDA) receptor in rat using [3H]CGS-19,755 as radioligand at 10 uM1994Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.
AID492185Selectivity ratio of Ki for human dopamine D4 receptor to Ki for human dopamine D2 long receptor2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Synthesis and characterization of selective dopamine D2 receptor antagonists. 2. Azaindole, benzofuran, and benzothiophene analogs of L-741,626.
AID3744Inhibition of [3H]8-OH-DPAT binding at serotonin 5-hydroxytryptamine 1A receptor from rat hippocampus tissue.1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Effect of linking bridge modifications on the antipsychotic profile of some phthalimide and isoindolinone derivatives.
AID141832Compound was tested for the binding affinity against rat cortical Muscarinic acetylcholine receptor M1 by Radio ligand [3H]pirenzepine binding assay.1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.
AID232327Ratio of APO Sterotype ED50 vs catalepsy ED501986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.
AID64802Displacement of [3H]-YM 09151 from african monkey Dopamine receptor D31995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
1-Phenyl-3-(aminomethyl)pyrroles as potential antipsychotic agents. Synthesis and dopamine receptor binding.
AID65726In vitro binding affinity for dopamine receptor D2 of rat nucleus accumbens labeled with [3H]spiperone1987Journal of medicinal chemistry, Jun, Volume: 30, Issue:6
Psychotropic agents: synthesis and antipsychotic activity of substituted beta-carbolines.
AID1704751Therapeutic index, ratio of ED50 for toxicity in po dosed Kunming mouse assessed as catalepsy to ED50 for antipsychotic activity in Kunming mouse assessed as inhibition of apomorphine-induced climbing behavior
AID1249735Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells2015ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
Multicomponent Synthesis and Biological Evaluation of a Piperazine-Based Dopamine Receptor Ligand Library.
AID1136351Neuroleptic activity in ip dosed Long-Evans rat assessed as increase in escape failure1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 4. Central nervous system depressants.
AID170884Percentage change in Total activity (anti psychotic) when compound administered at a doe of 0.125 mg/kg ip in rats1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID1283241Decrease in desmosterol levels in mouse Neuro2a cells by LC-MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts.
AID178868Compound was tested for the inhibition of apomorphine-induced stereotype1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.
AID277673Displacement of [3H]spiperone from human dopamine D3 expressed in CHO cell membrane2007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.
AID1601983Displacement of [3H]-raclopride from recombinant human D2 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT
AID1727501Displacement of [125I]-RHM-4 from sigma 2 receptor in rat liver membranes after 120 mins by microbeta scintillation counting method
AID62917Binding affinity against cloned human dopamine receptor D2 expressed in Chinese hamster ovary (CHO) K-1 cells by displacement of [3H]spiperone.1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
(Aryloxy)alkylamines as selective human dopamine D4 receptor antagonists: potential antipsychotic agents.
AID173705Percent decrease on dopamine agonist-induced rotation in unilaterally 6-OH-DA-lesioned rat at 0.25 mg/kg1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Troponoids. 6. Troponylpiperazines: a new class of dopamine agonists.
AID231638Binding affinity against the D2 dopamine receptor and ratio of IC50(+Na+) / IC50(-Na(+)) [from 2-4 experiments]1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
AID1215937Unbound intrinsic clearance in human intestinal cytosol at 50 to 1000 nM after 30 to 60 mins by HPLC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Significance of reductive metabolism in human intestine and quantitative prediction of intestinal first-pass metabolism by cytosolic reductive enzymes.
AID655663Displacement of [3H]-pentazocine from sigma 1 opioid receptor in rat liver homogenate by liquid scintillation counting2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
Homology Model and Docking-Based Virtual Screening for Ligands of the σ1 Receptor.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID195978effects on Sidman Avoidance performance in rats, number of escape failure (absolute change from control), p<0.01, dose(mg/Kg po) =11998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.
AID393002Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups.
AID1403514Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain cortex membranes incubated for 120 mins measured for 5 mins by scintillation counting method
AID1823675Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
AID157456Binding affinity was measured against phencyclidine (PCP) receptor in rat using [3H]TCP as radioligand1994Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.
AID1135928Neuroleptic activity in ip dosed ICR-DUB mouse assessed as survival administered 1 hr prior to d-amphetamine challenge measured after 24 hrs1978Journal of medicinal chemistry, Jan, Volume: 21, Issue:1
(1-(3-(Phenothiazin-10-yl)propyl)-4-piperidinyl)phenylmethanones, a novel class of long-acting neuroleptic agents.
AID1300808Displacement of [3H](+)-pentazocine from Sigma1 receptor in Dunkin Hartley guinea pig brain membrane after 120 mins by liquid scintillation counting analysis2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
One-pot synthesis and sigma receptor binding studies of novel spirocyclic-2,6-diketopiperazine derivatives.
AID1744234Displacement of [3H]-pentazocine from sigma-1 receptor in human Jurkat cell membrane incubated for 2 hr by liquid scintillation counting method2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management.
AID1213032Drug metabolism assessed as recombinant human UGT1A4 assessed as O-glucuronidation at 25 to 200 uM incubated for 60 mins by LC-MS/MS analysis in presence of 10 uM hecogenin relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID605697Displacement of [3H]SCH23390 from human D2long receptor expressed in CHO cells2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Bivalent dopamine D2 receptor ligands: synthesis and binding properties.
AID156831Compound was tested for its binding affinity towards PCP receptor in rat membranes in the presence of [3H]-(+)-SKF- 10,0471998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
(+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties.
AID169242Induced locomotor stimulation in non pre-treated rats by 13 umol/kg s.c. administration.1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID65919In vitro affinity against Dopamine receptor D42000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.
AID437148Inhibition of haloperidol-induced catalepsy in Swiss albino mouse assessed as time elapsed until release of forepaw from bar at 100 mg/kg, po administered 30 min prior to haloperidol challenge measured after 180 mins by bar test2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
Synthesis of some urea and thiourea derivatives of 3-phenyl/ethyl-2-thioxo-2,3-dihydrothiazolo[4,5-d]pyrimidine and their antagonistic effects on haloperidol-induced catalepsy and oxidative stress in mice.
AID110208Ability to inhibit apomorphine (APO) induced climbing behavior in mice by intraperitoneal administration of compound.; value may range from 0.17 to 0.151987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Antipsychotic activity of substituted gamma-carbolines.
AID711585Solubility of the compound2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID735277Displacement of [3H]-Di-o-tolyguanidine from guinea pig sigma2 receptor after 120 mins by liquid scintillation counting analysis2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Synthesis and biological evaluation of a new series of hexahydro-2H-pyrano[3,2-c]quinolines as novel selective σ1 receptor ligands.
AID265753Inhibition of apomorphine-induced climbing in ip dosed Swiss Webster mouse2006Bioorganic & medicinal chemistry letters, Jun-15, Volume: 16, Issue:12
Evaluation of the eutomer of 4-{3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl}-1-(4-fluorophenyl)butan-1-one, {(+)-SYA 09}, a pyrrolidine analog of haloperidol.
AID737906Displacement of (+)-[3H]pentazocine from rat brain sigma1 receptor by competitive binding assay2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Synthesis and evaluation of novel (18)F-labeled spirocyclic piperidine derivatives as σ1 receptor ligands for positron emission tomography imaging.
AID1213072Intrinsic clearance in recombinant human UGT1A9 measured per mg of protein at 10 to 400 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1136348Neuroleptic activity in Sprague-Dawley rat assessed as inhibition of Sidman avoidance at 1.25 mg/kg, po relative to control1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 4. Central nervous system depressants.
AID311935Partition coefficient, log P of the compound2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID65247Binding affinity was determined against Dopamine receptor D2 using [3H]spiperone1995Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21
Piperazinylalkyl heterocycles as potential antipsychotic agents.
AID62883Displacement of [3H]spiroperidol from dopamine receptor of rat corpus striatum homogenate1980Journal of medicinal chemistry, Jun, Volume: 23, Issue:6
Neuroleptic activity in 5-aryltetrahydro-gamma-carbolines.
AID177493Effect on half-maximal decrease of DOPA formation in rat striatal regions; In active (no significant effect at 1.4 pmol/kg ip)1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
C1- and C3-methyl-substituted derivatives of 7-hydroxy-2-(di-n-propylamino)tetralin: activities at central dopamine receptors.
AID1727502Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by microbeta scintillation counting method
AID1823672Displacement of [3H]-N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
AID1809448Antiangiogenic activity against VEGF-A stimulated human retinal endothelial cell assessed as cell proliferation measured after 48 hrs by crystal violet assay2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Haloperidol Metabolite II Valproate Ester (
AID65625Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells.1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Synthesis of (R,S)-2'-trans-7-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'- propenyl)-amino]tetralin (trans-7-OH-PIPAT): a new D3 dopamine receptor ligand.
AID1861731Cytotoxicity against ER/PR-negative HER2-positive human SK-BR-3 cells harbouring wild type p53 assessed as reduction in cell viability at 100 to 200 uM incubated for 48 hrs by resazurin dye based assay relative to control2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.
AID177252Compound was evaluated for pole-climb avoidance (escape failures) in rat after peroral administration.1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia.
AID1453237Displacement of [3H]DTG from sigma-2 receptor in rat liver membranes after 120 mins by microbeta scintillation counting method
AID1574667Displacement of [3H]DTG from sigma2 receptor in rat liver membranes after 120 mins by scintillation counting method2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Development of Novel Quinoxaline-Based κ-Opioid Receptor Agonists for the Treatment of Neuroinflammation.
AID40403Binding affinity against beta-1 adrenergic receptor in rat brain using [3H]DHA1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents.
AID415889Selectivity for sigma 1 receptor in guinea pig brain membrane over sigma 2 receptor in rat liver membrane2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
1,4-Diazepanes derived from (S)-serine--homopiperazines with improved sigma(1) (sigma) receptor affinity and selectivity.
AID1823823Displacement of [3H]-ketanserin from human human 5-HT2A receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
AID1901078Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membrane measured by competitive radioligand receptor binding assay2022European journal of medicinal chemistry, Feb-15, Volume: 230Synthesis of 8-aminomorphans with high KOR affinity.
AID308687Displacement of [3H]spiperone human cloned dopamine D2 receptor2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics.
AID63513Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.
AID1878190Binding affinity to dopamine D2S receptor (unknown origin) by radioligand displacement assay
AID170877Percentage change in Social interaction when compound administered at a doe of 0.05 mg/kg ip in rats1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID1415567Displacement of [3H]-ifenprodil from GluN2B receptor (unknown origin) expressed in mouse L (tk-) cell membranes after 120 mins by scintillation counting method2017MedChemComm, May-01, Volume: 8, Issue:5
Do GluN2B subunit containing NMDA receptors tolerate a fluorine atom in the phenylalkyl side chain?
AID1570060Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT
AID204145Ability to displace [3H](+)-pentazocine from Sigma opioid receptor type 1 of guinea pig brain2002Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22
Novel sigma receptor ligands. Part 2. SAR of spiro[[2]benzopyran-1,4'-piperidines] and spiro[[2]benzofuran-1,4'-piperidines] with carbon substituents in position 3.
AID298263Displacement of [3H]spiroperidol from human cloned dopamine D3 receptor2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
4-[omega-[4-arylpiperazin-1-yl]alkoxy]phenyl)imidazo[1,2-a]pyridine derivatives: fluorescent high-affinity dopamine D3 receptor ligands as potential probes for receptor visualization.
AID4357The compound was tested binding affinity against 5-hydroxytryptamine 1A receptor from rat brain using [3H]8-OH-DPAT as radioligand at 10e-6 M.1999Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.
AID596436Biodistribution in haloperidol-pretreated ICR mouse spleen at 1 mg/kg, iv pretreated 5 mins before haloperidol challenge measured after 60 mins postinjection (Rvb = 4.35 +/- 0.66 %ID/g)2011Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9
Synthesis and biological evaluation of novel 4-benzylpiperazine ligands for sigma-1 receptor imaging.
AID1393366Displacement of [3H]-8-OH-DPAT from human 5-HT1AR expressed in HEK293 cell membranes after 1 hr by microbeta counting method
AID65817Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 2: asymmetric synthesis and biological evaluation.
AID705723Displacement of [3H](+)-pentazocine from Sigma1 receptor in rat liver homogenate2012Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
New positron emission tomography (PET) radioligand for imaging σ-1 receptors in living subjects.
AID181422Conditioned avoidance response in rats after oral administration1993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system.
AID1558955Displacement of [3H]-DAMGO from human MOR expressed in CHOK1 cell membranes incubated for 60 mins by liquid scintillation counting method2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual μ-Opioid Receptor Agonists and σ
AID64005Binding affinity towards human Dopamine receptor D4.2 in CHO cells1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1458657Displacement of [3H]-methylspiperone from human D2 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Novel 3-(1,2,3,6-Tetrahydropyridin-4-yl)-1H-indole-Based Multifunctional Ligands with Antipsychotic-Like, Mood-Modulating, and Procognitive Activity.
AID4793Compound was evaluated In vitro for its activity by binding to 5-hydroxytryptamine 2 receptor in the rat brain using [3H]ketanserin as radioligand.1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents.
AID476063Displacement of [3H](+)-pentazocine from sigma 2 receptor in rat cerebral cortex membrane by scintillation counting2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Sigma-1 ligands: Tic-hydantoin as a key pharmacophore.
AID177133In vivo antipsychotic activity measured by the induction of catalepsy in rats after po administration.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID4027Binding affinity was evaluated against 5-hydroxytryptamine 1A receptor on rat hippocampus using [3H]8-OH-DPAT as radioligand.; ND = Not determined1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists.
AID50074Ability to lower arterial blood pressure in cat at 100 ug/kg; reversed1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
1-(Aminomethyl)-6,7-dihydroxytetralin derivatives: synthesis and assessment of dopamine-like effects.
AID342790Toxicity in Sprague-Dawley rat assessed as induction of cataleptogenic behavior at 0.3 mg/kg, ip2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID65243Affinity for Dopamine receptor D21998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.
AID35285In vitro binding affinity at Alpha-1 adrenergic receptor in rat cortical tissues2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors.
AID1462752Displacement of [3H]ifenprodil from human NR1-1a/NR2B receptor expressed in Mouse L(tk-) cell membranes incubated for 120 mins by scintillation counting method2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Replacement of benzylic hydroxy group by vinyl or hydroxymethyl moiety at the 3-benzazepine scaffold retaining GluN2B affinity.
AID221062Inhibition of apomorphine-induced climbing behavior in mice, after peroral administration1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1861732Cytotoxicity against ER/PR-positive HER2-negative human MCF7 cells harbouring p53 R175H mutant assessed as reduction in cell viability at 100 uM incubated for 48 hrs by resazurin dye based assay relative to control2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.
AID418676Cytotoxicity against human A427 cells after 96 hrs by crystal violet staining2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Dancing of the second aromatic residue around the 6,8-diazabicyclo[3.2.2]nonane framework: influence on sigma receptor affinity and cytotoxicity.
AID619349Displacement of (-)-[3H]pentazocine from sigma 1 receptor in rat brain membrane after 120 mins2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Synthesis and pharmacological evaluation of indole-based sigma receptor ligands.
AID752209Binding affinity to Sigma receptor (unknown origin) by radioligand displacement assay2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
AID4442Binding affinity for 5-hydroxytryptamine 1A receptor determined using [3H]8-OH-DPAT as radioligand2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1511008Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membranes in the presence of sigma1 receptor ligand (+)-pentazocine incubated for 120 mins by scintillation counting method2019European journal of medicinal chemistry, Oct-15, Volume: 180Discovery of new potent dual sigma receptor/GluN2b ligands with antioxidant property as neuroprotective agents.
AID674364Inhibition of human ERG expressed in HEK293 cells coexpressing Kir2.3 after 30 mins by FluxOR based FLIPR assay2012Journal of natural products, Jun-22, Volume: 75, Issue:6
Isolation and structural elucidation of cyclic tetrapeptides from Onychocola sclerotica.
AID1213080Drug metabolism assessed as human liver microsomes assessed as O-glucuronide measured at 25 uM by LC-MS/MS analysis in presence of 10 uM hecogenin relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1506085Displacement of (+)-[3H]pentazocine from human sigma1 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.
AID410336Displacement of [3H]mesulergine from 5HT2C receptor in CRL:(HA) BR albino guinea pig cortex by scintillation spectrometry2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
AID171230Side effect liability of compound at intraperitoneal dose of 0.5 mg/kg on 6.2 (A9 units)dopamine neurons in the nigrostriatal in rat1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID37007Binding affinity towards Alpha-1 adrenergic receptor binding site using [3H]prazosin.1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
AID1393367Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
AID311932Inhibition of ASM in human H4 cells assessed as residual activity at 10 uM2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID301866Displacement of [3H]spiperone from dopamine D2 receptor in rat brain2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
Rational design, synthesis and evaluation of (6aR( *),11bS( *))-1-(4-fluorophenyl)-4-{7-[4-(4-fluorophenyl)-4-oxobutyl]1,2,3,4,6,6a,7,11b,12,12a(RS)-decahydropyrazino[2',1':6,1]pyrido[3,4-b]indol-2-yl}-butan-1-one as a potential neuroleptic agent.
AID65078Binding affinity against dopamine receptor D2 from rat corpus striatum by using radioligand [3H]sulpiride1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bridged gamma-carbolines and derivatives possessing selective and combined affinity for 5-HT2 and D2 receptors.
AID170878Percentage change in Social interaction when compound administered at a doe of 0.125 mg/kg ip in rats1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID1861730Cytotoxicity against ER/PR-positive HER2-negative human MCF7 cells harbouring p53 R175H mutant assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based assay2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.
AID226336Tested for [3H]DTG binding to sigma-2 receptor in NG108-15 membrane1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID113719Inhibition of noradrenaline lethal effects in mice as alpha-1 induced adrenoceptor antagonist activity1998Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5
Novel antipsychotic agents with dopamine autoreceptor agonist properties: synthesis and pharmacology of 7-[4-(4-phenyl-1-piperazinyl)butoxy]-3,4-dihydro-2(1H)-quinolinone derivatives.
AID132130Tested in vivo for their ability to induction of catalepsy in mice1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents.
AID64960Ability to displace [3H]spiperone (0.3 nM) from CHO cells of human Dopamine receptor D32003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
AID4356Binding affinity towards 5-hydroxytryptamine 1A receptor of rat brain synaptosomal preparations1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects.
AID228503The selectivity was calculated as pKi [3H]spiperone minus pKi [3H]SCH-23,390.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Synthesis and antidopaminergic activity of some 3-(aminomethyl)tetralones as analogues of butyrophenone.
AID330537Increase in phospho-AMPK levels in H1RKO mouse hyphalamic slices at 500 nM after 30 mins by Western blotting2007Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9
From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID194377Effect of compound (0.2 mg/kg ip) on the concentration of DOPAC/DA in rat mesolimbic region1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID481107Displacement of [3H]ditolylguanidine from sigma2 receptor in rat liver membrane2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives.
AID161283Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.12003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Characterization of HERG potassium channel inhibition using CoMSiA 3D QSAR and homology modeling approaches.
AID178397Effective dose for inhibition of spontaneous motor activity in rats1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.
AID1288457Displacement of [3H](+)-pentazocine from human sigma1 receptor by PDSP assay2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Tetrahydroprotoberberine alkaloids with dopamine and σ receptor affinity.
AID1213079Drug metabolism assessed as recombinant human UGT1A4 assessed as O-glucuronidation at 25 to 200 uM incubated for 60 mins by LC-MS/MS analysis in presence of 10 uM gemfibrozil relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1213055Drug metabolism assessed as recombinant human UGT2B15 assessed as N-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID169437Potential antipsychotic activity was assessed by measuring the ability to block the conditioned avoidance response(CAR) in rats on oral administration.1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Antipsychotic activity of substituted gamma-carbolines.
AID176804In vivo activity administered intraperitoneally was determined by pole climb avoidance in rat1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID242943Ratio of dopamine receptor D3 and D4 ki values2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.
AID1213048Drug metabolism assessed as recombinant human UGT1A6 assessed as N-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1728274Displacement of [3H]-pentazocine from sigma1 receptor in guinea pig brain membrane incubated for 120 mins by liquid scintillation counting method2021European journal of medicinal chemistry, Jan-15, Volume: 210Novel σ
AID35289In vitro binding affinity towards alpha-1 adrenergic receptor in rat frontal cortex homogenate using of [3H]prazosin as radioligand2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.
AID130881Inhibition of apomorphine induced mouse climbing, administered intraperitoneally1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID243053Ratio of inhibitory constant for 5-hydroxytryptamine 2A receptor to that of dopamine receptor D2 2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Synthesis and binding affinity of novel 3-aminoethyl-1-tetralones, potential atypical antipsychotics.
AID274704Antipsychotic activity in Sprague-Dawley rat assessed as ability to reverse apomorphine effect on prepulse inhibition of the startle response at 1 mg/kg, sc2006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Design and synthesis of novel derivatives of the muscarinic agonist tetra(ethylene glycol)(3-methoxy-1,2,5-thiadiazol-4-yl) [3-(1-methyl-1,2,5,6-tetrahydropyrid-3-yl)-1,2,5-thiadiazol-4-yl] ether (CDD-0304): effects of structural modifications on the bind
AID1123527Neuroleptic activity in Wistar HLA rat assessed as inhibition of methamphetamine-induced stereotyped behavior at 0.2 mg/kg, ip administered 20 mins before methamphetamine challenge measured every 30 mins for 3 hrs followed by every 1 hr for further 3 hrs1979Journal of medicinal chemistry, Jun, Volume: 22, Issue:6
Synthesis of 2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole derivatives and their central nervous system activities.
AID1213070Drug metabolism assessed as recombinant human UGT1A9 assessed as O-glucuronidation at 10 to 400 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID62886compound was tested for inhibition of 0.5 nM [3H]spiroperidol binding to dopamine receptor from rat striatal membrane.1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Neuroleptic activity of chiral trans-hexahydro-gamma-carbolines.
AID1809443Displacement of [3H](+)-pentazocine from sigma 2 receptor in guinea pig brain membranes after 120 mins by microbeta scintillation counting method2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Haloperidol Metabolite II Valproate Ester (
AID235774Therapeutic ratio by Subcutaneous dose of administration (quotient ED50 catalepsy/ED50 climbing)1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID586715Intrinsic activity at human D2 receptor expressed in human HEK293 cells assessed as inhibition of forskolin-dependent accumulation of [3H]-cyclic AMP at 10 times Ki by spectrophotometric analysis2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Synthesis and pharmacological evaluation of fluorine-containing D₃ dopamine receptor ligands.
AID1597396Displacement of [3H]-(+)-MK-801 from NMDA PCP binding site in pig brain cortex membrane at 1 uM incubated for 120 mins by scintillation counting method relative to control
AID679764TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: ? uM, Haloperidol: 100 uM) in MDR1-expressing MDCKII cells2002The Journal of pharmacology and experimental therapeutics, Dec, Volume: 303, Issue:3
Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs.
AID64974Binding affinity against cloned human dopamine receptor D3 expressed in Chinese hamster ovary (CHO) K-1 cells by displacement of [3H]spiperone.1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
(Aryloxy)alkylamines as selective human dopamine D4 receptor antagonists: potential antipsychotic agents.
AID65740In vitro binding affinity towards dopamine receptor D2 in rat striatal membranes by [3H]sulpiride displacement.1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Examination of the D2/5-HT2 affinity ratios of resolved 5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indoles: an enantioselective approach toward the design of potential atypical antipsychotics.
AID1185968Displacement of [3H]Mesulergine from rat 5-HT2C receptor by liquid scintillation counting2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Further evaluation of the tropane analogs of haloperidol.
AID61498Binding affinity towards Dopamine receptor D11987Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.
AID142870Binding affinity was measured against muscarinic (M2) receptor at 10 uM in rat using [3H]QN as radioligand1994Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.
AID87514Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID61615Inhibition of [35S]GTP-gamma-S, binding to cell membranes expressing dopamine D2A receptor at 1 uM1999Bioorganic & medicinal chemistry letters, Aug-02, Volume: 9, Issue:15
Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor.
AID458633Displacement of [3H]spiperone from human dopamine D2 receptor at high affinity state expressed in HEK293 cells2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
AID259125Displacement of [3H]PD 128907 from rat ventral striatal membrane dopamine D3-like receptor2006Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2
Design of novel hexahydropyrazinoquinolines as potent and selective dopamine D3 receptor ligands with improved solubility.
AID1071723Antipsychotic activity in po dosed Kunming mouse assessed as reduction in MK801-induced hyperactivity compound administered 30 mins prior to MK801 challenge measured for 90 mins post challenge2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics.
AID1393476Effect on failure incidence during conditioned avoidance response test in ip dosed Sprague-Dawley rat administered 60 mins prior to testing
AID1655191Displacement of [3H]-(+)pentazocine from sigma-1 receptor in guinea pig brain membranes after 120 mins by scintillation counting method2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Synthesis, Cytotoxicity Evaluation, and Computational Insights of Novel 1,4-Diazepane-Based Sigma Ligands.
AID63087In vitro ability to inhibit the binding of [3H]spiperone to cloned human Dopamine receptor D2 using apomorphine induced climbing test in male Swiss mice2003Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21
The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+.
AID65127Displacement of the radioligand [3H]YM-09151-2 from cloned human Dopamine receptor D3 expressed in CHO cells2002Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
Design and synthesis of a piperazinylalkylisoxazole library for subtype selective dopamine receptor ligands.
AID4824In vitro binding affinity was measured on serotonergic 5-hydroxytryptamine 2 receptor by displacement of [3H]- ketanserin1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents.
AID62443Inhibition of binding of 1.6 nM [3H]haloperidol to dopamine receptor by 50%1981Journal of medicinal chemistry, Sep, Volume: 24, Issue:9
Synthesis and evaluation of 1,2,3,4-tetrahydro[1]benzothieno[2,3-h]isoquinolines as dopamine antagonists.
AID1462755Displacement of [3H](+)-Pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Replacement of benzylic hydroxy group by vinyl or hydroxymethyl moiety at the 3-benzazepine scaffold retaining GluN2B affinity.
AID619351Selectivity ratio of Ki for sigma 1 receptor in rat brain membrane to sigma 2 receptor in rat brain membrane2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Synthesis and pharmacological evaluation of indole-based sigma receptor ligands.
AID113718Inhibition of the GBL-induced increase in DOPA synthesis in mice; IA = inactive1998Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5
Novel antipsychotic agents with dopamine autoreceptor agonist properties: synthesis and pharmacology of 7-[4-(4-phenyl-1-piperazinyl)butoxy]-3,4-dihydro-2(1H)-quinolinone derivatives.
AID195963effects on Sidman Avoidance performance in rats, number of Avoidance performance(% change from control) p<0.001 dose(mg/Kg po) =11998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.
AID231707Ratio between binding affinities of dopamine D2 and serotonin 5-HT 2A receptors1998Bioorganic & medicinal chemistry letters, Dec-15, Volume: 8, Issue:24
Butyrophenone analogues in the carbazole series: synthesis and determination of affinities at D2 and 5-HT2A receptors.
AID61677Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
Synthesis and atypical antipsychotic profile of some 2-(2-piperidinoethyl)benzocycloalkanones as analogues of butyrophenone.
AID188454Drug pretreatment vs. vehicle pretreatment; statistical analysis by Student's t test at 0.25 mg/kg1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Troponoids. 6. Troponylpiperazines: a new class of dopamine agonists.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID112271Inhibition of apomorphine induced climbing affects in mice by administering the compound perorally in mice1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID113154Dopaminergic antagonistic activity was determined in vivo by antagonising apomorphine induced climbing behavior (APO) in mice by oral administration2003Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3
SLV310, a novel, potential antipsychotic, combining potent dopamine D2 receptor antagonism with serotonin reuptake inhibition.
AID6022Compound was tested for the Binding affinity against N1e-115 neuroblastoma 5-hydroxytryptamine 3 receptor by Radio ligand [3H]GR-65630 binding assay.1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.
AID303622Selectivity for guinea pig brain sigma 1 receptor to rat liver sigma 2 receptor2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Synthesis of bicyclic sigma receptor ligands with cytotoxic activity.
AID1204343Displacement of [3H]N-methylspiperone from human recombinant dopamine D2 receptor expressed in CHOK1 cells assessed as total radioligand binding at 1 uM incubated for 60 mins by microbeta plate reader based method2015European journal of medicinal chemistry, Jun-05, Volume: 97Structure-activity relationships and molecular studies of novel arylpiperazinylalkyl purine-2,4-diones and purine-2,4,8-triones with antidepressant and anxiolytic-like activity.
AID231655Binding ratio of -log Ki between D2 and M receptors1993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study.
AID301867Displacement of [3H]ketanserin from 5HT2A receptor in rat brain2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
Rational design, synthesis and evaluation of (6aR( *),11bS( *))-1-(4-fluorophenyl)-4-{7-[4-(4-fluorophenyl)-4-oxobutyl]1,2,3,4,6,6a,7,11b,12,12a(RS)-decahydropyrazino[2',1':6,1]pyrido[3,4-b]indol-2-yl}-butan-1-one as a potential neuroleptic agent.
AID303629Growth inhibition of human A427 cells after 96 hrs2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Synthesis of bicyclic sigma receptor ligands with cytotoxic activity.
AID185023Minimum effective dose required in the catalepsy experiment in rats2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 2: asymmetric synthesis and biological evaluation.
AID1197502Displacement of [3H](+)Pentazocine from sigma 1 receptor in human Jurkat cells after 120 mins by liquid scintillation counting analysis2015European journal of medicinal chemistry, Mar-06, Volume: 92Synthesis and pharmacological evaluation of benzannulated derivatives as potent and selective sigma-1 protein ligands.
AID393184Displacement of [3H](+)-pentazocine from sigma1 opioid receptor in guinea pig brain by solid scintillation counting2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
Relationships between the structure of 6-substituted 6,8-diazabicyclo[3.2.2]nonan-2-ones and their sigma receptor affinity and cytotoxic activity.
AID625277FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of less concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
AID391273Displacement of [3H]spiperone from human cloned dopamine D2 receptor2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Synthesis, binding affinity, and molecular docking analysis of new benzofuranone derivatives as potential antipsychotics.
AID112392Tremor after subcutaneous administration in mice was determined; nt=Not tested1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Muscarinic agonists with antipsychotic-like activity: structure-activity relationships of 1,2,5-thiadiazole analogues with functional dopamine antagonist activity.
AID231653Binding ratio of -log Ki between 5-HT2 and D2 receptors1993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study.
AID1649553Inhibition of human ERG expressed in HEK293 cells measured after 30 mins by FluxOR dye based FLIPR TETRA assay2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
AID63842In vitro binding affinity for Dopamine receptor D42001Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10
Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic?
AID391476Displacement of [3H]di-o-tolylguanidine from sigma 2 receptor in rat liver membrane2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Thiophene bioisosteres of spirocyclic sigma receptor ligands. 1. N-substituted spiro[piperidine-4,4'-thieno[3,2-c]pyrans].
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID711579Inhibition of human dopamine D4 receptor2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID1127304Displacement of [3H]-DTG from sigma 2 receptor in Dunkin Hartley guinea pig membrane after 120 mins by liquid scintillation counting analysis in the presence of sigma 1 receptor blocker (-)-SKF-100472014European journal of medicinal chemistry, May-22, Volume: 79Synthesis and biological evaluation of a novel sigma-1 receptor antagonist based on 3,4-dihydro-2(1H)-quinolinone scaffold as a potential analgesic.
AID1420188Cytotoxicity against human PANC1 cells at 50 uM after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
New piperidine-based derivatives as sigma receptor ligands. Synthesis and pharmacological evaluation.
AID1411899Drug excretion in human urine2018MedChemComm, May-01, Volume: 9, Issue:5
Schizophrenia: synthetic strategies and recent advances in drug design.
AID114064Oral effective dose required for inhibition of apomorphine-induced climbing in mice1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID168895Compound was tested for inhibition of ethanol potentiation in rat when administered perorally1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.
AID63866Inhibitory concentration against human Dopamine receptor D4.2 in CHO cells1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID238489Binding affinity for human recombinant dopamine D2 receptor2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 receptor selectivity.
AID232372Ratio of affinity for D2 and D4 receptors1998Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7
Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist.
AID177821Effective dose against DOPA accumulation in rat brain limbic region after reserpine pretreatment by subcutaneous administration; No significant effect at 0.5 mg/kg intraperitoneal administration1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Novel dopamine receptor agonists and antagonists with preferential action on autoreceptors.
AID629461Displacement of [3H]spiperone from human DRD2 Long receptor expressed in chinese hamster CHO cells by radioligand binding assay2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Development of a bivalent dopamine D₂ receptor agonist.
AID330561Displacement of [3H]mepyramine from H1R in rat brain2007Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9
From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase.
AID231650Binding affinity ratio against rat cortical tissue 5-HT2 versus human D2, calculated using pKi (-logKi) values2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors.
AID301865Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
Rational design, synthesis and evaluation of (6aR( *),11bS( *))-1-(4-fluorophenyl)-4-{7-[4-(4-fluorophenyl)-4-oxobutyl]1,2,3,4,6,6a,7,11b,12,12a(RS)-decahydropyrazino[2',1':6,1]pyrido[3,4-b]indol-2-yl}-butan-1-one as a potential neuroleptic agent.
AID1207158Inhibition of Na channel (species unknown)2011Cardiovascular research, Jul-01, Volume: 91, Issue:1
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID1597395Displacement of [3H] ifenprodil from GluN2B/GluN1a (unknown origin) expressed in mouse L(tk-) cell membranes incubated for 120 mins by scintillation counting method
AID203845Binding affinity towards sigma 2 receptor site in rat liver membranes using [3H]DTG as radioligand in presence of (+)-pentazocine.1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Synthesis and quantitative structure-activity relationships of N-(1-benzylpiperidin-4-yl)phenylacetamides and related analogues as potent and selective sigma1 receptor ligands.
AID301868Selectivity ratio of pKi for rat brain 5HT2A receptor to pKi for rat brain dopamine D2 receptor2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
Rational design, synthesis and evaluation of (6aR( *),11bS( *))-1-(4-fluorophenyl)-4-{7-[4-(4-fluorophenyl)-4-oxobutyl]1,2,3,4,6,6a,7,11b,12,12a(RS)-decahydropyrazino[2',1':6,1]pyrido[3,4-b]indol-2-yl}-butan-1-one as a potential neuroleptic agent.
AID177903Inhibition of firing rates of dopaminergic neurons in the substantia nigra pars compacta by intravenous injection in rats1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives.
AID61158In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical an
AID64439Inhibition of [3H](S)-sulpiride binding in striatal homogenates of rat brain1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
(S)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-[125I]iodo- 2-methoxybenzamide hydrochloride, a new selective radioligand for dopamine D-2 receptors.
AID177507In vivo inhibition of apomorphine-mediated stereotypy in rats administered subcutaneously at 20 mg/kg expressed as ED50 (mg/kg)1993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study.
AID62728Compound was tested for anti-dopamine activity in vitro by its ability to displace [3H]spiperone from rat brain striatal preparations,1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Potential neuroleptic agents. 4. Chemistry, behavioral pharmacology, and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides.
AID239597Affinity for human EMP expressed in ERG2 deficient strain of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine as radioligand2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening.
AID598815Displacement of [3H]N-methylspiperone from human D2 receptor expressed in HEK cells2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Molecular hybridization of 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecane-3-ol with sigma (σ) receptor ligands modulates off-target activity and subtype selectivity.
AID163467The compound was tested for its affinity against HIV-2 protease1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
HIV protease: a novel chemotherapeutic target for AIDS.
AID1215948Unbound intrinsic clearance in human intestinal S9 fraction at 50 to 1000 nM after 30 to 60 mins by HPLC-MS/MS analysis in presence of NADPH2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Significance of reductive metabolism in human intestine and quantitative prediction of intestinal first-pass metabolism by cytosolic reductive enzymes.
AID113681Inhibition of apomorphine-induced climbing following s.c. administration in mice.1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Muscarinic agonists with antipsychotic-like activity: structure-activity relationships of 1,2,5-thiadiazole analogues with functional dopamine antagonist activity.
AID1213046Drug metabolism assessed as recombinant human UGT1A1 assessed as N-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID139074Antagonism of apomorphine in reserpinized mice when a dose of 2.7 micro mol/kg is administered intraperitoneally1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 1. Synthesis and structure-activity relationships of 2,3,3a,4,5,9b-hexahydro-1H-benz[e]indole derivatives.
AID277979Induction of catalepsy in ip dosed rat after 60 min by crossed-leg position test2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.
AID1570059Displacement of [3H]ketanserin from human 5HT2A receptor expressed in HEK293 cells incubated for 1.5 hrs by Cheng-Prusoff analysis based microbeta scintillation counting method2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT
AID62164Competition in vitro with the dopamine receptor D2 antagonist [3H]spiperone, for binding sites on calf caudate membranes.1993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system.
AID346460Displacement of radiolabeled haloperidol from sigma opioid receptor2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.
AID176775In vivo DOPA accumulation in reserpine pretreated rat limbic system after 1.4 umol/kg ip; I denotes inactive1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists.
AID301871Blockade of secondary conditioned avoidance response in ip dosed rat2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
Rational design, synthesis and evaluation of (6aR( *),11bS( *))-1-(4-fluorophenyl)-4-{7-[4-(4-fluorophenyl)-4-oxobutyl]1,2,3,4,6,6a,7,11b,12,12a(RS)-decahydropyrazino[2',1':6,1]pyrido[3,4-b]indol-2-yl}-butan-1-one as a potential neuroleptic agent.
AID619549Selectivity ratio of Ki for guinea pig brain sigma 1 receptor to Ki for rat liver sigma 2 receptor2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Combination of two pharmacophoric systems: synthesis and pharmacological evaluation of spirocyclic pyranopyrazoles with high σ₁ receptor affinity.
AID1456755Inhibition of human dopamine D4 receptor2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Return of D
AID5246Affinity for 5-hydroxytryptamine 2 receptor1998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.
AID130874Inhibition against apomorphine-induced climbing, after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID1174073Displacement of [3H](+)-pentazocine from sigma1 receptor in guinea pig brain membranes after 180 mins by scintillation counting method2014Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23
Synthesis, GluN2B affinity and selectivity of benzo[7]annulen-7-amines.
AID232307Dopamine D2/D3 ratio of the compound2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Synthesis and structure-activity relationships of naphthamides as dopamine D3 receptor ligands.
AID185044Minimum effective dose that produced a significant effect relative to the amphetamine alone control using a Fisher's LSD post hoc test (P<0.05)2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.
AID232152Ratio of 5-HT2A receptor to that of dopamine 2 (D2) receptor in human2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.
AID1213051Drug metabolism assessed as recombinant human UGT1A9 assessed as N-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1453236Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes after 120 mins by microbeta scintillation counting method
AID1185969Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Further evaluation of the tropane analogs of haloperidol.
AID240820Inhibitory concentration against IKr potassium channel2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
The pharmacophore hypotheses of I(Kr) potassium channel blockers: novel class III antiarrhythmic agents.
AID239086Inhibitory constant against dopamine D2 receptor using 0.2 nM [3H]-spiperone2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands.
AID180345Activity against the suppression of high base line self stimulation with electrodes in the medial forebrain of the posterior hypothalamus of male hooded rats (Peroral admin.)1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents.
