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)
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.
diphenylprolinol silyl ether: structure in first source
ID Source | ID |
---|---|
PubMed CID | 3559 |
CHEMBL ID | 54 |
CHEBI ID | 5613 |
SCHEMBL ID | 8264 |
MeSH ID | M0009771 |
PubMed CID | 129696643 |
MeSH ID | M0009771 |
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 |
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.
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.
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.
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.
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.
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.
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.
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.
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.
Excerpt | Relevance | Reference |
---|---|---|
" 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 |
Role | Description |
---|---|
serotonergic antagonist | Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or serotonergic agonists. |
first generation antipsychotic | Antipsychotic 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 antagonist | A drug that binds to but does not activate dopamine receptors, thereby blocking the actions of dopamine or exogenous agonists. |
antidyskinesia agent | Any compound which can be used to treat or alleviate the symptoms of dyskinesia. |
antiemetic | A 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] |
Class | Description |
---|---|
hydroxypiperidine | |
organofluorine compound | An organofluorine compound is a compound containing at least one carbon-fluorine bond. |
aromatic ketone | A ketone in which the carbonyl group is attached to an aromatic ring. |
tertiary alcohol | A 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. |
monochlorobenzenes | Any 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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 0.0126 | 0.0032 | 45.4673 | 12,589.2998 | AID2517 |
acetylcholinesterase | Homo sapiens (human) | Potency | 89.3584 | 0.0025 | 41.7960 | 15,848.9004 | AID1347395 |
glp-1 receptor, partial | Homo sapiens (human) | Potency | 28.1838 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 2.6679 | 0.1000 | 20.8793 | 79.4328 | AID488773; AID588453 |
15-lipoxygenase, partial | Homo sapiens (human) | Potency | 25.1189 | 0.0126 | 10.6917 | 88.5700 | AID887 |
RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 22.6023 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 23.2584 | 0.0041 | 10.8903 | 31.5287 | AID493107; AID504467 |
Fumarate hydratase | Homo sapiens (human) | Potency | 29.5659 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
NFKB1 protein, partial | Homo sapiens (human) | Potency | 0.2818 | 0.0282 | 7.0559 | 15.8489 | AID895; AID928 |
TDP1 protein | Homo sapiens (human) | Potency | 23.8939 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
GLI family zinc finger 3 | Homo sapiens (human) | Potency | 9.5018 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
Thrombopoietin | Homo sapiens (human) | Potency | 6.3096 | 0.0251 | 7.3048 | 31.6228 | AID917; AID918 |
AR protein | Homo sapiens (human) | Potency | 36.1173 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID743036; AID743042; AID743054 |
caspase 7, apoptosis-related cysteine protease | Homo sapiens (human) | Potency | 54.4827 | 0.0133 | 26.9810 | 70.7614 | AID1346978 |
thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 39.8107 | 0.0013 | 18.0743 | 39.8107 | AID926 |
nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 35.9767 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224839; AID1224893 |
progesterone receptor | Homo sapiens (human) | Potency | 43.2771 | 0.0004 | 17.9460 | 75.1148 | AID1346795 |
regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 1.7923 | 0.5318 | 15.4358 | 37.6858 | AID504845 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 9.7717 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
EWS/FLI fusion protein | Homo sapiens (human) | Potency | 23.1592 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 1.7783 | 0.2818 | 9.7212 | 35.4813 | AID2326 |
glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 52.6430 | 0.0002 | 14.3764 | 60.0339 | AID720691; AID720692 |
retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 61.1306 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552 |
estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 62.1472 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1224842; AID1224848; AID1224849 |
farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 54.9410 | 0.3758 | 27.4851 | 61.6524 | AID743220 |
pregnane X nuclear receptor | Homo sapiens (human) | Potency | 4.5815 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982; AID720659 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 53.6968 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID743079; AID743091 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 4.3649 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
polyprotein | Zika virus | Potency | 29.5659 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
glucocerebrosidase | Homo sapiens (human) | Potency | 0.7943 | 0.0126 | 8.1569 | 44.6684 | AID2101 |
peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 44.2150 | 0.0010 | 24.5048 | 61.6448 | AID743212 |
vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 29.8787 | 0.0237 | 23.2282 | 63.5986 | AID588543; AID743223 |
arylsulfatase A | Homo sapiens (human) | Potency | 4.2562 | 1.0691 | 13.9551 | 37.9330 | AID720538 |
caspase-3 | Homo sapiens (human) | Potency | 54.4827 | 0.0133 | 26.9810 | 70.7614 | AID1346978 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 0.0251 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 68.5896 | 0.0016 | 28.0151 | 77.1139 | AID1259385 |
v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 17.3739 | 0.0578 | 21.1097 | 61.2679 | AID1159526 |
cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 9.0568 | 0.0020 | 7.5337 | 39.8107 | AID891 |
peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 60.1198 | 23.9341 | 23.9341 | 23.9341 | AID1967 |
cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 31.6228 | 0.0063 | 6.9043 | 39.8107 | AID883 |
D(1A) dopamine receptor | Homo sapiens (human) | Potency | 7.6386 | 0.0224 | 5.9449 | 22.3872 | AID488981; AID488982; AID488983 |
potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 0.2375 | 0.0178 | 9.6374 | 44.6684 | AID588834 |
thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 38.1972 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743066; AID743067 |
serine/threonine-protein kinase mTOR isoform 1 | Homo sapiens (human) | Potency | 23.2809 | 0.0037 | 8.6189 | 23.2809 | AID2667; AID2668 |
nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 26.9526 | 0.0006 | 27.2152 | 1,122.0200 | AID651741; AID743202; AID743219 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 35.4813 | 0.0079 | 8.2332 | 1,122.0200 | AID2546 |
geminin | Homo sapiens (human) | Potency | 17.1558 | 0.0046 | 11.3741 | 33.4983 | AID624296; AID624297 |
peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 28.6954 | 0.0056 | 12.3677 | 36.1254 | AID624032 |
cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 4.0871 | 0.0316 | 10.2792 | 39.8107 | AID884; AID885 |
transient receptor potential cation channel subfamily V member 1 | Homo sapiens (human) | Potency | 11.2202 | 0.0912 | 0.0912 | 0.0912 | AID488979 |
muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 10.2175 | 0.0010 | 6.0009 | 35.4813 | AID943; AID944 |
lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 20.8114 | 0.0200 | 10.7869 | 31.6228 | AID912 |
Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 4.0871 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 15.8489 | 0.3162 | 12.7657 | 31.6228 | AID881 |
Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 61.1306 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 4.0871 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 4.0871 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 4.0871 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 61.1306 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 4.0871 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 4.0871 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 4.0871 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 4.0871 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 4.0871 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 4.0871 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 4.0871 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 22.6091 | 0.0063 | 8.2350 | 39.8107 | AID881; AID883 |
D(1A) dopamine receptor | Sus scrofa (pig) | Potency | 23.2809 | 0.0037 | 8.1081 | 23.2809 | AID2667 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 4.0871 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 4.0871 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 4.0871 | 1.0000 | 12.2248 | 31.6228 | AID885 |
TAR DNA-binding protein 43 | Homo sapiens (human) | Potency | 0.5623 | 1.7783 | 16.2081 | 35.4813 | AID652104 |
GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 4.0871 | 1.0000 | 12.2248 | 31.6228 | AID885 |
ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 18.8336 | 0.0119 | 17.9420 | 71.5630 | AID651632 |
Ataxin-2 | Homo sapiens (human) | Potency | 18.8336 | 0.0119 | 12.2221 | 68.7989 | AID651632 |
Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 4.0871 | 1.0000 | 12.2248 | 31.6228 | AID885 |
ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 4.2562 | 0.0601 | 10.7453 | 37.9330 | AID485368 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Albumin | Rattus norvegicus (Norway rat) | Kd | 96.9000 | 1.4700 | 6.5317 | 9.3100 | AID1215123 |
Major prion protein | Homo sapiens (human) | EC50 (µMol) | 10.0000 | 0.3000 | 4.9000 | 10.0000 | AID161627 |
HLA class I histocompatibility antigen, A alpha chain | Homo sapiens (human) | Kd | 10.0000 | 2.5000 | 4.3750 | 10.0000 | AID1398702 |
D(2) dopamine receptor | Homo sapiens (human) | Kd | 0.0005 | 0.0000 | 0.6459 | 9.5000 | AID1616723 |
D(4) dopamine receptor | Homo sapiens (human) | EC50 (µMol) | 5.0085 | 0.0014 | 0.0889 | 2.2300 | AID246503; AID63858 |
Mu-type opioid receptor | Homo sapiens (human) | EC50 (µMol) | 10.0000 | 0.0000 | 0.3263 | 9.4000 | AID1558957 |
D(3) dopamine receptor | Homo sapiens (human) | Kd | 0.3162 | 0.0000 | 0.0748 | 0.3162 | AID256759 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
UDP-glucuronosyltransferase 1A9 | Homo sapiens (human) | Km | 174.0000 | 5.0000 | 6.8300 | 10.0000 | AID1213070 |
ATP-dependent translocase ABCB1 | Homo sapiens (human) | Km | 33.0000 | 0.0140 | 3.7172 | 10.0000 | AID681619 |
Cytochrome P450 3A4 | Homo sapiens (human) | INH | 26.2000 | 1.7000 | 2.8500 | 4.0000 | AID711572 |
D(2) dopamine receptor | Homo sapiens (human) | Kb | 0.0014 | 0.0004 | 1.6549 | 10.0000 | AID62581 |
D(2) dopamine receptor | Homo sapiens (human) | pKi | 0.0091 | 0.0069 | 0.0078 | 0.0091 | AID63251 |
D(1A) dopamine receptor | Homo sapiens (human) | Kb | 0.0014 | 0.0014 | 3.6671 | 10.0000 | AID62581 |
D(4) dopamine receptor | Homo sapiens (human) | Kb | 0.0014 | 0.0014 | 3.6671 | 10.0000 | AID62581 |
D(4) dopamine receptor | Homo sapiens (human) | pKi | 0.0080 | 0.0073 | 0.0077 | 0.0080 | AID63699 |
D(1B) dopamine receptor | Homo sapiens (human) | Kb | 0.0014 | 0.0014 | 3.6671 | 10.0000 | AID62581 |
UDP-glucuronosyltransferase 1A4 | Homo sapiens (human) | Km | 64.0000 | 7.0000 | 7.0000 | 7.0000 | AID1213067 |
D(3) dopamine receptor | Homo sapiens (human) | Kb | 0.0014 | 0.0014 | 1.5843 | 10.0000 | AID62581 |
D(3) dopamine receptor | Homo sapiens (human) | pKi | 0.0083 | 0.0066 | 0.0072 | 0.0083 | AID65437 |
Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | K0.5 | 0.2150 | 0.0001 | 0.4036 | 4.8000 | AID88009 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1645848 | NCATS Kinetic Aqueous Solubility Profiling | 2019 | Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14 | Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity. |
AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS 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. |
AID1508591 | NCATS Rat Liver Microsome Stability Profiling | 2020 | Scientific reports, 11-26, Volume: 10, Issue:1 | Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models. |
AID1508612 | NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Highly predictive and interpretable models for PAMPA permeability. |
AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The 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. |
AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The 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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. 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. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. 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. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. 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. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The 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. |
AID1347151 | Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings 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. |
AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection | 2020 | ACS 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. |
AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
AID414524 | Hypothermic activity in Sprague-Dawley rat assessed as decrease in core body temperature at 5 mg/kg, ip at time of maximal body temperature decrease | 2009 | Journal 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. |
AID1213026 | Drug metabolism assessed as human liver microsomes assessed as O-glucuronide measured per mg of protein at 25 uM by LC-MS/MS analysis | 2012 | Drug 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. |
AID63637 | Ratio of Ki(uM) of D2 receptor to the Ki(uM) of 5-hydroxytryptamine 2 receptor | 1992 | Journal 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. |
AID203982 | Displacement of [3H]DTG from sigma opioid receptor of homogenized guinea pig whole brain | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | Radiosynthesis of sigma receptor ligands for positron emission tomography: 11C- and 18F-labeled guanidines. |
AID176235 | Inhibitory activity in apomorphine antagonism test at a dose of 20 mg/kg, sc | 1994 | Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4 | Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study. |
AID232561 | Ratio of ED50 for inhibition of catalepsy induction to stereotypy induction | 1981 | Journal 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. |
AID239296 | Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand | 2005 | Journal 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. |
AID177633 | Compound was evaluated in vivo for antagonist activity against apomorphine induced behavioral syndrome such as Hyperactivity in rat after intraperitoneal administration; activity value ranges from 0.27-0.35 | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | Potential neuroleptic agents. 3. Chemistry and antidopaminergic properties of substituted 6-methoxysalicylamides. |
AID1185976 | Antipsychotic activity in ip dosed Swiss-Webster mouse assessed as inhibition of APO-induced climbing behavior after 30 mins | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17 | Further evaluation of the tropane analogs of haloperidol. |
AID1409514 | Therapeutic index, ratio of ED50 for catalepsy in Kunming mouse to ED50 for MK-801-induced hyperactivity in Kunming mouse | 2018 | Journal 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. |
AID298492 | Displacement of [3H]prazosin from adrenergic alpha1 receptor in rat cerebral cortex | 2007 | Journal 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. |
AID5035 | Binding affinity against 5-hydroxytryptamine 2 receptor from rat cortical synaptosomal membrane using radioligand [3H]ketanserin. | 1993 | Journal 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. |
AID62338 | Evaluated for binding towards Dopamine receptor D2 using [3H]-spiperone as radioligand, in cloned mammalian receptors expressed in CHO-K1 cells | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
AID232553 | Ratio of ED50 for antagonism of apomorphine induced stereotypy to ED50 for antagonism of apomorphine induced climbing | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16 | Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents. |
AID410137 | Inhibition of dopamine D2 receptor-mediated apomorphine-induced cage climbing behavior in Swiss albino mouse at 1 mg/kg, ip | 2008 | Bioorganic & 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. |
AID4334 | Affinity against the 5-hydroxytryptamine receptor 1A using [3H]WB-4101. | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | N-aryl-N'-benzylpiperazines as potential antipsychotic agents. |
AID410535 | Toxicity 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 test | 2009 | Journal 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. |
AID28236 | Unbound fraction (tissues) | 2002 | Journal 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. |
AID1336363 | Displacement of [3H]DTG from sigma receptor in human Jurkat cells measured after 120 mins by scintillation counting method | 2017 | Bioorganic & 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 |
AID1853686 | Cytotoxicity against human HEK293 cells assessed as reduction in cell viability at 200 uM incubated for 24 hrs by resazurin assay | 2021 | RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11 | Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from |
AID1213088 | Drug metabolism assessed as human liver microsomes assessed as velocity of N-glucuronidation at 100 uM by LC-MS/MS analysis | 2012 | Drug 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. |
AID63700 | Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+. |
AID227718 | Binding energy by using the equation deltaG obsd = -RT ln KD | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Functional group contributions to drug-receptor interactions. |
AID1318840 | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes after 120 mins by scintillation counting method | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Computer-assisted design, synthesis, binding and cytotoxicity assessments of new 1-(4-(aryl(methyl)amino)butyl)-heterocyclic sigma 1 ligands. |
AID298485 | Displacement of [3H]mesulergine from 5HT2C receptor expressed in CHO cells | 2007 | Journal 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. |
AID139070 | Antagonism of apomorphine in reserpinized mice when a dose of 0.3 micro mol/kg is administered intraperitoneally | 1993 | Journal 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. |
AID64296 | Inhibition of [3H]methylspiperone binding to rat striatal membrane Dopamine receptor D2 | 1998 | Journal 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). |
AID1169871 | Antipsychotic-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 mins | 2014 | Journal 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. |
AID255170 | Ratio of inhibitory concentration against rat opioid receptor sigma 2 and guinea pig opioid sigma 1 | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective sigma1 ligands. Part 1. |
AID61669 | Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand. | 2000 | Journal 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. |
AID63234 | Selectivity is the ratio of binding affinities for human Dopamine receptor D2 to that of Dopamine receptor D3 | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10 | Design and synthesis of a piperazinylalkylisoxazole library for subtype selective dopamine receptor ligands. |
AID1686281 | Cytotoxicity in HREC assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells. |
AID444055 | Fraction absorbed in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID1060809 | Displacement of [3H]-(+)-pentazocine from guinea pig brain sigma1 receptor after 150 mins by scintillation counting analysis | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | From NMDA receptor antagonists to discovery of selective σ₂ receptor ligands. |
AID705726 | Displacement of [3H](+)-pentazocine from Sigma1 receptor in rat brain homogenate | 2012 | Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19 | New positron emission tomography (PET) radioligand for imaging σ-1 receptors in living subjects. |
AID1335651 | Therapeutic 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 mouse | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics. |
AID3460 | Affinity towards 5-hydroxytryptamine 1A receptor in membranes from bovine hippocampus using [3H]OH-DPAT | 1998 | Journal 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. |
AID576612 | Inhibition of human ERG | 2011 | European 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. |
AID301906 | Induction of catalepsy in Mill Hill hooded rat at 1 mg/kg after 30-180 min | 2007 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21 | Two new phenylpiperazines with atypical antipsychotic potential. |
AID5483 | Binding affinity towards 5-hydroxytryptamine 2A receptor from rat frontal cortex using [3H]ketanserin as radioligand | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
AID239052 | Inhibition of [3H]-spiperone binding to human Dopamine receptor D2 | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
AID1853687 | Cytotoxicity against human A549 cells assessed as reduction in cell viability at 50 to 200 uM incubated for 24 hrs by resazurin assay | 2021 | RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11 | Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from |
AID298489 | Displacement of [3H]paraxetine from human 5HT transporter expressed in HEK293 cells | 2007 | Journal 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. |
AID194380 | Effect of compound (0.2 mg/kg ip) on the concentration of HVA in rat mesolimbic region | 1993 | Journal 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. |
AID3760 | In vitro binding affinity was measured on serotonergic 5-hydroxytryptamine 1A receptor by displacement of [3H]- tetralin | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16 | Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents. |
AID203697 | Binding affinity towards sigma 1 receptor was determined in guinea pig brain membrane using [3H](+)-pentazocine as radioligand | 1994 | Journal 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. |
AID298032 | Acid dissociation constant, pKa of the compound | 2007 | Journal 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. |
AID342788 | Blockade of apomorphine-induced climbing stereotypy in Swiss Webster mouse after 30 mins | 2008 | Bioorganic & 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. |
AID588219 | FDA HLAED, gamma-glutamyl transferase (GGT) increase | 2004 | Current 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. |
AID1511009 | Selectivity ratio of Ki for sigma1 receptor in guinea pig brain membranes to Ki for sigma2 receptor in rat liver membranes | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Discovery of new potent dual sigma receptor/GluN2b ligands with antioxidant property as neuroprotective agents. |
AID177491 | Effect on half-maximal decrease of DOPA formation in rat limbic regions; In active (no significant effect at 1.4 pmol/kg ip) | 1987 | Journal 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. |
AID224647 | Area under curve(AUC) value of Dopamine level after second treatment(7.4 umol/kg) in dialysates collected from rat striatum | 2002 | Journal 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. |
AID4061 | Compound was evaluated for its binding affinity with 5-hydroxytryptamine 1A receptor using membranes prepared from rat cerebral cortex | 1998 | Journal 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. |
AID1210015 | Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate after 8 mins by LC-MS/MS analysis | 2012 | Drug 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. |
AID176734 | Dose (administered orally) inhibiting apomorphine-induced stereotypy in rats | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
AID280704 | Increase in apoptosis in albino Wistar rat primary 14 DIV astroglial cells at 25 uM after 24 hrs by TUNEL assay relative to control | 2007 | Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5 | Novel sigma receptor ligands: synthesis and biological profile. |
AID243274 | Binding affinity towards dopamine receptor D3 was determined | 2005 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8 | The role of QSAR in dopamine interactions. |
AID203686 | Compound tested for binding affinity towards sigma 1 receptor in quinea pig brain membranes using [3H](+)-pentazocine as the radioligand. | 1998 | Journal 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. |
AID1221963 | Transporter 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 LY335979 | 2011 | Drug 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. |
AID1256682 | Neurotoxicity 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) | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics. |
AID239200 | Inhibitory constant against sigma receptor type 2 using 3 nM [3H]ditolylguanidine | 2005 | Journal 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. |
AID629462 | Displacement of [3H]spiperone from human DRD2 short receptor expressed in chinese hamster CHO cells by radioligand binding assay | 2011 | Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22 | Development of a bivalent dopamine D₂ receptor agonist. |
AID1901323 | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane by competitive radioligand receptor binding assay | |||
AID280721 | Activity at sigma 2 receptor in rat astroglial cells | 2007 | Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5 | Novel sigma receptor ligands: synthesis and biological profile. |
AID128984 | Anticonvulsant activity against electroshock-induced convulsions, after 1 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
AID1664665 | Displacement of [3H]-N-Methylspiperone from human dopamine D2 receptor expressed in stable fibroblast cells incubated for 90 mins by microbeta counting method | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Structural manipulation of aporphines via C10 nitrogenation leads to the identification of new 5-HT |
AID578855 | Displacement of [3H]-(+)-pentazocine from Sigma1-receptor in guinea pig brain membrane | 2011 | Bioorganic & 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. |
AID588216 | FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase | 2004 | Current 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. |
AID1744232 | Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes incubated for 1 hr by liquid scintillation counting method | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1 | Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management. |
AID298490 | Displacement of [3H]pirenzepine from human M1 receptor expressed in CHO cells | 2007 | Journal 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. |
AID1144199 | Acute toxicity in ip dosed Swiss-Webster mouse assessed as ataxia administered as single dose after 72 hrs | 1976 | Journal of medicinal chemistry, Jan, Volume: 19, Issue:1 | Synthesis and biological actions of 2-substituted quinolizidines. |
AID63811 | Displacement of [3H]NPA from rat brain Dopamine receptor D2 | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
AID1462754 | Displacement of [3H]-(+)-MK-801 from PCP binding site of NMDA receptor in pig brain cortex at 1 uM | 2017 | Bioorganic & 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. |
AID397743 | Inhibition of human ERG channel | 2009 | Journal 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. |
AID61675 | Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate | 2002 | Journal 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. |
AID393359 | Displacement of [3H](+)-pentazocine from sigma 1 receptor in rat liver membrane | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Substituted benzo[d]oxazol-2(3H)-one derivatives with preference for the sigma1 binding site. |
AID1213033 | Drug 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 control | 2012 | Drug 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. |
AID130873 | Inhibition against apomorphine-induced climbing, after 1 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
AID178710 | Compound was tested for the antagonistic activity against amphetamine-induced stereotypy in rats; (5 mg/kg administered ip 5 hr after the test compound) | 1986 | Journal of medicinal chemistry, Jan, Volume: 29, Issue:1 | Neuroleptic activity of chiral trans-hexahydro-gamma-carbolines. |
AID23095 | Ratio of pKi of 5-HT2A receptor to that of D2 receptor | 2000 | Journal 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. |
AID36122 | The compound was tested against Alpha-1 adrenergic receptor for percent displacement of radioligand at 10e-6 M | 1999 | Journal 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. |
AID1197504 | Selectivity ratio of Ki for sigma2 receptor in human Jurkat cells to Ki for sigma1 receptor human Jurkat cells | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Synthesis and pharmacological evaluation of benzannulated derivatives as potent and selective sigma-1 protein ligands. |
AID1596351 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay | |||
AID1318841 | Displacement of [3H]-DTG from sigma2 receptor in rat liver membranes after 120 mins by scintillation counting method | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Computer-assisted design, synthesis, binding and cytotoxicity assessments of new 1-(4-(aryl(methyl)amino)butyl)-heterocyclic sigma 1 ligands. |
AID1650560 | Displacement 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 method | 2020 | Bioorganic & 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. |
AID1335648 | Inhibition 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 mins | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics. |
AID266791 | Reduction 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, ip | 2006 | Journal 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. |
AID185004 | Compound is tested for concomitant ability to antagonize the locomotor activity induced by Di-Pr-5,6-ADTN | 1994 | Journal 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. |