AID1759953Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane measured after 120 mins by solid scintillation counting method
AID1207217Inhibition of hERG K channel2011Cardiovascular research, Jul-01, Volume: 91, Issue:1
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID177689Effective dose against DOPA accumulation in rat brain limbic region after no pretreatment by subcutaneous administration1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Novel dopamine receptor agonists and antagonists with preferential action on autoreceptors.
AID141538Binding affinity against Muscarinic acetylcholine receptor in rat brain using [3H]- QNB1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents.
AID62868Inhibition of [3H]spiperone binding to dopamine receptor from rat corpus striatal membranes1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Buspirone analogues. 1. Structure-activity relationships in a series of N-aryl- and heteroarylpiperazine derivatives.
AID1519020Displacement of [3H]di-o-tolylguanidine from sigma2 receptor in rat liver membranes measured after 120 mins by solid scintillation counting method
AID351593Selectivity ratio of Ki for sigma 1 receptor in guinea pig brain membrane to Ki for sigma 2 receptor in rat liver homogenates2009Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10
Synthesis of spirocyclic sigma1 receptor ligands as potential PET radiotracers, structure-affinity relationships and in vitro metabolic stability.
AID1210017Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1213037Drug metabolism assessed as recombinant human UGT1A3 assessed as O-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1461562Displacement of [3H]spiperone from human D2short receptor expressed in CHO cell membranes by radioligand binding assay2017Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19
Potent haloperidol derivatives covalently binding to the dopamine D2 receptor.
AID1146535Neuroleptic activity in po dosed STD-ddY mouse assessed as inhibition of spontaneous motor activity by measuring number of revolution of cage for 5 mins1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
AID1152669Displacement of [3H]N-methylspiperone from human recombinant D2 receptor expressed in CHO-K1 cell membrane after 60 mins by liquid scintillation counting analysis2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel arylsulfonamide derivatives with 5-HT₆/5-HT₇ receptor antagonism targeting behavioral and psychological symptoms of dementia.
AID176805In vivo activity administered intraperitoneally was determined by pole climb escape failures in rat1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID294440Displacement of [3H]spiperone from human cloned dopamine receptor D2 long expressed in CHO cells2007European journal of medicinal chemistry, Jul, Volume: 42, Issue:7
Asymmetric synthesis of chiral piperazinylpropylisoxazoline ligands for dopamine receptors.
AID458639Reduction in 3,4-dihydroxyphenylacetic acid level in Sprague-Dawley rat striatum at 1 umol/kg, sc relative to saline treated control2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
AID65146In vitro ability to inhibit the binding of [3H]7-OH-DPAT to cloned human Dopamine receptor D3 using apomorphine induced climbing test in male Swiss mice2003Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21
The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+.
AID1146541Acute toxicity in po dosed STD-ddY mouse assessed as mortality up to 7 days1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
AID1189659Displacement of [3H]-7-OH-DPAT from dopamine D3 receptor in rat olfactory tubercle by scintillation counting method2015European journal of medicinal chemistry, Jan-27, Volume: 90Haloperidol metabolite II prodrug: asymmetric synthesis and biological evaluation on rat C6 glioma cells.
AID64154In vitro binding affinity against Dopamine D2 receptor in rat striatal tissue.1993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study.
AID1855447Toxicity in ICR mouse assessed as effect on motor coordination at 1 mg/kg, sc micromol/kg, sc by rotarod test
AID392765Displacement of [3H]N-methylspiperone from human dopamine D2 receptor by liquid scintillation counting2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups.
AID1213042Drug metabolism assessed as recombinant human UGT2B4 assessed as O-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID61804Binding affinity towards human D4.2 receptor1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID228677Delta ED50 value by Subcutaneous administration (ED50 catalepsy-ED50 Climbing)1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID177950Antagonistic activity against apomorphine-induced stereotypy, after 1 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID418668Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane by scintillation analysis2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Dancing of the second aromatic residue around the 6,8-diazabicyclo[3.2.2]nonane framework: influence on sigma receptor affinity and cytotoxicity.
AID29337Ionisation constant (pKa)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID420787Antagonist activity at human 5HT3A receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced inward Na+ current at >= 10 uM2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Molecular properties of psychopharmacological drugs determining non-competitive inhibition of 5-HT3A receptors.
AID131364Effect on skeletal muscle tone, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID178920Effective dose required for antipsychotic activity was evaluated by rat CAR assay1998Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.
AID1718133Antagonist activity at dopamine D2 receptor (unknown origin)2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.
AID191610Anti psychotic effect Social interaction when compound administered at a doe of 0.05 mg/kg ip in rats1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID213410Compound was tested to block the inhibition of tyrosine hydroxylase by apomorphine at 1 uM1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Synthesis and anxiolytic activity of a series of pyrazino[1,2-a][1,4]benzodiazepine derivatives.
AID338174Displacement of [3H]DTG from sigma opioid receptor assessed as specific binding relative to total binding1993Journal of natural products, Apr, Volume: 56, Issue:4
The role of receptor binding in drug discovery.
AID524790Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID1616728Antagonist activity at SNAP-tagged human D2LR expressed in Flp-In CHO cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation at 10 uM preincubated with compound followed by forskolin and dopamine addition an
AID1187746Selectivity index, ratio of IC50 for for human D2LR to IC50 for human D3R by beta-galactosidase based beta-arrestin recruitment assay2014Journal of medicinal chemistry, Aug-28, Volume: 57, Issue:16
Design, synthesis, and structure-activity relationship studies of a series of [4-(4-carboxamidobutyl)]-1-arylpiperazines: insights into structural features contributing to dopamine D3 versus D2 receptor subtype selectivity.
AID444006Displacement of [3H]DTG from sigma2 receptor in rat cerebral cortex cell membrane2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane.
AID109881Effect at an intraperitoneal dose of 10 mg/kg against methamphetamine-induced hyperlocomotion in mice1999Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6
Design, synthesis, structure-activity relationships, and biological characterization of novel arylalkoxyphenylalkylamine sigma ligands as potential antipsychotic drugs.
AID188453Drug pretreatment vs. vehicle pretreatment; statistical analysis by Student''s t test at 0.1 mg/kg; NS-Not Significant1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Troponoids. 6. Troponylpiperazines: a new class of dopamine agonists.
AID1071724Antipsychotic activity in po dosed Kunming mouse assessed as reversal of apomorphine-induced cage climbing response compound administered 30 mins prior to apomorphine challenge measured for 30 mins post challenge2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics.
AID1704748Antipsychotic activity in Kunming mouse assessed as inhibition of MK801-induced locomotor activity administered orally 30 mins prior to MK801 challenge and measured for 90 mins
AID226339Affinity to sigma-1-receptor, using [3H]pentazocine as radioligand in homogenates of guinea pig brain membranes2001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Methylated analogues of methyl (R)-4-(3,4-dichlorophenylacetyl)- 3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate (GR-89,696) as highly potent kappa-receptor agonists: stereoselective synthesis, opioid-receptor affinity, receptor selectivity, and functio
AID63794Binding Affinity was determined against Dopamine receptor D2 in rat striatal membranes using [3H]- spiperone radioligand.2000Journal of medicinal chemistry, Feb-24, Volume: 43, Issue:4
Binding and preliminary evaluation of 5-hydroxy- and 10-hydroxy-2,3, 12,12a-tetrahydro-1H-[1]benzoxepino[2,3,4-ij]isoquinolines as dopamine receptor ligands.
AID229190Inhibition of specific binding of [3H]DTG to sigma binding site in Guinea pig brain membranes1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites.
AID1478366Binding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting method2018Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
(+)-Methyl (1R,2S)-2-{[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]methyl}-1-phenylcyclopropanecarboxylate [(+)-MR200] Derivatives as Potent and Selective Sigma Receptor Ligands: Stereochemistry and Pharmacological Properties.
AID204772Binding affinity towards sigma receptor binding site 2 using [3H]DTG of whole rat brain homogenates except cerebellum1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
AID414523Hypothermic activity in Sprague-Dawley rat assessed as time duration of maximal body temperature decrease at 5 mg/kg, ip2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Comparison of N-terminal modifications on neurotensin(8-13) analogues correlates peptide stability but not binding affinity with in vivo efficacy.
AID1221961Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1532589Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins2019European journal of medicinal chemistry, Jan-15, Volume: 162Novel multitarget-directed ligands targeting acetylcholinesterase and σ
AID61533Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand1996Journal of medicinal chemistry, Aug-02, Volume: 39, Issue:16
1-aryl-4-[(1-tetralinyl)alkyl]piperazines: alkylamido and alkylamino derivatives. Synthesis, 5-HT1A receptor affinity, and selectivity. 3.
AID351592Displacement of [3H]di-o-tolylguanidine from sigma 2 receptor in rat liver homogenates by solid scintillation analysis2009Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10
Synthesis of spirocyclic sigma1 receptor ligands as potential PET radiotracers, structure-affinity relationships and in vitro metabolic stability.
AID114430Antagonism of SKF 10047 -induced hypermotility (% vs controls) dose(mg/Kg po) = 11998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.
AID63547In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice2003Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21
The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+.
AID4363The compound was tested for its binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 radioligand in rat hippocampus1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Pyrrole mannich bases as potential antipsychotic agents.
AID239905Inhibitory constant towards dopamine D2 receptor was determined2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Synthesis and binding affinity of novel 3-aminoethyl-1-tetralones, potential atypical antipsychotics.
AID224646Area under curve(AUC) value of DOPAC level after second treatment(7.4 umol/kg) in dialysates collected from rat striatum.2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID1393479Reversal of ketamine-induced working social withdrawal in Sprague-Dawley rat at 0.1 mg/kg, ip pretreated for 60 mins followed by ketamine administration
AID204714In vitro binding affinity for serotonin reuptake sites in rat frontal cortex membranes by [3H]paroxetine displacement.2003Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3
SLV310, a novel, potential antipsychotic, combining potent dopamine D2 receptor antagonism with serotonin reuptake inhibition.
AID239912Inhibitory constant towards 5-hydroxytryptamine 2C receptor (5-HT2C)2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Synthesis and binding affinity of novel 3-aminoethyl-1-tetralones, potential atypical antipsychotics.
AID36583Induction of ptosis after subcutaneous administration at alpha-1 adrenergic receptor in rat1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Characterization of potent and selective antagonists at postsynaptic 5-HT1A receptors in a series of N4-substituted arylpiperazines.
AID203850Selectivity ratio for sigma 2 receptor site in rat liver membranes and sigma 1 receptor site in quinea pig brain membranes1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Synthesis and quantitative structure-activity relationships of N-(1-benzylpiperidin-4-yl)phenylacetamides and related analogues as potent and selective sigma1 receptor ligands.
AID224643Area under curve(AUC) value of DOPAC level after first treatment(0.74 umol/kg) in dialysates collected from rat striatum.2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID524796Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID467612Fraction unbound in human plasma2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID150618Concentration required for 50% inhibition at binding site of human P-Glycoprotein (P-gp) in one-affinity model2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID65280Tested for binding affinity towards human D3 receptor using [3H]spiperone as radioligand1994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
The discovery and structure-activity relationships of 1,2,3,6-tetrahydro-4-phenyl-1-[(arylcyclohexenyl)alkyl]pyridines. Dopamine autoreceptor agonists and potential antipsychotic agents.
AID1650559Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membranes incubated for 120 mins by scintillation counting method2020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Thiophene bioisosteres of GluN2B selective NMDA receptor antagonists: Synthesis and pharmacological evaluation of [7]annuleno[b]thiophen-6-amines.
AID628576Toxicity in albino mouse assessed as induction of catalepsy measured at 30 mins intervals until 240 mins2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, computational studies and preliminary pharmacological evaluation of 2-[4-(aryl substituted) piperazin-1-yl] N, N-diphenylacetamides as potential antipsychotics.
AID1213093Drug metabolism assessed as recombinant human UGT1A4 assessed as O-glucuronidation at 25 to 200 uM incubated for 60 mins by LC-MS/MS analysis in presence of 10 uM niflumic acid relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID4812Inhibition of [3H]ketanserin binding to dopamine 5-hydroxytryptamine 2 receptor1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles.
AID1487358Antagonist activity at human D2L receptor expressed in CHO cell membranes assessed as dissociation rate constant after 15 mins by liquid scintillation counting method2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID1782427Displacement of [3H]-LSD from 5HT2A receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
2-Phenylcyclopropylmethylamine Derivatives as Dopamine D
AID640309Displacement of [3H]LSD from human 5HT7 receptor by liquid scintillation counting2012Bioorganic & medicinal chemistry, Feb-01, Volume: 20, Issue:3
Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.
AID1210016Inhibition of CYP2C8 in human liver microsomes using paclitaxel as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1146538Toxicity in po dosed albino Wistar rat assessed as induction of catalepsy after 8 hrs1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
AID176222Effective in vivo peroral dose against induction of catalepsy in rats1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.
AID1213047Drug metabolism assessed as recombinant human UGT1A3 assessed as N-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID142943Inhibition of [3H]N-methylscopolamine binding to Muscarinic acetylcholine receptor M2 of rat heart membranes1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
(+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties.
AID177715In vivo suppression of the conditioned avoidance response (CAR) in rats after po administration of the compound2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.
AID251584Relative binding affinity against 5-hydroxytryptamine 2A and dopamine D2 receptors2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies.
AID277669Selectivity for dopamine D3 over dopamine D42007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.
AID181425Compound was tested for the presence of catalepsy (CAT) in rats after oral administration1993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system.
AID226340Binding affinity for sigma 2 opioid receptor, measured on rat liver membranes using [3H]- DTG as radioligand in the presence of (+)-pentazocine2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
Synthesis and structure-activity relationships of N-(1-benzylpiperidin-4-yl)arylacetamide analogues as potent sigma1 receptor ligands.
AID1701185Displacement of [3H]-DTG from sigma2 receptor in guinea pig brain membranes incubated for 120 mins by liquid scintillation counting method2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
EST64454: a Highly Soluble σ
AID5951Binding affinity towards serotonin 5-hydroxytryptamine 2C receptor2004Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics.
AID1511006Displacement of [3H]ifenprodil from GluN1a/GluN2B (unknown origin) expressed in mouse L(tk-) cell membranes after 120 mins by solid scintillation counting method2019European journal of medicinal chemistry, Oct-15, Volume: 180Discovery of new potent dual sigma receptor/GluN2b ligands with antioxidant property as neuroprotective agents.
AID1292380Absorption half life in psychotic patient (9 patients) at 3.5 +/- 1.2 mg, iv by reversed phase HPLC method1987Psychopharmacology, , Volume: 91, Issue:4
Pharmacokinetics of haloperidol in psychotic patients.
AID194153The percent loss of escape responding was determined for the estimated effective dose 50 values for CAR block1989Journal of medicinal chemistry, May, Volume: 32, Issue:5
Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy.
AID1718134Binding affinity to sigma-2 receptor (unknown origin)2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.
AID1136082Displacement of [3H]-DA from dopamine receptor in calf caudate membranes after 15 mins by liquid scintillation counting analysis1978Journal of medicinal chemistry, Apr, Volume: 21, Issue:4
5-Chloro-2-phenyl-1-benzo[b]thiophene-3-alkanimines, potential antipsychotic agents.
AID1307728Inhibition of of human TREK1 expressed in whole COS cells assessed as reduction in channel currents2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Perspectives on the Two-Pore Domain Potassium Channel TREK-1 (TWIK-Related K(+) Channel 1). A Novel Therapeutic Target?
AID1593894Displacement of [3H]-DTG from sigma 2 receptor (unknown origin) expressed in HEK293T cell membranes2019Bioorganic & medicinal chemistry, 06-15, Volume: 27, Issue:12
New analogs of SYA013 as sigma-2 ligands with anticancer activity.
AID1851837Displacement of [3H]DTG from sigma-2 receptor in Sprague-Dawley rat liver membrane incubated for 90 mins in presence of by liquid scintillation counter analysis (+)-pentazocine by liquid scintillation counter analysis2022RSC medicinal chemistry, Aug-17, Volume: 13, Issue:8
Development of tumor-targeting aza-vesamicol derivatives with high affinity for sigma receptors for cancer theranostics.
AID65301Inhibition of [35 S] GTP gamma S binding to cell membranes expressing Dopamine receptor D3 with dopamine1996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Novel (R)-2-amino-5-fluorotetralins: dopaminergic antagonists and inverse agonists.
AID1211296Unbound fraction in plasma (unknown origin) under normal atmospheric condition at pH 7.72 after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID112708Hypothermia in mice after perorla administration1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
10-Piperazinyl-4H-theino[3,2-b][1,5]- and -[3,4-b][1,5]benzodiazepines as potential neuroleptics.
AID1213057Drug metabolism assessed as human liver microsomes assessed as O-glucuronide retention time at 100 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1144250Induction of ptosis in Wistar rat at 1 to 6 mg/kg, ip1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Synthesis and biological actions of 2-substituted quinolizidines.
AID1213062Drug metabolism assessed as recombinant human UGT1A4 assessed as velocity of O-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID169289Antipsychotic activity was assessed by ability to block response of rats trained to avoid an electrical shock (inhibition of self-jump and/or discrete trial conditioned avoidance response(CAR) upon ip administration; value ranges from 0.12-0.331987Journal of medicinal chemistry, Jun, Volume: 30, Issue:6
Psychotropic agents: synthesis and antipsychotic activity of substituted beta-carbolines.
AID410529Antipsychotic activity in NMRI mouse assessed as reduction in methamphetamine-induced locomotor activity administered 30 mins prior to testing measured for 60 mins2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
AID1185961Displacement of [3H]LSD from human 5-HT7 receptor by liquid scintillation counting2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Further evaluation of the tropane analogs of haloperidol.
AID177823Effective dose against DOPA accumulation in rat brain striatal region after no pretreatment by subcutaneous administration1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Novel dopamine receptor agonists and antagonists with preferential action on autoreceptors.
AID1292394Unbound fraction in psychotic patient (9 patients) at 3.5 +/- 1.2 mg, iv by reversed phase HPLC method1987Psychopharmacology, , Volume: 91, Issue:4
Pharmacokinetics of haloperidol in psychotic patients.
AID224645Area under curve(AUC) value of HVA level after first treatment(0.74 umol/kg) in dialysates collected from rat striatum.2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID492184Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Synthesis and characterization of selective dopamine D2 receptor antagonists. 2. Azaindole, benzofuran, and benzothiophene analogs of L-741,626.
AID635315Displacement of [125I]IAF from sigma 2 receptor in human RT4 cells at 10 uM after 30 mins preincubation by photoaffinity labeling experiment2011Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24
Electron-donating para-methoxy converts a benzamide-isoquinoline derivative into a highly Sigma-2 receptor selective ligand.
AID1062948Displacement of [3H]spiperone from human D2 receptor2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis and biological evaluation of a series of aminoalkyl-tetralones and tetralols as dual dopamine/serotonin ligands.
AID5363Binding affinity towards serotonin 5-hydroxytryptamine 2A receptor2004Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics.
AID1597398Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membranes incubated for 120 mins by scintillation counting method
AID1215122Percentage unbound in solid supported porcine brain membrane vesicles at 5 uM by TRANSIL assay2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID410332Displacement of [3H]spiperone from dopamine D2 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
AID113690Inhibition of p-chloroamphetamine-induced hyperactivity in mice.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID1511007Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes incubated for 120 mins by solid scintillation counting method2019European journal of medicinal chemistry, Oct-15, Volume: 180Discovery of new potent dual sigma receptor/GluN2b ligands with antioxidant property as neuroprotective agents.
AID173070Percent change in serum prolactin in adult male Dawley rats after intraperitoneal administration.1993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system.
AID5337In vitro ability to displace [3H]ketanserin binding from 5-hydroxytryptamine 2A receptor in rat striatal membrane.1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical an
AID204001The compound was tested for its binding affinity towards Sigma opioid receptor in guinea pig brain membranes1991Journal of medicinal chemistry, Dec, Volume: 34, Issue:12
Novel 1-phenylpiperazine and 4-phenylpiperidine derivatives as high-affinity sigma ligands.
AID598817Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Molecular hybridization of 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecane-3-ol with sigma (σ) receptor ligands modulates off-target activity and subtype selectivity.
AID138756Ability to stimulate dopaminergic systems by effect on locomotor activity in reserpinized mice when a dose of 0.3 micro mol/kg is administered intraperitoneally1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 1. Synthesis and structure-activity relationships of 2,3,3a,4,5,9b-hexahydro-1H-benz[e]indole derivatives.
AID64198Tested for binding affinity towards human D2L receptor using [3H]spiperone as radioligand1994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
The discovery and structure-activity relationships of 1,2,3,6-tetrahydro-4-phenyl-1-[(arylcyclohexenyl)alkyl]pyridines. Dopamine autoreceptor agonists and potential antipsychotic agents.
AID1308629Growth inhibition of human HL60 cells incubated for 48 hrs by MTT assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity?
AID711576Inhibition of sigma 2 receptor2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID259124Displacement of [3H]spiperone from rat brain dopamine D2-like receptor2006Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2
Design of novel hexahydropyrazinoquinolines as potent and selective dopamine D3 receptor ligands with improved solubility.
AID1809446Antiproliferative activity against VEGF-A stimulated human retinal endothelial cell assessed as reduction in cell viability measured after 72 hrs by MTT assay2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Haloperidol Metabolite II Valproate Ester (
AID387866Displacement of [3H]YM-09151-2 from human dopamine D2S receptor in membrane suspensions by liquid scintillation counter2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Synthesis of 1-arylpiperazyl-2-phenylcyclopropanes designed as antidopaminergic agents: cyclopropane-based conformationally restricted analogs of haloperidol.
AID175146Dose required for producing 20% block of escape responding in rats after peroral administration1981Journal of medicinal chemistry, Sep, Volume: 24, Issue:9
A dopamine receptor model and its application in the design of a new class of rigid pyrrolo[2,3-g]isoquinoline antipsychotics.
AID185022Minimum effective dose required for significant dose dependent reduction of amphetamine-induced locomotor activity in male Sprague-Dawley rats on subcutaneous administration (30 min prior to receiving amphetamine 0.5 mg/kg)2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 2: asymmetric synthesis and biological evaluation.
AID598495Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain by scintillation analyzer2011Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10
Design, synthesis and pharmacological evaluation of spirocyclic σ(1) receptor ligands with exocyclic amino moiety (increased distance 1).
AID130893Inhibition of induction of ataxia in mouse after intraperitoneal administration1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines.
AID1462133Selectivity index, ratio of Ki for sigma1 receptor in guinea pig brain membranes to Ki for sigma2 receptor in rat liver membranes2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Chiral-pool synthesis of 1,2,4-trisubstituted 1,4-diazepanes as novel σ
AID517710Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Bioisosteric replacement leading to biologically active [2.2]paracyclophanes with altered binding profiles for aminergic G-protein-coupled receptors.
AID1213081Drug metabolism assessed as human liver microsomes assessed as O-glucuronide measured at 25 uM by LC-MS/MS analysis in presence of 10 uM niflumic acid relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID63997Binding affinity towards dopamine receptor D22004Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics.
AID231526Ratio of binding affinity towards D2 to D1 receptor was measured1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study.
AID254454In vitro inhibitory constant against [3H]paroxetine binding to rat frontal cortex membrane serotonin reuptake site; NA= not active2005Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
Synthesis, structure-activity relationships, and biological properties of 1-heteroaryl-4-[omega-(1H-indol-3-yl)alkyl]piperazines, novel potential antipsychotics combining potent dopamine D2 receptor antagonism with potent serotonin reuptake inhibition.
AID176370Conditioned avoidance response activity was determined by the ability to block the conditioned avoidance of a foot shock (ip)1995Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21
Piperazinylalkyl heterocycles as potential antipsychotic agents.
AID63365In vitro affinity against Dopamine receptor D12000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.
AID586713Intrinsic activity at human D3 receptor expressed in human HEK293 cells assessed as inhibition of forskolin-dependent accumulation of [3H]-cyclic AMP at 10 times Ki by spectrophotometric analysis2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Synthesis and pharmacological evaluation of fluorine-containing D₃ dopamine receptor ligands.
AID1071720Therapeutic index, ratio of ED50 for induction of catalepsy to ED50 for antipsychotic activity in po dosed Kunming mouse assessed as reduction in MK801-induced hyperactivity2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID113115Antagonism of apomorphine-induced climbing in mice when administered perorally 60 min prior to apomorphine (1 mg/kg)1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
AID63805Compound was measured for the inhibition of [3H]spiperone binding to striatal membrane Dopamine receptor D21998Bioorganic & medicinal chemistry letters, Dec-15, Volume: 8, Issue:24
Butyrophenone analogues in the carbazole series: synthesis and determination of affinities at D2 and 5-HT2A receptors.
AID540225Volume of distribution at steady state in dog after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID169189Conditioned avoidance responding in rat after subcutaneous administration (0.3 mg/kg); expressed as avoidance response/response failure; 9/551998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Muscarinic agonists with antipsychotic-like activity: structure-activity relationships of 1,2,5-thiadiazole analogues with functional dopamine antagonist activity.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID64962Ability to displace [3H]spiperone from human cloned Dopamine receptor D3 expressed in CHO K-1 cells in vitro.1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents.
AID439070Displacement of [3H]mesulergine from human 5HT2C receptor2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.
AID410333Displacement of [3H]7OH-DPAT from dopamine D3 receptor expressed in Sf9 cells by scintillation spectrometry2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
AID1380704Displacement of [3H]methylspiperonee from recombinant human D2 receptor expressed in HEK293 cells cell membranes after 60 mins by liquid scintillation counting method
AID1144210Depression of forced motor activity in Swiss-Webster mouse at 2.5 mg/kg, ip after 30 mins by rotarod test relative to control1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Synthesis and biological actions of 2-substituted quinolizidines.
AID65288Ability to displace [3H]spiperone from human dopamine receptor D3 (hD3) receptor stably expressed in HEK293 cells.1997Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15
4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor.
AID295929Displacement of [3H]ditolylguanidine from sigma 2 receptor in Sprague-Dawley rat liver membrane2007European journal of medicinal chemistry, Oct, Volume: 42, Issue:10
Synthesis of bridged piperazines with sigma receptor affinity.
AID29423HPLC capacity factor (k')2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID704016Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain homogenates2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Enantiomerically pure 1,3-dioxanes as highly selective NMDA and σ₁ receptor ligands.
AID24452logY value was determined2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.
AID1189657Displacement of [3H]-(+)-pentazocine from sigma 1 receptor guinea pig brain membranes incubated for 150 mins by scintillation counting method2015European journal of medicinal chemistry, Jan-27, Volume: 90Haloperidol metabolite II prodrug: asymmetric synthesis and biological evaluation on rat C6 glioma cells.
AID177081Compound was evaluated for inhibition of apomorphine-induced stereotypy behavior in rats after intraperitoneal administration.1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia.
AID4136Binding affinity towards 5-hydroxytryptamine 1A receptor binding site using [3H]8-OH-DPAT. 1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
AID1467941Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 150 mins by liquid scintillation counting method2017Journal of medicinal chemistry, 12-14, Volume: 60, Issue:23
Novel Sigma Receptor Ligand-Nitric Oxide Photodonors: Molecular Hybrids for Double-Targeted Antiproliferative Effect.
AID36891Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding; ND = ''Not determined''.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID619548Displacement of [3H]ditolylguanidine from rat liver sigma 2 receptor by scintillation counting2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Combination of two pharmacophoric systems: synthesis and pharmacological evaluation of spirocyclic pyranopyrazoles with high σ₁ receptor affinity.
AID204780Binding affinity was measured on Sigma receptor type 2 with rat liver membranes and [3H]- DTG as ligand.2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Radioiodinated N-(2-diethylaminoethyl)benzamide derivatives with high melanoma uptake: structure-affinity relationships, metabolic fate, and intracellular localization.
AID239347Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening.
AID1762086Therapeutic index, ratio of ED50 for induction of catalepsy in po dosed mouse to ED50 for antipsychotic activity in po dosed mouse assessed as suppression of apomorphine-induced climbing2021Bioorganic & medicinal chemistry letters, 05-15, Volume: 40Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID64438Inhibition of 0.1 nM of [125I]- (S)-N-(1-Ethyl-pyrrolidin-2-ylmethyl)-5-iodo-2-methoxy-benzamide binding in striatal homogenates of rat brain1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
(S)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-[125I]iodo- 2-methoxybenzamide hydrochloride, a new selective radioligand for dopamine D-2 receptors.
AID517709Displacement of [3H]Spiperone from human dopamine D3 receptor expressed in CHO cells2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Bioisosteric replacement leading to biologically active [2.2]paracyclophanes with altered binding profiles for aminergic G-protein-coupled receptors.
AID337890Displacement of [3H]DTG from sigma opioid receptor1993Journal of natural products, Apr, Volume: 56, Issue:4
The role of receptor binding in drug discovery.
AID517706Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Bioisosteric replacement leading to biologically active [2.2]paracyclophanes with altered binding profiles for aminergic G-protein-coupled receptors.
AID1292390Absorption half life in psychotic patient (9 patients) at 2.9 +/- 1.2 mg, po by reversed phase HPLC method1987Psychopharmacology, , Volume: 91, Issue:4
Pharmacokinetics of haloperidol in psychotic patients.
AID139075Antagonism of apomorphine in reserpinized mice when a dose of 2.7 micro mol/kg is administered intraperitoneally1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives.
AID538760Displacement of [3H]di-o-tolylguanidine from sigma2 receptor rat liver membranes after 180 mins scintillation counting2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Conformationally constrained NR2B selective NMDA receptor antagonists derived from ifenprodil: Synthesis and biological evaluation of tetrahydro-3-benzazepine-1,7-diols.
AID186044Locomotor activity in male Wistar rats after a dose of 0.3 uM/kg, 30 min before 1 mg/kg of apomorphine administration1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.
AID418678Cytotoxicity against human DAN-G cells after 96 hrs by crystal violet staining2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Dancing of the second aromatic residue around the 6,8-diazabicyclo[3.2.2]nonane framework: influence on sigma receptor affinity and cytotoxicity.
AID204445Binding affinity for sigma receptor using [3H](+)-pentazocine in guinea pig brain homogenates1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
Synthesis and biological evaluation of conformationally restricted 2-(1-pyrrolidinyl)-N-[2-(3,4-dichlorophenyl)ethyl]-N-methylethylenediam ines as sigma receptor ligands. 1. Pyrrolidine, piperidine, homopiperidine, and tetrahydroisoquinoline classes.
AID177723Induction of catalepsy in rats was determined after 2 hr of intraperitoneal administration of the compound1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID342775Binding affinity to human cloned dopamine D1 receptor2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID410338Binding affinity to human ERG expressed in HEK293 cells by whole cell patch clamp method2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
AID138761Ability to stimulate dopaminergic systems by effect on locomotor activity in reserpinized mice when a dose of 2.7 micro mol/kg is administered intraperitoneally1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives.
AID62571Compound was evaluated for the competitive binding with [3H]NCA binding to Canine striatal membranes.1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
Aporphines. 58. N-(2-chloroethyl) [8,9-2H]norapomorphine, an irreversible ligand for dopamine receptors: synthesis and application.
AID176655Subcutaneous dose to inhibit apomorphine-induced stereotyped behavior in 50% of rats1981Journal of medicinal chemistry, Oct, Volume: 24, Issue:10
Synthesis and neuroleptic activity of benzamides. Cis-N-(1-benzyl-2-methylpyrrolidin-3-yl)-5-chloro-2-methoxy-4-(methylamino)benzamide and related compounds.
AID1546908Displacement of [3H]spiperone from human D2S receptor expressed in CHO-K1 cells at 10 uM by radioligand competitive binding analysis relative to control
AID232353Ratio of CAR ED50 vs catalepsy ED501986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.
AID255689Effective dose against apomorphine-induced climbing behavior in mice upon oral administration (Dopaminergic antagonist)2005Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
Synthesis, structure-activity relationships, and biological properties of 1-heteroaryl-4-[omega-(1H-indol-3-yl)alkyl]piperazines, novel potential antipsychotics combining potent dopamine D2 receptor antagonism with potent serotonin reuptake inhibition.
AID1210013Inhibition of recombinant CYP2J2 (unknown origin)-mediated terfenadine hydroxylation assessed as remaining activity at 30 uM after 5 mins by LC-MS analysis relative to control2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID113544Induction of catalepsy in mice.1998Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5
Novel antipsychotic agents with dopamine autoreceptor agonist properties: synthesis and pharmacology of 7-[4-(4-phenyl-1-piperazinyl)butoxy]-3,4-dihydro-2(1H)-quinolinone derivatives.
AID1221964Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID277986Antagonist activity against rat D2 receptor assessed as [35S]GTPgammaS binding relative to quinelorane2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.
AID547621Cytotoxicity against BESM cells after 88 hrs by HTS assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.
AID61387Ability to inhibit the specific binding of [3H]- spiroperidol to Dopamine receptor D2 in rat striatal membrane preparation by 50%1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Combined analgesic/neuroleptic activity in N-butyrophenone prodine-like compounds.
AID1398702Binding affinity to human biotinylated HLA-A2 by surface plasmon resonance assay2018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
Discovery of small molecule inhibitors of adenovirus by disrupting E3-19K/HLA-A2 interactions.
AID1292391Terminal half life in psychotic patient (9 patients) at 2.9 +/- 1.2 mg, po by reversed phase HPLC method1987Psychopharmacology, , Volume: 91, Issue:4
Pharmacokinetics of haloperidol in psychotic patients.
AID65934Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.
AID1215127Ratio of fraction unbound in solid supported porcine brain membrane vesicles at 5 uM by TRANSIL assay to fraction unbound in Wistar rat brain homogenate at 5 uM after 5 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID280722Activity at sigma 1 receptor in rat astroglial cells2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Novel sigma receptor ligands: synthesis and biological profile.
AID1853654Antibacterial activity against Mycobacterium tuberculosis H37Ra ATCC NRS22 assessed as inhibition of bacterial growth incubated upto 3 weeks hrs by resazurin dye based double-dilution method2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from
AID479242Displacement of [3H]spiperone form human dopamine D2 receptor by liquid scintillation counting2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Potent dihydroquinolinone dopamine D2 partial agonist/serotonin reuptake inhibitors for the treatment of schizophrenia.
AID115764Antipsychotic activity using locomotor activity (LMA)-inverted screen test in mice (i.p. admin.)1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents.
AID294441Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells2007European journal of medicinal chemistry, Jul, Volume: 42, Issue:7
Asymmetric synthesis of chiral piperazinylpropylisoxazoline ligands for dopamine receptors.
AID1726850Displacement of (+)-[3H]DTG from sigma 2 receptor in SPRD rat liver membrane incubated for 2 hrs by liquid scintillation counting method
AID1393472Antipsychotic activity in ip dosed Sprague-Dawley rat assessed as suppression of avoidance behavior by avoiding foot shock administered 60 mins prior to test by conditioned avoidance response test
AID1686300Effect on cell migration of in HREC at 2 uM incubated for 24 to 72 hrs by wound healing assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells.
AID1144214Depression of spontaneous motor activity in Swiss-Webster mouse at 10 mg/kg, ip by photocell cage test relative to control1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Synthesis and biological actions of 2-substituted quinolizidines.
AID36865In vitro inhibitory concentration against radioligand [3H]WB-4101 binding to rat cortical alpha-1 adrenergic receptor1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.
AID65087Binding affinity measured at the Dopamine receptor D2 by the inhibition of [3H]methylspiperone binding to rat striatum using unlabeled haloperidol for nonspecific binding.1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID1174258Displacement of [3H](+)-pentazocine from human sigma 1 receptor in human Jurkat cell membranes incubated for 2 hrs by liquid scintillation counting2015European journal of medicinal chemistry, Jan-07, Volume: 89Carboline- and phenothiazine-derivated heterocycles as potent SIGMA-1 protein ligands.
AID188455Drug pretreatment vs. vehicle pretreatment; statistical analysis by Student's t test at 0.5 mg/kg1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Troponoids. 6. Troponylpiperazines: a new class of dopamine agonists.
AID1853649Antibacterial activity against Mycobacterium smegmatis mc2 155 assessed as inhibition of bacterial growth incubated upto 3 weeks hrs by resazurin dye based double-dilution method2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from
AID646276Antipsychotic activity in CD1 mouse assessed as reduction in spontaneous locomotor activity measuring number of crossings at 0.5 to 1 mg/kg every 5 mins for 1 hr2012Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
Quinoline- and isoquinoline-sulfonamide derivatives of LCAP as potent CNS multi-receptor-5-HT1A/5-HT2A/5-HT7 and D2/D3/D4-agents: the synthesis and pharmacological evaluation.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID467611Dissociation constant, pKa of the compound2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID586708Displacement of [3H]-pentazocine from guinea pig sigma1 receptor by liquid scintillation counting2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Synthesis and pharmacological evaluation of fluorine-containing D₃ dopamine receptor ligands.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1601981Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT
AID492183Displacement of [125I]ABN from human dopamine D3 receptor expressed in HEK293 cells after 60 mins by gamma counting2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Synthesis and characterization of selective dopamine D2 receptor antagonists. 2. Azaindole, benzofuran, and benzothiophene analogs of L-741,626.
AID342786Binding affinity to rat NET2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID735278Displacement of [3H]-(+)-pentazocine from human sigma1 receptor transfected in HEK293 cells after 120 mins by liquid scintillation counting analysis2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Synthesis and biological evaluation of a new series of hexahydro-2H-pyrano[3,2-c]quinolines as novel selective σ1 receptor ligands.
AID1433419Displacement of [3H]-PTZ from sigma1 receptor in guinea pig brain membranes after 150 mins in presence of 250 uM DPH by liquid scintillation counting method
AID176323In vivo blocking of apomorphine induced hyperactivity following 1 mg/kg i.p. in rats after 60 min.1982Journal of medicinal chemistry, Nov, Volume: 25, Issue:11
Potential neuroleptic agents. 2,6-Dialkoxybenzamide derivatives with potent dopamine receptor blocking activities.
AID178704Antagonistic activity against amphetamine-induced stereotypy in rats; (5 mg/kg administered ip 1 hr after the test compound).1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Neuroleptic activity of chiral trans-hexahydro-gamma-carbolines.
AID1191388Displacement of (+)-[3H]pentazocine from guinea pig brain cortex sigma1 receptor by scintillation analyzer2015European journal of medicinal chemistry, Jan-27, Volume: 90Improving selectivity preserving affinity: new piperidine-4-carboxamide derivatives as effective sigma-1-ligands.
AID178242Inhibition of shelf-jump avoidance in rats after peroral administration.1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines.
AID277973Displacement of [3H]OH-DPAT from rat cortex 5HT1A receptor2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.
AID1853646Inhibition of Mycobacterium tuberculosis AAC(6')-Ie/APH(2'')-Ia assessed as inhbition at AAC(6')-Ie at 200 uM using NEO as substrate in presence of Acetyl-CoA by UV-Vis spectroscopy analysis2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from
AID180521The compound was tested for inhibition of sidman avoidance in rat1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents.
AID392767Ratio of Ki for human dopamine D2 receptor to Ki for human dopamine D4 receptor2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups.
AID776368Displacement of (+)-pentazocine from sigma-1 receptor in guinea pig brain cortex membrane after 120 mins by scintillation counting2013European journal of medicinal chemistry, Nov, Volume: 69New combination of pharmacophoric elements of potent σ₁ ligands: design, synthesis and σ receptor affinity of aminoethyl substituted tetrahydrobenzothiophenes.
AID1159367Displacement of (+)-pentazocine from sigma1 receptor in guinea pig brain cortex membrane by scintillation counting analysis2014European journal of medicinal chemistry, Aug-18, Volume: 83Identification, pharmacological evaluation and binding mode analysis of novel chromene and chromane based σ1 receptor ligands.
AID1506088Displacement of (-)-[3H]vesamicol from rat VAChT expressed in rat PC12 cell membranes after 60 mins by liquid scintillation counting method2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.
AID1211295Unbound fraction in plasma (unknown origin) at pH 7.63 after 6 hrs by equilibrium dialysis method in presence of 5% CO22011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID672151Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Hit-to-lead investigation of a series of novel combined dopamine D2 and muscarinic M1 receptor ligands with putative antipsychotic and pro-cognitive potential.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID6437In vitro binding affinity towards 5-hydroxytryptamine receptor 1A receptor by using [3H]8-OH-DPAT in rat hippocampal membranes.2000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
A structure-affinity relationship study on derivatives of N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a high-affinity and selective D(4) receptor ligand.
AID233293Selectivity ratio is Ki of human dopamine D2 receptor to that of human dopamine D4 receptor.1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
(Aryloxy)alkylamines as selective human dopamine D4 receptor antagonists: potential antipsychotic agents.
AID5155Affinity towards 5-hydroxytryptamine 2A receptor in membranes from bovine frontal cortex using [3H]ketanserin1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.
AID1461566Selectivity index, ratio of Ki for human D3 receptor expressed in CHO cell membranes to Ki for human D2short receptor expressed in CHO cell membranes2017Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19
Potent haloperidol derivatives covalently binding to the dopamine D2 receptor.
AID391747Displacement of [3H]spiroperidol from human cloned dopamine D2L receptor expressed in rat C6 cells2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III.
AID62007Displacement of [3H]-YM 09151 from african green monkey Dopamine receptor D21995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
1-Phenyl-3-(aminomethyl)pyrroles as potential antipsychotic agents. Synthesis and dopamine receptor binding.
AID65781Binding affinity of compound towards Dopamine receptor D3 using [3H]spiperone (1.2 nM) ligand in cortex was determined1997Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands.
AID1213039Drug metabolism assessed as recombinant human UGT1A7 assessed as O-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID176458Pole climb escape failures of rats was determined after 1 hr of intraperitoneal administration of the compound1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID1292392Oral bioavailability in psychotic patient (9 patients) at 2.9 +/- 1.2 mg by reversed phase HPLC method1987Psychopharmacology, , Volume: 91, Issue:4
Pharmacokinetics of haloperidol in psychotic patients.
AID1189645Displacement of [3H]-spiperone from dopamine D2 receptor in rat striatum by scintillation counting method2015European journal of medicinal chemistry, Jan-27, Volume: 90Haloperidol metabolite II prodrug: asymmetric synthesis and biological evaluation on rat C6 glioma cells.
AID64285In vitro ability to inhibit the binding of [3H]spiperone to dopamine receptor D2 in rat striatal membranes.1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds.
AID231649Binding affinity ratio against human dopamine D2L versus D4.2, calculated using pKi (-logKi) values2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors.
AID128671Antagonism of apomorphine-induced climbing behavior in mice after peroral administration1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2.
AID138926Antagonism of apomorphine for 10-20 minutes in reserpinized mice when a dose of 0.3 micro mol/kg is administered intraperitoneally1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives.
AID142687Binding affinity against muscarinic (M) receptor1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study.
AID63809Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID712768Displacement of [3H]DTG from sigma 2 receptor in rat PC12 cell membrane after 2 hrs by microbeta scintillation counting analysis2012ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12
From α4β2 Nicotinic Ligands to the Discovery of σ1 Receptor Ligands: Pharmacophore Analysis and Rational Design.
AID65133Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybrid pharmacophore- and structure-based database searching approach.
AID298487Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID1146539Ratio of ED50 for po dosed albino Wistar rat assessed as induction of catalepsy to ED50 for methamphetamine-induced stereotyped behavior in po dosed albino Wistar rat1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
AID1314058Displacement of [3H]di-o-tolylgluanidine from sigma 2 receptor in rat liver membranes after 2 hrs by scintillation counting2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Oxa-Pictet-Spengler reaction as key step in the synthesis of novel σ receptor ligands with 2-benzopyran structure.
AID303627Growth inhibition of human LCLC103H cells at 20 uM after 96 hrs relative to control2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Synthesis of bicyclic sigma receptor ligands with cytotoxic activity.
AID1213060Drug metabolism assessed as recombinant human UGT1A9 assessed as velocity of O-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID204788Binding effinity for sigma receptor using 2 nM of [3H]-DTG as radioligand, in membranes from brain minus cerebellum1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
AID138785Antagonism of apomorphine for 0-10 minutes in reserpinized mice when a dose of 2.7 micro mol/kg is administered intraperitoneally1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 1. Synthesis and structure-activity relationships of 2,3,3a,4,5,9b-hexahydro-1H-benz[e]indole derivatives.
AID239911Inhibitory constant towards 5-hydroxytryptamine 2A receptor (5-HT2A)2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Synthesis and binding affinity of novel 3-aminoethyl-1-tetralones, potential atypical antipsychotics.
AID1823673Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK293 cell membrane incubated for 60 mins by radioligand binding assay
AID1213040Drug metabolism assessed as recombinant human UGT1A8 assessed as O-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID524793Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID64268Inhibition of [3H]raclopride binding at Dopamine receptor D2 from rat striata.1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Effect of linking bridge modifications on the antipsychotic profile of some phthalimide and isoindolinone derivatives.
AID110211Ability to inhibit apomorphine (APO) induced stereotyped behavior in mice by intraperitoneal administration of compound.; value may range from 0.09 to 0.101987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Antipsychotic activity of substituted gamma-carbolines.
AID204615Compound was tested in vitro for its ability to displace radioligand (+)-[3H]-3-PPP from rat cortical sigma receptor1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.
AID737905Displacement of [3H]-1,3-di-o-tolylguanidine from rat liver sigma2 receptor by competitive binding assay2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Synthesis and evaluation of novel (18)F-labeled spirocyclic piperidine derivatives as σ1 receptor ligands for positron emission tomography imaging.
AID62909Displacement of [3H]spiperone from human Dopamine receptor D2 expressed in CHO cells1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors.
AID1724120Therapeutic index, ratio of ED50 for induction of catalepsy in po dosed mouse to ED50 for antipsychotic activity in po dosed mouse assessed as suppression of apomorphine-induced climbing2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID64825Binding affinity towards human Dopamine receptor D31999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID238699Binding affinity for human dopamine receptor D2 long2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.
AID1330099Displacement of [3H]DADLE from human DOR expressed in HEK cells measured after 90 mins by microbeta scintillation counting method2016Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
AID1189658Displacement of [3H]-DTG from sigma 2 receptor guinea pig brain membranes incubated for 120 mins by scintillation counting method2015European journal of medicinal chemistry, Jan-27, Volume: 90Haloperidol metabolite II prodrug: asymmetric synthesis and biological evaluation on rat C6 glioma cells.
AID1215945Metabolic stability in human intestinal S9 fraction assessed as compound remaining at 50 to 1000 nM after 60 mins by HPLC-MS/MS analysis in presence of NADH2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Significance of reductive metabolism in human intestine and quantitative prediction of intestinal first-pass metabolism by cytosolic reductive enzymes.
AID701161Displacement of [3H]di-o-tolylguanidine from sigma 2 receptor in guinea pig brain membranes after 120 mins by scintillation counter2012Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862).
AID298480Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
AID321566Ratio of Ki for rat sigma1 opioid receptor to Ki for rat sigma2 opioid receptor2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Conversion of a highly selective sigma-1 receptor-ligand to sigma-2 receptor preferring ligands with anticocaine activity.
AID1185970Displacement of [3H]QNB from human muscarinic M1 receptor by liquid scintillation counting2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Further evaluation of the tropane analogs of haloperidol.
AID1135532Antipsychotic activity in po dosed squirrel monkey assessed as inhibition of conditioned avoidance response measured as maximum number of shocks1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Synthesis and stereospecific antipsychotic activity of (-)-1-cyclopropylmethyl-4-(3-trifluoromethylthio-5H-dibenzo[a,d]cyclohepten-5-ylidene)piperidine.
AID711586Partition coefficient, log D of the compound at pH 7.42011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID705400Antipsychotic activity in sc dosed rat by conditioned avoidance response test2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
AID238350Binding affinity for human dopamine receptor D32005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.
AID35277Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in rat brain1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID524794Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID1724121Therapeutic index, ratio of ED50 for induction of catalepsy in po dosed mouse to ED50 for antipsychotic activity in po dosed mouse assessed as reduction in MK-801-induced hyperlocomotor activity2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID1136418Antipsychotic activity in mouse assessed as increase in brain dopamine turnover at 25 to 30 mg/kg, ip pretreated with 200 mg/kg, ip alpha-methyl-p-tyrosine tyrosine hydroxylase inhibitor1978Journal of medicinal chemistry, Sep, Volume: 21, Issue:9
Synthesis and biological evaluation of some 2-amino-4-aryl-3H-1,5-benzodiazepine analogues of clozapine.
AID5171Inhibitory concentration against human 5-HT2A receptor in BEK cells1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID111333Relative central nervous system(CNS) activity was measured in mice; Activity in >=6 assays1981Journal of medicinal chemistry, Sep, Volume: 24, Issue:9
Synthesis and evaluation of 1,2,3,4-tetrahydro[1]benzothieno[2,3-h]isoquinolines as dopamine antagonists.
AID7783Unbound fraction (plasma)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID176735Dose (administered orally) inhibiting spontaneous locomotor behavior in rats1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID1650557Displacement of [3H]ifenprodil from human recombinant GluN2B expressed in mouse L(tk-) cell membranes co-expressing GluN1a incubated for 120 mins by scintillation counting method2020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Thiophene bioisosteres of GluN2B selective NMDA receptor antagonists: Synthesis and pharmacological evaluation of [7]annuleno[b]thiophen-6-amines.
AID1851836Displacement of (+)-[3H]pentazocine from sigma-1 receptor in Sprague-Dawley rat cerebral membrane incubated for 90 mins by liquid scintillation counter analysis2022RSC medicinal chemistry, Aug-17, Volume: 13, Issue:8
Development of tumor-targeting aza-vesamicol derivatives with high affinity for sigma receptors for cancer theranostics.
AID177886Inhibition of apomorphine-induced stereotypy in Rat, after peroral administration1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics.
AID229192Inhibition of specific binding of [3H]NANM of sigma binding site in Guinea pig brain membranes1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites.
AID596437Biodistribution in haloperidol-pretreated ICR mouse lung at 1 mg/kg, iv pretreated 5 mins before haloperidol challenge measured after 60 mins postinjection (Rvb = 3.84 +/- 0.69 %ID/g)2011Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9
Synthesis and biological evaluation of novel 4-benzylpiperazine ligands for sigma-1 receptor imaging.
AID113713Inhibition of the APO-induced stereotyped behavior in mice1998Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5
Novel antipsychotic agents with dopamine autoreceptor agonist properties: synthesis and pharmacology of 7-[4-(4-phenyl-1-piperazinyl)butoxy]-3,4-dihydro-2(1H)-quinolinone derivatives.
AID1686277Displacement of [3H]-DTG from sigma2 receptor in guinea pig brain membranes by scintillation counting2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells.
AID438611Displacement of [3H]di-o-tolylguanidine from sigma 2 receptor in rat liver membrane after 180 mins by scintillation counting2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Evaluation of spirocyclic 3-(3-fluoropropyl)-2-benzofurans as sigma1 receptor ligands for neuroimaging with positron emission tomography.
AID63075Displacement of [3H]quinpirole from Dopamine receptor D21996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Novel (R)-2-amino-5-fluorotetralins: dopaminergic antagonists and inverse agonists.
AID190979Effect on dopamine agonist-induced rotation in unilaterally 6-OH-DA-lesioned rat at 0.25 mg/kg, ip; Compound 35 was injected subcutaneously at 75 mg/kg1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Troponoids. 6. Troponylpiperazines: a new class of dopamine agonists.
AID1210073Inhibition of CYP2C19 in human liver microsomes using omeprazole substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID233807The ratio of the IC50 value of Dopamine D2 receptor to that of serotonergic 5-HT2 receptor1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents.
AID1213082Drug metabolism assessed as human liver microsomes assessed as O-glucuronide measured at 25 uM by LC-MS/MS analysis in presence of 10 uM gemfibrozil relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1449796Displacement of [3H]-(+)-pentazocine from sigma1 in human MDA-MB-468 cell membranes2017Bioorganic & medicinal chemistry letters, 05-15, Volume: 27, Issue:10
Novel small molecule guanidine Sigma1 inhibitors for advanced prostate cancer.
AID1213075Drug metabolism assessed as recombinant human UGT2B7 assessed as O-glucuronidation measured per mg of protein at 10 to 400 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID65437Displacement of [3H]7-OH-DPAT from human Dopamine receptor D32004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species.
AID1179610Displacement of [3H]DTG from sigma 2 receptor in rat liver membranes in presence of (+)-pentazocine2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Pyridine analogues of spirocyclic σ₁ receptor ligands.
AID40407Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding; ND = 'Not determined'1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
AID114233Salivation after subcutaneous administration in mice; nt=Not tested1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Muscarinic agonists with antipsychotic-like activity: structure-activity relationships of 1,2,5-thiadiazole analogues with functional dopamine antagonist activity.
AID393361Selectivity ratio of Ki for rat liver sigma 2 receptor to Ki for rat liver sigma 1 receptor2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Substituted benzo[d]oxazol-2(3H)-one derivatives with preference for the sigma1 binding site.
AID1558956Displacement of [3H]-DAMGO from human MOR expressed in CHOK1 cell membranes at 10 uM incubated for 60 mins by liquid scintillation counting method2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual μ-Opioid Receptor Agonists and σ
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID1300809Displacement of [3H]-DTG from Sigma2 receptor in Sprague-Dawley rat liver membrane after 150 mins by liquid scintillation counting analysis in presence of sigma1 blocker (+)-pentazocine2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
One-pot synthesis and sigma receptor binding studies of novel spirocyclic-2,6-diketopiperazine derivatives.
AID234212Therapeutic ratio of ED50 of catalepsy to ED50 of climbing in rat models1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Synthesis and neuroleptic activity of a series of 1-[1-(benzo-1,4-dioxan-2-ylmethyl)-4-piperidinyl]benzim idazolone derivatives.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID538759Displacement of [3H](+)-pentazocine from sigma1 receptor guinea pig brain after 180 mins scintillation counting2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Conformationally constrained NR2B selective NMDA receptor antagonists derived from ifenprodil: Synthesis and biological evaluation of tetrahydro-3-benzazepine-1,7-diols.
AID65908Binding affinity towards dopamine receptor D2 by displacing [3H]spiperone radioligand in rat striatum1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Pyrrole mannich bases as potential antipsychotic agents.
AID1712206Displacement of [3H]-DTG from Sigma 2 receptor in guinea pig brain membrane incubated for 120 mins in presence of sigma1 blocker (+)-SKF-10047 by liquid scintillation counting method2016Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14
New bifunctional antioxidant/σ1 agonist ligands: Preliminary chemico-physical and biological evaluation.
AID223122Compound was evaluated for the effective dose that causes lethality in aggregated mice (group toxicity antagonism)1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Synthesis and antidopaminergic activity of some 3-(aminomethyl)tetralones as analogues of butyrophenone.
AID229186Inhibition of specific binding of [125I]-PIPAG to sigma binding site in Guinea pig brain membranes1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID592126Induction of apoptosis in mouse B16F10 cells expressing sigma receptor assessed as necrotic cells using annexin V/propidium iodide staining at 5 uM after 24 hrs by flow cytometry (Rvb = 0.25%)2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Structure-activity study to develop cationic lipid-conjugated haloperidol derivatives as a new class of anticancer therapeutics.
AID592128Induction of apoptosis in mouse B16F10 cells expressing sigma receptor assessed as late apoptotic cells using annexin V/propidium iodide staining at 5 uM after 24 hrs by flow cytometry (Rvb = 1.21%)2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Structure-activity study to develop cationic lipid-conjugated haloperidol derivatives as a new class of anticancer therapeutics.
AID1213085Drug excretion in human urine2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1215938Unbound intrinsic clearance in human liver cytosol at 50 to 1000 nM after 30 to 60 mins by HPLC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Significance of reductive metabolism in human intestine and quantitative prediction of intestinal first-pass metabolism by cytosolic reductive enzymes.
AID1136414Antipsychotic activity in mouse assessed as protection against amphetamine-induced lethality at 5 mg/kg, ip treated 30 mins before amphetamine challenge1978Journal of medicinal chemistry, Sep, Volume: 21, Issue:9
Synthesis and biological evaluation of some 2-amino-4-aryl-3H-1,5-benzodiazepine analogues of clozapine.
AID1221957Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID203916Binding affinity towards serotonin S1 receptor at 1.0 uM1987Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.
AID36798Binding affinity against alpha-2 adrenergic receptor in rat brain using [3H]- clonidine1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents.
AID5835Inhibitory constant was determined on 5-hydroxytryptamine 2C receptor of Bovine choroid plexus2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
New serotonin 5-HT(2A), 5-HT(2B), and 5-HT(2C) receptor antagonists: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo and heterocycloalkanones.
AID1570061Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT
AID393186Displacement of [3H]di-o-tolylguanidine from sigma2 opioid receptor in rat liver by solid scintillation counting2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
Relationships between the structure of 6-substituted 6,8-diazabicyclo[3.2.2]nonan-2-ones and their sigma receptor affinity and cytotoxic activity.
AID1570289Antagonist activity at human D2S receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation at 0.1 nM to 100 uM preincubated for 5 mins followed by dopamine and forskolin addition and
AID1135930Neuroleptic activity in ip dosed ICR-DUB mouse assessed as survival administered 16 hrs prior to d-amphetamine challenge measured after 24 hrs1978Journal of medicinal chemistry, Jan, Volume: 21, Issue:1
(1-(3-(Phenothiazin-10-yl)propyl)-4-piperidinyl)phenylmethanones, a novel class of long-acting neuroleptic agents.
AID296886Displacement of [3H]spiroperidol from human recombinant Dopamine D2 long receptor2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2.
AID204292Selectivity ratio Sigma opioid receptor type 1 to Sigma opioid receptor type 22002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.
AID169423Antipsychotic activity was assessed by ability to block response of rats trained to avoid an electrical shock (inhibition of self-jump and/or discrete trial conditioned avoidance response(CAR) upon po administration; value ranges from 0.1-3.51987Journal of medicinal chemistry, Jun, Volume: 30, Issue:6
Psychotropic agents: synthesis and antipsychotic activity of substituted beta-carbolines.
AID63699Displacement of [3H]spiperone from human Dopamine receptor D42004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species.
AID346264Displacement of [3H]spiroperidol from human cloned dopamine D2L receptor by liquid scintillation counting2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Design, synthesis, and binding affinities of potential positron emission tomography (PET) ligands with optimal lipophilicity for brain imaging of the dopamine D3 receptor. Part II.
AID1196314Displacement of [3H]N-methylspiperone from human recombinant dopamine D2 receptor expressed in CHOK1 cells incubated for 60 mins by scintillation counting method2015European journal of medicinal chemistry, Mar-06, Volume: 92Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.
AID141837Half-maximal inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M1 in rat frontal cortex homogenate2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID138781Antagonism of apomorphine for 0-10 minutes in reserpinized mice when a dose of 0.3 micro mol/kg is administered intraperitoneally1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 1. Synthesis and structure-activity relationships of 2,3,3a,4,5,9b-hexahydro-1H-benz[e]indole derivatives.
AID294444Selectivity for human dopamine D3 receptor over human dopamine D4 receptor2007European journal of medicinal chemistry, Jul, Volume: 42, Issue:7
Asymmetric synthesis of chiral piperazinylpropylisoxazoline ligands for dopamine receptors.
AID643383Induction of phospholipidosis in bovine corneal fibroblasts assessed as lamellar inclusion bodies after 72 hrs by light microscopy2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
In silico assay for assessing phospholipidosis potential of small druglike molecules: training, validation, and refinement using several data sets.
AID61845Selectivity ratio for Dopamine receptor D1 to Dopamine receptor D22002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
AID130391Hypothermia in mice after peroral administration1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
4-Piperazinyl-10H-thieno[2,3-b][1,5]benzodiazepines as potential neuroleptics.
AID169571Dose required for producing 50% block of avoidance responding in rats after peroral administration1981Journal of medicinal chemistry, Sep, Volume: 24, Issue:9
A dopamine receptor model and its application in the design of a new class of rigid pyrrolo[2,3-g]isoquinoline antipsychotics.
AID233509Ratio between pKi values of 5-HT2A and D2 receptors1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
Synthesis and atypical antipsychotic profile of some 2-(2-piperidinoethyl)benzocycloalkanones as analogues of butyrophenone.
AID132469The compound was tested for antagonistic activity against apomorphine induced climbing in the mouse, percentages are for reduction in climbing after peroral administration1999Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.
AID342782Binding affinity to human cloned histamine H1 receptor2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID1393475Reversal of ketamine-induced cognitive flexibility in ip dosed Sprague-Dawley rat administered 30 mins prior to ketamine administration by attentional set-shifting test
AID203846Compound was evaluated for its in vitro competition binding studies using sigma-ligand #NAME? in the presence of 1 uM dextrallorphan (sigma2 receptor) in the rat liver membranes.1998Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
Substituted halogenated arylsulfonamides: a new class of sigma receptor binding tumor imaging agents.
AID194373Effect of compound (0.2 mg/kg ip) on the concentration of DA in rat striatum1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID191611Anti psychotic effect Social interaction when compound administered at a doe of 0.125 mg/kg ip in rats1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID255065Inhibitory activity against opioid receptor sigma 1 in guinea pig cerebral cortex using [3H](+)-pentazocine as radio ligand at pH 7.5 for 150 min at 22 degree C 2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective sigma1 ligands. Part 2.
AID517713Displacement of [3H]Prazosin from adrenergic alpha1 receptor in pig cerebral cortex homogenates2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Bioisosteric replacement leading to biologically active [2.2]paracyclophanes with altered binding profiles for aminergic G-protein-coupled receptors.
AID170895Percentage change in chronic single unit sampling when compound given at a dose of 0.5 mg/kg ip in rats1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.
AID238492Binding affinity for human recombinant dopamine receptor D52004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 receptor selectivity.
AID170161Effect (60 min after administration of 200 (5.3 umol/kg) subcuteneous dose on DA release in brain dialysis model of rat1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.
AID1168796Displacement of [3H]Spiperone from D3 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Design, synthesis and evaluation of benzo[a]thieno[3,2-g]quinolizines as novel l-SPD derivatives possessing dopamine D1, D2 and serotonin 5-HT1A multiple action profiles.
AID1213027Drug metabolism assessed as human liver microsomes assessed as O-glucuronide measured per mg of protein at 100 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1415570Displacement of [3H]-di-o-tolylguanidine from sigma 2 receptor in rat liver membranes after 120 mins by scintillation counting analysis2017MedChemComm, May-01, Volume: 8, Issue:5
Do GluN2B subunit containing NMDA receptors tolerate a fluorine atom in the phenylalkyl side chain?
AID342781Binding affinity to human cloned 5HT2C receptor2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
AID27922Calculated partition coefficient (clogP)2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines.
AID176808Suppression of conditioned avoidance behavior in rats when administered perorally 60 min before measurement1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
AID596433Biodistribution in haloperidol-pretreated ICR mouse brain at 1 mg/kg, iv pretreated 5 mins before haloperidol challenge measured after 60 mins postinjection (Rvb = 3.64 +/- 0.66 %ID/g)2011Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9
Synthesis and biological evaluation of novel 4-benzylpiperazine ligands for sigma-1 receptor imaging.
AID246503Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo52004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand.
AID1853653Antibacterial activity against Mycobacterium bovis BCG ATCC 35734 assessed as inhibition of bacterial growth incubated upto 3 weeks hrs by resazurin dye based double-dilution method2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from
AID566431Displacement of [3H]DTG from sigma 2 receptor in guinea pig brain membrane after 120 mins by liquid scintillation counting2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Antiproliferative activity of phenylbutyrate ester of haloperidol metabolite II [(±)-MRJF4] in prostate cancer cells.
AID138925Antagonism of apomorphine for 10-20 minutes in reserpinized mice when a dose of 0.3 micro mol/kg is administered intraperitoneally1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Centrally acting serotonergic and dopaminergic agents. 1. Synthesis and structure-activity relationships of 2,3,3a,4,5,9b-hexahydro-1H-benz[e]indole derivatives.
AID61613Displacement of [3H]raclopride from human dopamine D2A receptors expressed in LtK cells1999Bioorganic & medicinal chemistry letters, Aug-02, Volume: 9, Issue:15
Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1185959Displacement of [3H] 8-OH-DPAT from human 5-HT1A receptor by liquid scintillation counting2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Further evaluation of the tropane analogs of haloperidol.
AID1177034Intrinsic agonist activity at human D2 long receptor expressed in HEK293 cells assessed as inhibition of a forskolin-dependent whole cell adenylyl cyclase activity after 20 mins relative to quinpirole2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Synthesis, pharmacological evaluation and molecular modeling studies of triazole containing dopamine D3 receptor ligands.
AID1335649Inhibition of apomorphine-induced climbing behavior in po dosed Chinese Kun Ming mouse administered for 30 mins followed by apomorphine challenge and measured for 10 to 30 mins2016European journal of medicinal chemistry, Nov-29, Volume: 124Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.
AID177741Activity to evoke catalepsy, after 1 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID1865089Selectivity index, ratio of Ki for displacement of [3H]DTG from sigma 2 receptor in rat liver membranes to Ki for displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane
AID87242Binding affinity towards human histamine H1 receptor2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Selective optimization of side activities: another way for drug discovery.
AID1185971Displacement of [3H]QNB from human muscarinic M2 receptor by liquid scintillation counting2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Further evaluation of the tropane analogs of haloperidol.
AID5324In vitro affinity against serotonin 5-hydroxytryptamine 2A receptor2000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.
AID605700Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Bivalent dopamine D2 receptor ligands: synthesis and binding properties.
AID391478Selectivity ratio, Ki for sigma 1 receptor in guinea pig brain membrane to Ki for sigma 2 receptor rat liver membrane2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Thiophene bioisosteres of spirocyclic sigma receptor ligands. 1. N-substituted spiro[piperidine-4,4'-thieno[3,2-c]pyrans].
AID1596347Induction of apoptosis in human MCF7 cells assessed as increase in caspase-3 activity at 20 uM incubated for 24 hrs by Ac-DEVD-pNA substrate-based colorimetric assay
AID65443Cataleptogenic effect against cloned human Dopamine receptor D3 in male Sprague-Dawley rats in a bar test2003Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21
The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+.
AID61079Binding affinity against dopamine D2 receptor1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study.
AID1209972Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID194378Effect of compound (0.2 mg/kg ip) on the concentration of DOPAC/DA in rat striatum1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
AID1213054Drug metabolism assessed as recombinant human UGT2B7 assessed as N-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution.
AID1655660Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membranes incubated for 1 hr by liquid scintillation counting method
AID410331Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
AID19424Partition coefficient (logD7.4)2001Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
ElogD(oct): a tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds.
AID36113Binding affinity towards human alpha-1 adrenergic receptor2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Selective optimization of side activities: another way for drug discovery.
AID131723Effective dose for inhibition of physostigmine induced lethality in mouse1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.
AID277975Displacement of [3H]YM-09151-2 from rat striatum D2 receptor2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.
AID427339Selectivity ratio of Ki for rat sigma1 receptor to Ki for rat sigma2 receptor2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Synthesis, biological evaluation, and three-dimensional in silico pharmacophore model for sigma(1) receptor ligands based on a series of substituted benzo[d]oxazol-2(3H)-one derivatives.
AID5479In vitro affinity towards 5-hydroxytryptamine 2A receptor using [3H]spiroperidol as radioligand in cortex1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents.
AID1861723Binding affinity to sigma 1 receptor (unknown origin) assessed as inhibition constant by radioligand binding assay2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.
AID176457Pole climb avoiding activity in rats was determined after 1 hr of intraperitoneal administration of the compound1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
AID4803Compound was measured for affinity at 5-hydroxytryptamine 2 receptor in rat cortical by [3H]spiroperidol displacement.1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
AID1686301Suppression of VEGF-A-induced cell migration in HREC assessed as effect on crossing cells count at 2 uM incubated for 24 to 72 hrs by wound healing assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells.
AID63076Inhibition of [3H]raclopride binding to Dopamine receptor D21996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Novel (R)-2-amino-5-fluorotetralins: dopaminergic antagonists and inverse agonists.
AID1135533Blockade of po dosed apomorphine-induced stereotyped behavior in Sprague-Dawley rat assessed as continuous sniffing, licking, gnawing, or biting1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Synthesis and stereospecific antipsychotic activity of (-)-1-cyclopropylmethyl-4-(3-trifluoromethylthio-5H-dibenzo[a,d]cyclohepten-5-ylidene)piperidine.
AID176743Dose inducing catalepsy in rats after oral administration1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
AID1861727Binding affinity to DOR (unknown origin) assessed as inhibition constant by radioligand binding assay2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.
AID61527In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1345235Rat 5-HT7 receptor (5-Hydroxytryptamine receptors)1996European journal of pharmacology, Dec-19, Volume: 317, Issue:2-3
Iloperidone binding to human and rat dopamine and 5-HT receptors.
AID1345291Human 5-HT7 receptor (5-Hydroxytryptamine receptors)1997British journal of pharmacology, Sep, Volume: 122, Issue:1
Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
AID1345833Human D3 receptor (Dopamine receptors)1992European journal of pharmacology, Apr-10, Volume: 225, Issue:4
Pharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor.
AID1345718Human D1 receptor (Dopamine receptors)1991Nature, Apr-18, Volume: 350, Issue:6319
Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
AID1345788Human D2 receptor (Dopamine receptors)1994Pharmacology, biochemistry, and behavior, Nov, Volume: 49, Issue:3
Characterization of the binding of SCH 39166 to the five cloned dopamine receptor subtypes.
AID1345788Human D2 receptor (Dopamine receptors)1992European journal of pharmacology, Apr-10, Volume: 225, Issue:4
Pharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor.
AID1345833Human D3 receptor (Dopamine receptors)1994The Journal of pharmacology and experimental therapeutics, Jan, Volume: 268, Issue:1
Expression and pharmacological characterization of the human D3 dopamine receptor.
AID624223Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A2004The Journal of pharmacology and experimental therapeutics, Sep, Volume: 310, Issue:3
Pharmacological characterization of AC-90179 [2-(4-methoxyphenyl)-N-(4-methyl-benzyl)-N-(1-methyl-piperidin-4-yl)-acetamide hydrochloride]: a selective serotonin 2A receptor inverse agonist.
AID1346037Human H1 receptor (Histamine receptors)2003Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Mar, Volume: 28, Issue:3
H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
AID624215Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1A1997The Journal of pharmacology and experimental therapeutics, Mar, Volume: 280, Issue:3
Interactions of (+)- and (-)-8- and 7-hydroxy-2-(di-n-propylamino)tetralin at human (h)D3, hD2 and h serotonin1A receptors and their modulation of the activity of serotoninergic and dopaminergic neurones in rats.
AID624223Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A1998The Journal of pharmacology and experimental therapeutics, Sep, Volume: 286, Issue:3
S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison w
AID1346732Human Kv10.1 (Voltage-gated potassium channels)2003British journal of pharmacology, Jan, Volume: 138, Issue:1
Inhibition of hEAG1 and hERG1 potassium channels by clofilium and its tertiary analogue LY97241.
AID1346867Human 5-HT2B receptor (5-Hydroxytryptamine receptors)1998Naunyn-Schmiedeberg's archives of pharmacology, Jan, Volume: 357, Issue:1
[3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor.
AID1345898Rat D3 receptor (Dopamine receptors)1990Nature, Sep-13, Volume: 347, Issue:6289
Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.
AID1345833Human D3 receptor (Dopamine receptors)2009Journal of psychopharmacology (Oxford, England), Jan, Volume: 23, Issue:1
Asenapine: a novel psychopharmacologic agent with a unique human receptor signature.
AID1345788Human D2 receptor (Dopamine receptors)1994The Journal of pharmacology and experimental therapeutics, Jan, Volume: 268, Issue:1
Expression and pharmacological characterization of the human D3 dopamine receptor.
AID1345788Human D2 receptor (Dopamine receptors)1994European journal of pharmacology, Jan-01, Volume: 266, Issue:1
Characterization of the human dopamine D3 receptor expressed in transfected cell lines.
AID1346919Rat 5-HT2A receptor (5-Hydroxytryptamine receptors)1998The Journal of pharmacology and experimental therapeutics, Jul, Volume: 286, Issue:1
Creation of a constitutively activated state of the 5-hydroxytryptamine2A receptor by site-directed mutagenesis: inverse agonist activity of antipsychotic drugs.
AID1345814Human D4 receptor (Dopamine receptors)2009Journal of psychopharmacology (Oxford, England), Jan, Volume: 23, Issue:1
Asenapine: a novel psychopharmacologic agent with a unique human receptor signature.
AID1346037Human H1 receptor (Histamine receptors)1996Psychopharmacology, Mar, Volume: 124, Issue:1-2
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID1345814Human D4 receptor (Dopamine receptors)1994Pharmacology, biochemistry, and behavior, Nov, Volume: 49, Issue:3
Characterization of the binding of SCH 39166 to the five cloned dopamine receptor subtypes.
AID1345879Human D5 receptor (Dopamine receptors)1991Nature, Apr-18, Volume: 350, Issue:6319
Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
AID1345215Mouse 5-HT7 receptor (5-Hydroxytryptamine receptors)1993Molecular pharmacology, Aug, Volume: 44, Issue:2
Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
AID1345235Rat 5-HT7 receptor (5-Hydroxytryptamine receptors)1994The Journal of pharmacology and experimental therapeutics, Mar, Volume: 268, Issue:3
Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
AID624231Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1D1996Psychopharmacology, Mar, Volume: 124, Issue:1-2
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)2003Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Mar, Volume: 28, Issue:3
H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)1996Psychopharmacology, Mar, Volume: 124, Issue:1-2
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID1346528Human 5-HT1D receptor (5-Hydroxytryptamine receptors)1996Psychopharmacology, Mar, Volume: 124, Issue:1-2
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)1998The Journal of pharmacology and experimental therapeutics, Sep, Volume: 286, Issue:3
S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison w
AID624215Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1A1998European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3
Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study.
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)2009Journal of psychopharmacology (Oxford, England), Jan, Volume: 23, Issue:1
Asenapine: a novel psychopharmacologic agent with a unique human receptor signature.
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)2004The Journal of pharmacology and experimental therapeutics, Sep, Volume: 310, Issue:3
Pharmacological characterization of AC-90179 [2-(4-methoxyphenyl)-N-(4-methyl-benzyl)-N-(1-methyl-piperidin-4-yl)-acetamide hydrochloride]: a selective serotonin 2A receptor inverse agonist.
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)1998European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3
Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study.
AID624215Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1A1998The Journal of pharmacology and experimental therapeutics, Sep, Volume: 286, Issue:3
S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison w
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)1998The Journal of pharmacology and experimental therapeutics, Sep, Volume: 286, Issue:3
S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison w
AID1345718Human D1 receptor (Dopamine receptors)2009Journal of psychopharmacology (Oxford, England), Jan, Volume: 23, Issue:1
Asenapine: a novel psychopharmacologic agent with a unique human receptor signature.
AID624222Antagonists at Rat 5-Hydroxytryptamine receptor 5-HT2A1998The Journal of pharmacology and experimental therapeutics, Jul, Volume: 286, Issue:1
Creation of a constitutively activated state of the 5-hydroxytryptamine2A receptor by site-directed mutagenesis: inverse agonist activity of antipsychotic drugs.
AID1345783Rat D2 receptor (Dopamine receptors)1990Nature, Sep-13, Volume: 347, Issue:6289
Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.
AID1346501Mouse Kir3.2 (Inwardly rectifying potassium channels)2000British journal of pharmacology, Apr, Volume: 129, Issue:8
Inhibition by various antipsychotic drugs of the G-protein-activated inwardly rectifying K(+) (GIRK) channels expressed in xenopus oocytes.
AID1345235Rat 5-HT7 receptor (5-Hydroxytryptamine receptors)1993Proceedings of the National Academy of Sciences of the United States of America, Sep-15, Volume: 90, Issue:18
Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
AID624218Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2B1998Naunyn-Schmiedeberg's archives of pharmacology, Jan, Volume: 357, Issue:1
[3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor.
AID1345833Human D3 receptor (Dopamine receptors)1994Pharmacology, biochemistry, and behavior, Nov, Volume: 49, Issue:3
Characterization of the binding of SCH 39166 to the five cloned dopamine receptor subtypes.
AID624223Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A2003Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Mar, Volume: 28, Issue:3
H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)1997The Journal of pharmacology and experimental therapeutics, Mar, Volume: 280, Issue:3
Interactions of (+)- and (-)-8- and 7-hydroxy-2-(di-n-propylamino)tetralin at human (h)D3, hD2 and h serotonin1A receptors and their modulation of the activity of serotoninergic and dopaminergic neurones in rats.
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)1996Psychopharmacology, Mar, Volume: 124, Issue:1-2
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID624215Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1A1996Psychopharmacology, Mar, Volume: 124, Issue:1-2
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID1345788Human D2 receptor (Dopamine receptors)1995European journal of pharmacology, Jun-23, Volume: 290, Issue:1
Pramipexole binding and activation of cloned and expressed dopamine D2, D3 and D4 receptors.
AID624223Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A1996Psychopharmacology, Mar, Volume: 124, Issue:1-2
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID1345814Human D4 receptor (Dopamine receptors)1993European journal of pharmacology, Jun-04, Volume: 236, Issue:3
Dopamine D4 versus D2 receptor selectivity of dopamine receptor antagonists: possible therapeutic implications.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID1224817Assays to identify small molecules inhibitory for eIF4E expression2015Chemistry & biology, Jul-23, Volume: 22, Issue:7
Internal Ribosome Entry Site-Based Bicistronic In Situ Reporter Assays for Discovery of Transcription-Targeted Lead Compounds.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508628Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1803434Binding Affinity Assay from Article 10.3109/14756366.2013.776556: \\Synthesis and dual D2 and 5-HT1A receptor binding affinities of 5-piperidinyl and 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones.\\2014Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 29, Issue:2
Synthesis and dual D2 and 5-HT1A receptor binding affinities of 5-piperidinyl and 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones.
AID1798075Radioligand Labeled Binding Assay from Article 10.1021/jm070487n: \\Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2.\\2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1745855NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1745854NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
AID1645871NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling in pH 5 buffer2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Using in vitro ADME data for lead compound selection: An emphasis on PAMPA pH 5 permeability and oral bioavailability.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (18,985)