AID1461563 | Displacement of [3H]spiperone from human D2short receptor L2.64C mutant expressed in HEK293T cell membranes by radioligand binding assay | 2017 | Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19 | Potent haloperidol derivatives covalently binding to the dopamine D2 receptor. |
AID1215944 | Intrinsic clearance in human intestinal S9 fraction at 50 to 1000 nM after 60 mins by HPLC-MS/MS analysis | 2013 | Drug 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. |
AID1280525 | Cataleptic activity in ip dosed C57BL/6J mouse measured after 60 mins | 2016 | Journal 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. |
AID176663 | Suppression of conditioned avoidance behavior in rats following p.o. administration. | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | 2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2. |
AID410334 | Displacement of [3H]8OH-DPAT from 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus by scintillation spectrometry | 2009 | Journal 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. |
AID5233 | Binding affinity for 5-hydroxytryptamine 2 receptor from striata of male Wistar rats by displacement of [3H]ketanserin | 2000 | Bioorganic & medicinal chemistry letters, Mar-06, Volume: 10, Issue:5 | N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]cyclohexanecarboxamides as selective 5-HT1A receptor agonists. |
AID1782419 | Displacement of [3H]-N-methylspiperone from D2 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
AID392049 | Cardiotoxicity 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 ECG | 2008 | European journal of medicinal chemistry, Nov, Volume: 43, Issue:11 | Identification of "toxicophoric" features for predicting drug-induced QT interval prolongation. |
AID65753 | Binding affinity towards baculovirus expressed rat dopamine D3 receptors | 1994 | Journal 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. |
AID1204344 | Displacement 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 method | 2015 | European journal of medicinal chemistry, Jun-05, Volume: 97 | Structure-activity relationships and molecular studies of novel arylpiperazinylalkyl purine-2,4-diones and purine-2,4,8-triones with antidepressant and anxiolytic-like activity. |
AID1215953 | Drug metabolism in human intestinal cytosol at 200 nM after 60 mins in presence of ondansetron | 2013 | Drug 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. |
AID1782429 | Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
AID711571 | Half life in human liver microsomes | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Synopsis of some recent tactical application of bioisosteres in drug design. |
AID178706 | Compound was tested for the antagonistic activity against amphetamine-induced stereotypy in rats; (5 mg/kg administered ip 24 hr after the test compound) | 1986 | Journal of medicinal chemistry, Jan, Volume: 29, Issue:1 | Neuroleptic activity of chiral trans-hexahydro-gamma-carbolines. |
AID1129880 | Displacement of [3H]-DTG from sigma-2 receptor in rat liver homogenates after 120 mins by scintillation counting analysis in presence of (+)-pentazocine | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | Synthesis, pharmacological evaluation, and σ1 receptor interaction analysis of hydroxyethyl substituted piperazines. |
AID540226 | Clearance in monkey after iv administration | 2006 | Drug 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. |
AID64299 | In vitro binding affinity for Dopamine D2 receptor of rat using [3H]YM-09151 as radioligand | 2002 | Journal 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. |
AID591693 | Induction 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%) | 2011 | Journal 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. |
AID65884 | Displacement of [3H]-Spiperone from Dopamine receptor D2 in rat striatum | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | 2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2. |
AID1813189 | Ratio 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 phenytoin | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Optimization of bifunctional piperidinamide derivatives as σ |
AID1309493 | Lipophilicity, log P of the compound | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores. |
AID1213065 | Drug metabolism assessed as human liver microsomes assessed as O-glucuronidation measured per mg of protein at 10 to 400 uM by LC-MS/MS analysis | 2012 | Drug 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. |
AID113114 | Antagonism of apomorphine-induced climbing in mice when administered intraperitoneally 60 min prior to apomorphine (1 mg/kg) | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | 2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1. |
AID1213034 | Drug 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 hecogenin | 2012 | Drug 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. |
AID1318843 | Selectivity ratio of Ki for sigma2 receptor in rat liver membranes to Ki for sigma1 receptor in guinea pig brain cortex membranes | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Computer-assisted design, synthesis, binding and cytotoxicity assessments of new 1-(4-(aryl(methyl)amino)butyl)-heterocyclic sigma 1 ligands. |
AID203998 | Inhibition of [3H]DTG binding to Sigma opioid receptor | 1991 | Journal 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. |
AID131875 | Effective dose required for inhibition of apomorphine(sc, 2.5 mg/kg ) induced stereotypy in mice on ip administration | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
AID1724119 | Induction of catalepsy in po dosed mouse by vertical grid and elevated bar test | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics. |
AID63226 | Ability to displace [3H]spiperone from human dopamine receptor D2 stably expressed in CHO cells. | 1997 | Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15 | 4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor. |
AID729709 | Antagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay | 2013 | Bioorganic & 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. |
AID65128 | Displacement of [3H]raclopride from Dopamine receptor D3 | 1996 | Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22 | Novel (R)-2-amino-5-fluorotetralins: dopaminergic antagonists and inverse agonists. |
AID1079938 | Chronic 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] | |||
AID1215951 | Drug metabolism in human intestinal cytosol at 200 nM after 60 mins in presence of flufenamic acid | 2013 | Drug 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. |
AID675970 | Displacement of [3H]-(+)pentazocine from guinea pig brain sigma 1-type opioid receptor after 120 mins by scintillation counting analysis | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Thiophene bioisosteres of spirocyclic σ receptor ligands: relationships between substitution pattern and σ receptor affinity. |
AID298486 | Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells | 2007 | Journal 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. |
AID29139 | Calculated dissociation constant (pKa, calculated with ACD/pKa) | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis). |
AID3992 | Binding 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. | 1998 | Journal 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). |
AID458634 | Selectivity ratio of Ki for human dopamine D2 receptor at low affinity state to Ki for human dopamine D2 receptor at high affinity state | 2010 | Journal 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). |
AID5558 | Compound was tested for the Binding affinity against rat frontal cortex 5-hydroxytryptamine 2A receptor by Radio ligand [3H]ketanserin binding assay. | 1996 | Journal 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. |
AID596434 | Biodistribution 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) | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Synthesis and biological evaluation of novel 4-benzylpiperazine ligands for sigma-1 receptor imaging. |
AID65814 | Binding affinity towards Dopamine type 2 receptor was determined by displacement assays using [3H]-YM 09151 as the competitive ligand | 2002 | Bioorganic & 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. |
AID711583 | Apparent permeability across human Caco2 cells | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Synopsis of some recent tactical application of bioisosteres in drug design. |
AID128987 | Anticonvulsant activity against tryptamine-induced convulsions, after 1 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
AID186042 | Locomotor activity in male Wistar rats after a dose of 0.003 uM/kg, 30 min before 1 mg/kg of apomorphine administration | 1997 | Journal 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. |
AID605698 | Displacement of [3H]spiperone from human D2short receptor expressed in CHO cells | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Bivalent dopamine D2 receptor ligands: synthesis and binding properties. |
AID229002 | Compound was measured for the inhibition of [3H]ketanserin binding to rat frontal cortex membrane (5-HT2A receptor) | 1998 | Bioorganic & 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. |
AID1309492 | Displacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting method | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores. |
AID169806 | Compound was assessed for its ability to block a conditioned avoidance response; Dose administered perorally is 1.25 mg/kg; 51-75%block | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8 | 4-Piperazinyl-10H-thieno[2,3-b][1,5]benzodiazepines as potential neuroleptics. |
AID62581 | Dopamine receptor antagonist activity in the superfused rabbit ear artery preparation | 1981 | Journal of medicinal chemistry, Jun, Volume: 24, Issue:6 | Synthesis and evaluation of novel alkylpiperazines as potential dopamine antagonists. |
AID224649 | Area under curve(AUC) value of DOPAC level after total treatment in dialysates collected from rat striatum. | 2002 | Journal 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. |
AID65950 | Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro | 1997 | Journal 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. |
AID588220 | Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset | 2008 | Toxicology mechanisms and methods, , Volume: 18, Issue:2-3 | Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models. |
AID701945 | Displacement of [3H]di-o-tolylguanidine from Sigma 2 receptor in rat liver membrane after 120 mins by scintillation counting | 2012 | Journal 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. |
AID1393522 | Reversal 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 | |||
AID781329 | pKa (acid-base dissociation constant) as determined by other workers | 2014 | Pharmaceutical research, Apr, Volume: 31, Issue:4 | Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds. |
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AID1185966 | Displacement of [3H]SCH23390 from human dopamine D5 receptor by liquid scintillation counting | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17 | Further evaluation of the tropane analogs of haloperidol. |
AID1213058 | Drug metabolism assessed as human liver microsomes assessed as retention time at 100 uM by LC-MS/MS analysis | 2012 | Drug 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. |
AID1185973 | Displacement of [3H]GBR12935 from human dopamine transporter by liquid scintillation counting | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17 | Further evaluation of the tropane analogs of haloperidol. |
AID177902 | Inhibition of firing rates of dopaminergic neurons in the substantia nigra pars compacta by intravenous injection in rats | 1993 | Journal 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. |
AID64985 | Binding 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' | 1998 | Journal 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). |
AID598812 | Displacement of [3H]DTG from sigma 2 receptor in rat brain homogenate | 2011 | Bioorganic & 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. |
AID1060807 | Selectivity ratio of Ki for guinea pig brain sigma1 receptor to Ki for guinea pig brain sigma2 receptor | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | From NMDA receptor antagonists to discovery of selective σ₂ receptor ligands. |
AID178321 | Compound was tested for anti-dopamine activity in vivo by its ability to inhibit apomorphine induced stereotypy in rat | 1986 | Journal 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. |
AID308688 | Ratio of pKi for human 5HT2A receptor to pKi for human D2 receptor | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics. |
AID36912 | Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta | 2003 | Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2 | New arylpiperazine derivatives with high affinity for alpha1A, D2 and 5-HT2A receptors. |
AID1546907 | Displacement of [3H]spiperone from human D2S receptor expressed in CHO-K1 cells by radioligand competitive binding analysis | |||
AID161281 | Inhibition of human Potassium channel HERG expressed in mammalian cells | 2003 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16 | Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods. |
AID596438 | Biodistribution 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) | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Synthesis and biological evaluation of novel 4-benzylpiperazine ligands for sigma-1 receptor imaging. |
AID65559 | Evaluated for binding towards Dopamine receptor D2 using [3H]N-0437 as radioligand from rat striatal membrane | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
AID1473740 | Inhibition 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 assay | 2013 | Toxicological 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. |
AID1462132 | Displacement of [3H]-DTG from sigma2 receptor in rat liver membranes after 120 mins by liquid scintillation counting | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17 | Chiral-pool synthesis of 1,2,4-trisubstituted 1,4-diazepanes as novel σ |
AID62590 | Ability 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 administration | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists. |
AID1314060 | Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 2 hrs by scintillation counting | 2016 | Bioorganic & 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. |
AID138929 | Antagonism of apomorphine for 10-20 minutes in reserpinized mice when a dose of 2.7 micro mol/kg is administered intraperitoneally | 1993 | Journal 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. |
AID112952 | Compound was tested for inhibition of norepinephrine lethality in mouse when administered perorally | 1986 | Journal 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. |
AID65562 | Inhibition of [3H]spiperone binding to rat striatal membrane Dopamine receptor D2 | 1990 | Journal of medicinal chemistry, Apr, Volume: 33, Issue:4 | Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds. |
AID1478368 | Selectivity index, ratio of Ki for sigma2 receptor in guinea pig brain membrane to Ki for sigma2 receptor in guinea pig brain membrane | 2018 | Journal 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. |
AID235773 | Therapeutic ratio by Peroral dose of administration (quotient ED50 catalepsy/ED50 climbing) | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
AID63237 | Inhibition of [35 S] GTP gamma S binding to cell membranes expressing Dopamine receptor D2 | 1996 | Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22 | Novel (R)-2-amino-5-fluorotetralins: dopaminergic antagonists and inverse agonists. |
AID1123526 | Neuroleptic 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 hrs | 1979 | Journal 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. |
AID342784 | Binding affinity to human cloned 5HT2A receptor | 2008 | Bioorganic & 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. |
AID517708 | Displacement of [3H]Spiperone from human dopamine D2 short receptor expressed in CHO cells | 2010 | Journal 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. |
AID1210074 | Inhibition of CYP1A2 in human liver microsomes using phenacetin substrate by LC-MS/MS method | 2013 | Drug 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. |
AID395325 | Lipophilicity, log P by microemulsion electrokinetic chromatography | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
AID129968 | Compound was evaluated for inhibition of apomorphine-induced climbing in mouse after peroral administration. | 1992 | Journal 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. |
AID1330100 | Displacement of [3H]DAMGO from human MOR expressed in HEK cells after 90 mins by microbeta scintillation counting method | 2016 | Bioorganic & 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. |
AID729710 | Agonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay | 2013 | Bioorganic & 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. |
AID176324 | In vivo blocking of apomorphine induced stereotypies following 1 mg/kg i.p. in rats after 60 min. | 1982 | Journal of medicinal chemistry, Nov, Volume: 25, Issue:11 | Potential neuroleptic agents. 2,6-Dialkoxybenzamide derivatives with potent dopamine receptor blocking activities. |
AID592132 | Induction 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%) | 2011 | Journal 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. |
AID1123528 | Neuroleptic 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 hrs | 1979 | Journal 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. |
AID1409611 | AUC (cytotoxicity %) of compound against Vero E6 cells by MTT assay. | 2020 | Nature, 07, Volume: 583, Issue:7816 | A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
AID138782 | Antagonism of apomorphine for 0-10 minutes in reserpinized mice when a dose of 0.3 micro mol/kg is administered intraperitoneally | 1993 | Journal 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. |
AID1616727 | Agonist 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 | |||
AID303620 | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Synthesis of bicyclic sigma receptor ligands with cytotoxic activity. |
AID1473741 | Inhibition 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 assay | 2013 | Toxicological 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. |
AID387868 | Selectivity ratio of Ki for human dopamine D2S receptor to Ki for human dopamine D4.2 receptor | 2008 | Bioorganic & 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. |
AID1308619 | Displacement of [3H](+)-Pentazocine from sigma 1 receptor in human RPMI8226 cell membranes | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity? |
AID1636357 | Drug 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 NA | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
AID593483 | Displacement 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 counting | 2011 | Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7 | Molecular properties affecting fast dissociation from the D2 receptor. |
AID418675 | Cytotoxicity against human RT4 cells after 96 hrs by crystal violet staining | 2009 | Journal 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. |
AID37376 | In vitro binding affinity towards alpha-2 adrenergic receptor in rat frontal cortex homogenate using of [3H]clonidine as radioligand | 2004 | Journal 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. |
AID61517 | Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate | 2002 | Journal 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. |
AID1532592 | Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in human Jurkat cell membranes after 2 hrs by liquid scintillation counting method | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Novel multitarget-directed ligands targeting acetylcholinesterase and σ |
AID65271 | Compound was evaluated for in vitro binding affinity towards Dopamine receptor D2 in rat striatum using [3H]- spiperone as radioligand | 1992 | Journal 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. |
AID65610 | Binding affinity towards Dopamine receptor D3 of rat using [3H]spiroperidol as radioligand | 2002 | Journal 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. |
AID131362 | Effect on Ataxia in mouse following i.p. administration. | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | N6-(2,2-diphenylethyl)adenosine, a novel adenosine receptor agonist with antipsychotic-like activity. |
AID177946 | Antagonistic activity against amphetamine-induced stereotypy, after 1 hour of peroral administration in rats | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
AID194372 | Effect of compound (0.2 mg/kg ip) on the concentration of DA in rat mesolimbic region | 1993 | Journal 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. |
AID177488 | Effect on Sidman conditioned avoidance in rat. | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | N6-(2,2-diphenylethyl)adenosine, a novel adenosine receptor agonist with antipsychotic-like activity. |
AID598814 | Displacement of [3H]SCH233930 from human D5 receptor expressed in HEK cells | 2011 | Bioorganic & 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. |
AID176780 | In vivo DOPA accumulation in reserpine pretreated rat striatum system after 1.4 umol/kg ip; I denotes inactive | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists. |
AID64426 | In vitro binding affinity was measured by displacement of [3H]- raclopride from D2 receptor isolated from the striata of male Dawley rats | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16 | Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents. |
AID218788 | Binding affinity towards dopamine receptor D2 was determined by displacement of [3H]spiroperidol from bovine nucleus caudate membranes. | 1987 | Journal 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. |
AID177492 | Effect on half-maximal decrease of DOPA formation in rat striatal regions | 1987 | Journal 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. |
AID203699 | Inhibition of [3H]pentazocine binding to sigma-1 sites in guinea pig brain membranes | 1998 | Journal of medicinal chemistry, May-07, Volume: 41, Issue:10 | (+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties. |
AID330538 | Orexigenic activity in H1RKO mouse | 2007 | Proceedings 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. |
AID5334 | Serotonergic activity of the compound. | 2000 | Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17 | GRid-INdependent descriptors (GRIND): a novel class of alignment-independent three-dimensional molecular descriptors. |
AID586709 | Displacement of [3H]-DTG from rat sigma2 receptor by liquid scintillation counting | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Synthesis and pharmacological evaluation of fluorine-containing D₃ dopamine receptor ligands. |
AID1213068 | Drug 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 analysis | 2012 | Drug 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. |
AID1686283 | Cytotoxicity in HREC assessed as reduction in cell viability incubated for 96 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells. |
AID1215936 | Unbound intrinsic clearance in human liver microsomes at 50 to 1000 nM after 30 to 60 mins by HPLC-MS/MS analysis | 2013 | Drug 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. |
AID1369086 | Displacement of [3H]-(+)-Pentazocine from sigma 1 receptor in guinea pig brain cortex membranes after 120 mins by scintillation counting analysis | 2018 | Bioorganic & 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. |
AID65785 | Binding affinity towards human Dopamine receptor D3 | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Selective optimization of side activities: another way for drug discovery. |
AID204012 | Inhibitory activity against Sigma opioid receptor | 1991 | Journal 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. |
AID317395 | Ratio of Ki for sigma2 receptor in Hartley guinea pig brain to Ki for sigma1 receptor in Hartley guinea pig brain | 2008 | Bioorganic & 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. |
AID177479 | Effect on Ataxia(ATX) in rat was measured as ED50 by perorally administration of compound. | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | N6-(2,2-diphenylethyl)adenosine, a novel adenosine receptor agonist with antipsychotic-like activity. |
AID1335652 | Therapeutic 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 mouse | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics. |
AID226426 | In vitro binding affinity for D2 receptor compared to that of 5-HT2 receptor | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
AID176744 | Dose inhibiting conditioned avoidance response in rats after oral administration | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
AID63534 | Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151 | 1997 | Journal 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. |
AID711577 | Inhibition of sigma 1 receptor | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Synopsis of some recent tactical application of bioisosteres in drug design. |
AID204153 | Sigma opioid receptor type 1 affinity in guinea pig brain by employing [3H](+)-pentazocine as radioligand. | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1. |
AID177887 | Inhibition of apomorphine-induced stereotypy in rats. | 1998 | Journal 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). |
AID303626 | Growth inhibition of human A427 cells at 20 uM after 96 hrs relative to control | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Synthesis of bicyclic sigma receptor ligands with cytotoxic activity. |
AID5279 | In vitro 5-hydroxytryptamine 2 receptor affinity by using [3H]-Spiperone as the radioligand in rat cortical tissue. | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | Antipsychotic activity of substituted gamma-carbolines. |
AID439069 | Displacement of [3H]spiperone from human dopamine D3 receptor | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21 | Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif. |
AID1053286 | Fraction unbound in rat brain homogenate at 5 uM after 4 hrs equilibrium dialysis method | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21 | Design, synthesis and discovery of picomolar selective α4β2 nicotinic acetylcholine receptor ligands. |
AID131419 | Potentiation against pentobarbital-induced sleeping, after 1 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
AID592113 | Induction 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%) | 2011 | Journal 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. |
AID705396 | Antipsychotic activity in sc dosed rat prepulse inhibition model | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Current landscape of phosphodiesterase 10A (PDE10A) inhibition. |
AID592133 | Induction 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%) | 2011 | Journal 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. |
AID588217 | FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase | 2004 | Current 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. |
AID194374 | Effect of compound (0.2 mg/kg ip) on the concentration of DOPAC in rat frontal cortex | 1993 | Journal 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. |
AID592131 | Induction 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%) | 2011 | Journal 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. |
AID87516 | Inhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranes | 1997 | Journal 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. |
AID266790 | Reduction 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, ip | 2006 | Journal 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. |
AID254420 | In vitro inhibitory constant against [3H]spiperone binding to human dopamine D2 receptor expressed in CHO cells | 2005 | Journal 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. |
AID1487359 | Antagonist activity at human D2L receptor expressed in CHO cell membranes assessed as residence time after 15 mins by liquid scintillation counting method | 2017 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16 | Influence of the cellular environment on ligand binding kinetics at membrane-bound targets. |
AID438612 | Selectivity ratio of Ki for sigma 2 receptor in rat liver membrane to Ki for sigma 1 receptor in guinea pig brain membrane | 2009 | Journal 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. |
AID5837 | In vitro affinity against serotonin (5-hydroxytryptamine 2C) receptor | 2000 | Journal 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. |
AID298491 | Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells | 2007 | Journal 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. |
AID540209 | Volume of distribution at steady state in human after iv administration | 2008 | Drug 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. |
AID1506086 | Displacement of (+)-[3H]pentazocine from sigma1 receptor in rat brain membranes after 60 mins by liquid scintillation counting method | 2018 | Journal 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. |
AID238940 | Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies. |
AID61358 | Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1 | 2003 | Journal 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. |
AID391277 | Ratio of pKi for human cloned 5HT2A receptor to pKi for human cloned dopamine D2 receptor | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Synthesis, binding affinity, and molecular docking analysis of new benzofuranone derivatives as potential antipsychotics. |
AID229516 | Ratio of IC50 value against dopamine receptor D2 to that of 5-hydroxytryptamine 3 receptor. | 1995 | Journal 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). |
AID1552399 | Displacement of [3H]-(+)pentazocine from sigma-1 receptor in guinea pig brain membranes after 120 mins by scintillation counting method | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16 | Modification of the 4-phenylbutyl side chain of potent 3-benzazepine-based GluN2B receptor antagonists. |
AID64187 | Compound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assay | 1996 | Journal 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. |
AID61620 | Inhibition of [35S]GTP-gamma-S, binding to cell membranes expressing dopamine D2A receptor at 100 uM dopamine | 1999 | Bioorganic & 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. |
AID63531 | Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand | 1996 | Journal 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. |
AID776367 | Displacement of [3H]DTG from sigma-2 receptor in rat liver membrane after 120 mins by scintillation counting | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | New combination of pharmacophoric elements of potent σ₁ ligands: design, synthesis and σ receptor affinity of aminoethyl substituted tetrahydrobenzothiophenes. |
AID1809442 | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 150 mins by microbeta scintillation counting method | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Haloperidol Metabolite II Valproate Ester ( |
AID195772 | Tested for locomotor activity by measuring accumulated counts/30 min in reserpine-non-pretreated rats | 1987 | Journal 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. |
AID63061 | Binding affinity towards human Dopamine receptor D2 using [3H]spiroperidol as radioligand | 2002 | Journal 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. |
AID672150 | Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining relative to acetylcholine | 2012 | Bioorganic & 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. |
AID437143 | Inhibition 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 test | 2009 | European 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. |
AID65564 | In vitro Dopamine receptor D2 affinity by using [3H]-Spiperone as the radioligand in rat limbic system at 1 uM concentration of compound | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | Antipsychotic activity of substituted gamma-carbolines. |
AID64271 | Binding affinity towards Dopamine receptor D2 of rat corpus striatum using [3H]spiperone as radioligand | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
AID190978 | Effect 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/kg | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Troponoids. 6. Troponylpiperazines: a new class of dopamine agonists. |
AID346018 | Displacement of [3H]spiroperidol from human cloned dopaminergic D2 receptor expressed in rat C6 cells | 2008 | Journal 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. |
AID133854 | Anticonvulsant activity against pentylenetetrazole-induced convulsions, after 1 hour of peroral administration in mouse at a dose of 20 mg/kg | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
AID1853647 | Inhibition of Mycobacterium tuberculosis AAC(3')-IV at 200 uM using NEO as substrate in presence of Acetyl-CoA by UV-Vis spectroscopy analysis | 2021 | RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11 | Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from |
AID303621 | Displacement of [3H]ditolylguanidine from sigma 2 receptor in rat liver membrane | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Synthesis of bicyclic sigma receptor ligands with cytotoxic activity. |
AID303628 | Growth inhibition of human MCF7 cells at 20 uM after 96 hrs relative to control | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Synthesis of bicyclic sigma receptor ligands with cytotoxic activity. |
AID1215124 | Binding affinity to Wistar rat brain lipid assessed as percentage unbound by TRANSIL assay | 2011 | Drug 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. |
AID1232316 | Volume of distribution at steady state in mouse | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Volume of Distribution in Drug Design. |
AID65888 | Tested for affinity against cloned mammalian dopamine autoreceptor (DA) D2 receptors expressed in CHO-K1 cells using [3H]spiperone as radioligand | 1994 | Journal 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. |
AID171875 | Antipsychotic efficacy of compound at intraperitoneal dose of 0.5 mg/kg on 6.8 (A10 units) dopamine neurons in the mesolimbic region of rat | 1995 | Journal 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). |
AID1768730 | Relative lipophilicity of the compound in methanol assessed as retardation factor by reversed-phase TLC analysis | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Estimation of the lipophilicity of purine-2,6-dione-based TRPA1 antagonists and PDE4/7 inhibitors with analgesic activity. |
AID629460 | Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane | 2011 | Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22 | Development of a bivalent dopamine D₂ receptor agonist. |
AID63351 | Compound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assay | 1996 | Journal 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. |
AID1636440 | Drug 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 NA | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
AID1409510 | Antipsychotic 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 mins | 2018 | Journal 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. |
AID1853648 | Inhibition of Mycobacterium tuberculosis AAC(2')-Ic at 200 uM using NEO as substrate in presence of Acetyl-CoA by UV-Vis spectroscopy analysis | 2021 | RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11 | Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from |
AID619350 | Displacement of [3H]di-o-tolylguanidine from sigma 2 receptor in rat brain membrane after 120 mins | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Synthesis and pharmacological evaluation of indole-based sigma receptor ligands. |
AID1853690 | Cytotoxicity against mouse J774.A1 cells assessed as reduction in cell viability at 100 uM incubated for 24 hrs by resazurin assay | 2021 | RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11 | Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from |
AID177732 | Inhibition against conditioned avoidance response, after 5 hour of peroral administration in rats | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
AID367547 | Selectivity ratio, Ki for sigma 1 receptor in guinea pig brain homogenates to Ki for sigma 2 receptor in rat liver homogenates | 2009 | Bioorganic & 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. |
AID230925 | Binding affinities for sigma-1 and sigma 2 receptors, ratio of IC50 | 1995 | Journal 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. |
AID592124 | Induction 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%) | 2011 | Journal 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. |
AID1782425 | Displacement of [3H]-SCH23390 from D3 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
AID176063 | Effect on the synthesis rates of dopamine in the rat ventral limbic brain region at 2.7 micro mol/kg. | 1993 | Journal 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. |
AID1853668 | Synergistic antibacterial activity against Mycobacterium smegmatis mc2 155 assessed as fold reduction in MIC value at 8 ug/ml in presence of clarithromycin by checkerboard assay | 2021 | RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11 | Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from |
AID1686276 | Displacement of [3H]-pentazocine from sigma1 receptor in guinea pig brain membranes by scintillation counting | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells. |
AID1136360 | Neuroleptic activity in squirrel monkey assessed as inhibition of Sidman avoidance at 0.75 mg/kg, po measured for 4 hrs | 1978 | Journal 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. |
AID549676 | Displacement of [3H]ditolylguanidine from sigma2 receptor in rat liver membrane by scintillation counting | 2011 | Bioorganic & 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. |
AID1191390 | Selectivity ratio of Ki for rat liver sigma2 receptor to Ki for guinea pig brain cortex sigma1 receptor | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Improving selectivity preserving affinity: new piperidine-4-carboxamide derivatives as effective sigma-1-ligands. |
AID156976 | Compound was tested for its affinity towards PCP receptor in rat brain membrane [3H]MK-801 as radioligand; ND = not determined | 1991 | Journal of medicinal chemistry, Dec, Volume: 34, Issue:12 | Novel 1-phenylpiperazine and 4-phenylpiperidine derivatives as high-affinity sigma ligands. |
AID1185963 | Displacement of [3H]N-methylspiperone from human dopamine D2 receptor by liquid scintillation counting | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17 | Further evaluation of the tropane analogs of haloperidol. |
AID180526 | The compound was tested for its ability to induced catalepsy in rats | 1985 | Journal 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. |
AID1129882 | Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in human RPMI8226 cell membranes after 120 mins by scintillation counting analysis | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | Synthesis, pharmacological evaluation, and σ1 receptor interaction analysis of hydroxyethyl substituted piperazines. |
AID65951 | Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells | 1996 | Journal 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. |
AID1292381 | Terminal half life in psychotic patient (9 patients) at 3.5 +/- 1.2 mg, iv by reversed phase HPLC method | 1987 | Psychopharmacology, , Volume: 91, Issue:4 | Pharmacokinetics of haloperidol in psychotic patients. |
AID1215125 | Percentage unbound in solid supported porcine brain membrane vesicles at 5 uM using four compound cocktail after 5 hrs by TRANSIL assay | 2011 | Drug 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. |
AID410335 | Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat cortex by scintillation spectrometry | 2009 | Journal 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. |
AID1144198 | Acute toxicity in ip dosed Swiss-Webster mouse assessed as tremor administered as single dose after 72 hrs | 1976 | Journal of medicinal chemistry, Jan, Volume: 19, Issue:1 | Synthesis and biological actions of 2-substituted quinolizidines. |
AID1393368 | Displacement of [3H]-raclopride from human D2LR expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method | |||
AID179827 | Tested for the inhibition of locomotor activity in rats intraperitoneally; value ranges from 0.21-0.3 mg/Kg | 1994 | Journal 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. |
AID1292382 | Terminal phase volume of distribution at steady state in psychotic patient (9 patients) at 3.5 +/- 1.2 mg, iv by reversed phase HPLC method | 1987 | Psychopharmacology, , Volume: 91, Issue:4 | Pharmacokinetics of haloperidol in psychotic patients. |
AID1209973 | Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate after 8 mins by LC-MS/MS analysis | 2012 | Drug 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. |
AID226337 | Binding affinity for sigma 1 opioid receptor, measured on guinea pig brain membranes using [3H]- (+)-pentazocine as radioligand | 2001 | Journal 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. |
AID62444 | Inhibition of binding of 5 nM [3H]dopamine to dopamine receptor by 50% | 1981 | Journal 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. |
AID1144217 | Depression of spontaneous motor activity in Swiss-Webster mouse at 5 mg/kg, ip by photocell cage test relative to control | 1976 | Journal of medicinal chemistry, Jan, Volume: 19, Issue:1 | Synthesis and biological actions of 2-substituted quinolizidines. |
AID1169867 | Antipsychotic-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 mins | 2014 | Journal 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. |
AID592134 | Induction 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%) | 2011 | Journal 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. |
AID418670 | Displacement of [3H]1,3-ditolylguanine from sigma 2 receptor in rat liver membrane by solid scintillation analysis | 2009 | Journal 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. |
AID234393 | ratio between ED50 values of DA receptor antagonist activity and catalepsy. | 1998 | Journal 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. |
AID1221962 | Efflux 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 LY335979 | 2011 | Drug 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. |
AID1292383 | Volume of distribution at steady state in psychotic patient (9 patients) at 3.5 +/- 1.2 mg, iv by reversed phase HPLC method | 1987 | Psychopharmacology, , Volume: 91, Issue:4 | Pharmacokinetics of haloperidol in psychotic patients. |
AID391475 | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane | 2008 | Journal 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]. |
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AID239010 | Inhibition of [125I]R91150 binding to human 5-hydroxytryptamine 2A receptor | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
AID180901 | The dose required to reduce the number of apomorphine induced rotation by 50% in rats with monolateral lesion of nigrostriatal tracts | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | Combined analgesic/neuroleptic activity in N-butyrophenone prodine-like compounds. |
AID5708 | Inhibition of [3H]mesulergine binding to 5-hydroxytryptamine 2C receptor in rat brain membranes | 1997 | Journal 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. |
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AID625279 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID116898 | Lethal dose in mice after perorla administration | 1980 | Journal 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. |
AID1744233 | Displacement of [3H]-DTG from sigma-2 receptor in guinea pig brain membrane incubated for 1 hr by liquid scintillation counting method | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1 | Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management. |
AID1169869 | Antipsychotic-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 mins | 2014 | Journal 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. |
AID395328 | Lipophilicity, log P of the compound | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
AID711574 | Half life in rat liver microsomes | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Synopsis of some recent tactical application of bioisosteres in drug design. |
AID176225 | Inhibition of apomorphine-induced stereotypy in rats via peroral route | 1992 | Journal 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. |
AID642496 | Displacement of [3H]-1,3-di(o-tolyl)guanidine from sigma 2 receptor in rat liver homogenates in the presence of (+)-pentazocine | 2012 | Bioorganic & 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. |
AID549675 | Selectivity ratio of Ki for guinea pig sigma1 receptor to Ki rat sigma2 receptor | 2011 | Bioorganic & 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. |
AID1867871 | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes measured after 120 mins by scintillation counting method | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Synthesis and biological evaluation of conformationally restricted GluN2B ligands derived from eliprodil. |
AID1285664 | Displacement of [3H]DTG from sigma receptor in human jurkat cells | 2016 | Bioorganic & 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. |
AID184035 | In vivo activity administered intraperitoneally was determined by social interaction of rat at 5.0 uM | 1991 | Journal 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. |
AID1744236 | Displacement of [3H]-DTG from sigma-2 receptor in human Jurkat cell membrane incubated for 1 hr by liquid scintillation counting method | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1 | Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management. |
AID1079935 | Cytolytic 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] | |||
AID181424 | Tested for the amphetamine induced stereotyped behavior in rats after oral administration | 1993 | Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7 | Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system. |
AID1308623 | Growth inhibition of human A427 cells incubated for 96 hrs by crystal violet assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity? |
AID711573 | Clearance in human liver microsomes | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Synopsis of some recent tactical application of bioisosteres in drug design. |
AID5018 | Effective dose through peroral route for in vivo inhibition against 5-hydroxytryptamine 2 receptor in male CF-1 mice by using radioligand [3H]ketanserin | 1993 | Journal 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. |
AID1213074 | Drug metabolism assessed as recombinant human UGT2B7 assessed as O-glucuronidation at 10 to 400 uM incubated for 60 mins by LC-MS/MS analysis | 2012 | Drug 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. |
AID298264 | Displacement of [3H]spiroperidol from human cloned dopamine D2L receptor | 2007 | Journal 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. |
AID177108 | ED50 value for catalepsy indicates the dose required to produce a 50% of maximum catalepsy score. parentheses value indicate 95% confidence limit. | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | Pyrrole mannich bases as potential antipsychotic agents. |
AID977599 | Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
AID1168800 | Antagonist activity at D2 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of quinpirole | 2014 | Bioorganic & 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. |
AID382243 | Binding affinity to adrenergic alpha1 receptor | 2008 | Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9 | Recent advances in selective alpha1-adrenoreceptor antagonists as antihypertensive agents. |
AID26304 | Partition coefficient (logD6.5) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID259127 | Selectivity ratio for dopamine D2-like receptor over dopamine D3 receptor | 2006 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2 | Design of novel hexahydropyrazinoquinolines as potent and selective dopamine D3 receptor ligands with improved solubility. |
AID130897 | Inhibition of locomotor activity in mouse after intraperitoneal administration | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines. |
AID203984 | In vitro binding affinity measured on sigma opioid receptor using [3H]DTG as radioligand | 1995 | Journal 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. |
AID5491 | Binding affinity towards 5-hydroxytryptamine 2A receptor binding site using [3H]ketanserin. | 1995 | Journal 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. |
AID63371 | Binding affinity against dopamine receptor D1 | 1994 | Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4 | Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study. |
AID1616722 | Displacement of PPHT-red from SNAP-tagged human D2LR expressed in CHOK1 cell membranes assessed as dissociation half-life by TR-FRET assay | |||
AID1861724 | Binding affinity to sigma 2 receptor (unknown origin) assessed as inhibition constant by radioligand binding assay | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
AID1433418 | Displacement of [3H]-PTZ from sigma1 receptor in guinea pig brain membranes after 150 mins in presence of DPH solvent by liquid scintillation counting method | |||
AID277985 | Antagonist activity against rat D2 receptor assessed effect on quinelorane-stimulated [35S]GTP-gamma-S binding | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities. |
AID701946 | Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting | 2012 | Journal 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. |
AID176662 | Suppression of conditioned avoidance behavior in rats after ip administration | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | 2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2. |
AID65894 | Tested for binding affinity towards rat striatal D2 receptor using [3H]spiperone as radioligand | 1994 | Journal 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. |
AID1861725 | Selectivity index, ratio of Ki for sigma 1 receptor (unknown origin) to Ki for sigma 2 receptor (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
AID223305 | Effective dose administered in apomorphine induced climbing test in mice (in vivo)value in parentheses represents 95% confidence limit | 2000 | Journal 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. |
AID1598360 | Antagonist 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 | |||
AID23695 | Partition coefficient (logP) | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
AID63682 | Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells. | 1997 | Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15 | 4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor. |
AID180551 | The compound was tested in vivo for induction of catalepsy in rat after ip administration | 1999 | Journal 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. |
AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
AID37370 | Half-maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor in rat frontal cortex homogenate | 2002 | Journal 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. |
AID1853639 | Potentiation 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 assay | 2021 | RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11 | Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from |
AID256758 | Displacement of [3H]spiroperidol from cloned human dopamine receptor D3 in CHO cell membrane | 2005 | Journal 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. |
AID1144202 | Depression of forced motor activity in Swiss-Webster mouse at 10 mg/kg, ip after 30 mins by rotarod test relative to control | 1976 | Journal of medicinal chemistry, Jan, Volume: 19, Issue:1 | Synthesis and biological actions of 2-substituted quinolizidines. |
AID194523 | Effect of compound on (0.2 mg/kg ip) the concentration of 5-HIAA in rat mesolimbic region | 1993 | Journal 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. |
AID37455 | Affinity for alpha-1 adrenergic receptor | 1998 | Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8 | Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors. |
AID458650 | Reduction in amphetamine-induced locomotor activity in Sprague-Dawley rat striatum at 1 umol/kg, sc relative to control | 2010 | Journal 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). |
AID1441553 | Displacement of [3H]-DTG from sigma 2 receptor in rat liver membranes after 120 mins by scintillation counting | 2017 | Journal 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. |
AID1409509 | Antipsychotic 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 dose | 2018 | Journal 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. |
AID1213036 | Drug metabolism assessed as recombinant human UGT1A1 assessed as O-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis | 2012 | Drug 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. |
AID176331 | Inhibition of d-amphetamine induced stereotypy in rats; i.p. treatment 1 hr before amphetamine. | 1986 | Journal 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. |
AID524791 | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
AID625280 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1409613 | Selectivity 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. | 2020 | Nature, 07, Volume: 583, Issue:7816 | A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
AID724161 | Displacement of (+)-[3H]pentazocine from sigma1 receptor in rat brain membranes | 2013 | Bioorganic & 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. |
AID517711 | Displacement of [3H]WAY-100635 from 5-HT1A receptor in pig cerebral cortex homogenates | 2010 | Journal 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. |
AID444008 | Antagonist activity at sigma2 receptor in guinea pig ileum longitudinal muscle assessed as inhibition of 5-HT-induced contractions | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane. |
AID1686280 | Cytotoxicity in HREC assessed as reduction in cell viability incubated for 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells. |
AID224650 | Area under curve(AUC) value of Dopamine level after total treatment in dialysates collected from rat striatum. | 2002 | Journal 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. |
AID1210071 | Inhibition of CYP3A4 in human liver microsomes using testosterone substrate by LC-MS/MS method | 2013 | Drug 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. |
AID176807 | Suppression of conditioned avoidance behavior in rats when administered intraperitoneally 60 min before measurement | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | 2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1. |
AID3699 | The binding affinity was measured on serotonin 5-hydroxytryptamine 1 receptor in rat brain tissue | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | Pyrrole mannich bases as potential antipsychotic agents. |
AID1878192 | Ratio of Ki for binding affinity to D2S (unknown origin) to Ki for binding affinity to D3R (unknown origin) | |||
AID566433 | Displacement radioligand form dopamine D3 receptor in rat olfactory tubercle by liquid scintillation counting | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Antiproliferative activity of phenylbutyrate ester of haloperidol metabolite II [(±)-MRJF4] in prostate cancer cells. |
AID65563 | Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate | 2002 | Journal 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. |
AID203698 | Compound was tested for its binding affinity towards sigma 1 receptor using [3H](+)-pentazocine from guinea pig brain | 1998 | Journal 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. |
AID170279 | Locomotor activity after reserpine pretreatment in rat; Not Tested | 1985 | Journal of medicinal chemistry, Aug, Volume: 28, Issue:8 | Novel dopamine receptor agonists and antagonists with preferential action on autoreceptors. |
AID444051 | Total clearance in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID1213083 | Drug 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 control | 2012 | Drug 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. |
AID113687 | Inhibition of head twitches-induced by 2,5-dimethoxy-4-iodoamphetamine in mice. | 1998 | Journal 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). |
AID63028 | Ability to inhibit [3H]haloperidol binding to dopamine receptor in rat striatal homogenate | 1985 | Journal 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. |
AID130864 | In vivo the ability to antagonize the apomorphine induced climbing response in mice | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16 | Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents. |
AID1441551 | Displacement of [3H]-(+)-pentazocine from sigma1-type opioid receptor in guinea pig cortex membranes after 120 mins by solid scintillation counting | 2017 | Journal 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. |
AID1478365 | Displacement of [3H]-(+)-DTG from sigma2 receptor in guinea pig brain membrane after 120 mins by liquid scintillation counting method | 2018 | Journal 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. |
AID1213092 | Drug 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 control | 2012 | Drug 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. |
AID131873 | Effective dose required for inhibition of apomorphine(sc, 2.5 mg/kg ) induced climbing in mice on ip administration | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
AID1213045 | Drug metabolism assessed as Sprague-Dawley rat liver microsomes assessed as velocity of O-glucuronidation at 100 uM by LC-MS/MS analysis | 2012 | Drug 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. |
AID138928 | Antagonism of apomorphine for 10-20 minutes in reserpinized mice when a dose of 2.7 micro mol/kg is administered intraperitoneally | 1993 | Journal 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. |
AID141682 | The compound was tested for inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor | 1985 | Journal 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. |
AID128163 | Activity of inclined screen in mouse, after 5 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
AID204443 | Ability to displace [3H](+)-pentazocine at sigma receptor in guinea pig brain membrane was determined | 1993 | Journal 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. |
AID737843 | Selectivity ratio of Ki for sigma 2 receptor in rat liver membranes to Ki for sigma 1 receptor in guinea pig brain membranes | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | Improvement of σ1 receptor affinity by late-stage C-H-bond arylation of spirocyclic lactones. |
AID1213049 | Drug metabolism assessed as recombinant human UGT1A7 assessed as N-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis | 2012 | Drug 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. |
AID138757 | Ability to stimulate dopaminergic systems by effect on locomotor activity in reserpinized mice when a dose of 0.3 micro mol/kg is administered intraperitoneally | 1993 | Journal 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. |
AID1146537 | Inhibition of apomorphine-induced stereotyped behavior in po dosed albino Wistar rat administered 2 hrs before apomorphine challenge measured after 20 mins | 1978 | Journal of medicinal chemistry, Nov, Volume: 21, Issue:11 | Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity. |
AID204596 | Binding affinity against sigma receptor of MCF cells | 1994 | Journal 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. |
AID1782426 | Displacement of [3H]-LSD from 5HT1A receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
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AID5197 | Binding affinity towards human serotonin 5-hydroxytryptamine 2A receptor | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Selective optimization of side activities: another way for drug discovery. |
AID1135932 | Neuroleptic activity in ip dosed ICR-DUB mouse assessed as survival administered 3 days prior to d-amphetamine challenge measured after 24 hrs | 1978 | Journal 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. |
AID1545633 | Displacement 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 control | 2019 | Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18 | Novel multitarget 5-arylidenehydantoins with arylpiperazinealkyl fragment: Pharmacological evaluation and investigation of cytotoxicity and metabolic stability. |
AID1209974 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate after 8 mins by LC-MS/MS analysis | 2012 | Drug 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. |
AID177958 | Antagonistic activity administered intraperitoneally on head twitches induced by 5- HTP | 1995 | Journal 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). |