TimeframeStudies, This Drug (%)All Drugs %
pre-19907703 (40.57)18.7374
1990's4114 (21.67)18.2507
2000's3523 (18.56)29.6817
2010's2797 (14.73)24.3611
2020's848 (4.47)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 119.29

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index119.29 (24.57)
Research Supply Index10.00 (2.92)
Research Growth Index4.42 (4.65)
Search Engine Demand Index228.84 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (119.29)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1,753 (8.62%)5.53%
Trials0 (0.00%)5.53%
Reviews779 (3.83%)6.00%
Reviews0 (0.00%)6.00%
Case Studies1,692 (8.32%)4.05%
Case Studies0 (0.00%)4.05%
Observational27 (0.13%)0.25%
Observational0 (0.00%)0.25%
Other16,079 (79.09%)84.16%
Other13 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (137)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Preventing ICU Subsyndromal Delirium Conversion to Delirium With Low Dose IV Haloperidol: A Double-Blind, Placebo-Controlled Pilot Study [NCT01174290]Phase 468 participants (Actual)Interventional2010-09-30Completed
Pharmacological Modulation of Belief Salience [NCT03754062]Phase 130 participants (Actual)Interventional2017-06-01Completed
Blood Lactate Levels in Patients Treated With Typical or Atypical Antipsychotics [NCT01139463]60 participants (Actual)Observational2008-06-30Completed
Phase I Clinical Trial. Study of the Impact of Pharmacogenetic Markers in Predicting the Appearance of Extrapyramidal Symptomatology After the Treatment With Typical vs. Atypical Antipsychotics, in Healthy Volunteers [NCT01259973]Phase 124 participants (Anticipated)Interventional2011-02-28Enrolling by invitation
"Efficacy of the Combination of Z-track and Airlock Techniques During Intramuscular Injection of Haloperidol Decanoate in Adult Patients With Schizophrenic or Related Disorder : A Multicenter Randomized Controlled Trial" [NCT05995457]84 participants (Anticipated)Interventional2023-09-01Not yet recruiting
TREC-Lebanon Trial: A Randomised Controlled Trial for Rapid Tranquilisation for Agitated Patients in the Emergency Setting [NCT03639558]Phase 4100 participants (Actual)Interventional2018-08-28Completed
Randomized Double-Blind Clinical Trial to Compare Haloperidol and Non-Pharmacologic Treatment Versus Non-Pharmacologic Treatment and Placebo, in Elderly Hospitalized Patients With Hypoactive Delirium [NCT02345902]Phase 360 participants (Anticipated)Interventional2016-01-31Recruiting
Feasibility of Prophylactic Haldol to Prevent Delirium in Cancer Patients [NCT03489551]Phase 417 participants (Actual)Interventional2011-11-30Completed
Investigating the Efficacy of Using Haloperidol vs. Metoclopramide for Treatment of Acute Headaches and Migraines in the Emergency Department: A Prospective Randomized Clinical Trial [NCT02972502]Phase 466 participants (Actual)Interventional2014-02-28Terminated(stopped due to PI lapsed institutional training)
Strategies for Persistent Agitated Delirium in Palliative Care [NCT03743649]Phase 2/Phase 3206 participants (Anticipated)Interventional2019-07-17Recruiting
A Comparison of Haloperidol 5mg IM vs Droperidol 2.5mg and Ondansetron for the Treatment of Hyperemesis in Cannabis Hyperemesis Syndrome [NCT05065567]Phase 238 participants (Actual)Interventional2021-08-30Terminated(stopped due to Lost too many patients to follow up, unable to enroll enough patients)
Evaluation of Negative Symptoms and Cognitive Function After Administration of Antipsychotics in Healthy Volunteer: a Double-blind, Randomized Trial of a Single Dose of Placebo, Haloperidol, Amisulpride, Risperidone and Aripiprazole [NCT01185418]80 participants (Actual)Observational2009-03-31Completed
Outcomes of Antipsychotic Medication Use in the Emergency Department: A Retrospective Comparison Study [NCT02504450]93 participants (Actual)Observational2015-04-30Completed
Neuroendocrine, Metabolite Substrates, Clinical Symptoms and Cognitive Function in Schizophrenia [NCT02423096]200 participants (Anticipated)Observational [Patient Registry]2013-12-31Recruiting
Intramuscular Olanzapine Versus Haloperidol or Midazolam for the Management of Acute Agitation in the Emergency Department - a Multicentre Randomised Clinical Trial [NCT02380118]Phase 4167 participants (Actual)Interventional2014-12-31Terminated(stopped due to Primary endpoint reached based on data projection from interim analysis.)
Risk of QT-prolongation and Torsade de Pointes in Patients Treated With Acute Medication in a University Hospital [NCT02068170]178 participants (Actual)Observational2014-02-28Completed
A Single Center, Randomized Controlled Prospective Double-blinded Trial Comparing Haloperidol to Standard Ondansetron Therapy for Control of Nausea and Vomiting in the Emergency Department [NCT04764344]Phase 460 participants (Actual)Interventional2021-04-01Completed
Haloperidol Versus Ondansetron for Cannabis Hyperemesis Syndrome (HaVOC): A Randomized Controlled Trial [NCT03056482]Phase 433 participants (Actual)Interventional2017-05-21Completed
Evaluation of the Necessity of Long-term Pharmacological Treatment With Antipsychotics for the Prevention of Relapse in Long-term Stabilized Schizophrenic Patients: a Randomized, Single-blind, Longitudinal Trial [NCT02307396]Phase 421 participants (Actual)Interventional2015-02-01Completed
Clozapine and Olanzapine in the Treatment of Violence in Schizophrenic Patients [NCT01123408]110 participants (Actual)Interventional1999-06-30Completed
A Prospective, Multi-centre, Randomised, Double-blind, Placebo-controlled Comparison of Intravenous Dexmedetomidine and Haloperidol in Treatment of Psychomotor Confusion After Heart Surgery [NCT01140529]Phase 33 participants (Actual)Interventional2010-05-31Terminated(stopped due to Slow recruitment)
A Prospective, Matched-Control, Randomized, Open-Label, Flexible-Dose, Study in Subjects With Recent-Onset Schizophrenia or Schizophreniform Disorder to Compare Disease Progression and Disease Modification Following Treatment With Paliperidone Palmitate L [NCT02431702]Phase 3337 participants (Actual)Interventional2015-07-08Completed
A Randomized Double-blind Multicenter Double-dummy Non-inferiority Trial of Inhaled Loxapine and Intramuscular Haloperidol + Lorazepam for the Reduction of Agitation [NCT03110900]Phase 42 participants (Actual)Interventional2017-09-30Terminated(stopped due to Sponsor Withdrawal)
Effects of Aripiprazole and Haloperidol on Mesolimbic System Functioning: A Pharmacological fMRI Study [NCT01161277]Phase 454 participants (Actual)Interventional2010-08-31Completed
Clinical Effectiveness Of The Newer Antipsychotic Compounds Olanzapine, Quetiapine And Aripiprazole In Comparison With Low Dose Conventional Antipsychotics (Haloperidol And Flupentixol) In Patients With Schizophrenia [NCT01164059]Phase 4149 participants (Actual)Interventional2010-02-28Completed
Early Clinical Evaluation of the Pharmacokinetics and Mechanism Based Pharmacodynamics of Haloperidol Using Positron Emission Tomography in Healthy Volunteers [NCT01193621]Phase 112 participants (Actual)Interventional2008-01-31Completed
A Multicenter, Randomized, Double-Blind, Fixed-Dose, 6-Week Trial of the Efficacy and Safety of Asenapine Compared With Placebo Using Haloperidol Positive Control in Subjects With an Acute Exacerbation of Schizophrenia [NCT00156104]Phase 3460 participants (Actual)Interventional2005-07-01Completed
Intravenous Haloperidol Versus Ondansetron for Treatment of Established Nausea and Vomiting in Patients Undergoing Surgery With General Anesthesia: A Randomized Clinical Trial [NCT02143531]Phase 4120 participants (Actual)Interventional2008-09-30Completed
Haldol/Diphenhydramine Versus Metoclopramide/Diphenhydramine for Treatment of Acute Headache in the Emergency Department: A Randomized Controlled Trial [NCT02098499]Phase 468 participants (Actual)Interventional2013-06-30Completed
A Double Blinded Randomized Trial of Ketamine Versus Haloperidol for Severe Prehospital Agitation [NCT02103881]Phase 40 participants (Actual)Interventional2014-04-30Withdrawn
Meth-OD: A Phase 2a Study of IXT-m200 in Patients With Toxicity From Methamphetamine Overdose [NCT04715230]Phase 220 participants (Actual)Interventional2021-06-30Terminated(stopped due to Sponsor decision based on slower than anticipated enrollment leading to fund exhaustion.)
Haloperidol Prophylaxis in Cardiac Surgery for Patients at Risk for Delirium: A Randomized Placebo-Controlled Pilot Study [NCT01862302]Phase 325 participants (Actual)Interventional2013-08-31Completed
A Randomized Blind Parallel Intramuscular Haloperidol-Controlled Multicenter Clinical Trial to Evaluate the Efficacy and Safety of Intramuscular Levosulpiride in the Treatment of Chinese Patients With Agitation Of Schizophrenia [NCT00866645]Phase 2/Phase 3240 participants (Anticipated)Interventional2009-02-28Completed
How Does the Brain Learn About Positive and Negative Things? [NCT06014606]150 participants (Actual)Interventional2021-03-01Completed
The Effect of Lamictal TM Augmentation of Haloperidol Decanoate in the Treatment of Resistant Schizophrenia Predominantly by Verbal Resistant Hallucinosis: Randomized, Double-blind, Placebo-controlled, Study [NCT00947375]Phase 4335 participants (Actual)Interventional2005-01-31Terminated(stopped due to All of the mentioned aim and objectives were achieved before the February 2007)
Efficacy of SCH 420814 to Reduce the Frequency or Severity of Neuroleptic Induced Akathisia [NCT00693472]Phase 246 participants (Actual)Interventional2007-08-15Terminated
A Randomized, Open Label, Rater Blind, Flexible Dose Multi-Center Study Comparing The Efficacy And Safety Of Intramuscular Ziprasidone With Haloperidol For Three Days In Patients With Agitation Of Schizophrenia [NCT00723606]Phase 3376 participants (Actual)Interventional2008-09-30Completed
Non-randomized Control Clinical Trial to Evaluate the Efficacy and Safety of Symptomatic Drug Therapy for Mild to Moderate Huntington's Disease Patients [NCT04071639]Phase 160 participants (Anticipated)Interventional2020-03-12Recruiting
A Prospective, Open Label, Non-comparative Trial to Determine the Incidence of Chemotherapy-Induced Nausea and Vomiting (CINV) Associated With the Docetaxel-Cyclophosphamide Regimen in Early Breast Cancer Patients [NCT01298193]Phase 4212 participants (Actual)Interventional2011-05-31Completed
Atypical Antipsychotics and Hyperglycemic Emergencies: Multicentre, Retrospective Cohort Study of Administrative Data [NCT02582736]725,489 participants (Actual)Observational2012-04-30Completed
Treatment of Clozapine-resistant Schizophrenia : Comparison Between Augmentation With Haloperidol and Electroconvulsive Therapy [NCT00753051]18 participants (Actual)Interventional2008-06-30Completed
Methylphenidate, Rivastigmine or Haloperidol in Hypoactive Delirium in Intensive Care Patients: a Randomized, Mono-blind Pilot Trial [NCT00599287]Phase 380 participants (Anticipated)Interventional2008-02-29Terminated(stopped due to Inclusion rate too low due to a lack of eligible patients and difficulties obtaining informed consent.)
A Randomized Open Label Study on the Efficacy, Tolerability, and Total Costs of Olanzapine Versus Conventional Antipsychotics in the Treatment of Acute Mania in Sweden [NCT00767715]Phase 411 participants (Actual)Interventional2004-10-31Terminated(stopped due to Trial discontinued due to low enrollment)
Metabolic Effects of Subchronic Dopamine D2 Receptor Blockade by Haloperidol in Healthy Humans [NCT00625014]8 participants (Actual)Interventional2005-03-31Completed
Metabolic Effects of Subchronic Dopamine D2 Receptor Blockade by Antipsychotic Drugs in Healthy Humans [NCT00625170]11 participants (Actual)Interventional2004-05-31Completed
A Comparison of Long-Acting Injectable Medications for Schizophrenia [NCT01136772]Phase 4311 participants (Actual)Interventional2011-03-31Completed
MIND-USA Study: Modifying the Impact of ICU-Associated Neurological Dysfunction [NCT01211522]Phase 3566 participants (Actual)Interventional2011-12-14Completed
Study of Evaluating Quetiapine in Improving Sleep Quality of Schizophrenia [NCT00642369]60 participants (Actual)Interventional2008-03-31Completed
GiSAS Trial: Aripiprazole, Olanzapine, and Haloperidol in the Long Term Treatment of Schizophrenia. [NCT01052389]Phase 4300 participants (Actual)Interventional2007-07-31Completed
[NCT00631722]80 participants (Actual)Interventional2007-05-31Completed
A Multicenter, Randomized, Double-blind, Parallel-controlled Injection of Olanzapine in the Treatment of Acute Agitation Associated With Schizophrenia and Bipolar I Disorder. [NCT05803642]Phase 3318 participants (Anticipated)Interventional2023-03-28Not yet recruiting
Intravenous Haloperidol for the Treatment of Headache in the Emergency Department [NCT02747511]Phase 4118 participants (Actual)Interventional2015-10-31Completed
An Open-Label, Single-Dose, Crossover Study to Determine the Bioequivalency of Generic Haloperidol Tablets vs. Haldol in Normal Volunteers. [NCT00946491]Phase 130 participants (Actual)Interventional1987-04-30Completed
Stroke Risk Among Users of Typical vs. Atypical Antipsychotics Stratified by Broad Age Group, a Post-authorization Safety Study [NCT04002700]1,234,412 participants (Actual)Observational2019-05-06Completed
A 12-Month Randomized, Open-Label Study of Caregiver Psycho-education and Skills Training in Patients Recently Diagnosed With Schizophrenia, Schizoaffective Disorder, or Schizophreniform Disorder and Receiving Paliperidone Palmitate or Oral Antipsychotic [NCT02600741]296 participants (Actual)Observational2015-07-24Completed
[NCT00838032]Phase 470 participants (Anticipated)Interventional2008-08-31Recruiting
Compare Efficacy and Safety Between Quetiapine and Haloperidol in Treatment Delirium [NCT00954603]Phase 352 participants (Actual)Interventional2009-06-30Terminated(stopped due to few delirious patients were enrolled.)
Efficacy and Safety of Risperidone Oral Solution Combination Clonazepam Versus Haloperidol IM Injection for Treatment of Acute Psychotic Agitation in Schizophrenia [NCT00859872]Phase 4198 participants (Actual)Interventional2008-08-31Completed
Treatment of Behavioral Symptoms in Alzheimer's Disease [NCT00009217]Phase 444 participants (Actual)Interventional1999-01-31Completed
Placebo- and Haloperidol-Controlled Double-Blind Trial of Olanzapine in Patients With Manic or Mixed Episode of Bipolar I Disorder [NCT00129220]Phase 3224 participants (Actual)Interventional2005-07-31Completed
Combination of Haloperidol and Magnesium for Delirium Prevention in Critically Ill Elderly Patients After Elective Major Surgery [NCT06168773]Phase 2/Phase 3135 participants (Actual)Interventional2022-11-01Completed
A Single Center, Single Dose, Open-label, Randomized, Two Period Crossover Pivotal Study to Determine the Bioequivalence of Two Formulations Containing Haloperidol 2 mg in Healthy Males and Females Under Fed Conditions [NCT04411953]Phase 132 participants (Actual)Interventional2019-11-15Completed
A Single Center, Single Dose, Open-label, Randomized, Two Period Crossover Pivotal Study to Determine the Bioequivalence of Two Formulations Containing Haloperidol 2 mg in Healthy Males and Females Under Fasting Conditions [NCT04411940]Phase 132 participants (Actual)Interventional2019-11-15Completed
Delirium in the ICU: a Prospective, Randomized, Trial of Placebo vs. Haloperidol vs. Ziprasidone [NCT00096863]Phase 2102 participants (Actual)Interventional2004-12-31Completed
A Comparison of Risperidone and Haloperidol for Prevention of Relapse in Subjects With Schizophrenia and Schizoaffective Disorders [NCT00253110]Phase 4396 participants (Actual)Interventional1996-05-31Completed
Optimization of Acute Treatment in First Episode Schizophrenic Patients by New Pharmacological Treatments [NCT00157378]Phase 4300 participants Interventional2000-11-30Active, not recruiting
Drug Interactions With Risk of QT-prolongation in a General Hospital: an Epidemiological Point Prevalence Study [NCT02043912]222 participants (Actual)Observational2013-07-31Completed
CSP #451 - The Clinical and Economic Impact of Olanzapine in the Treatment of Schizophrenia [NCT00007774]Phase 4600 participants (Anticipated)Interventional1998-03-31Completed
A Randomized, Multicenter Clinical Trial to Assess the Efficacy and Safety of Clozapine vs Treatment as Usual for Treatment-resistant Psychosis in Adolescents and Young Adults With Intellectual Disability. [NCT04529226]Phase 2114 participants (Anticipated)Interventional2020-11-26Recruiting
Longitudinal Comparative Effectiveness of Bipolar Disorder Therapies [NCT02893371]1,037,352 participants (Actual)Observational2016-09-30Completed
Topical Haloperidol: Evidence of Absorption After Topical Administration [NCT01684969]Early Phase 10 participants (Actual)Interventional2012-03-31Withdrawn(stopped due to lack of accrual and funding is about to expire.)
Haloperidol vs Olanzapine for the Management of ICU Delirium: A Randomized Clinical Trial [NCT00833300]200 participants (Anticipated)Interventional2008-06-30Terminated
Intravenous Immunoglobulins as Effective Treatment in Sydenham's Chorea [NCT00615797]20 participants (Actual)Interventional2002-05-31Completed
Intramuscular Clozapine in the Management of Aggression in Schizophrenic Patients [NCT00189995]Phase 30 participants (Actual)InterventionalWithdrawn
Double-Blind Long-term Study Comparing the Efficacy and Safety of Olanzapine Versus Haloperidol in Patients With Schizophrenia Previously Stabilized With Conventional Antipsychotic Treatment [NCT00191555]Phase 4360 participants Interventional2003-08-31Completed
A Comparison of Midazolam or Haloperidol Premedication Versus Placebo for Reducing Ketamine Induced Agitation After Adult Procedural Sedation in the Emergency Department [NCT02909465]Phase 4185 participants (Actual)Interventional2016-07-31Completed
An Open-label, Randomized Trial of Intramuscular (IM) Olanzapine Versus Intramuscular Combination of Haloperidol and Lorazepam in the Treatment of Acute Agitation in Schizophrenia [NCT00797277]Phase 367 participants (Actual)Interventional2006-07-31Completed
Safety and Efficacy of Four Intramuscular Interventions for the Management of Acute Psychomotor Agitation [NCT01485692]120 participants (Actual)Interventional2009-02-28Completed
[NCT00000179]Phase 30 participants InterventionalCompleted
Rapid Tranquilization of Violent or Agitated People in Psychiatric Emergency Settings- A Pragmatic Randomized Controlled Trial of Intramuscular Olanzepine Vs. Intramuscular Haloperidol + Promethazine. [NCT00455234]Phase 3300 participants Interventional2005-09-30Completed
A Double-Blind Randomized Comparison of the Efficacy and Safety of Intramuscular Olanzapine and Intramuscular Haloperidol in Acutely Agitated Patients With Schizophrenia [NCT00485901]Phase 350 participants (Actual)Interventional2004-07-31Completed
Pharmacokinetics of Understudied Drugs Administered to Children Per Standard of Care [NCT01431326]3,520 participants (Actual)Observational2011-11-30Completed
Metabolic Profile and Anthropometric Changes in Schizophrenia [NCT00534183]2,006 participants (Actual)Interventional2006-06-30Completed
A Multicenter, Randomized, Double-Blind, Placebo Controlled Study of Aripiprazole Monotherapy in the Treatment of Acutely Manic Patients With Bipolar I Disorder [NCT00097266]Phase 3615 participants Interventional2004-12-31Completed
Randomised Double-blind Placebo-controlled Study of Post-operative Haloperidol Versus Placebo for Prevention of Post-operative Delirium After Acute Hip Surgery [NCT00250237]Phase 3220 participants (Actual)Interventional2005-11-30Completed
Modulation of Regional Brain Activation in Schizophrenic Patients by Pharmacological Therapy With Amisulpride, Olanzapine or Haloperidol. A Study With Functional Magnetic Resonance Imaging (fMRI) and Diffusion Tensor Imaging (DTI) [NCT00419653]Phase 419 participants (Actual)Interventional2003-01-31Terminated(stopped due to Recruitment issues)
A Randomized Prospective Pilot Study Of Haloperidol In Addition To Standard Sedation In Mechanically Ventilated Patients With Delirium [NCT00429676]Phase 220 participants (Anticipated)Interventional2005-12-31Completed
One Year Maintenance Treatment With Low Dose Haloperidol vs. Risperidone in First-Episode Schizophrenia [NCT00159081]Phase 4159 participants (Actual)Interventional2000-11-30Completed
A Randomised Open Label Pilot Study of the Efficacy of Dexmedetomidine and Haloperidol in Ventilated Patients With ICU-associated Agitation and Delirium [NCT00505804]Phase 220 participants (Actual)Interventional2005-01-31Completed
Clozapine or Haloperidol in First Episode Schizophrenia [NCT00169091]Phase 432 participants (Actual)Interventional1996-03-31Terminated
Early Pharmacological Intervention to Prevent Delirium: Haloperidol Prophylaxis in Older Emergency Department Patients [NCT01530308]Phase 4242 participants (Actual)Interventional2012-11-30Completed
Early Recognition and Optimal Treatment of Delirium in Patients With Advanced Cancer [NCT01539733]101 participants (Actual)Interventional2010-03-31Completed
5HT3 Antagonism and Auditory Gating in Schizophrenia [NCT00018850]0 participants Interventional1998-06-30Completed
Predicting the Optimal Pharmacotherapy for Outpatients With Schizophrenia [NCT00018642]0 participants Interventional1997-04-30Completed
A Comparison of Two Different Treatments for Major Depression With Psychotic Features: Ziprasidone vs. Combined Sertraline and Haloperidol [NCT00340379]Phase 2/Phase 372 participants (Actual)Interventional2003-04-30Completed
Prospective Observational Investigation of Olanzapine Versus Haloperidol Versus Ziprasidone Versus Midazolam for the Treatment of Acute Undifferentiated Agitation in the Emergency Department [NCT03211897]737 participants (Actual)Observational2017-06-15Completed
Haloperidol and/or Chlorpromazine for Refractory Agitated Delirium in the Palliative Care Unit [NCT03021486]Phase 2/Phase 370 participants (Actual)Interventional2017-06-05Active, not recruiting
Re-hospital Agitation and Sedation Trial: A Randomized Controlled Trial of Haloperidol Versus Midazolam for the Sedation of the Agitated Patient [NCT01501123]10 participants (Actual)Interventional2011-11-30Completed
Oro-dispersible Olanzapine (Wafer) Versus Conventional Oral Haloperidol or Diazepam Tablets for the Management of Acute Agitation in the Accident and Emergency Department - a Multicentre Randomised Clinical Trial [NCT03246620]Phase 412 participants (Actual)Interventional2017-09-01Terminated(stopped due to The study was terminated prematurely due to difficulties in patient recruitment and associated potential for selection bias.)
Haloperidol vs. Valproate in the Management of Agitated Patients Presenting to the Emergency Department: A Randomized Clinical Trial [NCT01750541]Phase 356 participants (Actual)Interventional2012-12-31Completed
Randomized Multicentric Open-label Phase III Clinical Trial to Evaluate the Efficacy of Continual Treatment Versus Discontinuation Based in the Presence of Prodromes in a First Episode of Non-affective Psychosis. [NCT01765829]Phase 3104 participants (Anticipated)Interventional2012-11-30Recruiting
Prophylactic Haloperidol Use for Delirium in ICU Patients; a Randomized Placebo-controlled Double-blind Multicentre Trial [NCT01785290]Phase 41,800 participants (Actual)Interventional2013-06-30Completed
Randomized Controlled Trial Comparing Haloperidol, Quetiapine and Placebo in the Pharmacological Treatment of Delirium : The Haloquet Trial [NCT01811459]Phase 3107 participants (Actual)Interventional2013-02-28Completed
Preventing Post-Operative Delirium in Pneumonectomy, Esophagectomy and Thoracotomy Patients [NCT02213900]Phase 4135 participants (Actual)Interventional2013-09-30Completed
Correlation Between Cognitive Function and Relapse of Schizophrenia Regarding Dose Reduction in Patients Undergoing High-dose Antipsychotic Therapy [NCT03019887]139 participants (Actual)Interventional2011-04-30Completed
Valproic Acid for Treatment of Hyperactive or Mixed Delirium in ICU [NCT02343575]Phase 43 participants (Actual)Interventional2015-01-31Terminated(stopped due to We did not recruit the research assistant and terminated the study)
Open-label Randomized Controlled Trial of Oral Transmucosal Haloperidol and Olanzapine in the Treatment of Terminal Delirium [NCT04750395]Phase 280 participants (Anticipated)Interventional2021-09-01Recruiting
Managing Agitated Delirium With Neuroleptics and Anti-Epileptics as a Neuroleptic Sparing Strategy [NCT05431595]Phase 2/Phase 3150 participants (Anticipated)Interventional2022-07-19Enrolling by invitation
A Multicenter, Randomized, Double-Blind, Flexible-Dose, Long-Term Extension Trial of the Safety and Maintenance of Effect of Asenapine Using Haloperidol Positive Control in Subjects Who Complete Protocol 041023 [NCT00156104] [NCT00156065]Phase 3187 participants (Actual)Interventional2005-09-30Completed
"Absorption of ABH Gel (Ativan®, Lorazepam; Benadryl®, Diphenhydramine; and Haldol®, Haloperidol Gel) From the Skin of Normal Volunteers" [NCT01204255]11 participants (Actual)Interventional2010-11-15Completed
Phase 4 Study of Optimal Dose of Haloperidol [NCT01639599]150 participants (Actual)Interventional2012-03-31Completed
ORIC-I: Optimizing Recovery From Intensive Care: Mechanical Ventilation and Delirium [NCT00300391]Phase 340 participants (Actual)Interventional2006-03-31Terminated(stopped due to Insufficient recruitment to meet aims.)
Phase 2 Study of the Antipsychotic Effects of Sorghum Bicolor (JOBELYN) in the Treatment of Schizophrenia. [NCT02240173]Phase 1/Phase 2100 participants (Anticipated)Interventional2017-06-30Not yet recruiting
A Prospective Trial of Customized Adherence Enhancement Plus Long-acting Injectable Antipsychotic (CAE-L) in Individuals With Schizophrenia or Schizoaffective Disorder at Risk for Treatment Non-adherence and for Homelessness [NCT01152697]30 participants (Actual)Interventional2010-06-30Completed
Agents Intervening Against Delirium in Intensive Care Unit (AID-ICU) A Randomized, Blinded, Placebo-controlled Trial [NCT03392376]Phase 41,000 participants (Anticipated)Interventional2018-06-13Active, not recruiting
Comparative Effects of a D2 and Mixed D1-D2 Dopamine Antagonist on Gambling and Amphetamine Reinforcement in Pathological Gamblers and Healthy Controls [NCT02203786]Phase 260 participants (Actual)Interventional2009-09-30Completed
A Preliminary Double-Blind Randomized Controlled Trial of Haloperidol and Lorazepam for Delirium in Patients With Advanced Cancer Admitted to a Palliative Care Unit [NCT01949662]Phase 293 participants (Actual)Interventional2014-01-31Active, not recruiting
Real-time Decision Support for Postoperative Nausea and Vomiting (PONV) Prophylaxis [NCT02625181]27,034 participants (Actual)Interventional2016-07-31Completed
Reducing the Burden of Chronic Psychotic Disorders in Tanzania [NCT04327843]Phase 322 participants (Actual)Interventional2019-11-05Completed
Study of add-on Ramelteon Therapy on Sleep and Circadian Rhythm Disruption in Patients With Schizophrenia [NCT03075657]Phase 4120 participants (Actual)Interventional2017-05-01Completed
Baden PRIDe Trial - Baden Prevention and Reduction of Incidence of Postoperative Delirium Trial [NCT02433041]Phase 4200 participants (Actual)Interventional2013-07-31Completed
Pharmacovigilance in Gerontopsychiatric Patients [NCT02374567]Phase 3407 participants (Actual)Interventional2015-01-31Terminated
Haloperidol Compared to Dexamethasone in Lowering Postoperative Nausea and Vomiting and Pain in Adult After Laparoscopy [NCT05246631]Phase 480 participants (Actual)Interventional2020-01-01Completed
The Impact of Genetic Variation In Nicotinic Cholinergic Receptors on Functional Brain Networks Underlying Addiction Susceptibility [NCT01924468]Phase 176 participants (Actual)Interventional2013-08-14Completed
A 6-Week, Double-Blind, Randomized, Fixed-Dose, Parallel-Group Study of the Efficacy and Safety of Three Dose Levels of SM-13496 Compared to Placebo and Haloperidol in Patients With Schizophrenia Who Are Experiencing an Acute Exacerbation of Symptoms [NCT00044044]Phase 2356 participants (Actual)Interventional2002-07-31Completed
Quetiapine Versus Haloperidol in the Management of Hyperactive Delirium [NCT05690698]Phase 3100 participants (Actual)Interventional2023-04-09Completed
A Comparison Study of the Efficacy of a Rapid Titration of Quetiapine and Haloperidol in Agitated Adults in an Emergency Setting. [NCT00457366]Phase 472 participants (Actual)Interventional2006-05-31Completed
[NCT02493192]Phase 4110 participants (Anticipated)Interventional2015-07-31Not yet recruiting
Pharmacological Management of Delirium [NCT00842608]551 participants (Actual)Interventional2009-02-28Completed
Lurasidone Effects on Tissue Glutamate in Schizophrenia [NCT02199743]Phase 435 participants (Actual)Interventional2013-02-28Completed
Haloperidol vs Conventional Therapy for Gastroparesis [NCT02057549]Phase 436 participants (Actual)Interventional2012-11-30Terminated(stopped due to PI left institution)
Prospective Evaluation of Symptoms and Open Label Haloperidol in Cannabinoid Hyperemesis Syndrome (HALO) [NCT04176055]Phase 44 participants (Actual)Interventional2020-10-13Completed
A Concierge Model of Customized Adherence Enhancement Plus Long-acting Injectable Antipsychotic (CAL-C) in Individuals With Schizophrenia at Risk for Treatment Non-adherence and for Homelessness [NCT02085447]30 participants (Actual)Interventional2014-05-31Completed
Rapid Agitation Control With Ketamine in the Emergency Department (RACKED): a Randomized Controlled Trial [NCT03375671]Phase 281 participants (Actual)Interventional2018-05-29Completed
Delirium: Is Prophylactic Drug Therapy Useful in High Risk Patients as Defined by the Delirium Risk Prediction Model? [NCT03199950]Phase 41,366 participants (Anticipated)Interventional2017-06-23Recruiting
Efficacy of Haloperidol to Decrease the Burden of Delirium in Adult Critically Ill Patients (EuRIDICE): a Prospective Randomised Multi-center Double-blind Placebo-controlled Clinical Trial [NCT03628391]Phase 3142 participants (Actual)Interventional2018-02-22Terminated(stopped due to The study was stopped because of futility of being able to reach a one-day difference between treatment groups in the primary outcome of DCFD in the intended sample size.)
"A Randomized Trial of the Effectiveness of Topical ABH Gel (Ativan®, Lorazepam; Benadryl®, Diphenhydramine; and Haldol®, Haloperidol Gel) Versus Placebo in Patients With Nausea" [NCT01556932]22 participants (Actual)Interventional2012-03-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00044044 (4) [back to overview]Change From Baseline to the End of the Double-blind Treatment in the BPRS (Brief Psychiatric Rating Scale)Total Score
NCT00044044 (4) [back to overview]Change From Baseline to the End of the Double-blind Treatment in the CGI-S (Clinical Global Impression of Severity) Scores
NCT00044044 (4) [back to overview]Change From Baseline to the End of the Double-blind Treatment in the PANSS (Positive and Negative Syndrome Scale) Scores
NCT00044044 (4) [back to overview]Change From Baseline to the End of the Double-blind Treatment in the MADRS (Montgomery Asberg-Depression Scale) Scores
NCT00129220 (11) [back to overview]Percentage of Participants Who Switched to Syndromic Depression
NCT00129220 (11) [back to overview]Remission Rate of Manic Symptoms at 3 Weeks and 6 Weeks
NCT00129220 (11) [back to overview]Response Rate of Manic Symptoms at 3 Weeks and 6 Weeks
NCT00129220 (11) [back to overview]Maximum Change From Baseline During 6-Week Period in Drug-Induced Extrapyramidal Symptoms Scale (DIEPSS) Total Score
NCT00129220 (11) [back to overview]Remission Rate of Bipolar Disorder (Olanzapine Versus Haloperidol)
NCT00129220 (11) [back to overview]Change From Baseline to 6 Week Endpoint in Young Mania Rating Scale (YMRS)
NCT00129220 (11) [back to overview]Change From Baseline to 3 Week Endpoint in Young Mania Rating Scale (YMRS) Total Score
NCT00129220 (11) [back to overview]Change From Baseline to 6 Week Endpoint in Clinical Global Impressions - Bipolar Version (CGI-BP), Overall Severity of Illness
NCT00129220 (11) [back to overview]Percentage of Participants Who Switched to Symptomatic Depression
NCT00129220 (11) [back to overview]Change From Baseline to 3 Week and 6 Week Endpoints in the Positive Subscore of Positive and Negative Syndrome Scale (PANSS)
NCT00129220 (11) [back to overview]Change From Baseline to 3 Week and 6 Week Endpoints in Clinical Global Impression - Bipolar Version (CGI-BP) Mania Subscale
NCT00156065 (2) [back to overview]Loss of Effect Over Time
NCT00156065 (2) [back to overview]Median Survival Time of Effect
NCT00300391 (4) [back to overview]ICU Length of Stay
NCT00300391 (4) [back to overview]90-day All-cause Mortality
NCT00300391 (4) [back to overview]28-day All-cause Mortality
NCT00300391 (4) [back to overview]Duration of Mechanical Ventilation
NCT00340379 (3) [back to overview]21 Item Hamilton Depression Rating Scale
NCT00340379 (3) [back to overview]Clinical Global Impression Improvement Scale
NCT00340379 (3) [back to overview]Brief Psychiatric Rating Scale at 12 Weeks
NCT00457366 (1) [back to overview]Change in the PANSS-EC Score Among Participants From Baseline to 2 Hours After Administration of the Medication.
NCT00642369 (2) [back to overview]Percentage of Rapid Eye Movement Sleep
NCT00642369 (2) [back to overview]Percentage of Slow Wave Sleep
NCT00693472 (6) [back to overview]Part 1: Mean Global Clinical Impression at Day 14
NCT00693472 (6) [back to overview]Part 1: Mean Positive and Negative Symptom Scale for Schizophrenia (PANSS) Total Score at Day 14
NCT00693472 (6) [back to overview]Part 1: Number of Participants With Akathisia
NCT00693472 (6) [back to overview]Part 2: Mean GCI at Day 14
NCT00693472 (6) [back to overview]Part 2: Number of Participants Who Were Treatment Failures
NCT00693472 (6) [back to overview]Part 2: PANSS Total Score at Day 14
NCT00723606 (6) [back to overview]Change From Baseline in Brief Psychiatric Rating Scale (BPRS) Total Scores at 72 Hours
NCT00723606 (6) [back to overview]Change From Baseline in BPRS Agitation Subscale Score at 72 Hours
NCT00723606 (6) [back to overview]Change From Baseline in Behavioral Activity Rating Scale (BARS) at 72 Hours
NCT00723606 (6) [back to overview]Change From Baseline in Clinical Global Impressions Severity (CGI-S) Score at 72 Hours
NCT00723606 (6) [back to overview]Clinical Global Impression-Improvement (CGI-I) Score at 72 Hours
NCT00723606 (6) [back to overview]BPRS Agitation Subscale Response at 72 Hours
NCT00797277 (2) [back to overview]The Change of the Positive and Negative Symptom Scale Excited Component (PANSS-EC) Score From Baseline to 120 Minutes After First Injection
NCT00797277 (2) [back to overview]Change of the Agitation-Calmness Evaluation Scale (ACES) Score From Baseline to 120 Minutes After 1st Injection
NCT00842608 (3) [back to overview]Mortality
NCT00842608 (3) [back to overview]Hospital Length of Stay Post Randomization
NCT00842608 (3) [back to overview]Days Free of Delirium and Coma
NCT01136772 (2) [back to overview]Efficacy Failure
NCT01136772 (2) [back to overview]Changes in Psychiatric Symptoms
NCT01152697 (20) [back to overview]Global Psychopathology as Measured by the Clinical Global Impressions (CGI) at 12 Months
NCT01152697 (20) [back to overview]Treatment Satisfaction as Measured by the Participant Acceptability and Satisfaction Questionnaire at 25 Weeks
NCT01152697 (20) [back to overview]Treatment Satisfaction as Measured by the Participant Acceptability and Satisfaction Questionnaire at 12 Months
NCT01152697 (20) [back to overview]Treatment Adherence Behavior Score as Measured by the Morisky Medication Rating Scale at 12 Months
NCT01152697 (20) [back to overview]Change From Baseline in Adherence Attitude Score as Measured by the Attitude Toward Medication Questionnaire (AMQ) at 25 Weeks
NCT01152697 (20) [back to overview]Frequency of Health Resource Use in the Past 3 Months as Measured at 25 Weeks
NCT01152697 (20) [back to overview]Days Homeless Out of the Previous 6 Months as Measured at 12 Months
NCT01152697 (20) [back to overview]Adherence Attitude Score as Measured by the Drug Attitude Inventory (DAI) at 12 Months
NCT01152697 (20) [back to overview]Adherence Attitude Score as Measured by the Attitude Toward Medication Questionnaire (AMQ) at 12 Months
NCT01152697 (20) [back to overview]Treatment Adherence Score as Measured at 12 Months
NCT01152697 (20) [back to overview]Frequency of Health Resource Use Throughout Months 10, 11, and 12
NCT01152697 (20) [back to overview]Change in Social and Occupational Functioning Scale (SOFAS) as Measured at 25 Weeks
NCT01152697 (20) [back to overview]Change in Social and Occupational Functioning Scale (SOFAS) as Measured at 12 Months
NCT01152697 (20) [back to overview]Change in Serious Mental Illness Severity Score as Measured by the Brief Psychiatric Rating Scale (BPRS) at 25 Weeks
NCT01152697 (20) [back to overview]Change in Schizophrenia and Schizoaffective Disorder Symptom Severity Scale as Measured by the Positive and Negative Syndrome Scale (PANSS) at 25 Weeks
NCT01152697 (20) [back to overview]Change in Global Psychopathology as Measured by the Clinical Global Impressions (CGI) at 25 Weeks
NCT01152697 (20) [back to overview]Change From Baseline in Treatment Adherence Score as Measured at 25 Weeks
NCT01152697 (20) [back to overview]Change From Baseline in Treatment Adherence Behavior Score as Measured by the Morisky Medication Rating Scale at 25 Weeks
NCT01152697 (20) [back to overview]Change From Baseline in Days Homeless Out of the Previous 6 Months as Measured at 25 Weeks
NCT01152697 (20) [back to overview]Change From Baseline in Adherence Attitude Score as Measured by the Drug Attitude Inventory (DAI) at 25 Weeks
NCT01204255 (2) [back to overview]Side Effects
NCT01204255 (2) [back to overview]Lorazepam, Diphenyhydramine, Haloperidol Absorption
NCT01211522 (10) [back to overview]Delirium Duration
NCT01211522 (10) [back to overview]Delirium/Coma-free Days (DCFDs)
NCT01211522 (10) [back to overview]Number of Participants With Extrapyramidal Symptoms
NCT01211522 (10) [back to overview]Number of Participants With Neuroleptic Malignant Syndrome
NCT01211522 (10) [back to overview]Number of Participants With Torsades de Pointes
NCT01211522 (10) [back to overview]Time to Final ICU Discharge
NCT01211522 (10) [back to overview]Time to Hospital Discharge
NCT01211522 (10) [back to overview]Time to ICU Readmission
NCT01211522 (10) [back to overview]Time to Liberation From Mechanical Ventilation
NCT01211522 (10) [back to overview]Mortality
NCT01298193 (9) [back to overview]Impact of Chemotherapy-Induced Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 1
NCT01298193 (9) [back to overview]Impact of Chemotherapy-Induced Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 2
NCT01298193 (9) [back to overview]Total Impact of Chemotherapy-Induced Nausea and Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 1
NCT01298193 (9) [back to overview]Number of Participants With Complete Response (CR)
NCT01298193 (9) [back to overview]Number of Participants With Complete Response (CR) in Cycle 2 for Patient Without Complete Response in Cycle 1
NCT01298193 (9) [back to overview]Number of Participants With Treatment Related Adverse Events (AE) at Cycle 2
NCT01298193 (9) [back to overview]Impact of Chemotherapy-Induced Nausea on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 1
NCT01298193 (9) [back to overview]Impact of Chemotherapy-Induced Nausea on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 2
NCT01298193 (9) [back to overview]Total Impact of Chemotherapy-Induced Nausea and Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 2
NCT01556932 (1) [back to overview]The Change in Numeric Rating Scale in Self-reported Nausea From Baseline Minus 60 Minutes of Treatment.
NCT01639599 (4) [back to overview]Incidence of Extrapyramidal Symptoms
NCT01639599 (4) [back to overview]Incidence of Postoperative Nausea and Vomiting
NCT01639599 (4) [back to overview]Sedation Change in Recovery Room
NCT01639599 (4) [back to overview]Incidence of Cardiac Arrhythmia
NCT01949662 (4) [back to overview]Absolute Richmond Agitation-Sedation Scale Score at 8 Hour, Points
NCT01949662 (4) [back to overview]Change in Richmond Agitation-Sedation Scale Score (Baseline to 8 hr), Points
NCT01949662 (4) [back to overview]Change in Richmond Agitation-Sedation Scale Score From Baseline to 30 Min
NCT01949662 (4) [back to overview]Number of Participants With Richmond Agitation-Sedation Scale Score >=1 Within 8 hr
NCT02057549 (8) [back to overview]Pain Relief as Indicated by Number of Participants Not Requesting Additional Pain Medication
NCT02057549 (8) [back to overview]Emergency Department Length of Stay (EDLOS)
NCT02057549 (8) [back to overview]Pain Score as Measured by a Visual Analogue Scale (VAS)
NCT02057549 (8) [back to overview]Nausea Score as Measured by a Visual Analogue Scale (VAS)
NCT02057549 (8) [back to overview]Number of Participants Admitted to the Hospital After Emergency Department Visit
NCT02057549 (8) [back to overview]Nausea Score as Measured by a Visual Analogue Scale (VAS)
NCT02057549 (8) [back to overview]Nausea Relief as Indicated by Number of Participants Not Requesting Additional Antiemetic Medication
NCT02057549 (8) [back to overview]Pain Score as Measured by a Visual Analogue Scale (VAS)
NCT02085447 (22) [back to overview]Change in ASSIST GRS (Alcohol, Smoking and Substance Involvement Screening Test ) From Screen to Week 25
NCT02085447 (22) [back to overview]Change in PANSS (Positive and Negative Syndrome Scale; General Psychopathology) From Screen to Week 25
NCT02085447 (22) [back to overview]Percentage Change of Days of Sub-optimal Housing in the Past Six Months; Change From Screen to Week 25
NCT02085447 (22) [back to overview]Long-acting Injection (LAI) Adherence
NCT02085447 (22) [back to overview]Change in AMSQ (Attitudes Toward Mood Stabilizers Questionnaire) From Screen to Week 25
NCT02085447 (22) [back to overview]Change in AIMS (Abnormal Involuntary Movement Scale) From Baseline to Week 25
NCT02085447 (22) [back to overview]Change in PANSS (Positive and Negative Syndrome Scale; Composite Scale) From Screen to Week 25
NCT02085447 (22) [back to overview]Change in Hospitalizations (Psychiatric) in the Past 6 Months From Screen and Week 25
NCT02085447 (22) [back to overview]Change in Hospitalizations (Medical) in the Past 6 Months From Screen and Week 25
NCT02085447 (22) [back to overview]Change in ESRS-A (Extrapyramidal Symptoms Scale-Abbreviated; Akathisia)
NCT02085447 (22) [back to overview]Change in Tablets Routine Questionnaire (TRQ) (Past Month) From Screen to Week 25
NCT02085447 (22) [back to overview]Change in ESRS-A (Extrapyramidal Symptoms Scale-Abbreviated; Dystonia) From Screen to Week 25
NCT02085447 (22) [back to overview]Change in ESRS-A (Extrapyramidal Symptoms Scale-Abbreviated; Dyskinesia) From Screen to Week 25
NCT02085447 (22) [back to overview]Change in DAI (Drug Attitudes Index) From Screen to Week 25
NCT02085447 (22) [back to overview]Change in CGI (Clinical Global Impression) From Screen to Week 25
NCT02085447 (22) [back to overview]Change in BARS (Barnes Akathisia Rating Scale) From Screen to Week 25
NCT02085447 (22) [back to overview]Change in Tablets Routine Questionnaire (TRQ, Past Week) From Screen to Week 25 Visit
NCT02085447 (22) [back to overview]Change in SOFAS (Social and Occupational Functioning Assessment Scale) From Screen to Week 25
NCT02085447 (22) [back to overview]Change in SAS (Simpson Angus Scale) From Screen to Week 25
NCT02085447 (22) [back to overview]Change in PANSS (Positive and Negative Syndrome Scale; Positive Symptoms Scale) From Screen to Week 25
NCT02085447 (22) [back to overview]Change in PANSS (Positive and Negative Syndrome Scale; Negative Symptoms Scale) From Screen to Week 25
NCT02085447 (22) [back to overview]Change in ESRS-A (Extrapyramidal Symptoms Scale-Abbreviated; Parkinsonism) From Screen to Week 25
NCT02199743 (2) [back to overview]Brief Assessments of Cognition in Schizophrenia Scores (BACS)
NCT02199743 (2) [back to overview]Cerebral Glutamate Levels
NCT02203786 (6) [back to overview]Betting Behaviour in Laboratory-based Slot Machine Game
NCT02203786 (6) [back to overview]Subjective Reinforcement Self-report Scales
NCT02203786 (6) [back to overview]Speed of Play on Slot Machine Game
NCT02203786 (6) [back to overview]Diastolic Blood Pressure (DBP)
NCT02203786 (6) [back to overview]Cognitive Task Performance
NCT02203786 (6) [back to overview]Winnings on Slot Machine Upon Completion of Game
NCT02213900 (4) [back to overview]Efficacy of Low-dose Haloperidol in Reducing Days With Delirium
NCT02213900 (4) [back to overview]Efficacy of Low-dose Haloperidol in Reducing Delirium Incidence
NCT02213900 (4) [back to overview]Efficacy of Low-dose Haloperidol in Reducing Cognitive Impairment at Post-operative Follow-up
NCT02213900 (4) [back to overview]Efficacy of Low-dose Haloperidol in Reducing ICU and Hospital Length of Stay
NCT02343575 (5) [back to overview]Intensity of Delirium as Measured by the Intensive Care Delirium Screening Checklist (ICDSC) Delirium Severity Scale
NCT02343575 (5) [back to overview]Length of Hospital Stay
NCT02343575 (5) [back to overview]Time to Delirium Resolution
NCT02343575 (5) [back to overview]Use of as Needed Anti-psychotic Agent
NCT02343575 (5) [back to overview]Side Effects From Medications
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Speed of Processing Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Adjusted Intracortical Myelin (ICM) Fraction Score as Measured by Inversion Recovery (IR) and Spin Echo Magnetic Resonance Imaging (MRI)
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Attention/Vigilance Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Clinical Global Impression Severity (CGI-S) Score
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Cognition as Measured by the MATRICS Consensus Cognitive Battery (MCCB) Composite Score
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Functioning as Measured by the Personal and Social Performance (PSP) Total Score
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Medication Satisfaction Questionnaire (MSQ) Total Score
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Reasoning and Problem Solving: MCCB Domain
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Social Cognition Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Speed of Processing Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Verbal Learning Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Visual Learning Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 3 (Disease Modification): Change From Baseline in Adjusted Intracortical Myelin Fraction Score as Measured by Inversion Recovery (IR) and Spin Echo Magnetic Resonance Imaging (SE MRI)
NCT02431702 (31) [back to overview]Part 3 (Disease Modification): Change From Baseline in Cognition as Measured by the MATRICS Consensus Cognitive Battery (MCCB) Composite Score
NCT02431702 (31) [back to overview]Part 3 (Disease Modification): Personal and Social Performance (PSP) Total Observed Score
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Adjusted Intracortical Myelin Fraction Score as Measured by Inversion Recovery (IR) and Spin Echo Magnetic Resonance Imaging (MRI)
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Attention/Vigilance Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Clinical Global Impression Severity (CGI-S) Score
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Number of Participants With Change From Baseline in Severity of Psychotic Symptoms, as Measured by Clinician-Rated Dimensions of Psychosis Symptom Severity Scale (CRDPSS)
NCT02431702 (31) [back to overview]Part 3 (EDP): Number of Participants With Change From Baseline in Severity of Psychotic Symptoms, as Measured by CRDPSS
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Working Memory Score: MCCB Domain
NCT02431702 (31) [back to overview]Part-2 (Disease Progression): Time to First Treatment Failure
NCT02431702 (31) [back to overview]Part 3 (Extended Disease Progression [EDP]): Change From Baseline in Cognition as Measured by the MATRICS Consensus Cognitive Battery (MCCB) Composite Score
NCT02431702 (31) [back to overview]Part 3 (EDP): Time to First Treatment Failure
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Working Memory Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Visual Learning Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Verbal Learning Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Social Cognition Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Reasoning and Problem Solving: MCCB Domain
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Medication Satisfaction Questionnaire (MSQ) Score
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Functioning as Measured by the Personal and Social Performance (PSP) Total Score
NCT02625181 (4) [back to overview]Adherence to PONV Guidelines
NCT02625181 (4) [back to overview]PONV Incidence: Number of Participants With Postoperative Nausea and Vomiting
NCT02625181 (4) [back to overview]The Number of Prophylactic Interventions for PONV
NCT02625181 (4) [back to overview]Time to Discharge From the Postanesthesia Care Unit (PACU)
NCT02972502 (1) [back to overview]Change in Pain Score According to the Numeric Pain Intensity Scale
NCT03019887 (1) [back to overview]Number of Participants With Relapse
NCT03021486 (11) [back to overview]Perceived Comfort Level as Assessed by Caregiver
NCT03021486 (11) [back to overview]Memorial Delirium Assessment Scale (MDAS)
NCT03021486 (11) [back to overview]Change in Richmond Agitation Sedation Score (RASS) (0-24h)
NCT03021486 (11) [back to overview]Percentage of Participants With RASS Score -2 to 0
NCT03021486 (11) [back to overview]Change in Delirium Experience Questionnaire
NCT03021486 (11) [back to overview]Edmonton Expression Assessment System, ESAS
NCT03021486 (11) [back to overview]Change in RASS Score (0-30 Minutes)
NCT03021486 (11) [back to overview]Number of Participants With RASS Score of >=1
NCT03021486 (11) [back to overview]Perceived Comfort Level as Assessed by Nurse
NCT03021486 (11) [back to overview]Udvalg for Kliniske Undersogelser, UKU
NCT03021486 (11) [back to overview]Pattern of Medication Use
NCT03489551 (1) [back to overview]Side Effects and Tolerability of Haldol in Patients With Undergoing Hematopoietic Stem Cell Transplant
NCT03639558 (4) [back to overview]Time Patient Was Placed in Straitjacket/Restraint Post Intervention Treatment
NCT03639558 (4) [back to overview]Time Taken for Patient to Fall Asleep Post Intervention
NCT03639558 (4) [back to overview]Time Noted Where Important Adverse Effects Occurred Post Intervention
NCT03639558 (4) [back to overview]Number of Participants According to the Time Taken for Aggressive Behaviour to Change to Calm and Tranquil
NCT04327843 (11) [back to overview]ESRS-A Akathisia
NCT04327843 (11) [back to overview]ESRS-A Dyskinesia
NCT04327843 (11) [back to overview]ESRS-A Dystonia
NCT04327843 (11) [back to overview]ESRS-A Parkinsonism
NCT04327843 (11) [back to overview]Social and Occupational Functioning Scale (SOFAS)
NCT04327843 (11) [back to overview]Tablets Routine Questionnaire (TRQ)
NCT04327843 (11) [back to overview]Brief Psychiatric Rating Scale (BPRS)
NCT04327843 (11) [back to overview]Long-Acting Injectable Adherence (LAI Adherence): Count of Participants Who Received All LAI Injections:
NCT04327843 (11) [back to overview]Body Mass Index
NCT04327843 (11) [back to overview]Clinical Global Impressions (CGI)
NCT04327843 (11) [back to overview]Drug Attitude Inventory (DAI)
NCT04411940 (6) [back to overview]Apparent Terminal Elimination Half-Life (t½)
NCT04411940 (6) [back to overview]Area Under the Curve (0-t) (AUC(0-t))
NCT04411940 (6) [back to overview]Area Under the Curve(0-∞) (AUC(0-∞))
NCT04411940 (6) [back to overview]Terminal Elimination Rate Constant (λz)
NCT04411940 (6) [back to overview]Time to Maximum Concentration (Tmax)
NCT04411940 (6) [back to overview]Concentration Maximum (Cmax)
NCT04411953 (6) [back to overview]Concentration Maximum (Cmax)
NCT04411953 (6) [back to overview]Terminal Elimination Half-life (t½)
NCT04411953 (6) [back to overview]Time to Maximum Concentration (Tmax)
NCT04411953 (6) [back to overview]Terminal Elimination Rate Constant (λz)
NCT04411953 (6) [back to overview]Area Under the Curve(0-∞) (AUC(0-∞))
NCT04411953 (6) [back to overview]Area Under the Curve (0-t) (AUC(0-t))
NCT04715230 (12) [back to overview]Length of Patient Stay in the ED
NCT04715230 (12) [back to overview]Time Course and Degree of Normalization of Temperature
NCT04715230 (12) [back to overview]Number of Participants at Certain Degrees of Normalization of Blood Pressure Over Time
NCT04715230 (12) [back to overview]Time Course and Degree of Normalization of Agitation
NCT04715230 (12) [back to overview]Time Course and Degree of Normalization of Agitation
NCT04715230 (12) [back to overview]Time Course and Degree of Normalization of Agitation
NCT04715230 (12) [back to overview]Number of Patients With Treatment-related AEs as Measured by Physical Examinations
NCT04715230 (12) [back to overview]Number of Patients With Treatment-related AEs as Measured by Electrocardiogram
NCT04715230 (12) [back to overview]Number of Patients With Treatment-related AEs as Measured by Clinical Laboratory Testing
NCT04715230 (12) [back to overview]Number of Patients With Treatment-related Adverse Events (AEs) as Measured by Vital Signs
NCT04715230 (12) [back to overview]Number of Participants at Certain Degrees of Normalization of Heart Rate Over Time
NCT04715230 (12) [back to overview]Time Course and Degree of Normalization of Temperature