AID184992 | Compound is evaluated for locomotor activity in nonhabituated rats at 1.3 micro mol/kg of subcuteneous dose | 1994 | Journal 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. |
AID35274 | Evaluated for binding affinity against alpha-1 adrenergic receptor | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 | A rapid computational method for lead evolution: description and application to alpha(1)-adrenergic antagonists. |
AID65935 | In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement. | 1998 | Journal 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. |
AID437147 | Inhibition 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 test | 2009 | European 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. |
AID595907 | Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 150 mins | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10 | Novel potent and selective σ ligands: evaluation of their agonist and antagonist properties. |
AID566274 | Inhibition of rat sigma receptor | 2010 | Bioorganic & 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 |
AID176476 | Catalepsy interval defined as the time required for both fore limbs to be removed from the bar when administered intraperitoneally | 1990 | Journal of medicinal chemistry, Apr, Volume: 33, Issue:4 | Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds. |
AID63971 | Binding affinity for dopamine receptor D2 determined using [3H]spiperone | 2001 | Bioorganic & 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. |
AID1308625 | Growth inhibition of human 5637 cells incubated for 96 hrs by crystal violet assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity? |
AID457705 | Toxicity 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) | 2010 | Bioorganic & 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. |
AID1063796 | Displacement of [3H]N-Methylspiperone from dopamine D2 receptor (unknown origin) | 2014 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2 | The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds. |
AID1726851 | Selectivity index, ratio of Ki for human sigma1 receptor expressed in HEK293 cell membrane to Ki for sigma2 receptor in SPRD rat liver membrane | |||
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AID1433420 | Displacement 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 | |||
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AID1594272 | Displacement of [3H]-DTG from sigma2 receptor in guinea pig brain membranes after 120 mins in presence of sigma1 antagonist (+)-SKF10047 by microbeta scintillation counting method | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9 | Discovery of a novel class of potent and selective tetrahydroindazole-based sigma-1 receptor ligands. |
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AID36730 | Its affinity towards alpha-1 receptor using [3H]WB-4101 as radioligand in whole brain minus cerebellum | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents. |
AID1532588 | Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes at 1 uM after 60 mins relative to control | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Novel multitarget-directed ligands targeting acetylcholinesterase and σ |
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AID342778 | Binding affinity to human cloned dopamine D3 receptor | 2008 | Bioorganic & 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. |
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AID1135931 | Neuroleptic activity in ip dosed ICR-DUB mouse assessed as survival administered 2 days prior to d-amphetamine challenge measured after 24 hrs | 1978 | Journal 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. |
AID259123 | Displacement of [3H]SCH 23390 from rat caudate putamen dopamine D1-like receptor | 2006 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2 | Design of novel hexahydropyrazinoquinolines as potent and selective dopamine D3 receptor ligands with improved solubility. |
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AID36137 | In vitro binding affinity towards alpha-1 adrenergic receptor by using [3H]-prazosin in rat brain cortex membranes. | 2000 | Journal 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. |
AID37441 | Binding affinity was evaluated against Alpha-1 adrenergic receptor on rat cortex using [3H]prazosin as radioligand; ND = Not determined | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15 | Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists. |
AID1213069 | Intrinsic clearance in recombinant human UGT1A4 measured per mg of protein at 10 to 400 uM by LC-MS/MS analysis | 2012 | Drug 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. |
AID61619 | Inhibition of [35S]GTP-gamma-S, binding to cell membranes expressing dopamine D2A receptors at 100 uM | 1999 | Bioorganic & 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. |
AID1144195 | Acute toxicity in ip dosed Swiss-Webster mouse administered as single dose after 7 days | 1976 | Journal of medicinal chemistry, Jan, Volume: 19, Issue:1 | Synthesis and biological actions of 2-substituted quinolizidines. |
AID1300374 | Toxicity 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) | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Synthesis and Biological Evaluation of Novel σ1 Receptor Ligands for Treating Neuropathic Pain: 6-Hydroxypyridazinones. |
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AID1782428 | Displacement of [3H]-LSD from 5HT2C receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
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AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
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AID1853637 | Inhibition 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 | 2021 | RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11 | Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from |
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AID160798 | The irreversibility of the inactivation reaction of HIV-2 PR was assessed; NI =No detectable reversible reaction | 1994 | Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5 | Haloperidol-based irreversible inhibitors of the HIV-1 and HIV-2 proteases. |
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AID1128477 | Inhibition of conditioned avoidance response in Sprague-Dawley rat model at 2 mg/kg, po after 2 hrs by electric foot shock test | 2014 | Journal 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. |
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AID142719 | Binding affinity was measured against muscarinic (M1) receptor in rat using [3H]pirenzepine as radioligand | 1994 | Journal 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. |
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AID1409511 | Induction of catalepsy in po dosed Kunming mouse measured after 60 secs | 2018 | Journal 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. |
AID142225 | Binding affinity towards Muscarinic acetylcholine receptor in rat was determined | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships. |
AID277978 | Normalizing effect on methylphenidate-induced behaviours in ip dosed rat after 30 min | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities. |
AID1153309 | Antagonist 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 | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
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AID1288455 | Displacement of [3H]N-methylspiperone from human dopamine D2 receptor by PDSP assay | 2016 | Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9 | Tetrahydroprotoberberine alkaloids with dopamine and σ receptor affinity. |
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AID45980 | Compound was evaluated for the inhibition of [3H]haloperidol binding in calf brain homogenates | 1981 | Journal of medicinal chemistry, Jun, Volume: 24, Issue:6 | Synthesis and evaluation of novel alkylpiperazines as potential dopamine antagonists. |
AID715356 | Toxicity in rat assessed as increase in prolactin level up to 1.5 mg/kg, po | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18 | Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia. |
AID1147993 | Reduction 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 mins | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | 2,5-Bis(3,4-dimethoxybenzyl)cyclopentylamine, a peripheral dopamine blocking agent. |
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AID1127305 | Selectivity ratio of Ki for sigma 2 receptor in Dunkin Hartley guinea pig membrane to Ki for sigma 1 receptor in Dunkin Hartley guinea pig membrane | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Synthesis and biological evaluation of a novel sigma-1 receptor antagonist based on 3,4-dihydro-2(1H)-quinolinone scaffold as a potential analgesic. |
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AID588215 | FDA HLAED, alkaline phosphatase increase | 2004 | Current 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. |
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AID1191391 | Displacement of [3H]MK801 from pig brain cortex NMDA receptor PCP binding site at 1 uM by scintillation analyzer | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Improving selectivity preserving affinity: new piperidine-4-carboxamide derivatives as effective sigma-1-ligands. |
AID63064 | Binding affinity on human Dopamine receptor D2 expressed in CHO cells using radioligand [3H]-YM 09151 | 1997 | Journal 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. |
AID64295 | In vitro binding affinity at Dopamine receptor D2 in rat by displacing [3H]- spiperone from rat striatal membrane | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | Potential neuroleptic agents. 3. Chemistry and antidopaminergic properties of substituted 6-methoxysalicylamides. |
AID65494 | Inhibitory constant towards reuptake of [125I]-12 from dopamine transporter in rat striatal membranes | 1994 | Journal 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. |
AID1690209 | Displacement of [3H]-(+)-pentazocine from Sigma1 receptor in guinea pig cortex membranes incubated for 120 mins by scintillation counting method | |||
AID1144205 | Depression of forced motor activity in Swiss-Webster mouse at 5 mg/kg, ip after 30 mins by rotarod test relative to control | 1976 | Journal of medicinal chemistry, Jan, Volume: 19, Issue:1 | Synthesis and biological actions of 2-substituted quinolizidines. |
AID1415571 | Displacement of [3H](+)-Pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis | 2017 | MedChemComm, May-01, Volume: 8, Issue:5 | Do GluN2B subunit containing NMDA receptors tolerate a fluorine atom in the phenylalkyl side chain? |
AID640310 | Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting | 2012 | Bioorganic & 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. |
AID1215963 | Activity of recombinant carbonyl reductase (unknown origin) | 2013 | Drug 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. |
AID1297660 | Displacement of [3H]DTG from sigma2 receptor in rat liver homogenate incubated for 120 mins by solid scintillation counting analysis | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Benzimidazolone bioisosteres of potent GluN2B selective NMDA receptor antagonists. |
AID1185978 | Toxicity in ip dosed Sprague-Dawley rat assessed as catalepsy by crossed-legs position test | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17 | Further evaluation of the tropane analogs of haloperidol. |
AID439064 | Displacement of [3H]spiperone from human cloned dopamine D2 receptor | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21 | Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif. |
AID448644 | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain after 180 mins by scintillation counting | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis of sigma receptor ligands with unsymmetrical spiro connection of the piperidine moiety. |
AID63800 | Compound was evaluated for its affinity (pKi) to inhibit [3H]spiperone binding to the Dopamine receptor D2 | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Synthesis and antidopaminergic activity of some 3-(aminomethyl)tetralones as analogues of butyrophenone. |
AID161627 | Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells | 2003 | Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17 | Antimalarial drug quinacrine binds to C-terminal helix of cellular prion protein. |
AID1136138 | Ratio 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 rat | 1978 | Journal of medicinal chemistry, Jul, Volume: 21, Issue:7 | Neuroleptics related to butaclamol. Synthesis and some psychopharmacological effects of a series of 3-aryl analogues. |
AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
AID63347 | Binding affinity towards human Dopamine receptor D1 | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Selective optimization of side activities: another way for drug discovery. |
AID5218 | Ability to inhibit [3H]spiperone binding to 5-hydroxytryptamine 2 receptor determined in rat | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | 2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1. |
AID1809444 | Antiproliferative activity against VEGF-A stimulated human retinal endothelial cell assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Haloperidol Metabolite II Valproate Ester ( |
AID1215962 | Activity of carbonyl reductase in liver cytosol (unknown origin) assessed as enzyme-mediated drug metabolism | 2013 | Drug 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. |
AID1300373 | Toxicity 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) | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Synthesis and Biological Evaluation of Novel σ1 Receptor Ligands for Treating Neuropathic Pain: 6-Hydroxypyridazinones. |
AID317390 | Displacement of [3H](+)-PTZ from sigma1 receptor in Hartley guinea pig brain | 2008 | Bioorganic & 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. |
AID1704752 | Therapeutic 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 | |||
AID3756 | In vitro binding affinity for serotonin 5-hydroxytryptamine 1A receptor fof rat cerebral cortex using [3H]8-OH-DPAT as radioligand | 2002 | Journal 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. |
AID211852 | Acute toxicity on male outbred albino mice upon intraperitoneal administration | 1998 | Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3 | Design of N-acylprolyltyrosine "tripeptoid" analogues of neurotensin as potential atypical antipsychotic agents. |
AID184659 | Compound was evaluated for the inhibition of haloperidol induced catalepsy behavior in rats after sc administration; Inactive | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | 1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents. |
AID492187 | Displacement of [3H]DTG from sigma 2 receptor in rat liver homogenates after 1 hr by liquid scintillation counting | 2010 | Bioorganic & 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. |
AID750622 | Toxicity in po dosed mouse assessed as induction of catalepsy | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics. |
AID113543 | Induction of catalepsy in mice | 1998 | Journal 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. |
AID1861729 | Cytotoxicity 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 assay | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
AID49738 | Compound 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 inhibition | 1986 | Journal of medicinal chemistry, Dec, Volume: 29, Issue:12 | p-Dimethoxy-substituted trans-octahydrobenzo[f]- and -[g]quinolines: synthesis and assessment of dopaminergic agonist effects. |
AID4053 | Compound was evaluated for in vitro binding affinity towards 5-hydroxytryptamine 1A receptor in rat hippocampus using [3H]8-OH-DPAT as radioligand | 1992 | Journal 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. |
AID62736 | Affinity for Dopamine receptors in the rat striatum using [3H]spiroperidol displacement. | 1986 | Journal 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. |
AID150735 | High affinity constant at binding site of human P-Glycoprotein (P-gp) in two-affinity model | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis). |
AID1393470 | Therapeutic 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 | |||
AID1308624 | Growth inhibition of human LCLC-103H cells incubated for 96 hrs by crystal violet assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity? |
AID234273 | Selectivity is determined by the ratio of Ki for rat sigma 2 receptor to that of guinea pig sigma-1 receptor | 2001 | Journal 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. |
AID1063782 | Displacement of [3H](+)Pentazocine from sigma 1 receptor (unknown origin) | 2014 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2 | The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds. |
AID420668 | Inhibition of human ERG in MCF7 cells | 2009 | European 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. |
AID171010 | Change in rectal temperature induced by DiPr-5,6-ADTN at a dose of 2.7 umol/kg of compound by subcutaneous administration | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists. |
AID204304 | Ability to displace [3H]ditolylguanidine in the presence of 100 nM (+)-pentazocine from Sigma opioid receptor type 2 of rat liver | 2002 | Journal 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. |
AID176231 | Effective peroral dose for inhibition of conditioned avoidance response in rats | 1992 | Journal 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. |
AID298478 | Displacement of [3H]spiperone from human dopamine D2 receptor short form expressed in CHO cells | 2007 | Journal 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. |
AID177826 | Effective dose against DOPA accumulation in rat brain striatal region after reserpine pretreatment by subcutaneous administration; No significant effect at 0.5 mg/kg intraperitoneal administration | 1985 | Journal of medicinal chemistry, Aug, Volume: 28, Issue:8 | Novel dopamine receptor agonists and antagonists with preferential action on autoreceptors. |
AID243273 | Binding affinity towards dopamine receptor D2 was determined | 2005 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8 | The role of QSAR in dopamine interactions. |
AID63055 | Binding affinity towards cloned human Dopamine receptor D2 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand | 1996 | Journal 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. |
AID592127 | Induction 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%) | 2011 | Journal 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. |
AID1701184 | Displacement of [3H]-(+)-pentazocine from human sigma1 receptor expressed in HEK293 cell membranes incubated for 120 mins by liquid scintillation counting method | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | EST64454: a Highly Soluble σ |
AID5321 | Binding affinity towards 5-hydroxytryptamine 2A receptor using [3H]ketanserin | 2003 | Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2 | New arylpiperazine derivatives with high affinity for alpha1A, D2 and 5-HT2A receptors. |
AID177506 | In vivo inhibition of apomorphine induced stereotypy in rat by the compound administered intraperitoneally | 1991 | Journal 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. |
AID64601 | Neuroleptic activity in terms of [3H]spiroperidol binding in rat striatal membrane to Dopamine receptor D2 | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | Common stereospecificity of opioid and dopamine systems for N-butyrophenone prodine-like compounds. |
AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
AID65239 | Binding affinity towards Dopamine receptor D2 | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships. |
AID33271 | Compound was evaluated In vitro for its activity by binding to Alpha adrenergic receptor in the rat brain using [3H]prazosin as radioligand. | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | 1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents. |
AID170883 | Percentage change in Total activity (anti psychotic) when compound administered at a doe of 0.05 mg/kg ip in rats | 1996 | Journal 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. |
AID1071721 | Therapeutic 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 response | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics. |
AID1185977 | Toxicity in ip dosed Sprague-Dawley rat assessed as catalepsy by Bar test | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17 | Further evaluation of the tropane analogs of haloperidol. |
AID342777 | Binding affinity to human cloned dopamine D2 receptor | 2008 | Bioorganic & 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. |
AID303625 | Growth inhibition of human RT4 cells at 20 uM after 96 hrs relative to control | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Synthesis of bicyclic sigma receptor ligands with cytotoxic activity. |
AID233472 | Hill coefficient for [3H]-Raclopride binding for high and low affinity binding to dopamine D2 receptor | 1999 | Bioorganic & 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. |
AID113686 | Inhibition of grooming-induced by SKF 38393 in mice. | 1998 | Journal 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). |
AID492634 | Antipsychotic activity in ip dosed NMRI mouse assessed as reduction in spontaneous exploratory locomotor activity administered 30 mins prior to testing measured for 60 mins | 2010 | Journal 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. |
AID1213087 | Drug metabolism assessed as human liver microsomes assessed as velocity of O-glucuronidation at 100 uM by LC-MS/MS analysis | 2012 | Drug 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. |
AID588212 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
AID63849 | Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
AID444007 | Selectivity for human sigma1 receptor over rat sigma2 receptor | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane. |
AID1461564 | Displacement of [3H]spiperone from human D3 receptor expressed in CHO cell membranes by radioligand binding assay | 2017 | Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19 | Potent haloperidol derivatives covalently binding to the dopamine D2 receptor. |
AID113139 | Compound was tested in vivo for its ability to antagonize apomorphine-induced climbing response in mice upon intraperitoneal administration | 1998 | Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3 | Design of N-acylprolyltyrosine "tripeptoid" analogues of neurotensin as potential atypical antipsychotic agents. |
AID177487 | Effect on Motor activity(MA) in rat was measured as ED50 by perorally administration of compound. | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | N6-(2,2-diphenylethyl)adenosine, a novel adenosine receptor agonist with antipsychotic-like activity. |
AID5123 | In vitro binding affinity against rat 5-hydroxytryptamine 2 receptor. | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
AID481104 | Displacement of [3H](+)-pentazocine from sigma1 receptor in guinea pig brain membrane | 2010 | Journal 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. |
AID625290 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID130133 | Neuroleptic activity in vivo by ability to antagonise climbing in apomorphine dosed mice after intraperitoneal administration. | 1985 | Journal of medicinal chemistry, Jun, Volume: 28, Issue:6 | Synthesis and neuroleptic activity of 3-(1-substituted-4-piperidinyl)-1,2-benzisoxazoles. |
AID87531 | In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine | 2004 | Journal 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. |
AID1146536 | Inhibition of methamphetamine-induced stereotyped behavior in po dosed albino Wistar rat administered 2 hrs before methamphetamine challenge measured up to 3 hrs | 1978 | Journal of medicinal chemistry, Nov, Volume: 21, Issue:11 | Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity. |
AID457707 | Toxicity 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) | 2010 | Bioorganic & 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. |
AID112818 | Compound was tested for inhibition of Apomorphine induced climbing in Mice | 1996 | Journal 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. |
AID1249734 | Displacement of [3H]spiperone from human dopamine D2L receptor expressed in CHO cells | 2015 | ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8 | Multicomponent Synthesis and Biological Evaluation of a Piperazine-Based Dopamine Receptor Ligand Library. |
AID131420 | Potentiation against pentobarbital-induced sleeping, after 5 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
AID317391 | Displacement of [3H]DTG from sigma2 receptor in Hartley guinea pig brain | 2008 | Bioorganic & 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. |
AID61151 | Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
AID1292386 | Serum clearance in psychotic patient (9 patients) at 3.5 +/- 1.2 mg, iv by reversed phase HPLC method based model-dependent approach analysis | 1987 | Psychopharmacology, , Volume: 91, Issue:4 | Pharmacokinetics of haloperidol in psychotic patients. |
AID65885 | Affinity against the dopamine receptor D2 using [3H]spiperinone. | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | N-aryl-N'-benzylpiperazines as potential antipsychotic agents. |
AID113351 | In vivo effective dose for inhibition of apomorphine-induced climbing in mice after intraperitoneal administration at a dose 20 mg/kg | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents. |
AID22293 | Delta logD (logD6.5 - logD7.4) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID218670 | The compound was tested for inhibition of [3H]WB-4101 binding to alpha-1 adrenergic receptor of rat frontal cortex | 1985 | Journal 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. |
AID1079936 | Choleostatic 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] | |||
AID197732 | Cataleptogenic activity was evaluated for the compound as the 50% effective dose required to induce cataleptic effect in rats | 1987 | Journal 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. |
AID578857 | Selectivity ratio, ratio of Ki for pig sigma1 receptor to Ki for pig sigma2 receptor | 2011 | Bioorganic & 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. |
AID178517 | Inhibition of conditioned avoidance response (CAR) | 1986 | Journal 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. |
AID418677 | Cytotoxicity against human LCLC-103H cells after 96 hrs by crystal violet staining | 2009 | Journal 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. |
AID444056 | Fraction escaping gut-wall elimination in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID1638285 | Displacement of [3H]-DTG from sigma2 receptor in rat brain membranes after 120 mins in presence of (+)-pentazocine by radioligand binding assay | |||
AID342773 | Binding affinity to human cloned 5HT6 receptor | 2008 | Bioorganic & 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. |
AID5485 | Inhibition of [3H]ketanserin binding to rat frontal cortex membrane 5-hydroxytryptamine 2A receptor | 1998 | Journal 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). |
AID1129883 | Displacement of [3H]-DTG from sigma-2 receptor in human RT4 cell membranes after 120 mins by scintillation counting analysis in presence of (+)-pentazocine | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | Synthesis, pharmacological evaluation, and σ1 receptor interaction analysis of hydroxyethyl substituted piperazines. |
AID150405 | Compound was tested for its binding affinity towards Opioid receptors in rat membranes in the presence of [3H]naloxone | 1998 | Journal of medicinal chemistry, May-07, Volume: 41, Issue:10 | (+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties. |
AID729692 | Antagonist activity at dopamine D2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay | 2013 | Bioorganic & 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. |
AID1308628 | Growth inhibition of human MCF7 cells incubated for 96 hrs by crystal violet assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity? |
AID566432 | Displacement radioligand form dopamine D2 receptor in rat striatum by liquid scintillation counting | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Antiproliferative activity of phenylbutyrate ester of haloperidol metabolite II [(±)-MRJF4] in prostate cancer cells. |
AID194525 | Effect of compound on (0.2 mg/kg ip) the concentration of 5-HT in rat mesolimbic region | 1993 | Journal 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. |
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AID1809449 | Antiangiogenic activity against VEGF-A stimulated Human endothelial cell assessed as cell proliferation measured after 72 hrs by crystal violet assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Haloperidol Metabolite II Valproate Ester ( |
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AID1756662 | Displacement of [3H]N-methylspiperone from human D3 receptor expressed in HEK293T cells co-expressing CRE-Luc incubated for 60 mins by microbeta scintillation counting method | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the H |
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AID1079933 | Acute 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 | |||
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AID180915 | The inhibitory effect on the continuous avoidance was expressed as the dose to increase the number of electroshocks by 60% of the rats | 1981 | Journal 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. |
AID1823687 | Antagonist 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 | |||
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AID134417 | Lethal dose in mice after perorla administration | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8 | 4-Piperazinyl-10H-thieno[2,3-b][1,5]benzodiazepines as potential neuroleptics. |
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AID3730 | Binding affinity towards serotonin 5-HT1A receptor was determined in rat hippocampus using [3H]8-OH-DPAT as ligand | 1996 | Journal 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. |
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AID1809447 | Antiangiogenic activity against VEGF-A stimulated human retinal endothelial cell assessed as cell proliferation measured after 24 hrs by crystal violet assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Haloperidol Metabolite II Valproate Ester ( |
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AID61617 | Inhibition of [35S]GTP-gamma-S, binding to cell membranes expressing dopamine D2A receptors at 10 uM | 1999 | Bioorganic & 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. |
AID619547 | Displacement of (+)-[3H]pentazocine from guinea pig brain sigma 1 receptor after 180 mins by scintillation counting | 2011 | Journal 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. |
AID63692 | Selectivity is the ratio of binding affinities for human Dopamine receptor D4 to that of Dopamine receptor D3 | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10 | Design and synthesis of a piperazinylalkylisoxazole library for subtype selective dopamine receptor ligands. |
AID135326 | BBB penetration classification | 2000 | Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11 | Predicting blood-brain barrier permeation from three-dimensional molecular structure. |
AID5053 | Compound was tested for the inhibition of quipazine induced head twitches in rats | 1992 | Journal 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. |
AID753962 | Displacement of [3H]DTG from sigma2 receptor in Sprague-Dawley rat liver membrane after 150 mins by liquid scintillation counting analysis | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Synthesis and receptor binding studies of novel 4,4-disubstituted arylalkyl/arylalkylsulfonyl piperazine and piperidine-based derivatives as a new class of σ1 ligands. |
AID1300372 | Toxicity 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) | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Synthesis and Biological Evaluation of Novel σ1 Receptor Ligands for Treating Neuropathic Pain: 6-Hydroxypyridazinones. |
AID170896 | Percentage change in chronic single unit sampling when compound given at a dose of 0.5 mg/kg ip in rats (Expt-2) | 1996 | Journal 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. |
AID391274 | Displacement of [3H]ketanserin from human cloned 5HT2A receptor | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Synthesis, binding affinity, and molecular docking analysis of new benzofuranone derivatives as potential antipsychotics. |
AID61670 | Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1 | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Synthesis and antidopaminergic activity of some 3-(aminomethyl)tetralones as analogues of butyrophenone. |
AID729708 | Agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay | 2013 | Bioorganic & 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. |
AID1125902 | Displacement of [3H]methylspiperone from human D2L receptor expressed in HEK cell membrane after 90 mins by scintillation counting analysis | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8 | Discovery, optimization, and characterization of novel D2 dopamine receptor selective antagonists. |
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AID205267 | Inhibition 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 | 1985 | Journal 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. |
AID176733 | Dose (administered orally) inhibiting amphetamine-induced locomotor behavior in rats | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
AID142500 | In vitro inhibition of [3H]-Oxo-Mas binding to M1 and M4 receptors in rat brain homogenate; Not tested. | 1998 | Journal 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. |
AID5330 | Inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor rat frontal cortex membrane | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16 | Synthesis and atypical antipsychotic profile of some 2-(2-piperidinoethyl)benzocycloalkanones as analogues of butyrophenone. |
AID750624 | Antipsychotic 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-dose | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics. |
AID588218 | FDA HLAED, lactate dehydrogenase (LDH) increase | 2004 | Current 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. |
AID129967 | Compound was evaluated for inhibition of apomorphine-induced climbing in mouse after intraperitoneal administration. | 1992 | Journal 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. |
AID1213066 | Intrinsic clearance in human liver microsomes measured per mg of protein at 10 to 400 uM by LC-MS/MS analysis | 2012 | Drug 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. |
AID1704747 | Antipsychotic 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 | |||
AID61495 | Binding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligand | 1994 | Journal 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. |
AID64645 | Binding affinity for dopamine receptor D2 long expressed in Sf9 cells using [125I]IABN radioligand | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11 | Synthesis and structure-activity relationships of naphthamides as dopamine D3 receptor ligands. |
AID5205 | In vitro binding affinity towards 5-hydroxytryptamine 2A receptor in human using [3H]ketanserin as radioligand | 2004 | Journal 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. |
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AID5490 | Inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor from rat brain | 1997 | Journal 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. |
AID36016 | Displacement of [3H]prazosin from rat brain Alpha-1 adrenergic receptor | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
AID1125903 | Displacement of [3H]methylspiperone from human D3 receptor expressed in HEK293 cell membrane after 90 mins by scintillation counting analysis | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8 | Discovery, optimization, and characterization of novel D2 dopamine receptor selective antagonists. |
AID1782424 | Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
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AID1853655 | Antibacterial 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 method | 2021 | RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11 | Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from |
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AID204771 | Binding affinity towards Sigma receptor type 2 in whole rat brain homogenates except cerebellum using radioligand ([3H]DTG) binding assay. | 1995 | Journal 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. |
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AID1063780 | Displacement of [3H]DTG from sigma 2 receptor (unknown origin) | 2014 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2 | The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds. |
AID176749 | Dose required to induce 50% maximum catalepsy in rat | 1996 | Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. |
AID8002 | Observed volume of distribution | 2004 | Journal 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. |
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AID1318842 | Antagonist 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-100 | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Computer-assisted design, synthesis, binding and cytotoxicity assessments of new 1-(4-(aryl(methyl)amino)butyl)-heterocyclic sigma 1 ligands. |
AID5326 | Half-maximal inhibition of [3H]- Ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate | 2002 | Journal 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. |
AID1601980 | Displacement of [3H]-ketanserin from recombinant human 5HT2A receptor expressed in HEK293 cells measured after 1.5 hrs by microbeta scintillation counting analysis | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
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AID6563 | Binding affinity towards human 5-hydroxytryptamine 6 receptor | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). |
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AID1616723 | Displacement of PPHT-red from SNAP-tagged human D2LR expressed in CHOK1 cell membranes by TR-FRET assay | |||
AID131248 | Neuroleptic activity determined by its inhibitory effect on apomorphine-induced climbing behavior in mice by intraperitoneal administration in experiment 2 Range is 0.05-0.17 | 1987 | Journal 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. |
AID1865086 | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane measured after 120 mins by scintillation counting method | |||
AID1724117 | Antipsychotic activity in po dosed mouse assessed as reduction in MK-801-induced hyperlocomotor activity | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics. |
AID229188 | Inhibition of specific binding of [3H]3-PPP to sigma binding site in Guinea pig brain membranes | 1992 | Journal 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. |
AID457704 | Toxicity 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) | 2010 | Bioorganic & 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. |
AID239150 | Inhibition of [125I]iodosulpiride binding to human Dopamine receptor D3 | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
AID160777 | Binding affinity to HIV-1 protease | 1994 | Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12 | Three-dimensional pharmacophores from binding data. |
AID170115 | Compound was evaluated for its ability to block conditioned avoidance response (CAR) in rats; Dose administered perorally is 1.25 mg/kg; 51-75% block | 1980 | Journal 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. |
AID61547 | Compound was evaluated In vitro for its activity by binding to Dopamine receptor D2 in the rat brain using [3H]NPA as radioligand. | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | 1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents. |
AID1853651 | Antibacterial activity against Mycobacterium intracellulare ATCC 13950 assessed as inhibition of bacterial growth incubated upto 3 weeks hrs by resazurin dye based double-dilution method | 2021 | RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11 | Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from |
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AID5560 | Half-maximal inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate | 2002 | Journal 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. |
AID277987 | Activity at human D2 receptor expressed in Xenopus oocytes | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities. |
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AID1378105 | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes after 120 mins by microbeta scintillation counting method | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Deconstruction - reconstruction approach to analyze the essential structural elements of tetrahydro-3-benzazepine-based antagonists of GluN2B subunit containing NMDA receptors. |
AID5042 | Binding affinity against serotonin 5-hydroxytryptamine 2 receptor | 1994 | Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4 | Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study. |
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AID113716 | Inhibition of the GBL-induced increase in DOPA accumulation in mice(DA auto receptor agonist activity); IA = inactive | 1998 | Journal 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. |
AID65426 | Compound was tested for its binding affinity towards Dopamine receptor D2 using [3H]spiperone from rat striatum | 1998 | Journal 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. |
AID112713 | Tested for the apomorphine climbing behavior in mice after oral administration | 1993 | Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7 | Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system. |
AID65905 | Binding affinity towards dopamine D2 receptors in rat brain synaptosomal preparations | 1994 | Journal 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. |
AID176413 | Evaluated 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) | 1990 | Journal of medicinal chemistry, Apr, Volume: 33, Issue:4 | Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds. |
AID65622 | In vitro binding affinity towards Dopamine receptor D3 in Sf9 cell membranes using [3H]7-OH-DPAT as radioligand | 2004 | Journal 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. |
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AID221060 | Inhibition of apomorphine-induced climbing behavior in mice, after Intraperitoneal administration | 1996 | Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. |
AID1467943 | Selectivity ratio of Ki for sigma 1 receptor in guinea pig brain membranes to Ki for sigma 2 receptor (unknown origin) | 2017 | Journal of medicinal chemistry, 12-14, Volume: 60, Issue:23 | Novel Sigma Receptor Ligand-Nitric Oxide Photodonors: Molecular Hybrids for Double-Targeted Antiproliferative Effect. |
AID65100 | Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand | 1996 | Journal 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. |
AID1546909 | Displacement of [3H]spiperone from human D3 receptor expressed in CHO-K1 cells by radioligand competitive binding analysis | |||
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AID184626 | Compound was tested for its acute toxicity in rat after ip administration | 1986 | Journal 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. |
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AID233354 | The lipophilicity was measured in an octanol/water system at pH 7.4. | 2000 | Journal 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. |
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AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
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AID61618 | Inhibition of [35S]GTP-gamma-S, binding to cell membranes expressing dopamine D2A receptors at 10 uM | 1999 | Bioorganic & 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. |
AID711582 | Inhibition of human dopamine D1 receptor | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Synopsis of some recent tactical application of bioisosteres in drug design. |
AID1596350 | Selectivity ratio of Ki for sigma2 receptor (unknown origin) to Ki for sigma1 receptor in guinea pig brain cortex membranes | |||
AID176943 | Dose which blocks the hypothermic effect of apomorphine by 50% against Sprague-Dawley rats when administered intraperitoneally | 1990 | Journal of medicinal chemistry, Apr, Volume: 33, Issue:4 | Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds. |
AID51566 | Minimal effective dose required for signs of EPS in cebus monkeys | 1985 | Journal 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. |
AID298479 | Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells | 2007 | Journal 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. |
AID88009 | Displacement of [3H](-)-trans-H2-PAT from histamine H2 PAT binding site by competition binding assay. | 1999 | Journal 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. |
AID1185965 | Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17 | Further evaluation of the tropane analogs of haloperidol. |
AID665422 | Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver after 180 mins by solid scintillation counting in the presence of (+)-pentazocine | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Microwave assisted synthesis of spirocyclic pyrrolidines -σ1 receptor ligands with modified benzene-N-distance. |
AID204762 | Compound was evaluated for the binding affinity towards Sigma receptor type 1 using radioligand ([3H]-(+)- Pentazocine) binding assay. | 1995 | Journal 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. |
AID1288458 | Displacement of [3H]DTG from human sigma2 receptor by PDSP assay | 2016 | Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9 | Tetrahydroprotoberberine alkaloids with dopamine and σ receptor affinity. |
AID311524 | Oral bioavailability in human | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Hologram QSAR model for the prediction of human oral bioavailability. |
AID1174259 | Displacement of [3H]-DTG from human sigma 2 receptor in human Jurkat cell membranes incubated for 1 hr by liquid scintillation counting | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Carboline- and phenothiazine-derivated heterocycles as potent SIGMA-1 protein ligands. |
AID1861726 | Binding affinity to MOR (unknown origin) assessed as inhibition constant by radioligand binding assay | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
AID175170 | Compound 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 administration | 1986 | Journal 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. |
AID1552400 | Displacement of [3H]-Di-o-tolylguanidine from sigma-2 receptor in rat liver membranes after 120 mins by scintillation counting method | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16 | Modification of the 4-phenylbutyl side chain of potent 3-benzazepine-based GluN2B receptor antagonists. |
AID444050 | Fraction unbound in human plasma | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID711572 | Inhibition of CYP3A4 | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Synopsis of some recent tactical application of bioisosteres in drug design. |
AID1221960 | Apparent 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 LY335979 | 2011 | Drug 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. |
AID176087 | Effect on the synthesis rates of serotonin in the rat ventral limbic brain region 2.7 micro mol/kg. | 1993 | Journal 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. |
AID5328 | Displacement of [3H]-ketanserin from rat brain 5-hydroxytryptamine 2A receptor | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
AID112526 | In vivo analgesic activity in mice after subcutaneous administration by hot plate assay method. | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | Combined analgesic/neuroleptic activity in N-butyrophenone prodine-like compounds. |
AID181661 | Binding affinity against rat striatal membranes using [3H]spiroperidol as the radioligand after 2 hours of conditioned feeding | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
AID62771 | In vitro binding affinity at human cloned Dopamine receptor D2 by [3H]spiroperidol displacement. | 1998 | Journal 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. |
AID625292 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID173704 | Percent decrease on dopamine agonist-induced rotation in unilaterally 6-OH-DA-lesioned rat at 0.1 mg/kg | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Troponoids. 6. Troponylpiperazines: a new class of dopamine agonists. |
AID1686282 | Cytotoxicity in HREC assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells. |
AID1393468 | Antipsychotic 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 | |||
AID1297659 | Displacement of [3H]-(+)-Pentazocine from sigma1 receptor in guinea pig brain homogenate incubated for 120 mins by solid scintillation counting analysis | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Benzimidazolone bioisosteres of potent GluN2B selective NMDA receptor antagonists. |
AID63795 | Binding affinity towards Dopamine receptor D2 in rat frontal striatum using [3H]spiperone | 2003 | Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2 | New arylpiperazine derivatives with high affinity for alpha1A, D2 and 5-HT2A receptors. |
AID1449628 | Inhibition 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 method | 2012 | Drug 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. |
AID61326 | Compound was tested in vitro for its affinity towards rat striatal Dopamine receptor D2 labeled with [3H]- spiperone | 1986 | Journal 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. |
AID35436 | The compound was tested for its binding affinity towards alpha-1 adrenergic receptor by displacing [3H]WB-4101 radioligand in rat cerebral cortexc | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | Pyrrole mannich bases as potential antipsychotic agents. |
AID171952 | compound was evaluated for its ability to produce catalepsy activity in rats | 1980 | Journal 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. |
AID629463 | Displacement of [3H]spiperone from human dopamine D3 receptor expressed in chinese hamster CHO cells by radioligand binding assay | 2011 | Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22 | Development of a bivalent dopamine D₂ receptor agonist. |
AID61562 | Compound was measured for affinity at dopamine receptor D2 labeled with [3H]spiroperidol radioligand in striatum tissue | 1991 | Journal 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. |
AID1365723 | Solubility of compound in Middlebrook 7H9 broth media at pH 6.4 at 200 uM after 90 mins by UV-VIS spectrophotometric method | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | The antitubercular activity of various nitro(triazole/imidazole)-based compounds. |
AID175174 | Compound was tested for serum prolactin assay method in rats at 1 mg/kg dose after peroral administration | 1986 | Journal 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. |
AID141155 | Binding 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' | 1998 | Journal 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). |
AID681619 | TP_TRANSPORTER: ATP hydrolysis in membranes from MDR1-expressing insect cells | 2002 | Life sciences, May-31, Volume: 71, Issue:2 | In vitro P-glycoprotein affinity for atypical and conventional antipsychotics. |
AID591692 | Induction 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%) | 2011 | Journal 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. |
AID1054122 | Inhibition of human ERG | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Polypharmacology - foe or friend? |
AID110213 | Ability to inhibit apomorphine-induced climbing behavior in mice. | 1995 | Journal 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). |
AID492645 | Antipsychotic 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 mins | 2010 | Journal 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. |
AID1213056 | Drug metabolism assessed as recombinant human UGT2B17 assessed as N-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis | 2012 | Drug 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. |
AID131046 | Inhibition of spontaneous motor activity, after 5 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
AID176802 | In vivo activity administered intraperitoneally was determined by induction of catalepsy in rat | 1991 | Journal 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. |
AID184656 | Compound was evaluated for the inhibition of apomorphine induced stereotypy behavior in rats after sc administration. | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | 1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents. |
AID1409607 | IC50 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). | 2020 | Nature, 07, Volume: 583, Issue:7816 | A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
AID675977 | Selectivity index, ratio of Ki for guinea pig brain sigma1 receptor to Ki for rat liver sigma2 receptor | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Thiophene bioisosteres of spirocyclic σ receptor ligands: relationships between substitution pattern and σ receptor affinity. |
AID65425 | Inhibition of [3H]spiroperidol binding to Dopamine receptor D2 of rat striatal membranes | 1998 | Journal of medicinal chemistry, May-07, Volume: 41, Issue:10 | (+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties. |
AID753963 | Displacement of [3H](+)pentazocine from sigma1 receptor in Dunkin Hartley guinea pig brain membrane after 120 mins by liquid scintillation counting analysis | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Synthesis and receptor binding studies of novel 4,4-disubstituted arylalkyl/arylalkylsulfonyl piperazine and piperidine-based derivatives as a new class of σ1 ligands. |
AID63412 | Effective dose through peroral route for in vivo inhibition against dopamine receptor D2 in male CF-1 mice by using radioligand [3H]raclopride | 1993 | Journal 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. |
AID37361 | Compound was tested for the binding affinity against rat cortical Alpha-2 adrenergic receptor by Radio ligand ([3H]Rx-821002) binding assay | 1996 | Journal 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. |
AID467613 | Volume of distribution at steady state in human | 2009 | European 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. |
AID114076 | post-synaptic dopamine autoreceptor antagonist activity evaluated by inhibition of the apomorphine-induced stereotyped behavior in mice. | 1998 | Journal 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. |
AID1393365 | Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method | |||
AID444053 | Renal clearance in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID141838 | In vitro binding affinity towards M1 receptor of rat frontal cortex homogenate by using radioligand [3H]QNB | 2004 | Journal 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. |
AID1210069 | Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method | 2013 | Drug 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. |
AID1213024 | Intrinsic clearance in recombinant human UGT2B7 measured per mg of protein at 10 to 400 uM by LC-MS/MS analysis | 2012 | Drug 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. |
AID1655192 | Displacement of [3H]-Di-o-tolylguanidine from sigma-2 receptor in rat liver membranes after 120 mins by scintillation counting method | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Synthesis, Cytotoxicity Evaluation, and Computational Insights of Novel 1,4-Diazepane-Based Sigma Ligands. |
AID62168 | Affinity towards Dopamine receptor D2 in membranes from bovine striatum using [3H]raclopride | 1998 | Journal 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. |
AID204764 | Ratio of the binding affinities against Sigma receptor type 1 and Sigma receptor type 2 | 1995 | Journal 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. |
AID1420180 | Cytotoxicity against human SH-SY5Y cells at 50 uM after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19 | New piperidine-based derivatives as sigma receptor ligands. Synthesis and pharmacological evaluation. |
AID242944 | Ratio of dopamine receptor D2 long and D3 ki values | 2005 | Journal 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. |
AID321564 | Displacement of [3H](+)-pentazocine from opioid sigma1 receptor in rat brain homogenate | 2008 | Journal 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. |
AID35428 | Binding affinity towards alpha-1 adrenergic receptors in rat brain synaptosomal preparations | 1994 | Journal 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. |
AID1461561 | Displacement of [3H]spiperone from human D2long receptor expressed in CHO cell membranes by radioligand binding assay | 2017 | Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19 | Potent haloperidol derivatives covalently binding to the dopamine D2 receptor. |
AID1546911 | Displacement of [3H]spiperone from human D4.2 receptor expressed in CHO-K1 cells by radioligand competitive binding analysis | |||
AID203830 | Inhibition of [3H]DTG binding to sigma-2 sites of guinea pig brain membranes | 1998 | Journal of medicinal chemistry, May-07, Volume: 41, Issue:10 | (+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties. |
AID625283 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1532590 | Inhibition 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 control | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Novel multitarget-directed ligands targeting acetylcholinesterase and σ |
AID392048 | Cardiotoxicity 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 ECG | 2008 | European journal of medicinal chemistry, Nov, Volume: 43, Issue:11 | Identification of "toxicophoric" features for predicting drug-induced QT interval prolongation. |
AID592114 | Induction 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%) | 2011 | Journal 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. |
AID1215939 | Unbound intrinsic clearance in human intestinal S9 fraction at 50 to 1000 nM after 30 to 60 mins by HPLC-MS/MS analysis | 2013 | Drug 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. |
AID64612 | Displacement of [3H]spiroperidol from D2 dopamine receptor | 1994 | Journal 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. |
AID646280 | Antipsychotic activity in CD1 mouse assessed as inhibition of MK-801-induced hyperactivity measuring number of crossings measured every 5 mins for 1 hr | 2012 | Bioorganic & 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. |
AID763632 | Antipsychotic 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 challenge | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
AID1136368 | Non-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 mins | 1978 | Journal 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. |
AID640304 | Displacement of [3H]N-methylspiperone from human dopamine D3 receptor by liquid scintillation counting | 2012 | Bioorganic & 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. |
AID1393469 | Toxicity 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 | |||
AID204290 | Ratio of binding affinity towards Sigma opioid receptor type 1 versus Sigma opioid receptor type 2 | 2002 | Journal 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. |
AID410339 | Sedative activity in NMRI mouse assessed as reduction in spontaneous locomotor activity administered 30 mins prior to testing | 2009 | Journal 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. |
AID705398 | Antipsychotic activity in sc dosed rat assessed as decrease in phencyclidine-induced locomotor activity | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Current landscape of phosphodiesterase 10A (PDE10A) inhibition. |
AID112953 | Compound was tested for inhibition of physostigmine lethality in mouse when administered perorally | 1986 | Journal 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. |
AID387867 | Displacement of [3H]YM-09151-2 from human dopamine D4.2 receptor in membrane suspensions by liquid scintillation counter | 2008 | Bioorganic & 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. |
AID492186 | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain homogenates after 1 hr by liquid scintillation counting | 2010 | Bioorganic & 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. |
AID1123512 | Neuroleptic 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 hrs | 1979 | Journal 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. |