Change From Baseline to the End of the Double-blind Treatment in the BPRS (Brief Psychiatric Rating Scale)Total Score

"The BPRS consists of 18 ordered categorical items (from not present to extremely severe, on a 1- to 7-point scale), each developed to assess patient symptomatology in a relatively discrete symptom area. The BPRS will be extracted from the PANSS by adding the scores of the 18 items (P2 to P7, N1, N2, and G1 to G10) of the PANSS and will not be assessed separately. The minimum score on the BPRS is 18 and the maximum is 126. The higher number indicates a worsening of schizophrenia." (NCT00044044)
Timeframe: Baseline and 6 weeks

Interventionunits on a scale (Least Squares Mean)
20 mg-5.0
40 mg-5.2
80 mg-8.0
10 mg Haloperidol-9.8
Placebo-7.9

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Change From Baseline to the End of the Double-blind Treatment in the CGI-S (Clinical Global Impression of Severity) Scores

The CGI Severity (CGI-S) assesses the severity of illness of the patient relative to the particular population on a 7-point scale ranging from 1 (normal, not at all ill) to 7 (among the most extremely ill patients). (NCT00044044)
Timeframe: Baseline and 6 weeks

Interventionunits on a scale (Least Squares Mean)
20 mg-0.5
40 mg-0.4
80 mg-0.8
10 mg Haloperidol-0.8
Placebo-0.7

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Change From Baseline to the End of the Double-blind Treatment in the PANSS (Positive and Negative Syndrome Scale) Scores

The PANSS Positive and Negative Syndrome Scale)is a 30-item scale that evaluates positive, negative, and other symptoms in patients with schizophrenia. Each item is rated on a 7-point scale that ranges from 1 (absent) to 7 (extreme). Scores range from 30-210 with higher scores representing a worsening of schizophrenia. (NCT00044044)
Timeframe: Baseline and 6 weeks

Interventionunits on a scale (Least Squares Mean)
20 mg-7.1
40 mg-7.2
80 mg-13.6
10 mg Haloperidol-16.0
Placebo-12.3

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Change From Baseline to the End of the Double-blind Treatment in the MADRS (Montgomery Asberg-Depression Scale) Scores

The MADRS is a 10-item rating scale that assesses apparent and reported sadness, lassitude, pessimism, inner tension, suicidality, reduced sleep or appetite, difficulty in concentration, and lack of interest. Each item is scored on a 7-point scale with a score of 0 reflecting no symptoms and a score of 6 reflecting symptoms of maximum severity. (NCT00044044)
Timeframe: Baseline and 6 weeks

Interventionunits on scale (Least Squares Mean)
20 mg-1.3
40 mg-1.1
80 mg-2.5
10 mg Haloperidol-2.7
Placebo-1.9

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Percentage of Participants Who Switched to Syndromic Depression

Switch to syndromic depression was operationally defined by meeting both of the following criteria: At baseline, the symptoms did not meet the criteria for a mixed episode based on the Diagnostic and Statistical Manual of Mental Disorders Fourth Edition, Text Revision (DSM-IV-TR). The critiera were met for a Major Depressive Episode (MDE), at any point after randomization, based on DSM-IV-TR. Rather than the 2-week period required for an MDE in the DSM-IV-TR, the patient had to meet the criteria of an MDE for at least 7 consecutive days (during Weeks 1 through 6). (NCT00129220)
Timeframe: 3 weeks, 6 weeks

,,
Interventionpercentage of participants (Number)
3-Week Syndromic Depression Rate6-Week Syndromic Depression Rate
Haloperidol5.35.3
Olanzapine0.01.1
Placebo0.00.0

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Remission Rate of Manic Symptoms at 3 Weeks and 6 Weeks

Participants who had a YMRS total score of 12 or less were considered to be in remission of manic symptoms. YMRS is an 11-item scale that measures severity of manic episodes; total score ranges from 0 (normal) to 60 (severe). Remission Rate (percent) = number of patients meeting remission criteria divided by number of patients in treatment arm, multiplied by 100. (NCT00129220)
Timeframe: 3 weeks, 6 weeks

,,
Interventionpercentage of participants (Number)
3-Week Remission Rate6-Week Remission Rate
Haloperidol65.060.0
Olanzapine47.163.5
Placebo41.252.6

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Response Rate of Manic Symptoms at 3 Weeks and 6 Weeks

Participants who had 50 percent or more decrease from the baseline in YMRS total scores were defined as a responder. The YMRS is an 11-item scale that measures the severity of manic episodes. Four items are rated on a scale from 0 (symptom not present) to 8 (symptom extremely severe). The remaining items are rated on a scale from 0 (symptom not present) to 4 (symptom extremely severe). The YMRS total score ranges from 0 to 60. Response Rate (percent) = number of patients meeting response criterion for manic symptom divided by number of patients in treatment arm, multiplied by 100. (NCT00129220)
Timeframe: Baseline, 3 weeks, 6 weeks

,,
Interventionpercentage of participants (Number)
3 Week Response Rate6 Week Response Rate
Haloperidol65.065.0
Olanzapine51.067.3
Placebo44.355.7

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Maximum Change From Baseline During 6-Week Period in Drug-Induced Extrapyramidal Symptoms Scale (DIEPSS) Total Score

Drug Induced Extra-Pyramidal Symptoms Scale (DIEPSS) is a scale used to evaluate the severity of drug induced extra-pyramidal symptoms occurring during antipsychotic drug treatment. Scale consists of 8 individual symptom scales with scores ranging from 0 (none/normal) to 4 (severe). The total score is the sum of the 8 item scores, for a total range of 0 (normal) to 32 (severe). (NCT00129220)
Timeframe: Baseline to 6 weeks

,,
Interventionunits on a scale (Mean)
BaselineMaximum Change from Baseline
Haloperidol0.502.70
Olanzapine0.200.70
Placebo0.300.09

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Remission Rate of Bipolar Disorder (Olanzapine Versus Haloperidol)

Remission of bipolar disorder was defined as completing the 6-week period with meeting the criteria for Young Mania Rating Scale (YMRS) total score of 12 or less and 17-Item Hamilton Depression Rating Scale (HAMD-17) total scores of 7 or less at Week 6. YMRS is an 11-item scale measuring severity of manic episodes; total score ranges = 0 (normal) to 60 (severe). The 17-item HAMD measures depression severity; total score ranges = 0 (normal) to 52 (severe). Remission Rate (percent) = number of patients meeting remission criteria divided by number of patients in treatment arm, multiplied by 100. (NCT00129220)
Timeframe: 6 weeks

Interventionpercentage of participants (Number)
Olanzapine44.2
Haloperidol20.0

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Change From Baseline to 6 Week Endpoint in Young Mania Rating Scale (YMRS)

The YMRS is an 11-item scale that measures the severity of manic episodes. Four items are rated on a scale from 0 (symptom not present) to 8 (symptom extremely severe). The remaining items are rated on a scale from 0 (symptom not present) to 4 (symptom extremely severe). The YMRS total score ranges from 0 to 60. (NCT00129220)
Timeframe: Baseline, 6 weeks

Interventionunits on a scale (Mean)
Olanzapine-16.0
Haloperidol-14.7
Placebo-10.1

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Change From Baseline to 3 Week Endpoint in Young Mania Rating Scale (YMRS) Total Score

The YMRS is an 11-item scale that measures the severity of manic episodes. Four items are rated on a scale from 0 (symptom not present) to 8 (symptom extremely severe). The remaining items are rated on a scale from 0 (symptom not present) to 4 (symptom extremely severe). The YMRS total score ranges from 0 to 60. (NCT00129220)
Timeframe: Baseline, 3 weeks

Interventionunits on a scale (Mean)
Olanzapine-12.6
Haloperidol-14.3
Placebo-6.8

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Change From Baseline to 6 Week Endpoint in Clinical Global Impressions - Bipolar Version (CGI-BP), Overall Severity of Illness

A global rating scale for severity of patients adapted to bipolar disorder. Measures severity of the patient's overall severity of overall mood symptoms on a scale of 1 (normal, not at all ill) to 7 (among the most extremely ill patients). (NCT00129220)
Timeframe: Baseline, 6 weeks

Interventionunits on a scale (Mean)
Olanzapine-1.6
Haloperidol-1.3
Placebo-0.9

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Percentage of Participants Who Switched to Symptomatic Depression

Switch to symptomatic depression was defined as HAMD-17 total score ≥13 at any time in the participants with HAMD-17 total scores ≤7 at baseline. The 17-item HAMD measures depression severity. Each item was evaluated and scored using either a 5-point scale (e.g. absent, mild, moderate, severe, very severe) or a 3-point scale (e.g. absent, mild, marked). The total score of HAMD-17 may range from 0 (normal) to 52 (severe). (NCT00129220)
Timeframe: 3 weeks, 6 weeks

,,
Interventionpercentage of participants (Number)
3-Week Symptomatic Depression Rate6-Week Symptomatic Depression Rate
Haloperidol16.716.7
Olanzapine2.42.4
Placebo1.32.7

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Change From Baseline to 3 Week and 6 Week Endpoints in the Positive Subscore of Positive and Negative Syndrome Scale (PANSS)

Assesses positive symptoms associated with schizophrenia. 7 items make up the Positive scale (ex. delusions, conceptual disorganization, and hallucinatory behavior). Each item is rated on a scale from 1 (symptom not present) to 7 (symptoms extremely severe). Total Positive Subscale scores range from 7 to 49. For this study, the score was converted to 0 to 6 for each item range; hence, the total positive subscale score ranges from 0 to 42. (NCT00129220)
Timeframe: Baseline, 3 weeks, 6 weeks

,,
Interventionunits on a scale (Mean)
3-Week Change6-Week Change
Haloperidol-1.8-1.6
Olanzapine-1.8-2.2
Placebo-0.0-0.3

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Change From Baseline to 3 Week and 6 Week Endpoints in Clinical Global Impression - Bipolar Version (CGI-BP) Mania Subscale

A global rating scale for severity of patients adapted to bipolar disorder. Measures severity of the patient's overall severity of manic symptoms on a scale of 1 (normal, not at all ill) to 7 (among the most extremely ill patients). (NCT00129220)
Timeframe: Baseline, 3 weeks, 6 weeks

,,
Interventionunits on a scale (Mean)
3-Week Change6-Week Change
Haloperidol-1.7-1.9
Olanzapine-1.2-1.7
Placebo-0.6-1.0

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Loss of Effect Over Time

"Loss of effect in subjects who had >=30% decrease from baseline in Positive and Negative Syndrome Scale (PANSS) score at the end of the original trial (NCT00156104) preceding the long-term extension.~PANSS is a 30-item clinician-rated instrument for assessing symptoms of schizophrenia. Scores range from 30-210; higher scores indicate greater severity.~Loss of effect = increase in total PANSS >=30% from start of current study; subjective worsening of schizophrenia/request for dose increase; Clinical Global Impressions of Severity of Illness score >=6; discontinuation for lack of efficacy." (NCT00156065)
Timeframe: Throughout the 52 weeks of the trial.

,,
InterventionParticipants (Number)
<=Week 1>Week 1 to Week 2>Week 2 to Week 4>Week 4 to Week 8>Week 8 to Week 12>Week 12 to Week 16>Week 16 to Week 20>Week 20 to Week 24>Week 24 to Week 28>Week 28 to Week 32>Week 32 to Week 36>Week 36 to Week 40>Week 40 to Week 44>Week 44 to Week 48>Week 48 to Week 52
Asenapine/Asenapine15414311131300005
Haloperidol/Haloperidol643114100101002
Placebo/Asenapine731323000100002

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Median Survival Time of Effect

"Kaplan-Meier estimate of median time to loss of effect in subjects who had >=30% decrease from baseline in PANSS score at the end of the original trial (NCT00156104) preceding the long-term extension.~PANSS is a 30-item clinician-rated instrument for assessing symptoms of schizophrenia. Scores range from 30-210; higher scores indicate greater severity.~Loss of effect = increase in total PANSS >=30% from start of current study; subjective worsening of schizophrenia/request for dose increase; Clinical Global Impressions of Severity of Illness score >=6; discontinuation for lack of efficacy." (NCT00156065)
Timeframe: 52 Weeks

InterventionDays (Median)
Placebo/Asenapine57
Asenapine/Asenapine31
Haloperidol/Haloperidol85

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ICU Length of Stay

(NCT00300391)
Timeframe: Daily

Interventionday (Median)
Delirium9
Persistent Coma6
No Delirium7

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90-day All-cause Mortality

(NCT00300391)
Timeframe: 90 Days from enrollment in study

InterventionParticipants (Count of Participants)
Delirium4
Persistent Coma2
No Delirium1

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28-day All-cause Mortality

(NCT00300391)
Timeframe: Daily

InterventionParticipants (Count of Participants)
Delirium4
Persistent Coma2
No Delirium1

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Duration of Mechanical Ventilation

(NCT00300391)
Timeframe: daily

Interventionday (Median)
Delirium4.5
Persistent Coma6
No Delirium4

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21 Item Hamilton Depression Rating Scale

The scale rates 21 symptoms related to major depression. A total score of 0-7 is considered to be normal, scores of 20 or higher indicate moderately severe depression. Total scores range from a minimum of 0(not ill) to a maximum of 64 (severely ill). (NCT00340379)
Timeframe: 12 week

InterventionUnits on Hamilton Depression Scale (Mean)
Ziprasidone13.6
Sertraline/Haloperidol11.0

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Clinical Global Impression Improvement Scale

A 7 point scale that requires the clinician to assess how much the patient's illness has improved or worsened relative to a baseline state at the beginning of the intervention. and rated as: 1, very much improved; 2, much improved; 3, minimally improved; 4, no change; 5, minimally worse; 6, much worse; or 7, very much worse. Overall the scale goes from a minimum of 1(very much improved) to a maximum of 7(very much worse). (NCT00340379)
Timeframe: 12 weeks

Interventionunits on a Clinical Impressions Scale (Mean)
Ziprasidone3.1
Sertraline/Haloperidol2.5

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Brief Psychiatric Rating Scale at 12 Weeks

A rating scale used to measure psychiatric symptoms such as depression, anxiety, hallucinations and unusual behaviour. Each symptom is rated 1-7 and in this version a total of 24 symptoms are scored. Thus the total range of scores is from a minimum of 24 to a maximum of 168. Lower scores are considered better, so the minimum total score of 24 indicates someone with no psychiatric symptoms, while any score over 40 is considered at least moderately severe, with only the most severely ill patients scoring over 60. (NCT00340379)
Timeframe: 12 weeks

Interventionunits on a Psychiatric Rating scale (Mean)
Ziprasidone28.7
Sertraline/Haloperidol25.8

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Change in the PANSS-EC Score Among Participants From Baseline to 2 Hours After Administration of the Medication.