AID717103 | Selectivity ratio of Ki for sigma 2 receptor in rat PC12 cell membrane to Ki for sigma 1 receptor in rat brain membrane | 2012 | Bioorganic & 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. |
AID425652 | Total body clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Physicochemical determinants of human renal clearance. |
AID182041 | In vivo inhibition of apomorphine-mediated stereotypy in rats administered subcutaneously at 0.6 mg/kg expressed as percent inhibition | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
AID675971 | Displacement of [3H]-di-o-tolyguanidine from rat liver sigma 2 receptor after 180 mins by scintillation counting analysis | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Thiophene bioisosteres of spirocyclic σ receptor ligands: relationships between substitution pattern and σ receptor affinity. |
AID1686278 | Displacement of [3H]-spiperone from DRD2 in rat striatum by scintillation counting | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells. |
AID1185974 | Displacement of [3H]Nisoxetine from human Norepinephrine transporter by liquid scintillation counting | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17 | Further evaluation of the tropane analogs of haloperidol. |
AID239151 | Inhibition of [3H]7-OH-DPAT binding to Dopamine D3 receptor expressed in Sf9 cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies. |
AID65402 | Compound was evaluated for its binding affinity with Dopamine receptor D2 using membranes prepared from rat striatum | 1998 | Journal 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. |
AID1578090 | Unbound brain-to-plasma concentration ratio in rat | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Practical approaches to evaluating and optimizing brain exposure in early drug discovery. |
AID705725 | Displacement of [3H]di-o-tolylguanidine from Sigma2 receptor in rat brain homogenate | 2012 | Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19 | New positron emission tomography (PET) radioligand for imaging σ-1 receptors in living subjects. |
AID194375 | Effect of compound (0.2 mg/kg ip) on the concentration of DOPAC in rat mesolimbic region | 1993 | Journal 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. |
AID176251 | Intracranial self stimulation in rat was determined after 1 hr of intraperitoneal administration of the compound | 1995 | Journal 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). |
AID1718132 | Binding affinity to sigma-1 receptor (unknown origin) | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases. |
AID41473 | Binding affinity against beta-2 adrenergic receptor in rat brain using [3H]DHA | 1986 | Journal 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. |
AID490176 | Anticonvulsant activity in rat assessed as protection against maximal electric shock-induced seizures at 0.5 mL, ip | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Synthesis and antipsychotic and anticonvulsant activity of some new substituted oxa/thiadiazolylazetidinonyl/thiazolidinonylcarbazoles. |
AID1330104 | Selectivity ratio of Ki for sigma2 receptor in rat PC12 cells to Ki for guinea pig sigma1 receptor | 2016 | Bioorganic & 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. |
AID61499 | Affinity for Dopamine receptor D1 | 1998 | Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8 | Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors. |
AID65713 | Displacement of [3H]NPA from rat brain Dopamine receptor D2 | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
AID231654 | Binding ratio of -log Ki between D2 and D1 receptors | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
AID1655661 | Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor (unknown origin) incubated for 1 hr in presence of (+)SKF10047 by liquid scintillation counting method | |||
AID203829 | Binding affinity towards sigma 2 receptor using [3H]DTG in the presence of 200 nM (+)-NANM from guinea pig brain | 1998 | Journal 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. |
AID1712205 | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane incubated for 150 mins by liquid scintillation counting method | 2016 | Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14 | New bifunctional antioxidant/σ1 agonist ligands: Preliminary chemico-physical and biological evaluation. |
AID1532591 | Inhibition 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 method | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Novel multitarget-directed ligands targeting acetylcholinesterase and σ |
AID665421 | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane after 180 mins by solid scintillation counting | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Microwave assisted synthesis of spirocyclic pyrrolidines -σ1 receptor ligands with modified benzene-N-distance. |
AID203852 | The compound was tested for affinity towards sigma-3 receptor | 1994 | Journal 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. |
AID1478367 | Displacement of [3H]-spiperone from dopamine D2 receptor in rat strriatum after 15 mins by liquid scintillation counting method | 2018 | Journal 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. |
AID1768729 | Lipophilicity, logP of compound by shake flask method | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Estimation of the lipophilicity of purine-2,6-dione-based TRPA1 antagonists and PDE4/7 inhibitors with analgesic activity. |
AID517707 | Displacement of [3H]Spiperone from human dopamine D2 long receptor expressed in CHO cells | 2010 | Journal 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. |
AID87530 | Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate | 2002 | Journal 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. |
AID194381 | Effect of compound (0.2 mg/kg ip) on the concentration of HVA in rat striatum | 1993 | Journal 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. |
AID1546910 | Displacement of [3H]spiperone from human D3 receptor expressed in CHO-K1 cells at 10 uM by radioligand competitive binding analysis relative to control | |||
AID5012 | Inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2 receptor of guinea pig frontal cortex membranes | 1998 | Journal of medicinal chemistry, May-07, Volume: 41, Issue:10 | (+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties. |
AID49739 | Compound 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 inhibition | 1986 | Journal of medicinal chemistry, Dec, Volume: 29, Issue:12 | p-Dimethoxy-substituted trans-octahydrobenzo[f]- and -[g]quinolines: synthesis and assessment of dopaminergic agonist effects. |
AID1616720 | Displacement of PPHT-red from SNAP-tagged human D2LR expressed in CHOK1 cell membranes assessed as association rate constant by TR-FRET assay | |||
AID1153310 | Antagonist 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 qunipirole | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
AID63804 | Affinity against Dopamine receptor D2 | 2000 | Journal 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. |
AID1136084 | Ratio 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 membranes | 1978 | Journal of medicinal chemistry, Apr, Volume: 21, Issue:4 | 5-Chloro-2-phenyl-1-benzo[b]thiophene-3-alkanimines, potential antipsychotic agents. |
AID238855 | Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1 | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
AID255071 | Inhibitory 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 C | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective sigma1 ligands. Part 2. |
AID61788 | In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement. | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7 | Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist. |
AID1136359 | Neuroleptic activity in squirrel monkey assessed as inhibition of Sidman avoidance at 1 mg/kg, po measured for 4 hrs | 1978 | Journal 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. |
AID177555 | Ability to block apomorphine-induced stereotypy in rats. | 1995 | Journal 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). |
AID1221982 | Fraction absorbed in human | 2011 | Drug 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. |
AID109889 | Tail suspension test in mice, dose(mg/Kg ip) = 4;duration of immobility(% vs controls) | 1998 | Journal 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. |
AID204461 | Binding 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. | 1998 | Journal 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). |
AID367546 | Displacement of [3H]RHM-1 from sigma 2-type opioid receptor in rat liver homogenates | 2009 | Bioorganic & 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. |
AID196012 | Compound was evaluated in paw test for the forelimb retraction at effective dose of 20 (mg/kg) | 2002 | Journal 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. |
AID1146534 | Neuroleptic activity in po dosed STD-ddY mouse assessed as protection against methamphetamine-induced toxicity administered 1 hr before methamphetamine challenge measured after 24 hrs | 1978 | Journal of medicinal chemistry, Nov, Volume: 21, Issue:11 | Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity. |
AID280701 | Increase in TG-2 expression in albino Wistar rat primary 14 DIV astroglial cell at 25 uM after 24 hrs by CLSM analysis | 2007 | Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5 | Novel sigma receptor ligands: synthesis and biological profile. |
AID367548 | Partition coefficient, log P of the compound | 2009 | Bioorganic & 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. |
AID62746 | Intrinsic activity relative to quinpirole in the reversal of forskolin-stimulated cAMP accumulation in cells transfected with the human DA D2 receptor | 1994 | Journal 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. |
AID62465 | Ratio of IC50 evaluated by using [3H]DA to [3H]-HP | 1981 | Journal 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. |
AID1129361 | Unbound fraction in HEK293 cell homogenate at 0.1 uM by equilibrium dialysis based UPLC-MS/MS analysis | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | A high-throughput cell-based method to predict the unbound drug fraction in the brain. |
AID176254 | Intraperitoneal effective dose required for inhibition of apomorphine-induced stereotypy in rat | 1996 | Journal 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. |
AID1403515 | Displacement 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 | |||
AID178541 | Compound was tested for its ability to induce catalepsy in rats. | 1986 | Journal 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. |
AID1129878 | Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain cortex membranes after 120 mins by scintillation counting analysis | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | Synthesis, pharmacological evaluation, and σ1 receptor interaction analysis of hydroxyethyl substituted piperazines. |
AID5331 | Inhibitory constant on 5-hydroxytryptamine 2A receptor of Rat frontal cortex | 2002 | Journal 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. |
AID178179 | Inhibition of conditioned avoidance response in rat following s.c. administration. | 1998 | Journal 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. |
AID148465 | Ability to inhibit the specific binding of [3H]- dihydromorphine to opiate receptors in rat brain membrane preparation by 50% | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | Combined analgesic/neuroleptic activity in N-butyrophenone prodine-like compounds. |
AID61046 | Compound was tested in vivo for methyl phenidate-induced gnawing behavior antagonistic activity against dopamine receptor D2 in mice | 1992 | Journal 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. |
AID131589 | Suppression of aggressive behavior, after 5 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
AID4786 | Binding affinity towards 5-hydroxytryptamine 2 receptor measured using radioligand ([3H]spiperone) binding assay | 1986 | Journal 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. |
AID194379 | Effect of compound (0.2 mg/kg ip) on the concentration of HVA in rat frontal cortex | 1993 | Journal 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. |
AID540222 | Clearance in rat after iv administration | 2006 | Drug 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. |
AID1184609 | Displacement of [3H]spiperone from human D3 receptor stably expressed in CHO cell membranes by competitive binding assay | 2014 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16 | Synthesis and binding profile of haloperidol-based bivalent ligands targeting dopamine D(2)-like receptors. |
AID226334 | The Binding affinity was evaluated using [3H]DTG -(+)-Dextrallorphan] in rat liver | 1993 | Journal 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. |
AID1256684 | Neurotoxicity 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) | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics. |
AID1136369 | Non-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 mins | 1978 | Journal 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. |
AID717217 | Displacement of [3H](+)-pentazocine from sigma 1 receptor in rat brain membrane after 2.5 hrs by scintillation counting | 2012 | Bioorganic & 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. |
AID1411898 | Half life in im dosed human plasma | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Schizophrenia: synthetic strategies and recent advances in drug design. |
AID298493 | Displacement of [3H]RX 821002 from adrenergic alpha-2 receptor in rat cerebral cortex | 2007 | Journal 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. |
AID308686 | Displacement of [3H]mesulergine human cloned serotonin 5HT2C receptor | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics. |
AID135365 | Inhibitory activity against tremorine-induced tremors, after 1 hour of peroral administration in mouse at dose 20 mg/kg | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
AID1853650 | Antibacterial activity against Mycobacterium abscessus ATCC 19977 assessed as inhibition of bacterial growth incubated upto 3 weeks hrs by resazurin dye based double-dilution method | 2021 | RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11 | Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from |
AID224648 | Area under curve(AUC) value of HVA level after second treatment(7.4 umol/kg) in dialysates collected from rat striatum. | 2002 | Journal 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. |
AID1213038 | Drug metabolism assessed as recombinant human UGT1A6 assessed as O-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis | 2012 | Drug 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. |
AID640547 | Displacement of [3H]QNB from human M1 receptor by liquid scintillation counting | 2012 | Bioorganic & 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. |
AID180891 | The dosage at which 50% of the animals were cataleptic was measured after (ip) administration in male Sprague-Dawley rats | 1982 | Journal of medicinal chemistry, Nov, Volume: 25, Issue:11 | Potential neuroleptic agents. 2,6-Dialkoxybenzamide derivatives with potent dopamine receptor blocking activities. |
AID458632 | Displacement of [3H]spiperone from human dopamine D2 receptor at low affinity state expressed in HEK293 cells | 2010 | Journal 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). |
AID1877931 | Displacement of [3H]-DTG from Sprague-Dawley rat liver Sigma 2 receptor incubated for 120 mins in presence of [3H]-(+)-pentazocine by liquid scintillation counting analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation. |
AID205174 | The compound was tested for inhibition of sidman avoidance in squirrel monkeys | 1985 | Journal 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. |
AID298488 | Displacement of [3H]BLR-43694 from human 5HT3 receptor expressed in HEK293 cells | 2007 | Journal 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. |
AID408340 | Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique | 2008 | Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11 | Support vector machines classification of hERG liabilities based on atom types. |
AID1213064 | Drug metabolism assessed as human liver microsomes assessed as O-glucuronidation at 10 to 400 uM by LC-MS/MS analysis | 2012 | Drug 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. |
AID274128 | Displacement of [3H]Astemizole from hERG expressed in HEK293 cells at 10 uM | 2006 | Bioorganic & 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. |
AID1853667 | Synergistic antibacterial activity against Mycobacterium smegmatis mc2 155 assessed as fold reduction in MIC value at 8 ug/ml in presence of spectinomycin by checkerboard assay | 2021 | RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11 | Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from |
AID1127647 | Displacement of [3H]progesterone from sigma-1 opioid receptor in porcine liver microsome membranes | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18 | The σ2 receptor: a novel protein for the imaging and treatment of cancer. |
AID1179611 | Selectivity ratio of Ki for sigma 2 receptor in rat liver membranes to Ki for sigma 1 receptor in guinea pig brain cortex membranes | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Pyridine analogues of spirocyclic σ₁ receptor ligands. |
AID415887 | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane by liquid scintillation analyzer | 2009 | European 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. |
AID1597397 | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes incubated for 120 mins by scintillation counting method | |||
AID34586 | Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | Combined analgesic/neuroleptic activity in N-butyrophenone prodine-like compounds. |
AID1136083 | Displacement of [3H]-HALO from dopamine receptor in calf caudate membranes after 10 mins by liquid scintillation counting analysis | 1978 | Journal of medicinal chemistry, Apr, Volume: 21, Issue:4 | 5-Chloro-2-phenyl-1-benzo[b]thiophene-3-alkanimines, potential antipsychotic agents. |
AID427338 | Displacement of [3H]DTG from sigma2 receptor in rat liver membrane by liquid scintillation counting | 2009 | Journal 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. |
AID184872 | Minimum effective dose observed in rat catalepsy experiments | 2000 | Journal 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. |
AID65609 | Binding affinity to rat Dopamine receptor D3 expressed in CHO cells was determined using [125 I] iodosulpride as radioligand | 1996 | Journal 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. |
AID113872 | Intraperitoneal effective dose required for inhibition of apomorphine-induced climbing in mice | 1996 | Journal 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. |
AID1330103 | Displacement of [3H]DTG from sigma2 receptor in rat PC12 cells measured after 90 mins by microbeta scintillation counting method | 2016 | Bioorganic & 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. |
AID204152 | Inhibition of [3H]- pentazocine binding against alpha-1 from guinea pig brain | 1999 | Journal 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. |
AID62768 | Binding affinity to dopamine receptor D2 cloned from human, using [3H]- YM09151 as competitive ligand | 2000 | Journal 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. |
AID203688 | Compound was evaluated for its in vitro competition binding studies using sigma-ligand (0.05-10000 nM) - [3H](+)-pentazocine (sigma1 receptor) in guinea pig brain membranes | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14 | Substituted halogenated arylsulfonamides: a new class of sigma receptor binding tumor imaging agents. |
AID65767 | Half-maximal inhibition of [3H]7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate | 2002 | Journal 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. |
AID1596348 | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membranes incubated for 150 mins by scintillation counting method | |||
AID1378106 | Displacement of [3H]DTG from sigma2 receptor in rat liver membranes after 120 mins by microbeta scintillation counting method | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Deconstruction - reconstruction approach to analyze the essential structural elements of tetrahydro-3-benzazepine-based antagonists of GluN2B subunit containing NMDA receptors. |
AID142504 | The ability to displace [3H]QNB from Muscarinic acetylcholine receptor in rat brain membrane was determined | 1982 | Journal of medicinal chemistry, Oct, Volume: 25, Issue:10 | Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems. |
AID194369 | Effect of compound (0.2 mg/kg ip) on the concentration of 5-HIAA in rat striatum | 1993 | Journal 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. |
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AID1411897 | Half life in iv dosed human plasma | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Schizophrenia: synthetic strategies and recent advances in drug design. |
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AID1330101 | Displacement of [3H]U69593 from KOR (unknown origin) expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method | 2016 | Bioorganic & 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. |
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AID1292384 | Blood clearance in psychotic patient (9 patients) at 3.5 +/- 1.2 mg, iv by reversed phase HPLC method | 1987 | Psychopharmacology, , Volume: 91, Issue:4 | Pharmacokinetics of haloperidol in psychotic patients. |
AID168344 | Social interaction of rats was determined after 1 hr of intraperitoneal administration at 0.25 mg/kg | 1995 | Journal 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). |
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AID62723 | Ability to inhibit the binding of [3H]spiroperidol in rat striatal tissue | 1985 | Journal of medicinal chemistry, Jun, Volume: 28, Issue:6 | Synthesis and neuroleptic activity of 3-(1-substituted-4-piperidinyl)-1,2-benzisoxazoles. |
AID65245 | Binding affinity towards dopamine receptor D2 in rat striatal membranes | 2001 | Journal 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. |
AID448641 | Selectivity ratio of Ki for guinea pig brain sigma 1 receptor to Ki for rat liver sigma 2 receptor | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis of sigma receptor ligands with unsymmetrical spiro connection of the piperidine moiety. |
AID1686304 | Suppression 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 assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells. |
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AID1878191 | Binding affinity to dopamine D3 receptor (unknown origin) by radioligand displacement assay | |||
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AID1593895 | Selectivity 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 membranes | 2019 | Bioorganic & medicinal chemistry, 06-15, Volume: 27, Issue:12 | New analogs of SYA013 as sigma-2 ligands with anticancer activity. |
AID437146 | Inhibition 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 test | 2009 | European 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. |
AID395324 | Lipophilicity, log D at pH 7.4 by liquid chromatography | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
AID1655193 | Displacement of [3H]ifenprodil from GluN2B (unknown origin) expressed in mouse L(tk-) cell membranes co-expressing GluN1a incubated for 120 mins by scintillation counting method | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Synthesis, Cytotoxicity Evaluation, and Computational Insights of Novel 1,4-Diazepane-Based Sigma Ligands. |
AID112508 | In vivo Antipsychotic activity was quantified by induction of catalepsy in mice | 1999 | Journal 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 |
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AID591694 | Induction 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%) | 2011 | Journal 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. |
AID171689 | Catalytic action on male Wistar rats after subcutaneous administration of 0.003 mg/kg dose of compound | 1997 | Journal 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. |
AID173680 | Locomotor activity after no pretreatment in rat at high-dose region expressed as percent of saline control | 1985 | Journal of medicinal chemistry, Aug, Volume: 28, Issue:8 | Novel dopamine receptor agonists and antagonists with preferential action on autoreceptors. |
AID131214 | Lethal dose in mice by administered the compound intraperitoneally | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
AID1461568 | Selectivity 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 membranes | 2017 | Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19 | Potent haloperidol derivatives covalently binding to the dopamine D2 receptor. |
AID204448 | Inhibitory activity against sigma receptor isolated from guinea pig brain cortex membrane using [3H]DTG as radioligand | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives. |
AID605696 | Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Bivalent dopamine D2 receptor ligands: synthesis and binding properties. |
AID1462756 | Displacement of [3H]-di-o-tolylguanidine from sigma 2 receptor in rat liver membranes after 120 mins by scintillation counting analysis | 2017 | Bioorganic & 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. |
AID35270 | Compound was tested for the binding affinity against rat cortical Alpha-1 adrenergic receptor by radioligand [3H]prazosin binding assay. | 1996 | Journal 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. |
AID238941 | Inhibition of [3H]spiperone binding to rat dopamine D2 receptor | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies. |
AID1215946 | Intrinsic clearance in human intestinal S9 fraction at 50 to 1000 nM after 60 mins by HPLC-MS/MS analysis in presence of NADH | 2013 | Drug 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. |
AID62337 | Binding towards Dopamine receptor D2 expressed in CHO-K1 cells using [3H]U-86170 | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
AID227559 | Relative binding affinity for dopamine D2 and alpha receptors | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
AID1853652 | Antibacterial activity against Mycobacterium avium ATCC 25921 assessed as inhibition of bacterial growth incubated upto 3 weeks hrs by resazurin dye based double-dilution method | 2021 | RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11 | Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from |
AID196117 | effects on Sidman Avoidance performance in rats, number of shocks (absolute change from control), p<0.001, dose(mg/Kg po) =1 | 1998 | Journal 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. |
AID476062 | Displacement of [3H](+)-pentazocine from sigma 1 opioid receptor in human Jurkat cells by scintillation counting | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1 | Sigma-1 ligands: Tic-hydantoin as a key pharmacophore. |
AID1211298 | Dissociation constant, pKa of the compound | 2011 | Drug 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. |
AID665423 | Selectivity ratio of Ki for rat sigma 2 receptor to Ki for guinea pig sigma1 receptor | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Microwave assisted synthesis of spirocyclic pyrrolidines -σ1 receptor ligands with modified benzene-N-distance. |
AID37306 | Binding affinity was tested on Alpha-1 adrenergic receptor using radioligand [3H](+)-pentazocine binding assay. | 1996 | Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21 | Novel potent sigma 1 ligands: N-[omega-(tetralin-1-yl)alkyl]piperidine derivatives. |
AID63549 | In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes | 2002 | Journal 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. |
AID1473739 | Inhibition 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 assay | 2013 | Toxicological 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. |
AID1638284 | Displacement of [3H](+)-pentazocine from sigma1 receptor in rat brain membranes after 120 mins by radioligand binding assay | |||
AID1369084 | Displacement of [3H]-DTG from sigma 2 receptor in rat liver membranes after 120 mins by scintillation counting analysis | 2018 | Bioorganic & 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. |
AID1867872 | Displacement of [3H]-DTG from sigma 2 receptor in rat liver membrane measured after 120 mins by microbeta counting analysis | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Synthesis and biological evaluation of conformationally restricted GluN2B ligands derived from eliprodil. |
AID476061 | Selectivity ratio of IC50 for sigma 2 opioid receptor in rat cerebral cortex membrane to IC50 for sigma 1 opioid receptor in human Jurkat cells | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1 | Sigma-1 ligands: Tic-hydantoin as a key pharmacophore. |
AID63499 | Antagonistic activity against apomorphine-induced emesis, after 5 hour of peroral administration in dogs | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
AID1292388 | Ratio of steady state drug level in blood to plasma in psychotic patient at 3.5 +/- 1.2 mg, iv by reversed phase HPLC method | 1987 | Psychopharmacology, , Volume: 91, Issue:4 | Pharmacokinetics of haloperidol in psychotic patients. |
AID29925 | Volume of distribution in man (IV dose) | 2002 | Journal 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. |
AID308685 | Displacement of [3H]ketanserin human cloned serotonin 5HT2A receptor | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics. |
AID1215128 | Ratio, 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 cocktai | 2011 | Drug 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. |
AID1865087 | Displacement of [3H]DTG from sigma 2 receptor in rat liver membranes measured after 120 mins by scintillation counting method | |||
AID176414 | Evaluated 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) | 1990 | Journal of medicinal chemistry, Apr, Volume: 33, Issue:4 | Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds. |
AID301872 | Blockade of conditioned avoidance response in ip dosed rat | 2007 | Bioorganic & 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. |
AID63533 | Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand | 2002 | Journal 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. |
AID131051 | Inhibitory activity against tremorine-induced salivation, after 1 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
AID549678 | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane by scintillation counting | 2011 | Bioorganic & 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. |
AID277984 | Ratio of ED50 for catalepsy induction to ED50 for normalization in ip dosed rat | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities. |
AID178395 | Effective dose for ethanol potentiation in rats | 1992 | Journal 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. |
AID448410 | Displacement of [3H]spiperone from D2 receptor | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19 | Tetrahydrocarbazole-based serotonin reuptake inhibitor/dopamine D2 partial agonists for the potential treatment of schizophrenia. |
AID1704750 | Toxicity in po dosed Kunming mouse assessed as catalepsy | |||
AID1185964 | Displacement of [3H]N-methylspiperone from human dopamine D3 receptor by liquid scintillation counting | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17 | Further evaluation of the tropane analogs of haloperidol. |
AID65786 | Binding towards Dopamine receptor D3 expressed in CHO-K1 cells using [3H]spiperone | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
AID1861728 | Binding affinity to KOR (unknown origin) assessed as inhibition constant by radioligand binding assay | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
AID1061889 | Displacement of [3H]BTX-B from neuronal voltage-gated sodium channel in rat cerebral cortex synaptoneurosomes after 60 mins by scintillation counting | 2014 | Bioorganic & 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. |
AID4782 | Binding affinity towards serotonin 5-HT2 receptor was determined in rat cortex using [3H]spiperone as ligand | 1996 | Journal 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. |
AID140974 | In vitro binding affinity against Muscarinic acetylcholine receptors in rat brain. | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
AID177809 | Compound was evaluated in vivo for its antipsychotic activity for inhibition of apomorphine-induced stereotypy in rat | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents. |
AID367545 | Displacement of [3H](+)-pentazocine from sigma 1-type opioid receptor in guinea pig brain homogenates | 2009 | Bioorganic & 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. |
AID237685 | Lipophilicity determined as logarithm of the partition coefficient in the alkane/water system | 2005 | Journal 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). |
AID229212 | Binding affinity was evaluated against sigma-1 binding site in guinea pig, using [3H]- -(+)- Pentazocine | 1993 | Journal 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. |
AID160632 | The irreversibility of the inactivation reaction of HIV-1 PR was assessed; NI =No detectable reversible reaction | 1994 | Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5 | Haloperidol-based irreversible inhibitors of the HIV-1 and HIV-2 proteases. |
AID392764 | Displacement of [3H]N-methylspiperone from human dopamine D3 receptor by liquid scintillation counting | 2009 | Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4 | Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups. |
AID196771 | In vivo accumulation of L-DOPA was measured in striatum of rats | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
AID180162 | Antipsychotic activity at a dose 10 times the ED50 value for CAR block for production of catalepsy in the rat (following i.p. dosing) | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | Pyrrole mannich bases as potential antipsychotic agents. |
AID737845 | Displacement of [3H](+)-Pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | Improvement of σ1 receptor affinity by late-stage C-H-bond arylation of spirocyclic lactones. |
AID5561 | In vitro ability to displace [3H]ketanserin from 5-hydroxytryptamine 2A receptor in rat brain. | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
AID4128 | Inhibitory concentration against binding of 5-hydroxytryptamine 1A receptor from striata of male Wistar rats by displacement of [3H]8-OH-DPAT | 2000 | Bioorganic & medicinal chemistry letters, Mar-06, Volume: 10, Issue:5 | N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]cyclohexanecarboxamides as selective 5-HT1A receptor agonists. |
AID41748 | Compound was tested for the binding affinity against rat cortical Beta adrenergic receptor by Radio ligand [3H]dihydroalprenolol binding assay. | 1996 | Journal 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. |
AID64963 | Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in CHO cells | 1996 | Journal 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. |
AID1292377 | Terminal 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 analysis | 1987 | Psychopharmacology, , Volume: 91, Issue:4 | Pharmacokinetics of haloperidol in psychotic patients. |
AID1146540 | Ratio 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 rat | 1978 | Journal of medicinal chemistry, Nov, Volume: 21, Issue:11 | Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity. |
AID295928 | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane | 2007 | European journal of medicinal chemistry, Oct, Volume: 42, Issue:10 | Synthesis of bridged piperazines with sigma receptor affinity. |
AID131872 | Effective dose required for inhibition of DOI-induced head-twitches in mice on ip administration | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
AID4814 | Inhibition of [3H]ketanserin binding at 5-hydroxytryptamine 2 receptor from rat frontal cortex. | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | Effect of linking bridge modifications on the antipsychotic profile of some phthalimide and isoindolinone derivatives. |
AID592125 | Induction 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%) | 2011 | Journal 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. |
AID190818 | Total activity (anti psychotic) when compound administered at a doe of 0.05 mg/kg ip in rats | 1996 | Journal 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. |
AID37001 | Inhibition of [3H]prazosin binding to Alpha-1 adrenergic receptor in rat brain membranes | 1997 | Journal 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. |
AID230953 | Ratio of binding to dopamine D2A low/D2A high receptors | 1999 | Bioorganic & 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. |
AID1210070 | Inhibition of CYP2D6 in human liver microsomes using bufuralol substrate by LC-MS/MS method | 2013 | Drug 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. |
AID701162 | Displacement of [3H](+)pentazocine from human sigma 1 receptor transfected in HEK293 cell membranes after 120 mins by scintillation counter | 2012 | Journal 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). |
AID160616 | Binding affinity for HIV-1 protease | 1991 | Journal of medicinal chemistry, Aug, Volume: 34, Issue:8 | HIV protease: a novel chemotherapeutic target for AIDS. |
AID342780 | Ratio of Ki for human cloned dopamine D2 receptor to Ki for human cloned dopamine D4 receptor | 2008 | Bioorganic & 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. |
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AID3744 | Inhibition of [3H]8-OH-DPAT binding at serotonin 5-hydroxytryptamine 1A receptor from rat hippocampus tissue. | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | Effect of linking bridge modifications on the antipsychotic profile of some phthalimide and isoindolinone derivatives. |
AID141832 | Compound was tested for the binding affinity against rat cortical Muscarinic acetylcholine receptor M1 by Radio ligand [3H]pirenzepine binding assay. | 1996 | Journal 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. |
AID232327 | Ratio of APO Sterotype ED50 vs catalepsy ED50 | 1986 | Journal 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. |
AID64802 | Displacement of [3H]-YM 09151 from african monkey Dopamine receptor D3 | 1995 | Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25 | 1-Phenyl-3-(aminomethyl)pyrroles as potential antipsychotic agents. Synthesis and dopamine receptor binding. |
AID65726 | In vitro binding affinity for dopamine receptor D2 of rat nucleus accumbens labeled with [3H]spiperone | 1987 | Journal of medicinal chemistry, Jun, Volume: 30, Issue:6 | Psychotropic agents: synthesis and antipsychotic activity of substituted beta-carbolines. |
AID1704751 | Therapeutic 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 | |||
AID1249735 | Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells | 2015 | ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8 | Multicomponent Synthesis and Biological Evaluation of a Piperazine-Based Dopamine Receptor Ligand Library. |
AID1136351 | Neuroleptic activity in ip dosed Long-Evans rat assessed as increase in escape failure | 1978 | Journal 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. |
AID170884 | Percentage change in Total activity (anti psychotic) when compound administered at a doe of 0.125 mg/kg ip in rats | 1996 | Journal 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. |
AID1283241 | Decrease in desmosterol levels in mouse Neuro2a cells by LC-MS analysis | 2016 | Journal 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. |
AID178868 | Compound was tested for the inhibition of apomorphine-induced stereotype | 1986 | Journal 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. |
AID277673 | Displacement of [3H]spiperone from human dopamine D3 expressed in CHO cell membrane | 2007 | Journal 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. |
AID1601983 | Displacement of [3H]-raclopride from recombinant human D2 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
AID1727501 | Displacement of [125I]-RHM-4 from sigma 2 receptor in rat liver membranes after 120 mins by microbeta scintillation counting method | |||
AID62917 | Binding affinity against cloned human dopamine receptor D2 expressed in Chinese hamster ovary (CHO) K-1 cells by displacement of [3H]spiperone. | 1997 | Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25 | (Aryloxy)alkylamines as selective human dopamine D4 receptor antagonists: potential antipsychotic agents. |
AID173705 | Percent decrease on dopamine agonist-induced rotation in unilaterally 6-OH-DA-lesioned rat at 0.25 mg/kg | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Troponoids. 6. Troponylpiperazines: a new class of dopamine agonists. |
AID231638 | Binding affinity against the D2 dopamine receptor and ratio of IC50(+Na+) / IC50(-Na(+)) [from 2-4 experiments] | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | 2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1. |
AID1215937 | Unbound intrinsic clearance in human intestinal cytosol at 50 to 1000 nM after 30 to 60 mins by HPLC-MS/MS analysis | 2013 | Drug 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. |
AID655663 | Displacement of [3H]-pentazocine from sigma 1 opioid receptor in rat liver homogenate by liquid scintillation counting | 2011 | ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11 | Homology Model and Docking-Based Virtual Screening for Ligands of the σ1 Receptor. |
AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
AID195978 | effects on Sidman Avoidance performance in rats, number of escape failure (absolute change from control), p<0.01, dose(mg/Kg po) =1 | 1998 | Journal 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. |
AID393002 | Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting | 2009 | Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4 | Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups. |
AID1403514 | Displacement 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 | |||
AID1823675 | Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis | |||
AID157456 | Binding affinity was measured against phencyclidine (PCP) receptor in rat using [3H]TCP as radioligand | 1994 | Journal 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. |
AID1135928 | Neuroleptic activity in ip dosed ICR-DUB mouse assessed as survival administered 1 hr prior to d-amphetamine challenge measured after 24 hrs | 1978 | Journal 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. |
AID1300808 | Displacement of [3H](+)-pentazocine from Sigma1 receptor in Dunkin Hartley guinea pig brain membrane after 120 mins by liquid scintillation counting analysis | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 | One-pot synthesis and sigma receptor binding studies of novel spirocyclic-2,6-diketopiperazine derivatives. |
AID1744234 | Displacement of [3H]-pentazocine from sigma-1 receptor in human Jurkat cell membrane incubated for 2 hr by liquid scintillation counting method | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1 | Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management. |
AID1213032 | Drug 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 control | 2012 | Drug 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. |
AID605697 | Displacement of [3H]SCH23390 from human D2long receptor expressed in CHO cells | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Bivalent dopamine D2 receptor ligands: synthesis and binding properties. |
AID156831 | Compound was tested for its binding affinity towards PCP receptor in rat membranes in the presence of [3H]-(+)-SKF- 10,047 | 1998 | Journal of medicinal chemistry, May-07, Volume: 41, Issue:10 | (+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties. |
AID169242 | Induced locomotor stimulation in non pre-treated rats by 13 umol/kg s.c. administration. | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists. |
AID65919 | In vitro affinity against Dopamine receptor D4 | 2000 | Journal 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. |
AID437148 | Inhibition 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 test | 2009 | European 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. |
AID110208 | Ability to inhibit apomorphine (APO) induced climbing behavior in mice by intraperitoneal administration of compound.; value may range from 0.17 to 0.15 | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | Antipsychotic activity of substituted gamma-carbolines. |
AID711585 | Solubility of the compound | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Synopsis of some recent tactical application of bioisosteres in drug design. |
AID735277 | Displacement of [3H]-Di-o-tolyguanidine from guinea pig sigma2 receptor after 120 mins by liquid scintillation counting analysis | 2013 | Journal 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. |
AID265753 | Inhibition of apomorphine-induced climbing in ip dosed Swiss Webster mouse | 2006 | Bioorganic & 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. |
AID737906 | Displacement of (+)-[3H]pentazocine from rat brain sigma1 receptor by competitive binding assay | 2013 | Journal 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. |
AID1213072 | Intrinsic clearance in recombinant human UGT1A9 measured per mg of protein at 10 to 400 uM by LC-MS/MS analysis | 2012 | Drug 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. |
AID1136348 | Neuroleptic activity in Sprague-Dawley rat assessed as inhibition of Sidman avoidance at 1.25 mg/kg, po relative to control | 1978 | Journal 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. |
AID311935 | Partition coefficient, log P of the compound | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model. |
AID65247 | Binding affinity was determined against Dopamine receptor D2 using [3H]spiperone | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Piperazinylalkyl heterocycles as potential antipsychotic agents. |
AID62883 | Displacement of [3H]spiroperidol from dopamine receptor of rat corpus striatum homogenate | 1980 | Journal of medicinal chemistry, Jun, Volume: 23, Issue:6 | Neuroleptic activity in 5-aryltetrahydro-gamma-carbolines. |
AID177493 | Effect on half-maximal decrease of DOPA formation in rat striatal regions; In active (no significant effect at 1.4 pmol/kg ip) | 1987 | Journal 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. |
AID1727502 | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by microbeta scintillation counting method | |||
AID1823672 | Displacement of [3H]-N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis | |||
AID1809448 | Antiangiogenic activity against VEGF-A stimulated human retinal endothelial cell assessed as cell proliferation measured after 48 hrs by crystal violet assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Haloperidol Metabolite II Valproate Ester ( |
AID65625 | Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells. | 1993 | Journal 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. |
AID1861731 | Cytotoxicity 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 control | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
AID177252 | Compound was evaluated for pole-climb avoidance (escape failures) in rat after peroral administration. | 1992 | Journal 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. |
AID1453237 | Displacement of [3H]DTG from sigma-2 receptor in rat liver membranes after 120 mins by microbeta scintillation counting method | |||
AID1574667 | Displacement of [3H]DTG from sigma2 receptor in rat liver membranes after 120 mins by scintillation counting method | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Development of Novel Quinoxaline-Based κ-Opioid Receptor Agonists for the Treatment of Neuroinflammation. |
AID40403 | Binding affinity against beta-1 adrenergic receptor in rat brain using [3H]DHA | 1986 | Journal 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. |
AID415889 | Selectivity for sigma 1 receptor in guinea pig brain membrane over sigma 2 receptor in rat liver membrane | 2009 | European 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. |
AID1823823 | Displacement of [3H]-ketanserin from human human 5-HT2A receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method | |||
AID1901078 | Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membrane measured by competitive radioligand receptor binding assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Synthesis of 8-aminomorphans with high KOR affinity. |
AID308687 | Displacement of [3H]spiperone human cloned dopamine D2 receptor | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics. |
AID63513 | Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand | 1996 | Journal 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. |
AID1878190 | Binding affinity to dopamine D2S receptor (unknown origin) by radioligand displacement assay | |||
AID170877 | Percentage change in Social interaction when compound administered at a doe of 0.05 mg/kg ip in rats | 1996 | Journal 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. |
AID1415567 | Displacement of [3H]-ifenprodil from GluN2B receptor (unknown origin) expressed in mouse L (tk-) cell membranes after 120 mins by scintillation counting method | 2017 | MedChemComm, May-01, Volume: 8, Issue:5 | Do GluN2B subunit containing NMDA receptors tolerate a fluorine atom in the phenylalkyl side chain? |
AID1570060 | Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
AID204145 | Ability to displace [3H](+)-pentazocine from Sigma opioid receptor type 1 of guinea pig brain | 2002 | Journal 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. |
AID298263 | Displacement of [3H]spiroperidol from human cloned dopamine D3 receptor | 2007 | Journal 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. |
AID4357 | The compound was tested binding affinity against 5-hydroxytryptamine 1A receptor from rat brain using [3H]8-OH-DPAT as radioligand at 10e-6 M. | 1999 | Journal 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. |
AID596436 | Biodistribution 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) | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Synthesis and biological evaluation of novel 4-benzylpiperazine ligands for sigma-1 receptor imaging. |
AID1393366 | Displacement of [3H]-8-OH-DPAT from human 5-HT1AR expressed in HEK293 cell membranes after 1 hr by microbeta counting method | |||
AID65817 | Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand | 2002 | Bioorganic & 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. |
AID705723 | Displacement of [3H](+)-pentazocine from Sigma1 receptor in rat liver homogenate | 2012 | Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19 | New positron emission tomography (PET) radioligand for imaging σ-1 receptors in living subjects. |
AID181422 | Conditioned avoidance response in rats after oral administration | 1993 | Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7 | Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system. |
AID1558955 | Displacement of [3H]-DAMGO from human MOR expressed in CHOK1 cell membranes incubated for 60 mins by liquid scintillation counting method | 2020 | Journal 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 |
AID64005 | Binding affinity towards human Dopamine receptor D4.2 in CHO cells | 1996 | Journal 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. |
AID1474166 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index | 2016 | Drug 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. |
AID1458657 | Displacement of [3H]-methylspiperone from human D2 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting | 2017 | Journal 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. |
AID4793 | Compound was evaluated In vitro for its activity by binding to 5-hydroxytryptamine 2 receptor in the rat brain using [3H]ketanserin as radioligand. | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | 1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents. |
AID476063 | Displacement of [3H](+)-pentazocine from sigma 2 receptor in rat cerebral cortex membrane by scintillation counting | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1 | Sigma-1 ligands: Tic-hydantoin as a key pharmacophore. |
AID177133 | In vivo antipsychotic activity measured by the induction of catalepsy in rats after po administration. | 1998 | Journal 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). |
AID4027 | Binding affinity was evaluated against 5-hydroxytryptamine 1A receptor on rat hippocampus using [3H]8-OH-DPAT as radioligand.; ND = Not determined | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15 | Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists. |
AID50074 | Ability to lower arterial blood pressure in cat at 100 ug/kg; reversed | 1983 | Journal of medicinal chemistry, Jun, Volume: 26, Issue:6 | 1-(Aminomethyl)-6,7-dihydroxytetralin derivatives: synthesis and assessment of dopamine-like effects. |
AID342790 | Toxicity in Sprague-Dawley rat assessed as induction of cataleptogenic behavior at 0.3 mg/kg, ip | 2008 | Bioorganic & 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. |
AID65243 | Affinity for Dopamine receptor D2 | 1998 | Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8 | Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors. |
AID35285 | In vitro binding affinity at Alpha-1 adrenergic receptor in rat cortical tissues | 2002 | Journal 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. |
AID1462752 | Displacement of [3H]ifenprodil from human NR1-1a/NR2B receptor expressed in Mouse L(tk-) cell membranes incubated for 120 mins by scintillation counting method | 2017 | Bioorganic & 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. |
AID221062 | Inhibition of apomorphine-induced climbing behavior in mice, after peroral administration | 1996 | Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. |
AID540211 | Fraction unbound in human after iv administration | 2008 | Drug 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. |
AID1861732 | Cytotoxicity 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 control | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
AID418676 | Cytotoxicity against human A427 cells after 96 hrs by crystal violet staining | 2009 | Journal 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. |
AID619349 | Displacement of (-)-[3H]pentazocine from sigma 1 receptor in rat brain membrane after 120 mins | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Synthesis and pharmacological evaluation of indole-based sigma receptor ligands. |
AID752209 | Binding affinity to Sigma receptor (unknown origin) by radioligand displacement assay | 2013 | Bioorganic & 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. |
AID4442 | Binding affinity for 5-hydroxytryptamine 1A receptor determined using [3H]8-OH-DPAT as radioligand | 2001 | Bioorganic & 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. |
AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
AID1511008 | Displacement 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 method | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Discovery of new potent dual sigma receptor/GluN2b ligands with antioxidant property as neuroprotective agents. |
AID674364 | Inhibition of human ERG expressed in HEK293 cells coexpressing Kir2.3 after 30 mins by FluxOR based FLIPR assay | 2012 | Journal of natural products, Jun-22, Volume: 75, Issue:6 | Isolation and structural elucidation of cyclic tetrapeptides from Onychocola sclerotica. |
AID1213080 | Drug 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 control | 2012 | Drug 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. |
AID1506085 | Displacement of (+)-[3H]pentazocine from human sigma1 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method | 2018 | Journal 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. |
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AID171230 | Side effect liability of compound at intraperitoneal dose of 0.5 mg/kg on 6.2 (A9 units)dopamine neurons in the nigrostriatal in rat | 1995 | Journal 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). |
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AID330561 | Displacement of [3H]mepyramine from H1R in rat brain | 2007 | Proceedings 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. |
AID231650 | Binding affinity ratio against rat cortical tissue 5-HT2 versus human D2, calculated using pKi (-logKi) values | 2002 | Journal 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. |
AID301865 | Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain | 2007 | Bioorganic & 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. |
AID1207158 | Inhibition of Na channel (species unknown) | 2011 | Cardiovascular research, Jul-01, Volume: 91, Issue:1 | Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk. |
AID1597395 | Displacement of [3H] ifenprodil from GluN2B/GluN1a (unknown origin) expressed in mouse L(tk-) cell membranes incubated for 120 mins by scintillation counting method | |||
AID203845 | Binding affinity towards sigma 2 receptor site in rat liver membranes using [3H]DTG as radioligand in presence of (+)-pentazocine. | 1998 | Journal 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. |
AID301868 | Selectivity ratio of pKi for rat brain 5HT2A receptor to pKi for rat brain dopamine D2 receptor | 2007 | Bioorganic & 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. |
AID177903 | Inhibition of firing rates of dopaminergic neurons in the substantia nigra pars compacta by intravenous injection in rats | 1993 | Journal 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. |
AID61158 | In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane. | 1999 | Journal 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 |
AID64439 | Inhibition of [3H](S)-sulpiride binding in striatal homogenates of rat brain | 1988 | Journal 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. |
AID177507 | In vivo inhibition of apomorphine-mediated stereotypy in rats administered subcutaneously at 20 mg/kg expressed as ED50 (mg/kg) | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
AID62728 | Compound was tested for anti-dopamine activity in vitro by its ability to displace [3H]spiperone from rat brain striatal preparations, | 1986 | Journal 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. |
AID239597 | Affinity for human EMP expressed in ERG2 deficient strain of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine as radioligand | 2005 | Journal 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. |
AID598815 | Displacement of [3H]N-methylspiperone from human D2 receptor expressed in HEK cells | 2011 | Bioorganic & 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. |
AID163467 | The compound was tested for its affinity against HIV-2 protease | 1991 | Journal of medicinal chemistry, Aug, Volume: 34, Issue:8 | HIV protease: a novel chemotherapeutic target for AIDS. |
AID1215948 | Unbound 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 NADPH | 2013 | Drug 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. |
AID113681 | Inhibition of apomorphine-induced climbing following s.c. administration in mice. | 1998 | Journal 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. |
AID1213046 | Drug metabolism assessed as recombinant human UGT1A1 assessed as N-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis | 2012 | Drug 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. |
AID139074 | Antagonism of apomorphine in reserpinized mice when a dose of 2.7 micro mol/kg is administered intraperitoneally | 1993 | Journal 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. |
AID277979 | Induction of catalepsy in ip dosed rat after 60 min by crossed-leg position test | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities. |
AID1570059 | Displacement of [3H]ketanserin from human 5HT2A receptor expressed in HEK293 cells incubated for 1.5 hrs by Cheng-Prusoff analysis based microbeta scintillation counting method | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
AID62164 | Competition in vitro with the dopamine receptor D2 antagonist [3H]spiperone, for binding sites on calf caudate membranes. | 1993 | Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7 | Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system. |
AID346460 | Displacement of radiolabeled haloperidol from sigma opioid receptor | 2008 | Journal 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. |
AID176775 | In vivo DOPA accumulation in reserpine pretreated rat limbic system after 1.4 umol/kg ip; I denotes inactive | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists. |
AID301871 | Blockade of secondary conditioned avoidance response in ip dosed rat | 2007 | Bioorganic & 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. |