The PANSS-EC is the Positive and Negative Syndrome Score - Excited Component, which includes 5 items (excitement, hostility, tension, uncooperative, poor impulse control), which are rated from 1 (not present) to 7 (extremely severe); scores range from 5 to 35; mean scores ≥ 20 clinically correspond to severe agitation. This set of items detects differences between drug and placebo when evaluating acute agitation and aggression in psychiatric patients with different psychiatric pathologies (Montoya, A; Villadares, A; Lizan, L, et al., 2011). (NCT00457366)
Timeframe: Two hours

Interventionscore on a scale (Least Squares Mean)
Cocktail-11.0
Quetiapine-11.5

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Percentage of Rapid Eye Movement Sleep

The primary variable is the change of the percentage of rapid eye movement (REM)sleep from baseline to the 28th day (LOCF). (NCT00642369)
Timeframe: 28 days

,
Interventionpercentage of rapid eye movement sleep (Mean)
percentage at baselinepercentage on the 28th daypercentage change from baseline to the 28th day
Haloperidol13.210.4-2.7
Quetiapine Fumarate12.616.43.9

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Percentage of Slow Wave Sleep

The primary variable is the change of percentage of slow wave sleep (SWS) from baseline to the 28th day (LOCF). (NCT00642369)
Timeframe: 28 days

,
Interventionpercentage of slow wave sleep (Mean)
percentage at baselinepercentage on the 28th daypercentage change from baseline to the 28th day
Haloperidol8.66.3-2.3
Quetiapine Fumarate10.59.2-1.4

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Part 1: Mean Global Clinical Impression at Day 14

Global clinical impression (GCI) was administered to assess whether any deterioration is due to akathisia or uncontrolled psychoses. Score on a scale +2 to -2 (+2 represents much improvement, +1 some improvement, 0 no change, -1 some worsening, and -2 much worsening). (NCT00693472)
Timeframe: Day 14 of Part 1

InterventionScore on a scale (Mean)
Part 1: Preladenant0.9231
Part 1: Placebo1.7778

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Part 1: Mean Positive and Negative Symptom Scale for Schizophrenia (PANSS) Total Score at Day 14

"The PANSS is a 30-item clinician-rated instrument for assessing the symptoms of schizophrenia. It consists of 3 subscales: positive subscale (7 items), negative subscale (7 items), and general psychopathology subscale (16 items). Positive symptoms refer to an excess or distortion of normal mental status (e.g., delusions). Negative symptoms represent a diminution or loss of normal functions (e.g., emotional withdrawal).~For each item, symptom severity was rated on a 7-point scale, from 0=absent to 6=extreme. The PANSS total score for each participant was calculated as the sum of the rating assigned to each of the 30 PANSS items, and ranged from 0 to 180 with a higher score indicating greater severity of symptoms. Although the PANSS is traditionally scored with a range of 30-210, with a score of absent = 1 (for each item), for this analysis the range was set from 0-180, with a score of absent = 0 (for each item)." (NCT00693472)
Timeframe: Day 14 of Part 1

InterventionScore on a scale (Mean)
Part 1: Preladenant38.4615
Part 1: Placebo36.3333

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Part 1: Number of Participants With Akathisia

Incidence of akathisia is reported as the number of participants who experienced akathisia. Akathisia is defined as a score of 3 on the Barnes akathisia scale (BAS) for 3 consecutive intervals or an akathisia score (BAS) of ≥4 for any single day, or the use of a rescue medication within 13 days of initiating treatment with haloperidol and preladenant. The BAS is scored as follows: objective akathisia, subjective awareness of restlessness and subjective distress related to restlessness are rated on a 4-point scale from 0 - 3 and are summed yielding a total score ranging from 0 (no akathisia) to 9 (severe akathisia). (NCT00693472)
Timeframe: Up to 13 days

InterventionParticipants (Number)
Part 1: Preladenant0
Part 1: Placebo0

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Part 2: Mean GCI at Day 14

The GCI was administered to assess whether any deterioration is due to akathisia or uncontrolled psychoses. Score on a scale +2 to -2 (+2 represents much improvement, +1 some improvement, 0 no change, -1 some worsening, and -2 much worsening). (NCT00693472)
Timeframe: Day 14 of Part 2

InterventionScore on a scale (Mean)
Part 2: Preladenant0.6667
Part 2: Standard of Care2.0000

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Part 2: Number of Participants Who Were Treatment Failures

Incidence of treatment failure is reported as the number of participants who were treatment failures. A treatment failure is defined as the failure to achieve at least a 1 point reduction from baseline in BAS score at 24 to 26 hours following study treatment. The BAS is scored as follows: objective akathisia, subjective awareness of restlessness and subjective distress related to restlessness are rated on a 4-point scale from 0 - 3 and are summed yielding a total score ranging from 0 (no akathisia) to 9 (severe akathisia). (NCT00693472)
Timeframe: Up to 14 days

InterventionParticipants (Number)
Part 2: Preladenant4
Part 2: Standard of Care1

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Part 2: PANSS Total Score at Day 14

The PANSS is a 30-item clinician-rated instrument for assessing the symptoms of schizophrenia. It consists of 3 subscales: positive subscale (7 items), negative subscale (7 items), and general psychopathology subscale (16 items). Positive symptoms refer to an excess or distortion of normal mental status (e.g., delusions). Negative symptoms represent a diminution or loss of normal functions (e.g., emotional withdrawal). For each item, symptom severity was rated on a 7-point scale, from 0=absent to 6=extreme. The PANSS total score for each participant was calculated as the sum of the rating assigned to each of the 30 PANSS items, and ranged from 0 to 180 with a higher score indicating greater severity of symptoms. Although the PANSS is traditionally scored with a range of 30-210, with a score of absent = 1 (for each item), for this analysis the range was set from 0-180, with a score of absent = 0 (for each item). (NCT00693472)
Timeframe: Day 14 of Part 2

InterventionScore on a scale (Mean)
Part 2: Preladenant43.5000
Part 2: Standard of Care27.75

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Change From Baseline in Brief Psychiatric Rating Scale (BPRS) Total Scores at 72 Hours

BPRS is an 18-item clinician rated scale with 11 general symptom items, 5 positive-symptom items, and 2 negative symptom items scored on a 7-point scale (1=not present and 7=extremely severe), with higher score indicating greater severity of symptom. Total possible score range=18 to 126. Change: score at final visit minus score at baseline. (NCT00723606)
Timeframe: Baseline, 72 hours

Interventionscores on a scale (Least Squares Mean)
Ziprasidone-17.32
Haloperidol-18.44

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Change From Baseline in BPRS Agitation Subscale Score at 72 Hours

The BPRS agitation subscale score was composed of 4 questions (questions 2, 6, 10, 17). The BPRS agitation subscale score was obtained by summing the relevant individual items. Total possible score range=4 to 28. Change: score at final visit minus score at baseline. (NCT00723606)
Timeframe: Baseline, 72 hours

Interventionscores on a scale (Least Squares Mean)
Ziprasidone-6.97
Haloperidol-7.45

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Change From Baseline in Behavioral Activity Rating Scale (BARS) at 72 Hours

BARS measures the degree of agitated behavior using a 7-point scale describing increasing levels of activity (1 =difficult or unable to rouse; 2 = asleep but responds normally to verbal or physical contact; 3 = drowsy, appears sedated; 4 = quiet and awake [normal level of activity]; 5 = signs of overt [physical or verbal] activity, calms down with instructions; 6 = extremely or continuously active, not requiring restraint; 7 = violent, requires restraint. (NCT00723606)
Timeframe: Baseline, 72 hours

Interventionscores on a scale (Least Squares Mean)
Ziprasidone-0.93
Haloperidol-1.06

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Change From Baseline in Clinical Global Impressions Severity (CGI-S) Score at 72 Hours

CGI-S: 7-point clinician rated scale to assess severity of subject's current illness state; range: 1 (normal - not ill at all) to 7 (among the most extremely ill patients). Higher score = more affected. Change: score at observation minus score at baseline. (NCT00723606)
Timeframe: Baseline, 72 hours

Interventionscores on a scale (Least Squares Mean)
Ziprasidone-1.18
Haloperidol-1.21

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Clinical Global Impression-Improvement (CGI-I) Score at 72 Hours

CGI-I: 7-point clinician rated scale ranging from 1 (very much improved) to 7 (very much worse). Improvement is defined as a score of 1 (very much improved), 2 (much improved), or 3 (minimally improved) on the scale. Higher score = more affected. (NCT00723606)
Timeframe: 72 hours

Interventionscores on a scale (Least Squares Mean)
Ziprasidone2.52
Haloperidol2.55

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BPRS Agitation Subscale Response at 72 Hours

The BPRS agitation subscale score was composed of 4 questions (questions 2, 6, 10, 17). The BPRS agitation subscale score was obtained by summing the relevant individual items. Total possible score range=4 to 28. A response was defined as a > 30 percent reduction from baseline in BPRS agitation subscale score. (NCT00723606)
Timeframe: 72 hours

,
Interventionparticipants (Number)
ResponseNo Response
Haloperidol15529
Ziprasidone14939

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The Change of the Positive and Negative Symptom Scale Excited Component (PANSS-EC) Score From Baseline to 120 Minutes After First Injection

The primary efficacy measure was PANSS-EC, which was derived from the PANSS by its originators using a principal-components factor analysis, and includes the items of tension, uncooperativeness, hostility, poor impulse control and excitement.22 The score of each item ranges from 1 (normal) to 7 (most severe), with a total sum score ranging from 5 to 35. The changes in PANSS-EC from baseline to 2 hours after the first injection were compared. (NCT00797277)
Timeframe: from baseline to 120 minutes after first injection

Interventionunits on a scale (Mean)
1. IM Olanzapine-10.2
2. IM Haloperidol Plus Lorazepam-9.9

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Change of the Agitation-Calmness Evaluation Scale (ACES) Score From Baseline to 120 Minutes After 1st Injection

Agitation was further assessed by the Agitation Calmness Evaluation Scale (ACES) (Copyright 1998, Eli Lilly and Company), a single-item scale developed by Eli Lilly and Company on which 1 indicates marked agitation; 2, moderate agitation; 3, mild agitation; 4, normal; 5, mild calmness; 6, moderate calmness; 7, marked calmness; 8, deep sleep; and 9, unable to be aroused. (NCT00797277)
Timeframe: from baseline to 120 minutes after first injection

Interventionunits on a scale (Mean)
1. IM Olanzapine2.14
2. IM Haloperidol Pus Lorazepam2.23

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Mortality

(NCT00842608)
Timeframe: ICU, in-hospital, 30-days post hospitalization

InterventionParticipants (Count of Participants)
Haloperidol Eligible Intervention20
Haloperidol Eligible Usual Care32
Haldol-Ineligible Arm11
Haldol Ineligible Usual Care8

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Hospital Length of Stay Post Randomization

(NCT00842608)
Timeframe: Participants were followed for the duration of hospital stay, an average of 11 days

Interventiondays (Mean)
Haloperidol Eligible Intervention20.2
Haloperidol Eligible Usual Care18.6
Haldol-Ineligible Arm18.8
Haldol Ineligible Usual Care14.9

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Days Free of Delirium and Coma

(NCT00842608)
Timeframe: Admission through day 8 of stay

Interventiondays (Median)
Haloperidol Eligible Intervention4
Haloperidol Eligible Usual Care5
Haldol-Ineligible Arm4
Haldol Ineligible Usual Care5

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Efficacy Failure

Efficacy failure as indicated by psychiatric hospitalization, need for crisis intervention, clinical decision that oral antipsychotic medication cannot be discontinued in less than eight weeks, a clinical decision to discontinue the medication due to inadequate benefit, or the ongoing or repeated need for adjunctive antipsychotic medication. (NCT01136772)
Timeframe: 24 months

Interventionparticipants (Number)
Paliperidone Palmitate49
Haloperidol Decanoate47

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Changes in Psychiatric Symptoms

The Positive and Negative Syndrome Scale measures the core symptoms associated with schizophrenia. The measure includes 30 items rated from 1=absent to 7=extremely severe. Full range of scores is 30-210 with higher scores representing more severe illness. Reductions in symptoms over time represent improvement. (NCT01136772)
Timeframe: Baseline to 6 months

InterventionUnits on a scale (Mean)
Paliperidone Palmitate-6.87
Haloperidol Decanoate-6.40

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Global Psychopathology as Measured by the Clinical Global Impressions (CGI) at 12 Months

"Global psychopathology will be measured with the Clinical Global Impressions (CGI) (Guy 1976) a widely used scale which evaluates illness severity on a 1 to 7 point continuum. Severity of illness ratings on the CGI have reported reliability scores ranging from 0.41-0.66 (Guy 1976) Lower scores indicate improved outcomes. Higher scores indicate worse outcomes.~Illness scale: 1 - 7 (1 = Normal/not at all ill ; 7 = Among the most extremely ill patients) Global improvement scale: 1 - 7 (1 = Very much improved ; 7 = Very much worse)" (NCT01152697)
Timeframe: 12 months

Interventionunits on a scale (Mean)
SeverityGlobal Improvement
Patient Noncompliance3.172.42

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Treatment Satisfaction as Measured by the Participant Acceptability and Satisfaction Questionnaire at 25 Weeks

"Satisfaction will be measured by a seven item inventory taken by the participant.~Scale ranges from 1 (Strongly Agree) to 5 (Strongly Disagree). Lower scores indicate better outcomes, while higher scores indicate worse outcomes. The highest possible score is 35." (NCT01152697)
Timeframe: 25 weeks

Interventionunits on a scale (Mean)
Patient Noncompliance12.12

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Treatment Satisfaction as Measured by the Participant Acceptability and Satisfaction Questionnaire at 12 Months

"Satisfaction will be measured by a seven item inventory taken by the participant.~Scale ranges from 1 (Strongly Agree) to 5 (Strongly Disagree). Lower scores indicate better outcomes, while higher scores indicate worse outcomes. The highest possible score is 35." (NCT01152697)
Timeframe: 12 months

Interventionunits on a scale (Mean)
Patient Noncompliance12.33

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Treatment Adherence Behavior Score as Measured by the Morisky Medication Rating Scale at 12 Months

Four item inventory taken by participant with Scale Range: 0-4. Lower scores indicate better outcomes. (NCT01152697)
Timeframe: 12 months

Interventionunits on a scale (Mean)
Patient Noncompliance1.33

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Change From Baseline in Adherence Attitude Score as Measured by the Attitude Toward Medication Questionnaire (AMQ) at 25 Weeks

Nineteen item inventory taken by the participant with Scale Range:0-19. Lower scores indicate improved outcomes. (NCT01152697)
Timeframe: Baseline-25 weeks

Interventionunits on a scale (Mean)
BaselineWeek 25
Patient Noncompliance6.634.47

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Frequency of Health Resource Use in the Past 3 Months as Measured at 25 Weeks

The frequency of health resource use will be measured through interview of the participant. (NCT01152697)
Timeframe: 25 weeks

Interventiondays (Mean)
Patient Noncompliance20.18

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Adherence Attitude Score as Measured by the Drug Attitude Inventory (DAI) at 12 Months

Ten item inventory taken by the participant with a Scale Range: 0-10. Higher scores indicate improved outcomes. (NCT01152697)
Timeframe: 12 months

Interventionunits on a scale (Mean)
Patient Noncompliance7.00

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Adherence Attitude Score as Measured by the Attitude Toward Medication Questionnaire (AMQ) at 12 Months

Nineteen item inventory taken by the participant with Scale Range:0-19. Lower scores indicate improved outcomes. (NCT01152697)
Timeframe: 12 months

Interventionunits on a scale (Mean)
Patient Noncompliance2.43

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Treatment Adherence Score as Measured at 12 Months

A total treatment adherence score will calculated as a proportion of medications taken as reported from the participant, and evidenced by pill counts and documented medication injections. (NCT01152697)
Timeframe: 12 months

InterventionPercentage of doses (Mean)
Past WeekPast Month
Patient Noncompliance28.656

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Frequency of Health Resource Use Throughout Months 10, 11, and 12

The frequency of health resource use will be measured through interview of the participant. (NCT01152697)
Timeframe: Month 1-3, Month 10-12

Interventiondays (Mean)
3 Month12 Month
Patient Noncompliance19.3315.50

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Change in Social and Occupational Functioning Scale (SOFAS) as Measured at 25 Weeks

Life and Work Functional status will be evaluated using the Social and Occupational Functioning Scale (SOFAS), which is derived from the GAF (Global Assessment of Functioning). The GAF is a 100-point single-item scale which measures global functioning of psychiatric patients and is widely utilized in clinical studies involving Seriously Mentally Ill patients (Jones 1995). The reliability of the GAF ranges from 0.62-0.82. Higher scores indicate improved outcomes. (NCT01152697)
Timeframe: Baseline-25 weeks

Interventionunits on a scale (Mean)
BaselineWeek 25
Patient Noncompliance47.3558.65

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Change in Social and Occupational Functioning Scale (SOFAS) as Measured at 12 Months

Life and Work Functional status will be evaluated using the Social and Occupational Functioning Scale (SOFAS), which is derived from the GAF. The GAF is a 100-point single-item scale which measures global functioning of psychiatric patients and is widely utilized in clinical studies involving Seriously Mentally Ill patients (Jones 1995). The reliability of the GAF ranges from 0.62-0.82. Higher scores indicate improved outcomes. (NCT01152697)
Timeframe: Baseline-12 months

Interventionunits on a scale (Mean)
Baseline12 months
Patient Noncompliance45.3363.83

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Change in Serious Mental Illness Severity Score as Measured by the Brief Psychiatric Rating Scale (BPRS) at 25 Weeks

"The BPRS, developed by Overall and Gorham (1962), is a widely used, relatively brief scale that measures major psychotic and non-psychotic symptoms in individuals with SMI. The 18-item BPRS is well-validated and is perhaps the most researched instrument in psychiatry. Reliability coefficients are reported to be in the range of 0.56-0.87.~Scale Range: 18-126 Lower scores represent improved outcomes." (NCT01152697)
Timeframe: Baseline-25 weeks

Interventionunits on a scale (Mean)
BaselineWeek 25
Patient Noncompliance46.3732.84

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Change in Schizophrenia and Schizoaffective Disorder Symptom Severity Scale as Measured by the Positive and Negative Syndrome Scale (PANSS) at 25 Weeks

"The PANSS (Kay, Fiszbein, & Opler 1987) was created to assess both the positive and negative symptoms of schizophrenia such as hallucinations and emotional withdrawal, respectively. The scale rates 30 symptoms on a scale from 1 (absent) to 7 (extreme) and has been shown to limit bias between the assessment of positive and negative symptoms, providing a broad but balanced spectrum of the illness.~There are three subscales: positive symptoms, negative symptoms, general psychopathology. Potential responses to Items on all subscales range from 1 (absent) to 7 (extreme). Lower scores indicate lower symptoms and, therefore, better outcomes. Higher scores indicate more presence of symptoms and, therefore, worse outcomes.~Subscales are combined to produce a total score, which is summed from all of the subscales. Lower total scores indicate lower symptoms and, therefore, better outcomes. Higher total scores indicate more presence of symptoms and, therefore, worse outcomes." (NCT01152697)
Timeframe: Baseline-25 weeks

Interventionunits on a scale (Mean)
BaselineWeek 25
Patient Noncompliance46.3732.84

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Change in Global Psychopathology as Measured by the Clinical Global Impressions (CGI) at 25 Weeks

"Global psychopathology will be measured with the Clinical Global Impressions (CGI) (Guy 1976) a widely used scale which evaluates illness severity on a 1 to 7 point continuum. Severity of illness ratings on the CGI have reported reliability scores ranging from 0.41-0.66 (Guy 1976) Lower scores indicate improved outcomes. Higher scores indicate worse outcomes.~Illness scale: 1 - 7 (1 = Normal/not at all ill ; 7 = Among the most extremely ill patients) Global improvement scale: 1 - 7 (1 = Very much improved ; 7 = Very much worse)" (NCT01152697)
Timeframe: Baseline-25 weeks

Interventionunits on a scale (Mean)
Baseline - SeverityWeek 25 - SeverityBaseline - Global ImprovementWeek 25 - Global Improvement
Patient Noncompliance4.763.243.432.14

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Change From Baseline in Treatment Adherence Score as Measured at 25 Weeks

A total treatment adherence score will calculated as a proportion of medications taken as reported from the participant, and evidenced by pill counts and documented medication injections. (NCT01152697)
Timeframe: Baseline-25 weeks

InterventionPercentage of doses (Mean)
Past weekPast month
Patient Noncompliance30.9110.10

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Change From Baseline in Treatment Adherence Behavior Score as Measured by the Morisky Medication Rating Scale at 25 Weeks

Four item inventory taken by participant with Scale Range: 0-4. Lower scores indicate improved outcomes. (NCT01152697)
Timeframe: Baseline-25 weeks

Interventionunits on a scale (Mean)
BaselineWeek 25
Patient Noncompliance2.311.19

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Change From Baseline in Adherence Attitude Score as Measured by the Drug Attitude Inventory (DAI) at 25 Weeks

Ten item inventory taken by the participant with a Scale Range: 0-10. Higher scores indicate improved outcomes. (NCT01152697)
Timeframe: Baseline-25 weeks

Interventionunits on a scale (Mean)
BaselineWeek 25
Patient Noncompliance7.478.07

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Side Effects

(NCT01204255)
Timeframe: 3 months

InterventionTotal number of side effects (Number)
Application of Lorazepam, Diphenhydramine, Haloperidol0

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Lorazepam, Diphenyhydramine, Haloperidol Absorption

Level of lorazepam absorption measured by the serum concentration of the drug (NCT01204255)
Timeframe: 4 hours

Interventionng/ml (Mean)
lorazepam absorptiondiphenhydramine absorptionhaloperidol absorption
Application of Lorazepam, Diphenhydramine, Haloperidol0.080

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Delirium Duration

Duration of delirium during the intervention period (NCT01211522)
Timeframe: 14 days

Interventiondays (Median)
Haloperidol4
Ziprasidone4
Placebo4

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Delirium/Coma-free Days (DCFDs)

Defined as the number of days during the 14-day intervention period (beginning on the day of randomization) that the patient was alive and experienced neither delirium nor coma. (NCT01211522)
Timeframe: 14 days

Interventiondays (Median)
Haloperidol8
Ziprasidone8
Placebo7

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Number of Participants With Extrapyramidal Symptoms

(NCT01211522)
Timeframe: 14 days plus 4-day post-study drug period (if longer than 14 days)

InterventionParticipants (Count of Participants)
Haloperidol1
Ziprasidone1
Placebo1

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Number of Participants With Neuroleptic Malignant Syndrome

(NCT01211522)
Timeframe: 14 days plus 4-day post-study drug period (if longer than 14 days)

InterventionParticipants (Count of Participants)
Haloperidol0
Ziprasidone0
Placebo0

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Number of Participants With Torsades de Pointes

(NCT01211522)
Timeframe: 14 days plus 4-day post-study drug period (if longer than 14 days)

InterventionParticipants (Count of Participants)
Haloperidol2
Ziprasidone0
Placebo0

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Time to Final ICU Discharge

"Days from randomization to final, successful ICU discharge, where successful indicates that discharge was followed by at least 48 hours alive. ICU discharge is represented by readiness for ICU discharge indicated by a physician order for transfer to a lower level of care even if a bed availability problems prevent actual discharge from the ICU." (NCT01211522)
Timeframe: 90 days

Interventiondays (Median)
Haloperidol5
Ziprasidone6
Placebo5

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Time to Hospital Discharge

"Days from randomization to successful hospital discharge, where successful indicates that discharge was followed by at least 48 hours alive." (NCT01211522)
Timeframe: 90 days

Interventiondays (Median)
Haloperidol13
Ziprasidone12
Placebo13

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Time to ICU Readmission

Days from first ICU discharge to next ICU readmission. (NCT01211522)
Timeframe: 90 days after first ICU discharge

Interventiondays (Median)
Haloperidol5
Ziprasidone5
Placebo4

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Time to Liberation From Mechanical Ventilation

"Days from randomization to successful liberation from mechanical ventilation, where successful indicates that liberation was followed by at least 48 hours alive and without reinitiation of invasive or noninvasive ventilation." (NCT01211522)
Timeframe: 30 days

Interventiondays (Median)
Haloperidol2
Ziprasidone3
Placebo3

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Mortality

Deaths within the specified timeframe (NCT01211522)
Timeframe: 30-day and 90-day

,,
InterventionParticipants (Count of Participants)
30-day mortality90-day mortality
Haloperidol5073
Placebo5063
Ziprasidone5365

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Impact of Chemotherapy-Induced Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 1

"To determine the incidence of vomiting associated with the Docetaxel-Cyclophosphamide regimen in early breast cancer patients, a Functional Living Index-Emesis (FLIE) questionnaire was collected on treatment Day 1 (prior to initiation of chemotherapy) and Day 6, which referenced the entire treatment period since the initiation of chemotherapy for non clinical responders (NCR) against clinical responders (CR).~The FLIE questionnaire is a validated, patient-reported instrument to measure the impact of vomiting on daily life. There are 9 vomiting-related items, each on a 7-point scale. Results are reported as a vomiting score. For the purposes of this study, higher scores indicate less impairment on daily life as a result of vomiting (better outcome) (Maximum 63, Minimum 9)." (NCT01298193)
Timeframe: Up to day 6

Interventionscore on a scale (Mean)
Cycle 1 pre-chemotherapy NCR patientsCycle 1 post-chemotherapy NCR patientsCycle 1 pre-chemotherapy CR patientsCycle 1 post-chemotherapy CR patients
Aprepitant23.8627.4623.5324.15

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Impact of Chemotherapy-Induced Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 2

"To determine the incidence of vomiting associated with the Docetaxel-Cyclophosphamide regimen in early breast cancer patients, a Functional Living Index-Emesis (FLIE) questionnaire was collected on treatment Day 1 (prior to initiation of chemotherapy) and Day 6, which referenced the entire treatment period since the initiation of chemotherapy for non clinical responders (NCR) against clinical responders (CR).~The FLIE questionnaire is a validated, patient-reported instrument to measure the impact of vomiting on daily life. There are 9 items, each on a 7-point scale. Results are reported as a vomiting score. For the purposes of this study, higher scores indicate less impairment on daily life as a result of vomiting (better outcome) (Maximum 63, Minimum 9)." (NCT01298193)
Timeframe: Up to day 6

Interventionscore on a scale (Mean)
Cycle 2 pre-chemotherapy NCR patientsCycle 2 post-chemotherapy NCR patientsCycle 2 pre-chemotherapy CR patientsCycle 2 post-chemotherapy CR patients
Aprepitant NCR20.0928.1923.7123.43

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Total Impact of Chemotherapy-Induced Nausea and Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 1

"To determine the incidence of Chemotherapy-Induced Nausea and Vomiting associated with the Docetaxel-Cyclophosphamide regimen in early breast cancer patients, a Functional Living Index-Emesis (FLIE) questionnaire was collected on treatment Day 1 (prior to initiation of chemotherapy) and Day 6, which referenced the entire treatment period since the initiation of chemotherapy for non clinical responders (NCR) against clinical responders (CR).~The FLIE questionnaire is a validated, patient-reported instrument to measure the impact of Chemotherapy-Induced Nausea and Vomiting on daily life. There are 18 items, each on a 7-point scale. Results are reported as a total score. For the purposes of this study, higher scores indicate less impairment on daily life as a result of nausea or vomiting (better outcome) (Maximum 126, Minimum 18)." (NCT01298193)
Timeframe: Up to day 6

Interventionscore on a scale (Mean)
Cycle 1 pre-chemotherapy NCR patientsCycle 1 post-chemotherapy NCR patientsCycle 1 pre-chemotherapy CR patientsCycle 1 post-chemotherapy CR patients
Aprepitant43.759.242.544.22

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Number of Participants With Complete Response (CR)

Complete response is defined as no vomiting and no use of rescue treatment within the first cycle of Docetaxel-Cyclophosphamide for the treatment of early-stage breast cancer patients. A vomiting episode is defined as one or more episodes of emesis (expulsion of stomach contents through the mouth) or retches (an attempt to vomit that is not productive of stomach contents). Distinct vomiting episodes are, by definition, separated by the absence of emesis and retching for at least 1 minute. The timing (date and time) of each vomiting episode will be recorded by the patient in each cycle diary at the time of occurrence. Assessments of efficacy will begin at the initiation of chemotherapy infusion (0 hours) until the morning of Day 6 (approximately 120 hours) after chemotherapy during 1-2 cycles. (NCT01298193)
Timeframe: Up to 21 days after cycle 1 of chemotherapy treatment

InterventionParticipants (Count of Participants)
Observational Phase (First Cycle):161

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Number of Participants With Complete Response (CR) in Cycle 2 for Patient Without Complete Response in Cycle 1

To evaluate in cycle 2 the efficacy of aprepitant (days 1, 2 and 3) as secondary prevention in patients without complete response in cycle 1. A vomiting episode is defined as one or more episodes of emesis (expulsion of stomach contents through the mouth) or retches (an attempt to vomit that is not productive of stomach contents). Distinct vomiting episodes are, by definition, separated by the absence of emesis and retching for at least 1 minute. The timing (date and time) of each vomiting episode will be recorded by the patient in each cycle diary at the time of occurrence. Assessments of efficacy will begin at the initiation of chemotherapy infusion (0 hours) until the morning of Day 6 (approximately 120 hours) after chemotherapy during 1-2 cycles. (NCT01298193)
Timeframe: Up to cycle 2, and average of 6 weeks

InterventionParticipants (Count of Participants)
Aprepitant NCR12

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Impact of Chemotherapy-Induced Nausea on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 1

"To determine the incidence of nausea associated with the Docetaxel-Cyclophosphamide regimen in early breast cancer patients, a Functional Living Index-Emesis (FLIE) questionnaire was collected on treatment Day 1 (prior to initiation of chemotherapy) and Day 6, which referenced the entire treatment period since the initiation of chemotherapy for non clinical responders (NCR) against clinical responders (CR).~The FLIE questionnaire is a validated, patient-reported instrument to measure the impact of Chemotherapy-Induced Nausea and vomiting on daily life. There are 9 nausea-related items, each on a 7-point scale. Results are reported as a nausea score. For the purposes of this study, higher scores indicate less impairment on daily life as a result of nausea (better outcome) (Maximum 63, Minimum 9)." (NCT01298193)
Timeframe: Up to day 6

Interventionscore on a scale (Mean)
Cycle 1 pre-chemotherapy NCR patientsCycle 1 post-chemotherapy NCR patientsCycle 1 pre-chemotherapy CR patientsCycle 1 post-chemotherapy CR patients
Aprepitant19.8531.7318.9320.27

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Impact of Chemotherapy-Induced Nausea on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 2

"To determine the incidence of Nausea associated with the Docetaxel-Cyclophosphamide regimen in early breast cancer patients, a Functional Living Index-Emesis (FLIE) questionnaire was collected on treatment Day 1 (prior to initiation of chemotherapy) and Day 6, which referenced the entire treatment period since the initiation of chemotherapy for non clinical responders (NCR) against clinical responders (CR).~The FLIE questionnaire is a validated, patient-reported instrument to measure the impact of Nausea on daily life. There are 9 items, each on a 7-point scale. Results are reported as a nausea score. For the purposes of this study, higher scores indicate less impairment on daily life as a result of nausea (better outcome) (Maximum 63, Minimum 9)." (NCT01298193)
Timeframe: Up to day 6

Interventionscore on a scale (Mean)
Cycle 2 pre-chemotherapy NCR patientsCycle 2 post-chemotherapy NCR patientsCycle 2 pre-chemotherapy CR patientsCycle 2 post-chemotherapy CR patients
Aprepitant NCR17.7136.1619.5724.30

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Total Impact of Chemotherapy-Induced Nausea and Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 2

"To determine the total incidence of Chemotherapy-Induced Nausea and Vomiting associated with the Docetaxel-Cyclophosphamide regimen in early breast cancer patients, a Functional Living Index-Emesis (FLIE) questionnaire was collected on treatment Day 1 (prior to initiation of chemotherapy) and Day 6, which referenced the entire treatment period since the initiation of chemotherapy for non clinical responders (NCR) against clinical responders (CR).~The FLIE questionnaire is a validated, patient-reported instrument to measure the impact of Chemotherapy-Induced Nausea and Vomiting on daily life. There are 18 items, each on a 7-point scale. Results are reported as a total score. For the purposes of this study, higher scores indicate less impairment on daily life as a result of nausea or vomiting (better outcome) (Maximum 126, Minimum 18)." (NCT01298193)
Timeframe: Up to day 6

Interventionscore on a scale (Mean)
Cycle 2 pre-chemotherapy NCR patientsCycle 2 post-chemotherapy NCR patientsCycle 2 pre-chemotherapy CR patientsCycle 2 post-chemotherapy CR patients
Aprepitant NCR37.864.443.2847.7

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The Change in Numeric Rating Scale in Self-reported Nausea From Baseline Minus 60 Minutes of Treatment.

"The outcome measure for change was calculated from value at baseline minus value at 60 minutes. Subjects were asked to rate their nausea on a 0 (no nausea) to 10 (worst possible nausea) scale. Subjects who were eligible were randomly assigned to two sequences: one sequence used ABH gel first and then placebo; and the other sequence used placebo first and then ABH gel. We assumed that there was no carry-over effect from the first treatment to the second. A paired t-test was used to compare if ABH gel is not better than the placebo gel. A repeated measure analysis was used to compare the two treatment sequences. This endpoint was chosen as the drug gel because it is typically used as a prn (as needed) gel in actual practice, when relief is needed in short order." (NCT01556932)
Timeframe: 60 minutes after application

Interventionunits on a scale (Mean)
ABH Gel1.70
Placebo0.90

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Incidence of Extrapyramidal Symptoms

(NCT01639599)
Timeframe: postoperative 24 hours

Interventionparticipants (Number)
Dexamethasone0
Dexamethasone, Haloperiol 1mg0
Dexamethasone + Haloperidol 2mg0

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Incidence of Postoperative Nausea and Vomiting

incidence of nausea, vomiting and requirement for rescue antiemetics (NCT01639599)
Timeframe: postoperative 24 hours

Interventionparticipants (Number)
Dexamethasone21
Dexamethasone, Haloperiol 1mg11
Dexamethasone + Haloperidol 2mg10

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Sedation Change in Recovery Room

measurement of sedation change using a visual analogue scale (visual analogue scale; the minimum: 0 = widely awake and the maximum: 10 = maximally asleep) (NCT01639599)
Timeframe: postoperative 30, 60, 90, and 120 min

,,
Interventionscore on a scale (Mean)
postoperative 30 minpostoperative 60 minpostoperative 90 minpostoperative 120 min
Dexamethasone4.64.43.53.0
Dexamethasone + Haloperidol 2mg5.55.04.74.3
Dexamethasone, Haloperiol 1mg4.74.44.03.2

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Incidence of Cardiac Arrhythmia

cardiac arrhythmia on continuous standard lead EKG monitoring (NCT01639599)
Timeframe: postoperative 2 hours

InterventionParticipants (Count of Participants)
Dexamethasone0
Dexamethasone, Haloperiol 1mg0
Dexamethasone + Haloperidol 2mg0

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Absolute Richmond Agitation-Sedation Scale Score at 8 Hour, Points

Absolute score of Richmond Agitation-Sedation Scale at 8 hr, points. Richmond Agitation-Sedation Score ranged from -5 (unarousable) to +4 (very agitated) , where 0 denotes a calm and alert patient. (NCT01949662)
Timeframe: 8 hours

Interventionscore on a scale (Mean)
Intervention Group (Lorazepam & Haloperidol)-2.5
Control Group (Placebo & Haloperidol)-0.7

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Change in Richmond Agitation-Sedation Scale Score (Baseline to 8 hr), Points

The primary outcome was change in Richmond Agitation-Sedation Scale score from baseline to 8 hours after treatment administration. Richmond Agitation-Sedation Score ranged from -5 (unarousable) to +4 (very agitated) , where 0 denotes a calm and alert patient. (NCT01949662)
Timeframe: Baseline to 8 hours

Interventionscore on a scale (Mean)
Intervention Group (Lorazepam & Haloperidol)-4.1
Control Group (Placebo & Haloperidol)-2.3

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Change in Richmond Agitation-Sedation Scale Score From Baseline to 30 Min

Change in Richmond Agitation-Sedation Scale score from baseline to 30 min. Richmond Agitation-Sedation Score ranged from -5 (unarousable) to +4 (very agitated) , where 0 denotes a calm and alert patient. (NCT01949662)
Timeframe: Baseline to 30 minutes

Interventionscore on a scale (Mean)
Intervention Group (Lorazepam & Haloperidol)-3.6
Control Group (Placebo & Haloperidol)-1.6

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Number of Participants With Richmond Agitation-Sedation Scale Score >=1 Within 8 hr

Number of participants with Richmond Agitation-Sedation Scale score >=1 within 8 hr. Richmond Agitation-Sedation Score ranged from -5 (unarousable) to +4 (very agitated) , where 0 denotes a calm and alert patient. (NCT01949662)
Timeframe: Baseline to 8 hours

InterventionParticipants (Count of Participants)
Intervention Group (Lorazepam & Haloperidol)8
Control Group (Placebo & Haloperidol)22

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Pain Relief as Indicated by Number of Participants Not Requesting Additional Pain Medication

(NCT02057549)
Timeframe: 1 hour after study medication given

InterventionParticipants (Count of Participants)
Haloperidol Plus Conventional Therapy11
Conventional Therapy5

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Emergency Department Length of Stay (EDLOS)

"The time frame starts from the moment of receiving the study drug to the time when the decision for final disposition is made. Usually after symptoms are controlled, patients are given a PO challenge (food or drink) in order to establish if they are OK to go home. If symptoms return, additional medications are given, the treatment is consider failed and they are admitted to the Hospital.~Patients will not be followed up if admitted to any service. The study ends when final disposition is made.~Patients follow up after final disposition is not part of the study and will not be done." (NCT02057549)
Timeframe: at the time the decision for final disposition is made (about 8 hours)

Interventionhours (Median)
Haloperidol Plus Conventional Therapy4.8
Conventional Therapy9

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Pain Score as Measured by a Visual Analogue Scale (VAS)

The Visual Analogue Scale (VAS) ranges from 0-10, with 0 being the absence of pain and 10 the worst imaginable pain. (NCT02057549)
Timeframe: 1 hour after study medication given

Interventionunits on a scale (Mean)
Haloperidol Plus Conventional Therapy3.13
Conventional Therapy7.17

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Nausea Score as Measured by a Visual Analogue Scale (VAS)

The Visual Analogue Scale (VAS) ranges from 1-5, with 1 being minimal nausea and 5 being severe nausea. (NCT02057549)
Timeframe: 1 hour after study medication given

Interventionunits on a scale (Mean)
Haloperidol Plus Conventional Therapy1.83
Conventional Therapy3.39

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Number of Participants Admitted to the Hospital After Emergency Department Visit

(NCT02057549)
Timeframe: 2 hours after study medication given

InterventionParticipants (Count of Participants)
Haloperidol Plus Conventional Therapy4
Conventional Therapy13

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Nausea Score as Measured by a Visual Analogue Scale (VAS)

The Visual Analogue Scale (VAS) ranges from 1-5, with 1 being minimal nausea and 5 being severe nausea. (NCT02057549)
Timeframe: before study medication given

Interventionunits on a scale (Mean)
Haloperidol Plus Conventional Therapy4.53
Conventional Therapy4.11

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Nausea Relief as Indicated by Number of Participants Not Requesting Additional Antiemetic Medication

(NCT02057549)
Timeframe: 1 hour after study medication given

InterventionParticipants (Count of Participants)
Haloperidol Plus Conventional Therapy11
Conventional Therapy13

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Pain Score as Measured by a Visual Analogue Scale (VAS)

The Visual Analogue Scale (VAS) ranges from 0-10, with 0 being the absence of pain and 10 the worst imaginable pain. (NCT02057549)
Timeframe: before study medication given

Interventionunits on a scale (Mean)
Haloperidol Plus Conventional Therapy8.50
Conventional Therapy8.28

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Change in ASSIST GRS (Alcohol, Smoking and Substance Involvement Screening Test ) From Screen to Week 25

The ASSIST was used to measure drug use. A total score is derived by combining item scores (minimum score = 0; maximum score = 382). Higher scores indicate higher risk of lifestyle problems, including health. (NCT02085447)
Timeframe: Screen, Week 25

Interventionunits on a scale (Mean)
CAE-L2.0

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Change in PANSS (Positive and Negative Syndrome Scale; General Psychopathology) From Screen to Week 25

The PANSS is used to assess patients for positive and negative symptoms of schizophrenia or schizoaffective disorder. The General Psychopathology Subscale consists of 16 questions. Each item is rated on a scale of 1 (Absent) to 7 (Extreme). Total scores range from 16-112 on the General Psychopathology scale. Higher scores indicate more symptoms of psychopathology. There is no aggregate score for this measure, as the subscales are to be scored separately. (NCT02085447)
Timeframe: Screen, Week 25

Interventionunits on a scale (Mean)
CAE-L24.7

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Percentage Change of Days of Sub-optimal Housing in the Past Six Months; Change From Screen to Week 25

Change in number of sub-optimal housing from the past 6 months from Screen and Week 25. This is calculated by subtracting the percent of sub-optimal housing at screen from the number of sub-optimal housing at week 25. (NCT02085447)
Timeframe: Screen, Week 25

Interventionpercentage of days (Mean)
CAE-L29.0

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Long-acting Injection (LAI) Adherence

Long-acting injection (LAI) adherence will be determined as a proportion of LAI (paliperidone palmitate or haloperidol decanoate) injections received at the appropriate time (within 7 days of scheduled time). (NCT02085447)
Timeframe: Week 25

Interventionpercentage of adherence (Mean)
CAE-L90.5

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Change in AMSQ (Attitudes Toward Mood Stabilizers Questionnaire) From Screen to Week 25

"The AMSQ/AMQ is used to measure attitudes towards medications. The scale contains 19 items. Responses which suggest positive attitudes towards medications are scored 0, while responses which suggest negative attitudes towards medications are scored 1. The items scores are added for a total score. Total scores range from 0 to 19. Lower total scores suggest more positive attitudes, while higher scores suggest more negative attitudes." (NCT02085447)
Timeframe: Screen, Week 25

Interventionunits on a scale (Mean)
CAE-L4.0

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Change in AIMS (Abnormal Involuntary Movement Scale) From Baseline to Week 25

"The AIMS is used to monitor for the development of involuntary movements that may occur as a result of certain psychotropic medication. It contains 14 items, 10 of which are rated on a scale of 0 (None) to 4 (Severe). The remaining four items are yes or no questions. Items 1 thru 7 are added for a total score, while item 8 is used as an overall severity index. Total scores range from 0 to 28. Higher scores indicate more adverse outcomes.Items 9 thru 12 provide additional information that may be useful in determining lip, jaw, and tongue movements." (NCT02085447)
Timeframe: Baseline, Week 25

Interventionunits on a scale (Mean)
CAE-L1.5

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Change in PANSS (Positive and Negative Syndrome Scale; Composite Scale) From Screen to Week 25

The PANSS is used to assess patients for positive and negative symptoms of schizophrenia or schizoaffective disorder. The Composite Scale is scored by subtracting the negative score from the positive score. This yields a bipolar index that ranges from -42 to +42. The bipolar composite scale simply expresses the direction and magnitude of difference between positive and negative syndromes. Scores >0 indicate there are more positive symptoms of schizophrenia endorsed, and scores <0 indicate there are more negative symptoms of schizophrenia endorsed. There is no aggregate score for this measure, as the subscales are to be scored separately. (NCT02085447)
Timeframe: Screen, Week 25

Interventionunits on a scale (Mean)
CAE-L.8

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Change in Hospitalizations (Psychiatric) in the Past 6 Months From Screen and Week 25

Change in number of psychiatric hospitalizations from the past 6 months from Screen and Week 25. This is calculated by subtracting the number of psychiatric hospitalizations at screen from the number of psychiatric hospitalizations at week 25. (NCT02085447)
Timeframe: Screen, Week 25

Interventionhospital visits (Mean)
CAE-L.2

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Change in Hospitalizations (Medical) in the Past 6 Months From Screen and Week 25

Change in number of psychiatric hospitalizations from the past 6 months from Screen and Week 25. This is calculated by subtracting the number of psychiatric hospitalizations at screen from the number of psychiatric hospitalizations at week 25. (NCT02085447)
Timeframe: Screen, Week 25

Interventionhospital visits (Mean)
CAE-L.2

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Change in ESRS-A (Extrapyramidal Symptoms Scale-Abbreviated; Akathisia)

For the subjective examination scoring is on a 4-point scale (0=Absent;1=Mild, 2=Moderate, 3=Severe). The evaluator takes into account the verbal report of the patient on: 1) the frequency and duration of the symptom during the day; 2) the number of days the symptom was present during the last week; and, 3) the subjective evaluation of the intensity of the symptom by the patient. The score for akathisia is separated from the Parkinsonism score and is based on the combined score of subjective akathisia (item 6 of the questionnaire) and objective akathisia (item 7 of the Parkinsonism/Akathisia objective examination). This subscore total ranges from 0 to 6. Higher scores indicate more severity. (NCT02085447)
Timeframe: Screen, Week 25

Interventionunits on a scale (Mean)
CAE-L.2

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Change in Tablets Routine Questionnaire (TRQ) (Past Month) From Screen to Week 25

The Tablets Routine Questionnaire (TRQ) determines the proportion of prescribed medication taken and is not dependent upon timing of medication provided that medication is consumed within the required day/24 hour period. This rating has demonstrated statistically significant association with past non-adherence, repeated past non-adherence, any non-adherence in the past month, and non-adherence in the past week. The TRQ format will be modified slightly to document all adherence values (an exact proportion) for each item. TRQ scores ranges from perfect adherence (0% missed) to missing all medication (100% missed). An average TRQ was calculated for individuals on more than one BD medication. (NCT02085447)
Timeframe: Screen, Week 25

Interventionpercentage of adherence (Mean)
CAE-L15.2

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Change in ESRS-A (Extrapyramidal Symptoms Scale-Abbreviated; Dystonia) From Screen to Week 25

For the subjective examination scoring is on a 4-point scale (0=Absent;1=Mild, 2=Moderate, 3=Severe). The evaluator takes into account the verbal report of the patient on: 1) the frequency and duration of the symptom during the day; 2) the number of days the symptom was present during the last week; and, 3) the subjective evaluation of the intensity of the symptom by the patient. The score for dystonia ranges from 0 to 60 (10 items), and is formed by including both acute and chronic dystonia, based on the dystonia examination. Higher scores indicate more severity. (NCT02085447)
Timeframe: Screen, Week 25

Interventionunits on a scale (Mean)
CAE-L0.0

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Change in ESRS-A (Extrapyramidal Symptoms Scale-Abbreviated; Dyskinesia) From Screen to Week 25

For the subjective examination scoring is on a 4-point scale (0=Absent;1=Mild, 2=Moderate, 3=Severe). The evaluator takes into account the verbal report of the patient on: 1) the frequency and duration of the symptom during the day; 2) the number of days the symptom was present during the last week; and, 3) the subjective evaluation of the intensity of the symptom by the patient. Score for TD, ranging from 0 to 42, is based on the sum of all seven items in the TD objective examination. Higher scores indicate more severe symptomology. (NCT02085447)
Timeframe: Screen, Week 25

Interventionunits on a scale (Mean)
CAE-L1.4

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Change in DAI (Drug Attitudes Index) From Screen to Week 25

The DAI contains ten true-false items. Correct responses are scored as +1, while incorrect responses are scored as 0. The highest possible score is 10, while the lowest possible score is 0. Higher scores indicate better drug attitudes, while lower scores indicate worse drug attitudes. (NCT02085447)
Timeframe: Screen, Week 25

Interventionunits on a scale (Mean)
CAE-L8.5

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Change in CGI (Clinical Global Impression) From Screen to Week 25

The CGI evaluates global psychopathology illness severity on a 7 point Likert Scale (minimum score = 1; maximum score = 7) with higher scores indicating worse pathology. (NCT02085447)
Timeframe: Screen, Week 25

Interventionunits on a scale (Mean)
CAE-L2.9

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Change in BARS (Barnes Akathisia Rating Scale) From Screen to Week 25

This scale is used to measure the presence of akathisia, as may result from use of certain psychotropic medications. The scale contains four items and the score for each item is added to produce the total score. Total scores range from 0 to 14. Higher scores indicate more adverse outcomes. (NCT02085447)
Timeframe: Screen, Week 25

Interventionunits on a scale (Mean)
CAE-L.3

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Change in Tablets Routine Questionnaire (TRQ, Past Week) From Screen to Week 25 Visit

The Tablets Routine Questionnaire (TRQ) determines the proportion of prescribed medication taken and is not dependent upon timing of medication provided that medication is consumed within the required day/24 hour period. This rating has demonstrated statistically significant association with past non-adherence, repeated past non-adherence, any non-adherence in the past month, and non-adherence in the past week. The TRQ format will be modified slightly to document all adherence values (an exact proportion) for each item. TRQ scores ranges from perfect adherence (0% missed) to missing all medication (100% missed). An average TRQ was calculated for individuals on more than one BD medication. (NCT02085447)
Timeframe: Screen, Week 25

Interventionpercentage of adherence (Mean)
CAE-L56.2

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Change in SOFAS (Social and Occupational Functioning Assessment Scale) From Screen to Week 25

Evaluates social and occupational functioning on a scale of 0 (Inadequate information) to 100 (Superior functioning). It is a one-item measure. (NCT02085447)
Timeframe: Screen, Week 25

Interventionunits on a scale (Mean)
CAE-L63.1

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Change in SAS (Simpson Angus Scale) From Screen to Week 25

The Simpson-Angus Scale is used to monitor for neurological and musculoskeletal side effects that may be a result of certain psychotropic medications. The scale consists of 10 questions which each can be rated on a scale of 0 to 4. Scores for each item are added to produce a total score. Total scores range from 0 to 40. Higher scores indicate more adverse outcomes. (NCT02085447)
Timeframe: Screen, Week 25

Interventionunits on a scale (Mean)
CAE-L0.0

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Change in PANSS (Positive and Negative Syndrome Scale; Positive Symptoms Scale) From Screen to Week 25

The PANSS is used to assess patients for positive and negative symptoms of schizophrenia or schizoaffective disorder. The Positive Symptoms Subscale consists of 7 questions. Each item is rated on a scale of 1 (Absent) to 7 (Extreme). Total scores for the Positive Symptoms Subscale range from 7-49. Higher scores indicate more symptoms of psychopathology. There is no aggregate score for this measure, as the subscales are to be scored separately. (NCT02085447)
Timeframe: Screen, Week 25

Interventionunits on a scale (Mean)
CAE-L21.2

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Change in PANSS (Positive and Negative Syndrome Scale; Negative Symptoms Scale) From Screen to Week 25

The PANSS is used to assess patients for positive and negative symptoms of schizophrenia or schizoaffective disorder. The Negative Symptoms Subscale consists of 7 questions. Each item is rated on a scale of 1 (Absent) to 7 (Extreme). Total scores for the Negative Symptoms Subscale range from 7-49. Higher scores indicate more symptoms of psychopathology. There is no aggregate score for this measure, as the subscales are to be scored separately. (NCT02085447)
Timeframe: Screen, Week 25

Interventionunits on a scale (Mean)
CAE-L12.1

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Change in ESRS-A (Extrapyramidal Symptoms Scale-Abbreviated; Parkinsonism) From Screen to Week 25

For the subjective examination scoring is on a 4-point scale (0=Absent;1=Mild, 2=Moderate, 3=Severe). The evaluator takes into account the verbal report of the patient on: 1) the frequency and duration of the symptom during the day; 2) the number of days the symptom was present during the last week; and, 3) the subjective evaluation of the intensity of the symptom by the patient. The score for Parkinsonism (including akathisia), ranges from 0 to 102 (17 items), and is based on all items of the Parkinsonism examination: tremor (0-48), gait and posture (0-6), postural stability (0-6), rigidity (0-24), expressive automatic movements (0-6), bradykinesia (0-6), akathisia (0-6). Higher scores indicate more severity. (NCT02085447)
Timeframe: Screen, Week 25

Interventionunits on a scale (Mean)
CAE-L0.0

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Brief Assessments of Cognition in Schizophrenia Scores (BACS)

"Mean of cognition was assessed by BACS, which measures neurocognitive function in schizophrenia. BACs is a validated, composite measure of cognition which is used in schizophrenia. It is composed of Verbal memory (range: 0-75), Working memory (range: 0-28), Motor speed (range: 0-100), Verbal Fluency (number of words generated), Information processing (range: 0-110) and Executive functions (range: 0-22).~Higher z-scores indicate a better performance and outcome. BACS composite score are represented as z-scores which can be positive or negative. There is no minimum or maximum as this is a continuous measure." (NCT02199743)
Timeframe: Baseline and 4 weeks

,
InterventionBACS composite score (z score) (Mean)
Baseline (week 0)week 4
Lurasidone-1.596573107-2.002433521
Non-Lurasidone-1.933853656-1.500292967

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Cerebral Glutamate Levels

"Mean values of cerebral glutamate levels was measured by high resolution 3T magnetic resonance spectroscopy (MRS) in the anterior cingulate cortex (ACC). Data were acquired from the dorsal anterior cingulate cortex (ACC) using single voxel localized PRESS (TE1, TE2) = (32, 65) ms with an 8-channel head coil in a 3T whole-body scanner (Philips Medical Systems). Voxel size was 30x20x15 mm3 (9 mL) and were placed over the bilateral anterior cingulate cortex (ACC). All values are normalized to water.~More negative values represent less cerebral glutamate levels." (NCT02199743)
Timeframe: Baseline and 4 weeks

,
Interventionrelative unit (RU as compared to water) (Mean)
Baseline (week 0)week 4
Lurasidone-1.434662171-1.412294235
Non-Lurasidone-1.933853656-1.838991525

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Betting Behaviour in Laboratory-based Slot Machine Game

Risk taking was operationally defined as credits wagered per spin (mean computed for total spins) (NCT02203786)
Timeframe: 1x per test session (total of 4 test sessions) for duration of the study: 4 weeks (1 session/week)

,,,
Interventioncredits/spin on slot machine (Mean)
Mean bet under drugMean bet under placebo
Fluphenazine - Controls14.412.2
Fluphenazine - Pathological Gamblers16.016.1
Haloperidol - Controls11.69.5
Haloperidol - Pathological Gamblers12.810.4

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Subjective Reinforcement Self-report Scales

Self-reported Confidence to Refrain from Gambling (0 - 10) was assessed at test session baseline, before the slot machine and after the slot machine (Phase 1); and before amphetamine and at peak amphetamine (Phase 2). The maximum score (10) denotes complete confidence to refrain from gambling (i.e., NO urge or compulsion to gamble); the minimum score (0) denotes complete lack of confidence to refrain from gambling (i.e., overwhelming urge to gamble). Scores between 10 and 0 denote intermediate confidence to refrain from gambling with LOWER scores denoting less confidence to refrain from gambling -- i.e., GREATER urge or compulsive motivation to gamble. Scores shown are based on single item visual analogue ratings 0-10 from each participant at the specified time point. The mean (SD) of these single item ratings is presented for each sub-group. (NCT02203786)
Timeframe: At key points in testing: immediately after the slot machine game, and at expected peak subjective-behavioral effects for amphetamine (90-minutes post-capsule administration).

,,,
Interventionunits on a scale (Mean)
Drug - Confidence not to gamble after slot machinePlacebo - Confidence not to gamble after slot machDrug - Confidence not to gamble at peak amphetaminPlac -Confidence not to gamble at peak amphetamine
Fluphenazine - Controls9.38.29.89.3
Fluphenazine - Pathological Gamblers4.84.86.45.7
Haloperidol - Controls9.599.89.4
Haloperidol - Pathological Gamblers4.84.25.25.5

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Speed of Play on Slot Machine Game

Number of individual spins in a 15-minute slot machine game. Each spin corresponds to one wager. (NCT02203786)
Timeframe: 15-minutes

,,,
Interventionindividual spins/15-minutes (Mean)
Spins/15-minutes under DrugSpins/15-minutes under Placebo
Fluphenazine - Controls71.866.7
Fluphenazine - Pathological Gamblers78.568.4
Haloperidol - Controls66.472.2
Haloperidol - Pathological Gamblers76.988.6

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Diastolic Blood Pressure (DBP)

Measure changes from baseline, especially physiologic reactivity to the slot machine and amphetamine. (NCT02203786)
Timeframe: At key points in testing: immediately after the slot machine game (change from session baseline), and at expected peak subjective-behavioral effects for amphetamine (90-minutes post-capsule administration)(change from session baseline).

,,,
Interventionmm Hg (Mean)
Drug-Change in DBP pre-to-post slot machinePlacebo-Change in DBP pre-to-post slot machineDrug-Change in DBP pre-amphetamine to peak amphPlacebo-Change in DBP pre-amphetamine to peak amp
Fluphenazine - Controls23.61932.736.3
Fluphenazine - Pathological Gamblers2221.632.135.2
Haloperidol - Controls15.119.128.526.6
Haloperidol - Pathological Gamblers20.222.527.233.6

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Cognitive Task Performance

Response time to words (gambling, alcohol, positive affect, negative affect) as a percentage of neutral categorized words (parts of a building). This provides an index of the relative salience of stimuli from these four categories against a baseline of reaction to words with no clinical relevance or emotional valence. Smaller scores indicate faster relative response time to the test stimuli vs. neutral stimuli (i.e., greater salience) (NCT02203786)
Timeframe: At key points during testing: immediately after the slot machine, at expected peak subjective-behavioral effects for amphetamine (90-minutes post-capsule administration)

,,,
Interventionpercentage of neutral categorized words (Mean)
post-slots-GAM words under drugpost-slots-ALC words under drugpost-slots POS words under drugpost-slots NEG words under drugpost-slots GAM words under placebopost-slots ALC words under placebopost-slots POS words under placebopost-slots NEG words under placebopeak AMPH GAM words under drugpeak AMPH ALC words under drugpeak AMPH POS words under drugpeak AMPH NEG words under drugpeak AMPH GAM words under placebopeak AMPH ALC words under placebopeak AMPH POS words under placebopeak AMPH NEG words under placebo
Fluphenazine - Controls91.093.188.387.992.193.386.884.797.0100.396.398.796.997.595.196.7
Fluphenazine - Pathological Gamblers94.098.195.396.595.099.094.997.295.899.598.799.497.999.997.7100.0
Haloperidol - Controls94.896.593.789.697.297.093.792.398.199.197.296.896.8100.297.898.1
Haloperidol - Pathological Gamblers91.695.591.389.191.694.892.793.096.7101.298.299.595.099.998.499.0

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Winnings on Slot Machine Upon Completion of Game

Credits (NCT02203786)
Timeframe: 15-minutes

,,,
Interventioncredits (Mean)
Winnings (Final Credit Tally) under drugWinnings (Final Credit Tally) under Placebo
Fluphenazine - Controls544.3215
Fluphenazine - Pathological Gamblers277.8140.8
Haloperidol - Controls449.1339.2
Haloperidol - Pathological Gamblers239562.4

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Efficacy of Low-dose Haloperidol in Reducing Days With Delirium

Test the efficacy of low dose haloperidol in reducing the number of days with delirium among patients who are status post esophagectomy, pneumonectomy or thoracotomy compared to placebo. (NCT02213900)
Timeframe: Up to 30 days

InterventionDays with Delirium (Mean)
Haloperidol0.3
Placebo0.5

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Efficacy of Low-dose Haloperidol in Reducing Delirium Incidence

Test the efficacy of low dose haloperidol in reducing delirium incidence among patients who are status post esophagectomy, pneumonectomy or thoracotomy compared to placebo. (NCT02213900)
Timeframe: Up to 30 days

InterventionParticipants (Count of Participants)
Haloperidol15
Placebo19

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Efficacy of Low-dose Haloperidol in Reducing Cognitive Impairment at Post-operative Follow-up

Test the efficacy of low dose haloperidol in reducing cognitive impairment at post-operative follow-up among patients who are status post esophagectomy, pneumonectomy or thoracotomy compared to placebo. Cognitive status is assessed using the Repeatable Battery for the Assessment of Neuropsychological Status (RBANS). The RBANS measures attention, language, visuospatial/constructional abilities, and memory. It is made up of 12 subtests. The subtests produce 5 index scores and a total scale score. All the subtest scores are summed to calculate a Total Index score. The Total Index score is presented. The Total Index score scale is from 0-100 with higher scores indicating less cognitive impairment. (NCT02213900)
Timeframe: Up to 3 months after hospital discharge on average.

,
InterventionUnits on a scale (Mean)
Baseline RBANS Total Score3 Month RBANS Total Score
Haloperidol31.731.8
Placebo30.122.7

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Efficacy of Low-dose Haloperidol in Reducing ICU and Hospital Length of Stay

Test the efficacy of low dose haloperidol in reducing ICU and hospital length of stay among patients who are status post esophagectomy or pneumonectomy compared to placebo. (NCT02213900)
Timeframe: Date of hospital admission through date of hospital discharge, up to 3 weeks on average.

,
InterventionDays (Mean)
ICU Length of StayOverall Length of Stay
Haloperidol2.59.3
Placebo2.810.2

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Intensity of Delirium as Measured by the Intensive Care Delirium Screening Checklist (ICDSC) Delirium Severity Scale

The items include the assessment of: (1) consciousness ( deep sedation/coma, agitation, normal wakefulness, or light sedation); (2) inattention; (3) disorientation; (4) hallucination, delusion, or psychosis; (5) psychomotor agitation or retardation; (6) inappropriate speech or mood; (7) sleep-wake cycle disturbances; and (8) fluctuation of symptomatology. The maximum score is eight; scores of ≥4 indicate the presence of delirium and score zero is indicate not in delirium. Each item is scored 0-8. (NCT02343575)
Timeframe: Up to 5 days

Interventionscore on a scale (Mean)
Valproic Acid5
Placebo4

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Length of Hospital Stay

Participation in the study ended once delirium was resolved and the patient was off study drug. This outcome presents the total length of hospital stay, which may have been longer than participation in the study. (NCT02343575)
Timeframe: During expected average hospitalization (of 1 month)

Interventiondays (Mean)
Valproic Acid4
Placebo8

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Time to Delirium Resolution

Delirium resolution was defined as three negative Confusion Assessment Method (CAM) assessments, performed by nurses every 12 hours. (NCT02343575)
Timeframe: Up to 5 days

Interventiondays (Mean)
Valproic Acid2
Placebo1.5

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Use of as Needed Anti-psychotic Agent

Amount of Haldol administered. (NCT02343575)
Timeframe: Up to 5 days

Interventionmg (Mean)
Valproic Acid0
Placebo1

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Side Effects From Medications

Side effects may have included liver function test (LFT) increase, platelet decrease, bleeding, or QTc prolongation. (NCT02343575)
Timeframe: Up to 5 days

,
InterventionParticipants (Count of Participants)
LFT increasePlatelet decreaseBleedingQTc prolongation
Placebo0001
Valproic Acid0000

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Part 3 (EDP): Change From Baseline in Speed of Processing Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess speed of processing score of participants. The range of speed of processing score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP2.5
Part 3-OAP to OAP4.9

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Part 2 (Disease Progression): Change From Baseline in Adjusted Intracortical Myelin (ICM) Fraction Score as Measured by Inversion Recovery (IR) and Spin Echo Magnetic Resonance Imaging (MRI)

"The adjusted ICM fraction score is quantified as: 1. The volume of myelinated brain tissue is measured separately on co-localized IR and proton density (PD) MRI images, by outlining the boundary between gray matter and white matter on each image. 2. ICM is calculated from the difference of IR volume minus PD volume. 3. ICM is then expressed as a fraction of the total intracranial volume (ICM divided by intracranial volume). 4. The ICM fraction is then adjusted for effects of age, gender, and race/ethnicity in the sample of treated participants and healthy controls. A decrease in the adjusted ICM fraction score may be a sign of disease progression." (NCT02431702)
Timeframe: Baseline and Day 260

Interventionratio (Mean)
Part-2: Paliperidone Palmitate (PP)-0.001
Part-2: OAP-0.004

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Part 2 (Disease Progression): Change From Baseline in Attention/Vigilance Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess attention/vigilance score of participants. The range of attention/vigilance score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part-2: Paliperidone Palmitate (PP)3.2
Part-2: OAP0.7

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Part 2 (Disease Progression): Change From Baseline in Clinical Global Impression Severity (CGI-S) Score

"The Clinical Global Impression Severity (CGI-S) rating scale is used to rate the severity of a participant's overall clinical condition on a 7 point scale. The score ranges from 1 to 7, where 1 is equivalent to Normal, not at all ill and a rating of 7 is equivalent to Among the most extremely ill participants. Higher scores indicate worsening." (NCT02431702)
Timeframe: Baseline, up to 9 Months of Part 2

Interventionunits on a scale (Mean)
Part-2: Paliperidone Palmitate (PP)-0.2
Part-2: OAP-0.3

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Part 2 (Disease Progression): Change From Baseline in Cognition as Measured by the MATRICS Consensus Cognitive Battery (MCCB) Composite Score

The MATRICS Consensus Cognitive Battery is an instrument that contains 10 tests to measure cognitive performance in 7 cognitive domains: speed processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition. The composite score combines the individual scores of the 10 tests and scores them on a normative scale to derive a T-score and composites scores. The range of T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Month 9

InterventionT-score (Least Squares Mean)
Part-2: Paliperidone Palmitate (PP)2.0
Part-2: OAP2.8

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Part 2 (Disease Progression): Change From Baseline in Functioning as Measured by the Personal and Social Performance (PSP) Total Score

The Personal and Social Performance (PSP) scale assesses degree of a participant's dysfunction within 4 domains of behavior: 1) socially useful activities, 2) personal and social relationships, 3) self-care, and 4) disturbing and aggressive behavior. Each domain was assessed on a 6-point scale, from 1 (absent) to 6 (very severe) (1 = absent, 2 = mild, 3 = manifest, 4 = marked, 5 = severe, and 6 = very severe). PSP total score was calculated as sum of all the domain scores and ranges from 1 to 100. Participants with score of 71 to 100 have mild degree of difficulty; from 31 to 70, varying degrees of disability; less than or equal to 30, functioning so poorly as to require intensive supervision. Higher score indicate better performance. (NCT02431702)
Timeframe: Baseline and Month 9

Interventionunits on a scale (Mean)
Part-2: Paliperidone Palmitate (PP)2.5
Part-2: OAP2.9

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Part 2 (Disease Progression): Change From Baseline in Medication Satisfaction Questionnaire (MSQ) Total Score

The Medication Satisfaction Questionnaire (MSQ) is a 7-point, verbally administered, Likert-type scale rated as follows: 1=Extremely Dissatisfied, 2=Very Dissatisfied, 3=Somewhat Dissatisfied, 4=Neither Satisfied Nor Dissatisfied, 5=Somewhat Satisfied, 6=Very Satisfied, 7=Extremely Satisfied. Worst value is 1 (Extremely Dissatisfied) and best value is 7 (Extremely Satisfied). Total score ranges from 1 to 7. Higher score indicate improvement. (NCT02431702)
Timeframe: Baseline and endpoint Part 2 (up to 9 Months)

Interventionunits on a scale (Mean)
Part-2: Paliperidone Palmitate (PP)-0.2
Part-2: OAP0.1

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Part 2 (Disease Progression): Change From Baseline in Reasoning and Problem Solving: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess reasoning and problem solving of participants. The range of reasoning and problem solving T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part-2: Paliperidone Palmitate (PP)0.2
Part-2: OAP2.8

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Part 2 (Disease Progression): Change From Baseline in Social Cognition Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess social cognition score of participants. The range of social cognition score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part-2: Paliperidone Palmitate (PP)0.3
Part-2: OAP1.6

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Part 2 (Disease Progression): Change From Baseline in Speed of Processing Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess speed of processing score of participants. The range of speed of processing T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part-2: Paliperidone Palmitate (PP)1.8
Part-2: OAP3.5

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Part 2 (Disease Progression): Change From Baseline in Verbal Learning Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess verbal learning score of participants. The range of verbal learning score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part-2: Paliperidone Palmitate (PP)1.3
Part-2: OAP1.0

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Part 2 (Disease Progression): Change From Baseline in Visual Learning Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess visual learning score of participants. The range of visual learning score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part-2: Paliperidone Palmitate (PP)1.3
Part-2: OAP1.4

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Part 3 (Disease Modification): Change From Baseline in Adjusted Intracortical Myelin Fraction Score as Measured by Inversion Recovery (IR) and Spin Echo Magnetic Resonance Imaging (SE MRI)

"The adjusted ICM fraction score is quantified as: 1. The volume of myelinated brain tissue is measured separately on co-localized IR and proton density (PD) MRI images, by outlining the boundary between gray matter and white matter on each image. 2. ICM is calculated from the difference of IR volume minus PD volume. 3. ICM is then expressed as a fraction of the total intracranial volume (ICM divided by intracranial volume). 4. The ICM fraction is then adjusted for effects of age, gender, and race/ethnicity in the sample of treated participants and healthy controls. A decrease in the adjusted ICM fraction score may be a sign of disease progression." (NCT02431702)
Timeframe: Baseline and Month 9 of Part 3

Interventionratio (Least Squares Mean)
Part 3-PP to PP-0.7
Part 3- OAP to PP (or Delayed-Start PP)-0.2
Part 3-OAP to OAP0.5

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Part 3 (Disease Modification): Change From Baseline in Cognition as Measured by the MATRICS Consensus Cognitive Battery (MCCB) Composite Score

The MATRICS Consensus Cognitive Battery is an instrument that contains 10 tests to measure cognitive performance in 7 cognitive domains: speed processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition. The composite score combines the individual scores of the 10 tests and scores them on a normative scale to derive a T-score and composites scores. The range of T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part 3- PP to PP-0.7
Part 3- OAP to PP (or Delayed-Start PP)-0.2
Part 3-OAP to OAP0.5

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Part 3 (Disease Modification): Personal and Social Performance (PSP) Total Observed Score

The Personal and Social Performance (PSP) scale assesses degree of a participant's dysfunction within 4 domains of behavior: 1) socially useful activities, 2) personal and social relationships, 3) self-care, and 4) disturbing and aggressive behavior. Score ranges from 1 to 100, divided into 10 equal intervals to rate degree of difficulty (1 = absent, 2 = mild, 3 = manifest, 4 = marked, 5 = severe, and 6 = very severe) in each of the 4 domains. Based on 4 domains there will be 1 transformed total score. Participants with score of 71 to 100 have mild degree of difficulty; from 31 to 70, varying degrees of disability; less than or equal to 30, functioning so poorly as to require intensive supervision. (NCT02431702)
Timeframe: Month 9 of Part 3

Interventionunits on a scale (Least Squares Mean)
Part 3-PP to PP67.6
Part 3- OAP to PP (or Delayed-Start PP)66.1
Part 3-OAP to OAP66.6

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Part 3 (EDP): Change From Baseline in Adjusted Intracortical Myelin Fraction Score as Measured by Inversion Recovery (IR) and Spin Echo Magnetic Resonance Imaging (MRI)

"The adjusted ICM fraction score is quantified as: 1. The volume of myelinated brain tissue is measured separately on co-localized IR and proton density (PD) MRI images, by outlining the boundary between gray matter and white matter on each image. 2. ICM is calculated from the difference of IR volume minus PD volume. 3. ICM is then expressed as a fraction of the total intracranial volume (ICM divided by intracranial volume). 4. The ICM fraction is then adjusted for effects of age, gender, and race/ethnicity in the sample of treated participants and healthy controls. A decrease in the adjusted ICM fraction score may be a sign of disease progression." (NCT02431702)
Timeframe: Baseline and 18 Months

Interventionratio (Mean)
Part 3-PP to PP-0.001
Part 3-OAP to OAP-0.003

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Part 3 (EDP): Change From Baseline in Attention/Vigilance Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess attention/vigilance score of participants. The range of attention/vigilance score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP2.4
Part 3-OAP to OAP0.7

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Part 3 (EDP): Change From Baseline in Clinical Global Impression Severity (CGI-S) Score

"The Clinical Global Impression Severity (CGI-S) rating scale is used to rate the severity of a participant's overall clinical condition on a 7 point scale. The total score ranges from 1 to 7, where 1 is equivalent to Normal, not at all ill and a rating of 7 is equivalent to Among the most extremely ill participants. Higher scores indicate worsening." (NCT02431702)
Timeframe: Baseline, up to 18 Months

Interventionunits on a scale (Mean)
Part 3-PP to PP-0.7
Part 3-OAP to OAP-0.7

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Part 2 (Disease Progression): Number of Participants With Change From Baseline in Severity of Psychotic Symptoms, as Measured by Clinician-Rated Dimensions of Psychosis Symptom Severity Scale (CRDPSS)

The CRDPSS is an 8-item measure that assesses the severity of mental health symptoms that are important across psychotic disorders, including delusions, hallucinations, disorganized speech, abnormal psychomotor behavior, negative symptoms. Each item on the measure is rated on a 5-point scale (0=none; 1=equivocal; 2=present, but mild; 3=present and moderate; and 4=present and severe). Total Score is taken as summation. A higher score indicates a more severe condition. Worsened or improved is defined as increase or decrease compared to baseline. (NCT02431702)
Timeframe: Baseline, up to 9 Months

InterventionParticipants (Count of Participants)
Hallucinations72513608Hallucinations72513614Delusions72513614Delusions72513608Disorganized Speech72513614Disorganized Speech72513608Abnormal Psychomotor Behavior72513614Abnormal Psychomotor Behavior72513608Negative Symptoms72513608Negative Symptoms72513614Impaired Cognition72513614Impaired Cognition72513608Mania72513608Mania72513614Depression72513608Depression72513614
UnchangedImprovedWorsened
Part-2: OAP19
Part-2: Paliperidone Palmitate (PP)29
Part-2: OAP73
Part-2: Paliperidone Palmitate (PP)14
Part-2: OAP33
Part-2: Paliperidone Palmitate (PP)10
Part-2: OAP20
Part-2: Paliperidone Palmitate (PP)23
Part-2: OAP70
Part-2: OAP35
Part-2: OAP13
Part-2: Paliperidone Palmitate (PP)36
Part-2: OAP85
Part-2: Paliperidone Palmitate (PP)12
Part-2: OAP27
Part-2: Paliperidone Palmitate (PP)9
Part-2: OAP14
Part-2: Paliperidone Palmitate (PP)37
Part-2: OAP86
Part-2: Paliperidone Palmitate (PP)4
Part-2: OAP25
Part-2: Paliperidone Palmitate (PP)16
Part-2: OAP61
Part-2: Paliperidone Palmitate (PP)17
Part-2: OAP39
Part-2: Paliperidone Palmitate (PP)13
Part-2: OAP29
Part-2: Paliperidone Palmitate (PP)22
Part-2: OAP52
Part-2: Paliperidone Palmitate (PP)15
Part-2: OAP44
Part-2: Paliperidone Palmitate (PP)1
Part-2: OAP7
Part-2: Paliperidone Palmitate (PP)47
Part-2: OAP107
Part-2: Paliperidone Palmitate (PP)2
Part-2: OAP11
Part-2: Paliperidone Palmitate (PP)7
Part-2: OAP28
Part-2: Paliperidone Palmitate (PP)33
Part-2: OAP74
Part-2: OAP23

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Part 3 (EDP): Number of Participants With Change From Baseline in Severity of Psychotic Symptoms, as Measured by CRDPSS

The CRDPSS is an 8-item measure that assesses the severity of mental health symptoms that are important across psychotic disorders, including delusions, hallucinations, disorganized speech, abnormal psychomotor behavior, negative symptoms. Each item on the measure is rated on a 5-point scale (0=none; 1=equivocal; 2=present, but mild; 3=present and moderate; and 4=present and severe). Total Score is taken as summation. A higher score indicates a more severe condition. Worsened or improved is defined as increase or decrease compared to baseline. (NCT02431702)
Timeframe: Baseline, up to 18 Months

InterventionParticipants (Count of Participants)
Hallucinations72513609Hallucinations72513610Delusions72513609Delusions72513610Disorganized Speech72513609Disorganized Speech72513610Abnormal Psychomotor Behavior72513609Abnormal Psychomotor Behavior72513610Negative Symptoms72513609Negative Symptoms72513610Impaired Cognition72513609Impaired Cognition72513610Mania72513609Mania72513610Depression72513609Depression72513610
WorsenedUnchangedImproved
Part 3-PP to PP3
Part 3-OAP to OAP8
Part 3-PP to PP27
Part 3-OAP to OAP29
Part 3-PP to PP11
Part 3-OAP to OAP10
Part 3-PP to PP6
Part 3-PP to PP21
Part 3-OAP to OAP20
Part 3-PP to PP14
Part 3-OAP to OAP17
Part 3-PP to PP2
Part 3-OAP to OAP36
Part 3-PP to PP12
Part 3-PP to PP4
Part 3-OAP to OAP2
Part 3-PP to PP32
Part 3-OAP to OAP37
Part 3-PP to PP5
Part 3-OAP to OAP4
Part 3-OAP to OAP22
Part 3-PP to PP19
Part 3-OAP to OAP21
Part 3-PP to PP10
Part 3-OAP to OAP9
Part 3-OAP to OAP23
Part 3-PP to PP17
Part 3-OAP to OAP15
Part 3-PP to PP0
Part 3-OAP to OAP3
Part 3-PP to PP40
Part 3-OAP to OAP39
Part 3-PP to PP1
Part 3-OAP to OAP5
Part 3-PP to PP7
Part 3-OAP to OAP6
Part 3-PP to PP26
Part 3-PP to PP8
Part 3-OAP to OAP12

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Part 2 (Disease Progression): Change From Baseline in Working Memory Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess working memory of participants. The range of working memory score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part-2: Paliperidone Palmitate (PP)-0.2
Part-2: OAP-0.8

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Part-2 (Disease Progression): Time to First Treatment Failure

Treatment failure is defined as the time from participant's randomization to first treatment failure, which was a composite endpoint consisting of any of the following: 1) Psychiatric hospitalization due to worsening symptoms; 2) Any deliberate self-injury, suicidal ideation or behavior, homicidal ideation or violent behavior that is clinically significant and needs immediate intervention as determined by the study physician; 3) New arrest/incarceration; 4) Discontinuation of antipsychotic treatment due to inadequate efficacy as determined by the study physician; 5) Discontinuation of antipsychotic treatment due to safety or tolerability as determined by the study physician; 6) Treatment supplementation with another antipsychotic due to inadequate efficacy as determined by the study physician; 7) Increase in the level of psychiatric services in order to prevent imminent psychiatric hospitalization as determined by the study physician. (NCT02431702)
Timeframe: From Day 1 up to 9 Months

Interventiondays (Median)
Part-2: Paliperidone Palmitate (PP)NA
Part-2: OAPNA

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Part 3 (Extended Disease Progression [EDP]): Change From Baseline in Cognition as Measured by the MATRICS Consensus Cognitive Battery (MCCB) Composite Score

The MATRICS Consensus Cognitive Battery is an instrument that contains 10 tests to measure cognitive performance in 7 cognitive domains: speed processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition. The composite score combines the individual scores of the 10 tests and scores them on a normative scale to derive a T-score and composites scores. The range of T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP1.6
Part 3-OAP to OAP3.2

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Part 3 (EDP): Time to First Treatment Failure

Treatment failure is defined as the time from participant's randomization to first treatment failure, which was a composite endpoint consisting of any of the following: 1) Psychiatric hospitalization due to worsening symptoms; 2) Any deliberate self-injury, suicidal ideation or behavior, homicidal ideation or violent behavior that is clinically significant and needs immediate intervention as determined by the study physician; 3) New arrest/incarceration; 4) Discontinuation of antipsychotic treatment due to inadequate efficacy as determined by the study physician; 5) Discontinuation of antipsychotic treatment due to safety or tolerability as determined by the study physician; 6) Treatment supplementation with another antipsychotic due to inadequate efficacy as determined by the study physician; 7) Increase in the level of psychiatric services in order to prevent imminent psychiatric hospitalization as determined by the study physician. (NCT02431702)
Timeframe: From Day 1 Up to 18 Months

Interventiondays (Median)
Part 3-PP to PPNA
Part 3-OAP to OAPNA

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Part 3 (EDP): Change From Baseline in Working Memory Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess working memory of participants. The range of working memory score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP-1.7
Part 3-OAP to OAP0.7

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Part 3 (EDP): Change From Baseline in Visual Learning Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess visual learning score of participants. The range of visual learning score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP0.2
Part 3-OAP to OAP-0.2

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Part 3 (EDP): Change From Baseline in Verbal Learning Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess verbal learning score of participants. The range of verbal learning score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP0.3
Part 3-OAP to OAP0.8

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Part 3 (EDP): Change From Baseline in Social Cognition Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess social cognition score of participants. The range of social cognition score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP-0.2
Part 3-OAP to OAP1.4

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Part 3 (EDP): Change From Baseline in Reasoning and Problem Solving: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess reasoning and problem solving score of participants. The range of reasoning and problem solving T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP3.4
Part 3-OAP to OAP4.7

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Part 3 (EDP): Change From Baseline in Medication Satisfaction Questionnaire (MSQ) Score

The Medication Satisfaction Questionnaire (MSQ) is a 7-point, verbally administered, Likert-type scale rated as follows: 1=Extremely Dissatisfied, 2=Very Dissatisfied, 3=Somewhat Dissatisfied, 4=Neither Satisfied Nor Dissatisfied, 5=Somewhat Satisfied, 6=Very Satisfied, 7=Extremely Satisfied. Worst value is 1 (Extremely Dissatisfied) and best value is 7 (Extremely Satisfied). Total score ranges from 1 to 7. Higher score indicate improvement. (NCT02431702)
Timeframe: Baseline, up to 18 Months

Interventionunits on a scale (Mean)
Part 3-PP to PP0.3
Part 3-OAP to OAP0.4

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Part 3 (EDP): Change From Baseline in Functioning as Measured by the Personal and Social Performance (PSP) Total Score

The Personal and Social Performance (PSP) scale assesses degree of a participant's dysfunction within 4 domains of behavior: 1) socially useful activities, 2) personal and social relationships, 3) self-care, and 4) disturbing and aggressive behavior. Each domain was assessed on a 6-point scale, from 1 (absent) to 6 (very severe) (1 = absent, 2 = mild, 3 = manifest, 4 = marked, 5 = severe, and 6 = very severe). PSP total score was calculated as sum of all the domain scores and ranges from 1 to 100. Participants with score of 71 to 100 have mild degree of difficulty; from 31 to 70, varying degrees of disability; less than or equal to 30, functioning so poorly as to require intensive supervision. Higher score indicate better performance. (NCT02431702)
Timeframe: Baseline and 18 Months

Interventionunits on a scale (Mean)
Part 3-PP to PP7.5
Part 3-OAP to OAP7.0

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Adherence to PONV Guidelines

PONV guideline adherence: percentage of patients who received the exact number of prophylactic interventions for PONV that were recommended by the decision support. (NCT02625181)
Timeframe: A specific time frame on the day of surgery: the start of admission at the holding room to the end of the anesthetic case

InterventionParticipants (Count of Participants)
Baseline Measurement666
CDS Email Recommendations5260
CDS Email + Real TIme Recommenations5863

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PONV Incidence: Number of Participants With Postoperative Nausea and Vomiting

The occurrence of PONV, as defined by the administration of antiemetics in the PACU between admission to PACU and discharge from PACU. (NCT02625181)
Timeframe: PACU recovery period

InterventionParticipants (Count of Participants)
Baseline Measurement139
CDS Email Recommendations1323
CDS Email + Real TIme Recommenations1343

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The Number of Prophylactic Interventions for PONV

the absolute number of prophylactic interventions applied between the admission of the patient in the holding room until admission to the PACU. (NCT02625181)
Timeframe: A specific time frame on the day of surgery: from the start of admission at the holding room to the end of the anesthetic case

Interventionprophylactic antiemetics administered (Mean)
Baseline Measurement2.196
CDS Email Recommendations2.176
CDS Email + Real TIme Recommenations2.129

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Time to Discharge From the Postanesthesia Care Unit (PACU)

This is the number of minutes from admission to the PACU until discharge, assessed up to 2 days (NCT02625181)
Timeframe: A specific time frame on the day of surgery: from the start of admission to the PACU to discharge from the PACU

Interventionminutes (Mean)
Baseline Measurement266
CDS Email Recommendations264
CDS Email + Real TIme Recommenations266

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Change in Pain Score According to the Numeric Pain Intensity Scale

Numeric Pain Intensity scale is a standard rating tool for pain, ranging from 0-10, with 0=no pain and 10=worst pain imaginable. (NCT02972502)
Timeframe: Change from baseline (prior to treatment) to 1 hour post treatment (1 hour)

Interventionunits on a scale (Mean)
Metoclopramide (Reglan)-2.86
Haloperidol (Haldol)-5.13

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Number of Participants With Relapse

The definition of relapse is as follows 1.50% or greater increase in total DIEPSS score, 2. an increase in the total PANSS score of 25% or more from baseline, 3. deliberate self-injury, 4. emergence of clinically significant suicidal ideation, 5. violent behavior resulting in clinically significant injury to another person or property damage. (NCT03019887)
Timeframe: One year after the baseline cognitive function test or three months after the end of dose reduction, whichever came first.

InterventionParticipants (Count of Participants)
Dose Reduction130

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Perceived Comfort Level as Assessed by Caregiver

"On day 1 (after initiation of blinded treatment), we asked the blinded caregivers to provide their overall impression of change in patient comfort level and the agitation level. The response ranged from strongly agree, agree, neutral, disagree, and strongly disagree. In this study, strongly agree and agree were combined for analysis. The participants who reported 'Agree' and 'Strongly Agree' responses to perceived comfort level have a high level of comfort (more comfortable). And similarly, the participants who reported 'Agree' and 'Strongly Agree' responses to perceived agitation level have a low level of agitation (less agitated)." (NCT03021486)
Timeframe: Baseline and 24 hour

,,
InterventionParticipants (Count of Participants)
Perceived To Have A High Level of Comfort (More Comfortable)Perceived To Have A Low Level of Agitation (Less Agitated)
Combination Group66
Escalation Group89
Rotation Group1010

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Memorial Delirium Assessment Scale (MDAS)

The Memorial Delirium Assessment Scale (MDAS) is a 10-item clinician-rated assessment scale validated for assessment of delirium in cancer patients. It examines the level of consciousness, disorientation, memory, recall, attention, disorganized thinking, perceptual disturbance, delusions, psychomotor activity and sleep, assigning a score between 0 to 3, for a total score between 0-30. A total score of 13 or higher indicates delirium. We measured the change in Memorial Delirium Rating scale between baseline and 24 hours. (NCT03021486)
Timeframe: Baseline and 24 hours

Interventionscore on a scale (Mean)
Escalation Group-2.7
Rotation Group1
Combination Group0.3

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Change in Richmond Agitation Sedation Score (RASS) (0-24h)

RASS score is a 10-point scale with scores ranging from +4 (very combative, violent) to -5 (unarousable). The primary outcome was mean change in RASS score between time 0 (immediately before initiation of masked treatment) and 24 h later. The Richmond Agitation-Sedation Scale (RASS) was developed by a multidisciplinary team at Virginia Commonwealth University in Richmond; it is a validated method used to avoid oversedation in the Intensive Care Unit. (NCT03021486)
Timeframe: Time 0 or Baseline and 24 hours after study medication administration

Interventionscore on a scale (Mean)
Escalation Group-3.6
Rotation Group-3.3
Combination Group-3.0

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Percentage of Participants With RASS Score -2 to 0

RASS score is a 10-point scale with scores ranging from +4 (very combative, violent) to -5 (unarousable). The Secondary outcome was the percentage of participants with target RASS score of -2 to 0 within the first 24 hours. The Richmond Agitation-Sedation Scale (RASS) was developed by a multidisciplinary team at Virginia Commonwealth University in Richmond; it is a validated method used to avoid over sedation in the Intensive Care Unit. (NCT03021486)
Timeframe: Time 0 or Baseline and 24 hours later.

InterventionParticipants (Count of Participants)
Escalation Group2
Rotation Group3
Combination Group5

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Change in Delirium Experience Questionnaire

This 14-item questionnaire examines both the recalled frequency of 7 delirium symptoms and associated distress in the rater: disorientation to time, disorientation to place, visual hallucinations, tactile hallucinations, auditory hallucinations, delusional thoughts and psychomotor agitation. The score for recalled frequency ranges between 0 and 4, where 0=not present, 1=a little of the time, 2=some of the time, 3=good part of the time, and 4=most or all of the time. The score for distress in the rater related to each delirium symptom also ranges from 0 to 4, where 0=no distress, 1=a little, 2=a fair amount, 3=very much and 4=extremely distressed. Due to an error in the data collection form, the last category was omitted as a choice and thus the score only ranged from 0 to 3. (NCT03021486)
Timeframe: Baseline and Day 3

,,
Interventionscore on a scale (Mean)
Nursing assessment, disorientation to time - frequencyNursing assessment, disorientation to place - frequencyNursing assessment, visual hallucination - frequencyNursing assessment, tactile hallucination - frequencyNursing assessment, auditory hallucination - frequencyNursing assessment, delusional thoughts - frequencyNursing assessment, psychomotor agitation- frequencyNursing assessment, disorientation to time - distressNursing assessment, disorientation to place - distressNursing assessment, visual hallucination - distressNursing assessment, tactile hallucination - distressNursing assessment, auditory hallucination - distressNursing assessment, delusional thoughts - distressNursing assessment, psychomotor agitation - distress
Combination Group0.20.3-0.7-0.9-0.40.2-0.4-0.5-0.4-0.4-0.5-0.2-0.1-0.8
Escalation Group-0.8-0.9-1-0.4-0.1-0.8-1.2-0.3-0.3-0.6-0.5-0.3-0.6-0.8
Rotation Group-0.8-0.800.10.10-0.8-0.3-0.30.1000-0.5

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Edmonton Expression Assessment System, ESAS

Edmonton Symptom Assessment System (ESAS) has been validated and widely used in different clinical settings, including the acute palliative care unit. It assessed the average symptom intensity of 10 symptoms over the past 24 hours. Each symptom was assessed using an 11-point numeric rating scale, ranging from 0 (none) to 10 (worst). It was measured as change in ESAS as Perceived by Caregivers between baseline and day 1, mean. (NCT03021486)
Timeframe: Baseline and 24 hours

,,
Interventionscore on a scale (Mean)
PainFatigueNauseaDepressionAnxietyDrowsinessAppetiteFeeling of well being*Shortness of breathSleep
Combination Group-1.11-0.4-0.8-0.90.70.100-2.7
Escalation Group-1.3-0.50.1-1.4-1.5-0.2-0.30.20.8-2.7
Rotation Group-4.1-3-1.8-1.2-4.8-0.6-0.6-1.6-2.2-5.1

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Change in RASS Score (0-30 Minutes)

RASS score is a 10-point scale with scores ranging from +4 (very combative, violent) to -5 (unarousable). The secondary outcome was mean change in RASS score between time 0 (immediately before initiation of masked treatment) and 30 minutes later. The Richmond Agitation-Sedation Scale (RASS) was developed by a multidisciplinary team at Virginia Commonwealth University in Richmond; it is a validated method used to avoid over sedation in the Intensive Care Unit. (NCT03021486)
Timeframe: Time 0 or Baseline and 30 minutes later.

Interventionscore on a scale (Mean)
Escalation Group-2.6
Rotation Group-2.4
Combination Group-2.1

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Number of Participants With RASS Score of >=1

RASS score is a 10-point scale with scores ranging from +4 (very combative, violent) to -5 (unarousable). The secondary outcome was the proportion of breakthrough restlessness participants with a RASS score of >=1 during the first 24 hours. The Richmond Agitation-Sedation Scale (RASS) was developed by a multidisciplinary team at Virginia Commonwealth University in Richmond; it is a validated method used to avoid oversedation in the Intensive Care Unit. (NCT03021486)
Timeframe: 0 or Baseline and 24 hours later

InterventionParticipants (Count of Participants)
Escalation Group12
Rotation Group7
Combination Group9

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Perceived Comfort Level as Assessed by Nurse

"On day 1 (after initiation of blinded treatment), we asked the blinded caregivers to provide their overall impression of change in patient comfort level and the agitation level. The response ranged from strongly agree, agree, neutral, disagree, and strongly disagree. In this study, strongly agree and agree were combined for analysis. The participants who reported 'Agree' and 'Strongly Agree' responses to perceived comfort level have a high level of comfort (more comfortable). And similarly, the participants who reported 'Agree' and 'Strongly Agree' responses to perceived agitation level have a low level of agitation (less agitated)." (NCT03021486)
Timeframe: Baseline and 24 hour

,,
InterventionParticipants (Count of Participants)
Perceived To Have A High Level of Comfort (More Comfortable)Perceived To Have A Low Level of Agitation (Less Agitated)
Combination Group77
Escalation Group98
Rotation Group98

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Udvalg for Kliniske Undersogelser, UKU

We also documented the selected adverse effects associated with neuroleptics using the Udvalg for Kliniske Undersogelser (UKU) side effects rating scale. Specifically, we assessed 8 neurologic symptoms (dystonia, rigidity, hypokinesia/akinesia, hyperkinesia, tremor, akathisia, epileptic seizures, paraesthesias). We are reporting only the neurologic symptoms (tremor and akathisia) that had changes during the study. Each item was assigned a score by the research coordinator 0 (absent) to 3 (most severe) based on symptom severity of the last 3 days. (NCT03021486)
Timeframe: Baseline and 3 days

,,
InterventionParticipants (Count of Participants)
Tremor (decreased)Akathisia (decreased)
Combination Group11
Escalation Group00
Rotation Group00

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Pattern of Medication Use

Use of neuroleptics and benzodiazepines during the first 24 hours was retrieved from the Medication Administration Record. (NCT03021486)
Timeframe: Baseline and 24 hours

,,
InterventionParticipants (Count of Participants)
Need for study med dose escalation in first 24 hrsBenzodiazepine use in first 24 hrs (scheduled)Benzodiazepine use in first 24 hrs (as needed)
Combination Group704
Escalation Group410
Rotation Group100

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Side Effects and Tolerability of Haldol in Patients With Undergoing Hematopoietic Stem Cell Transplant

Categorize and quantify adverse events from start of drug (day 1) to end of study drug per (CTCAE) version 4.0 (NCT03489551)
Timeframe: Daily, up to 14 days following transplant

InterventionAdverse Event (Number)
Oral Haldol in Patients Undergoing HSCT1

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Time Patient Was Placed in Straitjacket/Restraint Post Intervention Treatment

If patient was placed in a straitjacket post intervention due to aggression - this would be noted on the outcomes form which includes a checklist at certain time intervals 20,40,60 and 120 minutes post intervention treatment. (NCT03639558)
Timeframe: 20, 40, 60 and 120 minutes post intervention treatment

,
InterventionParticipants (Count of Participants)
Restraints at 20 minutesRestraints at 40 minutesRestraints at 60 minutesRestraints at 120 minutes
Haloperidol + Promethazine161395
Haloperidol + Promethazine + Chlorpromazine171086

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Time Taken for Patient to Fall Asleep Post Intervention

Patient has fallen asleep and is no longer aggressive post intervention treatment and will be noted on the outcomes form which includes a checklist of different time intervals: 20, 40, 60 and 120 minutes post intervention treatment. (NCT03639558)
Timeframe: 20, 40, 60 and 120 minutes post intervention treatment

,
InterventionParticipants (Count of Participants)
Asleep at 20 minutesAsleep at 40 minutesAsleep at 60 minutesAsleep at 120 minutes
Haloperidol + Promethazine291018
Haloperidol + Promethazine + Chlorpromazine092524

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Time Noted Where Important Adverse Effects Occurred Post Intervention

If patient exhibits any adverse effects post intervention treatment, this will be noted within the time frames. (NCT03639558)
Timeframe: 20, 40, 60 and 120 minutes post intervention treatment

InterventionParticipants (Count of Participants)
Haloperidol + Promethazine + Chlorpromazine0
Haloperidol + Promethazine0

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Number of Participants According to the Time Taken for Aggressive Behaviour to Change to Calm and Tranquil

Patient no longer exhibiting aggressive behavior both verbal and physical post intervention treatment. A primary measure of outcome form will contain a Calm or Tranquil column followed by four rows: 20 mins, 40 mins, 60 mins and 120 mins post intervention medication. The boxes would be ticked depending if the patient meets the primary measure of outcome within the time frame provided. (NCT03639558)
Timeframe: 20, 40, 60 and 120 minutes post intervention treatment

,
Interventionparticipants (Number)
Calm or tranquil at 20 minutesCalm or tranquil at 40 minutesCalm or tranquil at 60 minutesCalm or tranquil at 120 minutes
Haloperidol + Promethazine14253535
Haloperidol + Promethazine + Chlorpromazine18414547

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ESRS-A Akathisia

Extrapyramidal Symptoms Scale-Abbreviated version for akathisia- drug-induced akathisia consists of inner restlessness and urge to move. Items are measured on a 4 value scale: 0=absent, 3=severe, and higher values indicate more severe akathisia and worse outcomes. (NCT04327843)
Timeframe: Baseline to 6 months(25 weeks)

Interventionscore on a scale (Mean)
BaselineWeek 25
CAE + LAI Treatment0.280.00

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ESRS-A Dyskinesia

Extrapyramidal Symptoms Scale-Abbreviated version for Dyskinesia- drug-induced dyskinesia which is repetitive and involuntary movements. Each item is rated on a 4 point scale: 0=absent, 3=severe and higher values indicate greater severity of dyskinesia and worse outcomes. (NCT04327843)
Timeframe: Baseline to 6 months(25 weeks)

Interventionscore on a scale (Mean)
BaselineWeek 25
CAE + LAI Treatment0.170.11

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ESRS-A Dystonia

Extrapyramidal Symptoms Scale-Abbreviated version for dystonia- drug-induced dystonia is a muscle disorder in which movements are jerky or twisting. Due to the 0.00 values at baseline and 25 weeks, unable to perform t-test and get a p value so no statistical analysis section is reported for this Outcome Measure. Each item is rated on a 4 point scale: 0=absent, 3=severe with the higher numbers indicating worse dystonia and worse outcomes. (NCT04327843)
Timeframe: Baseline to 6 months(25 weeks)

Interventionscore on a scale (Mean)
BaselineWeek 25
CAE + LAI Treatment0.000.00

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ESRS-A Parkinsonism

Extrapyramidal Symptoms Scale-Abbreviated version for Parkinsonism. It looks at drug-induced Parkinsonism which is made up of motor disturbances. Rigidity, tremor, reduced facial expression/speech, impaired gait/posture, postural instability, and bradykinesia. Each item is rated on a 4 point scale: 0=absent, 3=severe. The higher the value the more severe the Parkinsonism and worst outcomes. (NCT04327843)
Timeframe: Baseline to 6 months(25 weeks)

Interventionscore on a scale (Mean)
Baseline25 Weeks
CAE + LAI Treatment0.060.06

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Social and Occupational Functioning Scale (SOFAS)

The SOFAS measures social and occupational functioning independent of the overall severity of the individual's psychological symptoms. The minimum score is 0 and the maximum score is 100. A higher rating implies a higher level of functioning. (NCT04327843)
Timeframe: Baseline to 6 month visit

Interventionscore on a scale (Mean)
Baseline25 Weeks
CAE + LAI Treatment62.1768.39

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Tablets Routine Questionnaire (TRQ)

The TRQ evaluates adherence to medications via a brief self-report instrument that has been validated in populations with bipolar disorder medication adherence. The TRQ identifies nonadherent individuals, defined as those who miss 20-30% or more of their medication in the last week or month. Total scores are represented as a percentage and range from 0 to 100, with higher scores indicating a greater level of nonadherence (higher scores indicate worse adherence to medications). (NCT04327843)
Timeframe: Change from Baseline to 6 month visit

Interventionpercentage of change in adherence (Mean)
TRQ Week adherenceTRQ Month adherence
CAE + LAI Treatment-57-23

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Brief Psychiatric Rating Scale (BPRS)

The BPRS measures levels of mania. There are 24 items, scored on a 7-point scale ranging from 0 to 6. Total scores range from 0 to 42, with higher scores indicating higher levels of mania. (NCT04327843)
Timeframe: Baseline to 6 month visit

Interventionscore on a scale (Mean)
Baseline25-Weeks
CAE + LAI Treatment27.0025.06

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Long-Acting Injectable Adherence (LAI Adherence): Count of Participants Who Received All LAI Injections:

LAI injection adherence will be determined as a count of participants who received LAI injections at the appropriate time (within 7 days of scheduled time). (NCT04327843)
Timeframe: Baseline to 6 month visit

InterventionParticipants (Count of Participants)
CAE + LAI Treatment18

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Body Mass Index

Body Mass Index kg/m^2 of participants (NCT04327843)
Timeframe: Baseline to Month 6(week 25)

Interventionkg/m^2 (Mean)
Baseline25 Weeks
CAE + LAI Treatment22.7922.92

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Clinical Global Impressions (CGI)

The minimum possible score is 1 and the maximum score is 7. A higher score implies a worse condition. (NCT04327843)
Timeframe: Baseline to 6 month visit

Interventionunits on a scale (Mean)
Baseline25 Weeks
CAE + LAI Treatment2.882.24

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Drug Attitude Inventory (DAI)

DAI-10 scoring ranges from -10 to +10 with a total score >0 indicating a positive attitude toward psychiatric medications and a total score of <0 indicating a negative attitude toward psychiatric medications. (NCT04327843)
Timeframe: Baseline to 6 month visit

Interventionscore on a scale (Mean)
Baseline25 Weeks
CAE + LAI Treatment7.899.83

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Apparent Terminal Elimination Half-Life (t½)

The apparent terminal elimination half-life (t½) is defined as the time necessary for the concentration of a drug to decrease by a factor of one-half in the terminal phase. (NCT04411940)
Timeframe: pre-dose (0 hours), and at 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 16, 24, 30, 36, 48, 72, 96, 120, 144, 168, 192 hours post dose

InterventionHours (Mean)
Reference Product (Treatment A)62.31
Test Product (Treatment B)65.99

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Area Under the Curve (0-t) (AUC(0-t))

Area under the plasma concentration versus time curve from time zero to t, where t is the time of the timepoint of the last quantifiable concentration of haloperidol in the blood plasma. The curve is constructed by plotting the concentration of haloperidol in the blood plasma against the time for each blood sample. (NCT04411940)
Timeframe: pre-dose (0 hours), and at 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 16, 24, 30, 36, 48, 72, 96, 120, 144, 168, 192 hours post dose

Interventionh*ng/ml (Mean)
Reference Product (Treatment A)20.10
Test Product (Treatment B)19.89

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Area Under the Curve(0-∞) (AUC(0-∞))

Area under the plasma concentration versus time curve from time zero to ∞, where ∞ is the timepoint of the last quantifiable concentration of haloperidol in the blood plasma, plus it's elimination rate constant. AUC(0-∞) = AUC(0-t) + AUC(t-∞). (NCT04411940)
Timeframe: pre-dose (0 hours), and at 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 16, 24, 30, 36, 48, 72, 96, 120, 144, 168, 192 hours post dose

Interventionh*ng/ml (Mean)
Reference Product (Treatment A)22.16
Test Product (Treatment B)22.28

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Terminal Elimination Rate Constant (λz)

Terminal elimination rate constant (λz) is a mathematical estimate calculated using log-linear regression of the terminal portions of a blood plasma concentration versus time curve. (NCT04411940)
Timeframe: pre-dose (0 hours), and at 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 16, 24, 30, 36, 48, 72, 96, 120, 144, 168, 192 hours post dose

Intervention1/h (Mean)
Reference Product (Treatment A)0.01194
Test Product (Treatment B)0.01124

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Time to Maximum Concentration (Tmax)

The timepoint at which the maximum concentration of haloperidol as measured by bioanalysis of the blood plasma is observed. (NCT04411940)
Timeframe: pre-dose (0 hours), and at 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 16, 24, 30, 36, 48, 72, 96, 120, 144, 168, 192 hours post dose

InterventionHours (Mean)
Reference Product (Treatment A)4.394
Test Product (Treatment B)4.406

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Concentration Maximum (Cmax)

The maximum observed concentration of haloperidol as measured by bioanalysis of the blood plasma is referred to as the Cmax. (NCT04411940)
Timeframe: pre-dose (0 hours), and at 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 16, 24, 30, 36, 48, 72, 96, 120, 144, 168, 192 hours post dose

Interventionng/ml (Mean)
Reference Product (Treatment A)0.9092
Test Product (Treatment B)0.8711

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Concentration Maximum (Cmax)

The maximum observed concentration of haloperidol as measured by bioanalysis of the blood plasma is referred to as the Cmax. (NCT04411953)
Timeframe: pre-dose (0 hours), and at 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 16, 24, 30, 36, 48, 72, 96, 120, 144, 168, 192 hours post dose

Interventionng/ml (Mean)
Reference Product (Treatment A)1.326
Test Product (Treatment B)1.293

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Terminal Elimination Half-life (t½)

The apparent terminal elimination half-life (t½) is defined as the time necessary for the concentration of a drug to decrease by one-half in the terminal phase. (NCT04411953)
Timeframe: pre-dose (0 hours), and at 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 16, 24, 30, 36, 48, 72, 96, 120, 144, 168, 192 hours post dose

InterventionHours (Mean)
Reference Product (Treatment A)69.12
Test Product (Treatment B)70.19

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Time to Maximum Concentration (Tmax)

The timepoint at which the maximum concentration of haloperidol as measured by bioanalysis of the blood plasma is observed. (NCT04411953)
Timeframe: pre-dose (0 hours), and at 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 16, 24, 30, 36, 48, 72, 96, 120, 144, 168, 192 hours post dose

InterventionHours (Mean)
Reference Product (Treatment A)4.871
Test Product (Treatment B)3.839

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Terminal Elimination Rate Constant (λz)

Terminal elimination rate constant (λz) is a mathematical estimate calculated using log-linear regression of the terminal portions of a blood plasma concentration against time curve. (NCT04411953)
Timeframe: pre-dose (0 hours), and at 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 16, 24, 30, 36, 48, 72, 96, 120, 144, 168, 192 hours post dose

Intervention1/h (Mean)
Reference Product (Treatment A)0.01114
Test Product (Treatment B)0.01152

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Area Under the Curve(0-∞) (AUC(0-∞))

Area under the plasma concentration versus time curve from time zero to ∞, where ∞ is the timepoint of the last quantifiable concentration of haloperidol in the blood plasma, plus it's elimination rate constant. AUC(0-∞) = AUC(0-t) + AUC(t-∞). (NCT04411953)
Timeframe: pre-dose (0 hours), and at 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 16, 24, 30, 36, 48, 72, 96, 120, 144, 168, 192 hours post dose

Interventionh*ng/ml (Mean)
Reference Product (Treatment A)30.61
Test Product (Treatment B)31.34

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Area Under the Curve (0-t) (AUC(0-t))

Area under the plasma concentration versus time curve from time zero to t, where t is the time of the timepoint of the last quantifiable concentration of haloperidol in the blood plasma. The curve is constructed by plotting the concentration of haloperidol in the blood plasma against the time for each blood sample. (NCT04411953)
Timeframe: pre-dose (0 hours), and at 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 16, 24, 30, 36, 48, 72, 96, 120, 144, 168, 192 hours post dose

Interventionh*ng/ml (Mean)
Reference Product (Treatment A)27.75
Test Product (Treatment B)28.46

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Length of Patient Stay in the ED

ED length of stay as measured by discharge time minus start of treatment time (NCT04715230)
Timeframe: Start of treatment until discharge

Interventionhours (Mean)
IXT-m200 Low Dose (0.5 g)8.940
IXT-m200 High Dose (2 g)8.031
Treatment as Usual (TAU)10.196

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Time Course and Degree of Normalization of Temperature

Temperature over time (NCT04715230)
Timeframe: Baseline and hours 0.5, 1, 2, 3, 4, and 8 post-dose or until discharge.

Interventiondegrees Fahrenheit (Mean)
Baseline1 hour2 hoursDischarge
Treatment as Usual (TAU)98.1097.797.798.10

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Number of Participants at Certain Degrees of Normalization of Blood Pressure Over Time

Blood pressure over time; reported as the number of participants with blood pressure out of normal range (i.e., diastolic >110 or <50 mmHg, or systolic >180 or <90 mmHg)) (NCT04715230)
Timeframe: Baseline and hours 0.5, 1, 2, 3, 4, and 8 post-dose or until discharge.

InterventionParticipants (Count of Participants)Participants (Count of Participants)
Baseline72425221Baseline72425222Baseline724252230.5 hour724252220.5 hour724252230.5 hour724252211 hour724252211 hour724252221 hour724252232 hours724252212 hours724252222 hours724252233 hours724252213 hours72425222Prior to discharge72425222Prior to discharge72425223
NormalLowHigh
Treatment as Usual (TAU)4
IXT-m200 High Dose (2 g)1
IXT-m200 Low Dose (0.5 g)0
Treatment as Usual (TAU)0
IXT-m200 Low Dose (0.5 g)8
Treatment as Usual (TAU)3
IXT-m200 High Dose (2 g)7
IXT-m200 High Dose (2 g)0
IXT-m200 Low Dose (0.5 g)7
IXT-m200 High Dose (2 g)5
IXT-m200 Low Dose (0.5 g)1
IXT-m200 High Dose (2 g)2
Treatment as Usual (TAU)1

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Time Course and Degree of Normalization of Agitation

Agitation/sedation scores over time as measured by Agitation/Calmness Evaluation Score (ACES). The minimum value is 1 (highly agitated) and the highest value is 9 (completely sedated). A score of 3-5 is considered normal. (NCT04715230)
Timeframe: Baseline and hours 0.5, 1, 2, 3, 4, and 8 post-dose or until discharge.

Interventionscore on a scale (Mean)
Baseline0.5 hour1 hour2 hours3 hours4 hours
IXT-m200 High Dose (2 g)2.3.63.94.03.01.0

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Time Course and Degree of Normalization of Agitation

Agitation/sedation scores over time as measured by Agitation/Calmness Evaluation Score (ACES). The minimum value is 1 (highly agitated) and the highest value is 9 (completely sedated). A score of 3-5 is considered normal. (NCT04715230)
Timeframe: Baseline and hours 0.5, 1, 2, 3, 4, and 8 post-dose or until discharge.

Interventionscore on a scale (Mean)
Baseline0.5 hour1 hour2 hours3 hours
IXT-m200 Low Dose (0.5 g)2.14.14.64.07.0

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Time Course and Degree of Normalization of Agitation

Agitation/sedation scores over time as measured by Agitation/Calmness Evaluation Score (ACES). The minimum value is 1 (highly agitated) and the highest value is 9 (completely sedated). A score of 3-5 is considered normal. (NCT04715230)
Timeframe: Baseline and hours 0.5, 1, 2, 3, 4, and 8 post-dose or until discharge.

Interventionscore on a scale (Mean)
Baseline0.5 hour1 hour2 hours
Treatment as Usual (TAU)2.83.95.84.8

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Number of Participants at Certain Degrees of Normalization of Heart Rate Over Time

Heart rate over time reported as number of participants with heart rate high (>120 beats/min), normal, or low (<40 beats/min). (NCT04715230)
Timeframe: Baseline and hours 0.5, 1, 2, 3, 4, and 8 post-dose or until discharge.

InterventionParticipants (Count of Participants)Participants (Count of Participants)
Baseline72425221Baseline72425222Baseline724252230.5 hour724252220.5 hour724252230.5 hour724252211 hour724252211 hour724252221 hour724252232 hours724252222 hours724252212 hours724252233 hours724252213 hours72425222Prior to discharge72425222Prior to discharge72425223
HighNormalLow
IXT-m200 Low Dose (0.5 g)0
IXT-m200 Low Dose (0.5 g)8
Treatment as Usual (TAU)4
IXT-m200 High Dose (2 g)0
Treatment as Usual (TAU)0
IXT-m200 Low Dose (0.5 g)7
IXT-m200 High Dose (2 g)8
Treatment as Usual (TAU)3
IXT-m200 Low Dose (0.5 g)1
IXT-m200 Low Dose (0.5 g)6
IXT-m200 High Dose (2 g)5
Treatment as Usual (TAU)2
IXT-m200 High Dose (2 g)2
IXT-m200 High Dose (2 g)1
Treatment as Usual (TAU)1

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Time Course and Degree of Normalization of Temperature

Temperature over time (NCT04715230)
Timeframe: Baseline and hours 0.5, 1, 2, 3, 4, and 8 post-dose or until discharge.

,
Interventiondegrees Fahrenheit (Mean)
Baseline0.5 hour1 hour2 hours3 hoursDischarge
IXT-m200 High Dose (2 g)98.2598.5298.4898.3899.5098.0
IXT-m200 Low Dose (0.5 g)98.298.0598.4598.5099.1097.40

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