AID619549 | Selectivity ratio of Ki for guinea pig brain sigma 1 receptor to Ki for rat liver sigma 2 receptor | 2011 | Journal 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. |
AID1456755 | Inhibition of human dopamine D4 receptor | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17 | Return of D |
AID5246 | Affinity for 5-hydroxytryptamine 2 receptor | 1998 | Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8 | Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors. |
AID130874 | Inhibition against apomorphine-induced climbing, after 5 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
AID1174073 | Displacement of [3H](+)-pentazocine from sigma1 receptor in guinea pig brain membranes after 180 mins by scintillation counting method | 2014 | Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23 | Synthesis, GluN2B affinity and selectivity of benzo[7]annulen-7-amines. |
AID232307 | Dopamine D2/D3 ratio of the compound | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11 | Synthesis and structure-activity relationships of naphthamides as dopamine D3 receptor ligands. |
AID185044 | Minimum effective dose that produced a significant effect relative to the amphetamine alone control using a Fisher's LSD post hoc test (P<0.05) | 2000 | Journal 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. |
AID232152 | Ratio of 5-HT2A receptor to that of dopamine 2 (D2) receptor in human | 2004 | Journal 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. |
AID1213051 | Drug metabolism assessed as recombinant human UGT1A9 assessed as N-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis | 2012 | Drug 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. |
AID1453236 | Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes after 120 mins by microbeta scintillation counting method | |||
AID1185969 | Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17 | Further evaluation of the tropane analogs of haloperidol. |
AID240820 | Inhibitory concentration against IKr potassium channel | 2004 | Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18 | The pharmacophore hypotheses of I(Kr) potassium channel blockers: novel class III antiarrhythmic agents. |
AID239086 | Inhibitory constant against dopamine D2 receptor using 0.2 nM [3H]-spiperone | 2005 | Journal 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. |
AID180345 | Activity 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.) | 1985 | Journal 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. |
AID1759953 | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane measured after 120 mins by solid scintillation counting method | |||
AID1207217 | Inhibition of hERG K channel | 2011 | Cardiovascular research, Jul-01, Volume: 91, Issue:1 | Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk. |
AID177689 | Effective dose against DOPA accumulation in rat brain limbic region after no pretreatment by subcutaneous administration | 1985 | Journal of medicinal chemistry, Aug, Volume: 28, Issue:8 | Novel dopamine receptor agonists and antagonists with preferential action on autoreceptors. |
AID141538 | Binding affinity against Muscarinic acetylcholine receptor in rat brain using [3H]- QNB | 1986 | Journal 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. |
AID62868 | Inhibition of [3H]spiperone binding to dopamine receptor from rat corpus striatal membranes | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Buspirone analogues. 1. Structure-activity relationships in a series of N-aryl- and heteroarylpiperazine derivatives. |
AID1519020 | Displacement of [3H]di-o-tolylguanidine from sigma2 receptor in rat liver membranes measured after 120 mins by solid scintillation counting method | |||
AID351593 | Selectivity ratio of Ki for sigma 1 receptor in guinea pig brain membrane to Ki for sigma 2 receptor in rat liver homogenates | 2009 | Bioorganic & 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. |
AID1210017 | Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate after 8 mins by LC-MS/MS analysis | 2012 | Drug 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. |
AID1213037 | Drug metabolism assessed as recombinant human UGT1A3 assessed as O-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis | 2012 | Drug 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. |
AID1461562 | Displacement of [3H]spiperone from human D2short receptor expressed in CHO cell membranes by radioligand binding assay | 2017 | Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19 | Potent haloperidol derivatives covalently binding to the dopamine D2 receptor. |
AID1146535 | Neuroleptic activity in po dosed STD-ddY mouse assessed as inhibition of spontaneous motor activity by measuring number of revolution of cage for 5 mins | 1978 | Journal of medicinal chemistry, Nov, Volume: 21, Issue:11 | Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity. |
AID1152669 | Displacement of [3H]N-methylspiperone from human recombinant D2 receptor expressed in CHO-K1 cell membrane after 60 mins by liquid scintillation counting analysis | 2014 | Journal 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. |
AID176805 | In vivo activity administered intraperitoneally was determined by pole climb escape failures in rat | 1991 | Journal 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. |
AID294440 | Displacement of [3H]spiperone from human cloned dopamine receptor D2 long expressed in CHO cells | 2007 | European journal of medicinal chemistry, Jul, Volume: 42, Issue:7 | Asymmetric synthesis of chiral piperazinylpropylisoxazoline ligands for dopamine receptors. |
AID458639 | Reduction in 3,4-dihydroxyphenylacetic acid level in Sprague-Dawley rat striatum at 1 umol/kg, sc relative to saline treated control | 2010 | Journal 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). |
AID65146 | In 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 mice | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+. |
AID1146541 | Acute toxicity in po dosed STD-ddY mouse assessed as mortality up to 7 days | 1978 | Journal of medicinal chemistry, Nov, Volume: 21, Issue:11 | Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity. |
AID1189659 | Displacement of [3H]-7-OH-DPAT from dopamine D3 receptor in rat olfactory tubercle by scintillation counting method | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Haloperidol metabolite II prodrug: asymmetric synthesis and biological evaluation on rat C6 glioma cells. |
AID64154 | In vitro binding affinity against Dopamine D2 receptor in rat striatal tissue. | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
AID1855447 | Toxicity in ICR mouse assessed as effect on motor coordination at 1 mg/kg, sc micromol/kg, sc by rotarod test | |||
AID392765 | Displacement of [3H]N-methylspiperone from human dopamine D2 receptor by liquid scintillation counting | 2009 | Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4 | Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups. |
AID1213042 | Drug metabolism assessed as recombinant human UGT2B4 assessed as O-glucuronidation at 100 uM incubated for 60 mins by LC-MS/MS analysis | 2012 | Drug 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. |
AID61804 | Binding affinity towards human D4.2 receptor | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
AID228677 | Delta ED50 value by Subcutaneous administration (ED50 catalepsy-ED50 Climbing) | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
AID177950 | Antagonistic activity against apomorphine-induced stereotypy, after 1 hour of peroral administration in rats | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
AID418668 | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane by scintillation analysis | 2009 | Journal 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. |
AID29337 | Ionisation constant (pKa) | 2002 | Journal 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. |
AID420787 | Antagonist activity at human 5HT3A receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced inward Na+ current at >= 10 uM | 2009 | European journal of medicinal chemistry, Jun, Volume: 44, Issue:6 | Molecular properties of psychopharmacological drugs determining non-competitive inhibition of 5-HT3A receptors. |
AID131364 | Effect on skeletal muscle tone, after 1 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
AID178920 | Effective dose required for antipsychotic activity was evaluated by rat CAR assay | 1998 | Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8 | Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors. |
AID1718133 | Antagonist activity at dopamine D2 receptor (unknown origin) | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases. |
AID191610 | Anti psychotic effect Social interaction when compound administered at a doe of 0.05 mg/kg ip in rats | 1996 | Journal 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. |
AID213410 | Compound was tested to block the inhibition of tyrosine hydroxylase by apomorphine at 1 uM | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8 | Synthesis and anxiolytic activity of a series of pyrazino[1,2-a][1,4]benzodiazepine derivatives. |
AID338174 | Displacement of [3H]DTG from sigma opioid receptor assessed as specific binding relative to total binding | 1993 | Journal of natural products, Apr, Volume: 56, Issue:4 | The role of receptor binding in drug discovery. |
AID524790 | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
AID1616728 | Antagonist 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 | |||
AID1187746 | Selectivity index, ratio of IC50 for for human D2LR to IC50 for human D3R by beta-galactosidase based beta-arrestin recruitment assay | 2014 | Journal 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. |
AID444006 | Displacement of [3H]DTG from sigma2 receptor in rat cerebral cortex cell membrane | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane. |
AID109881 | Effect at an intraperitoneal dose of 10 mg/kg against methamphetamine-induced hyperlocomotion in mice | 1999 | Journal 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. |
AID188453 | Drug pretreatment vs. vehicle pretreatment; statistical analysis by Student''s t test at 0.1 mg/kg; NS-Not Significant | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Troponoids. 6. Troponylpiperazines: a new class of dopamine agonists. |
AID1071724 | Antipsychotic 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 challenge | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics. |
AID1704748 | Antipsychotic 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 | |||
AID226339 | Affinity to sigma-1-receptor, using [3H]pentazocine as radioligand in homogenates of guinea pig brain membranes | 2001 | Journal 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 |
AID63794 | Binding Affinity was determined against Dopamine receptor D2 in rat striatal membranes using [3H]- spiperone radioligand. | 2000 | Journal 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. |
AID229190 | Inhibition of specific binding of [3H]DTG to sigma binding site in Guinea pig brain membranes | 1992 | Journal 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. |
AID1478366 | Binding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting method | 2018 | Journal 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. |
AID204772 | Binding affinity towards sigma receptor binding site 2 using [3H]DTG of whole rat brain homogenates except cerebellum | 1995 | Journal 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. |
AID414523 | Hypothermic activity in Sprague-Dawley rat assessed as time duration of maximal body temperature decrease at 5 mg/kg, ip | 2009 | Journal 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. |
AID1221961 | Apparent 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 LY335979 | 2011 | Drug 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. |
AID1532589 | Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Novel multitarget-directed ligands targeting acetylcholinesterase and σ |
AID61533 | Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand | 1996 | Journal 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. |
AID351592 | Displacement of [3H]di-o-tolylguanidine from sigma 2 receptor in rat liver homogenates by solid scintillation analysis | 2009 | Bioorganic & 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. |
AID114430 | Antagonism of SKF 10047 -induced hypermotility (% vs controls) dose(mg/Kg po) = 1 | 1998 | Journal 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. |
AID63547 | In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+. |
AID4363 | The compound was tested for its binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 radioligand in rat hippocampus | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | Pyrrole mannich bases as potential antipsychotic agents. |
AID239905 | Inhibitory constant towards dopamine D2 receptor was determined | 2005 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12 | Synthesis and binding affinity of novel 3-aminoethyl-1-tetralones, potential atypical antipsychotics. |
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AID1393479 | Reversal of ketamine-induced working social withdrawal in Sprague-Dawley rat at 0.1 mg/kg, ip pretreated for 60 mins followed by ketamine administration | |||
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AID1189657 | Displacement of [3H]-(+)-pentazocine from sigma 1 receptor guinea pig brain membranes incubated for 150 mins by scintillation counting method | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Haloperidol metabolite II prodrug: asymmetric synthesis and biological evaluation on rat C6 glioma cells. |
AID177081 | Compound was evaluated for inhibition of apomorphine-induced stereotypy behavior in rats after intraperitoneal administration. | 1992 | Journal 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. |
AID4136 | Binding affinity towards 5-hydroxytryptamine 1A receptor binding site using [3H]8-OH-DPAT. | 1995 | Journal 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. |
AID1467941 | Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 150 mins by liquid scintillation counting method | 2017 | Journal of medicinal chemistry, 12-14, Volume: 60, Issue:23 | Novel Sigma Receptor Ligand-Nitric Oxide Photodonors: Molecular Hybrids for Double-Targeted Antiproliferative Effect. |
AID36891 | Binding 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''. | 1998 | Journal 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). |
AID619548 | Displacement of [3H]ditolylguanidine from rat liver sigma 2 receptor by scintillation counting | 2011 | Journal 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. |
AID204780 | Binding affinity was measured on Sigma receptor type 2 with rat liver membranes and [3H]- DTG as ligand. | 2000 | Journal 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. |
AID239347 | Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand | 2005 | Journal 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. |
AID1762086 | Therapeutic 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 climbing | 2021 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 40 | Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect. |
AID64438 | Inhibition of 0.1 nM of [125I]- (S)-N-(1-Ethyl-pyrrolidin-2-ylmethyl)-5-iodo-2-methoxy-benzamide binding in striatal homogenates of rat brain | 1988 | Journal 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. |
AID517709 | Displacement of [3H]Spiperone from human dopamine D3 receptor expressed in CHO cells | 2010 | Journal 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. |
AID337890 | Displacement of [3H]DTG from sigma opioid receptor | 1993 | Journal of natural products, Apr, Volume: 56, Issue:4 | The role of receptor binding in drug discovery. |
AID517706 | Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes | 2010 | Journal 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. |
AID1292390 | Absorption half life in psychotic patient (9 patients) at 2.9 +/- 1.2 mg, po by reversed phase HPLC method | 1987 | Psychopharmacology, , Volume: 91, Issue:4 | Pharmacokinetics of haloperidol in psychotic patients. |
AID139075 | Antagonism of apomorphine in reserpinized mice when a dose of 2.7 micro mol/kg is administered intraperitoneally | 1993 | Journal 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. |
AID538760 | Displacement of [3H]di-o-tolylguanidine from sigma2 receptor rat liver membranes after 180 mins scintillation counting | 2010 | Bioorganic & 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. |
AID186044 | Locomotor activity in male Wistar rats after a dose of 0.3 uM/kg, 30 min before 1 mg/kg of apomorphine administration | 1997 | Journal 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. |
AID418678 | Cytotoxicity against human DAN-G cells after 96 hrs by crystal violet staining | 2009 | Journal 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. |
AID204445 | Binding affinity for sigma receptor using [3H](+)-pentazocine in guinea pig brain homogenates | 1992 | Journal 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. |
AID177723 | Induction of catalepsy in rats was determined after 2 hr of intraperitoneal administration of the compound | 1995 | Journal 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). |
AID342775 | Binding affinity to human cloned dopamine D1 receptor | 2008 | Bioorganic & 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. |
AID410338 | Binding affinity to human ERG expressed in HEK293 cells by whole cell patch clamp method | 2009 | Journal 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. |
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AID62571 | Compound was evaluated for the competitive binding with [3H]NCA binding to Canine striatal membranes. | 1984 | Journal 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. |
AID176655 | Subcutaneous dose to inhibit apomorphine-induced stereotyped behavior in 50% of rats | 1981 | Journal 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. |
AID1546908 | Displacement of [3H]spiperone from human D2S receptor expressed in CHO-K1 cells at 10 uM by radioligand competitive binding analysis relative to control | |||
AID232353 | Ratio of CAR ED50 vs catalepsy ED50 | 1986 | Journal 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. |
AID255689 | Effective dose against apomorphine-induced climbing behavior in mice upon oral administration (Dopaminergic antagonist) | 2005 | Journal 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. |
AID1210013 | Inhibition of recombinant CYP2J2 (unknown origin)-mediated terfenadine hydroxylation assessed as remaining activity at 30 uM after 5 mins by LC-MS analysis relative to control | 2012 | Drug 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. |
AID113544 | Induction of catalepsy in mice. | 1998 | Journal 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. |
AID1221964 | Transporter 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 LY335979 | 2011 | Drug 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. |
AID277986 | Antagonist activity against rat D2 receptor assessed as [35S]GTPgammaS binding relative to quinelorane | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities. |
AID547621 | Cytotoxicity against BESM cells after 88 hrs by HTS assay | 2010 | Antimicrobial 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. |
AID61387 | Ability to inhibit the specific binding of [3H]- spiroperidol to Dopamine receptor D2 in rat striatal membrane preparation by 50% | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | Combined analgesic/neuroleptic activity in N-butyrophenone prodine-like compounds. |
AID1398702 | Binding affinity to human biotinylated HLA-A2 by surface plasmon resonance assay | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Discovery of small molecule inhibitors of adenovirus by disrupting E3-19K/HLA-A2 interactions. |
AID1292391 | Terminal half life in psychotic patient (9 patients) at 2.9 +/- 1.2 mg, po by reversed phase HPLC method | 1987 | Psychopharmacology, , Volume: 91, Issue:4 | Pharmacokinetics of haloperidol in psychotic patients. |
AID65934 | Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand | 2000 | Journal 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. |
AID1215127 | Ratio 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 method | 2011 | Drug 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. |
AID280722 | Activity at sigma 1 receptor in rat astroglial cells | 2007 | Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5 | Novel sigma receptor ligands: synthesis and biological profile. |
AID1853654 | Antibacterial activity against Mycobacterium tuberculosis H37Ra ATCC NRS22 assessed as inhibition of bacterial growth incubated upto 3 weeks hrs by resazurin dye based double-dilution method | 2021 | RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11 | Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from |
AID479242 | Displacement of [3H]spiperone form human dopamine D2 receptor by liquid scintillation counting | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9 | Potent dihydroquinolinone dopamine D2 partial agonist/serotonin reuptake inhibitors for the treatment of schizophrenia. |
AID115764 | Antipsychotic activity using locomotor activity (LMA)-inverted screen test in mice (i.p. admin.) | 1985 | Journal 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. |
AID294441 | Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells | 2007 | European journal of medicinal chemistry, Jul, Volume: 42, Issue:7 | Asymmetric synthesis of chiral piperazinylpropylisoxazoline ligands for dopamine receptors. |
AID1726850 | Displacement of (+)-[3H]DTG from sigma 2 receptor in SPRD rat liver membrane incubated for 2 hrs by liquid scintillation counting method | |||
AID1393472 | Antipsychotic 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 | |||
AID1686300 | Effect on cell migration of in HREC at 2 uM incubated for 24 to 72 hrs by wound healing assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells. |
AID1144214 | Depression of spontaneous motor activity in Swiss-Webster mouse at 10 mg/kg, ip by photocell cage test relative to control | 1976 | Journal of medicinal chemistry, Jan, Volume: 19, Issue:1 | Synthesis and biological actions of 2-substituted quinolizidines. |
AID36865 | In vitro inhibitory concentration against radioligand [3H]WB-4101 binding to rat cortical alpha-1 adrenergic receptor | 1992 | Journal 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. |
AID65087 | Binding affinity measured at the Dopamine receptor D2 by the inhibition of [3H]methylspiperone binding to rat striatum using unlabeled haloperidol for nonspecific binding. | 1998 | Journal 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). |
AID1174258 | Displacement of [3H](+)-pentazocine from human sigma 1 receptor in human Jurkat cell membranes incubated for 2 hrs by liquid scintillation counting | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Carboline- and phenothiazine-derivated heterocycles as potent SIGMA-1 protein ligands. |
AID188455 | Drug pretreatment vs. vehicle pretreatment; statistical analysis by Student's t test at 0.5 mg/kg | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Troponoids. 6. Troponylpiperazines: a new class of dopamine agonists. |
AID1853649 | Antibacterial activity against Mycobacterium smegmatis mc2 155 assessed as inhibition of bacterial growth incubated upto 3 weeks hrs by resazurin dye based double-dilution method | 2021 | RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11 | Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from |
AID646276 | Antipsychotic 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 hr | 2012 | Bioorganic & 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. |
AID625288 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID467611 | Dissociation constant, pKa of the compound | 2009 | European 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. |
AID586708 | Displacement of [3H]-pentazocine from guinea pig sigma1 receptor by liquid scintillation counting | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Synthesis and pharmacological evaluation of fluorine-containing D₃ dopamine receptor ligands. |
AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
AID1601981 | Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
AID492183 | Displacement of [125I]ABN from human dopamine D3 receptor expressed in HEK293 cells after 60 mins by gamma counting | 2010 | Bioorganic & 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. |
AID342786 | Binding affinity to rat NET | 2008 | Bioorganic & 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. |
AID735278 | Displacement of [3H]-(+)-pentazocine from human sigma1 receptor transfected in HEK293 cells after 120 mins by liquid scintillation counting analysis | 2013 | Journal 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. |
AID1433419 | Displacement 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 | |||
AID176323 | In vivo blocking of apomorphine induced hyperactivity following 1 mg/kg i.p. in rats after 60 min. | 1982 | Journal of medicinal chemistry, Nov, Volume: 25, Issue:11 | Potential neuroleptic agents. 2,6-Dialkoxybenzamide derivatives with potent dopamine receptor blocking activities. |
AID178704 | Antagonistic activity against amphetamine-induced stereotypy in rats; (5 mg/kg administered ip 1 hr after the test compound). | 1986 | Journal of medicinal chemistry, Jan, Volume: 29, Issue:1 | Neuroleptic activity of chiral trans-hexahydro-gamma-carbolines. |
AID1191388 | Displacement of (+)-[3H]pentazocine from guinea pig brain cortex sigma1 receptor by scintillation analyzer | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Improving selectivity preserving affinity: new piperidine-4-carboxamide derivatives as effective sigma-1-ligands. |
AID178242 | Inhibition of shelf-jump avoidance in rats after peroral administration. | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines. |
AID277973 | Displacement of [3H]OH-DPAT from rat cortex 5HT1A receptor | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities. |
AID1853646 | Inhibition 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 analysis | 2021 | RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11 | Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from |
AID180521 | The compound was tested for inhibition of sidman avoidance in rat | 1985 | Journal 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. |
AID392767 | Ratio of Ki for human dopamine D2 receptor to Ki for human dopamine D4 receptor | 2009 | Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4 | Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups. |
AID776368 | Displacement of (+)-pentazocine from sigma-1 receptor in guinea pig brain cortex membrane after 120 mins by scintillation counting | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | New combination of pharmacophoric elements of potent σ₁ ligands: design, synthesis and σ receptor affinity of aminoethyl substituted tetrahydrobenzothiophenes. |
AID1159367 | Displacement of (+)-pentazocine from sigma1 receptor in guinea pig brain cortex membrane by scintillation counting analysis | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Identification, pharmacological evaluation and binding mode analysis of novel chromene and chromane based σ1 receptor ligands. |
AID1506088 | Displacement of (-)-[3H]vesamicol from rat VAChT expressed in rat PC12 cell membranes after 60 mins by liquid scintillation counting method | 2018 | Journal 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. |
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AID1461566 | Selectivity index, ratio of Ki for human D3 receptor expressed in CHO cell membranes to Ki for human D2short receptor expressed in CHO cell membranes | 2017 | Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19 | Potent haloperidol derivatives covalently binding to the dopamine D2 receptor. |
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AID62007 | Displacement of [3H]-YM 09151 from african green monkey Dopamine receptor D2 | 1995 | Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25 | 1-Phenyl-3-(aminomethyl)pyrroles as potential antipsychotic agents. Synthesis and dopamine receptor binding. |
AID65781 | Binding affinity of compound towards Dopamine receptor D3 using [3H]spiperone (1.2 nM) ligand in cortex was determined | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands. |
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AID176458 | Pole climb escape failures of rats was determined after 1 hr of intraperitoneal administration of the compound | 1995 | Journal 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). |
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AID142687 | Binding affinity against muscarinic (M) receptor | 1994 | Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4 | Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study. |
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AID1823673 | Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK293 cell membrane incubated for 60 mins by radioligand binding assay | |||
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AID204615 | Compound was tested in vitro for its ability to displace radioligand (+)-[3H]-3-PPP from rat cortical sigma receptor | 1992 | Journal 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. |
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AID238699 | Binding affinity for human dopamine receptor D2 long | 2005 | Journal 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. |
AID1330099 | Displacement of [3H]DADLE from human DOR expressed in HEK cells measured after 90 mins by microbeta scintillation counting method | 2016 | Bioorganic & 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. |
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AID298480 | Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells | 2007 | Journal 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. |
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AID705400 | Antipsychotic activity in sc dosed rat by conditioned avoidance response test | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Current landscape of phosphodiesterase 10A (PDE10A) inhibition. |
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AID35277 | Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in rat brain | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
AID524794 | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
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AID5171 | Inhibitory concentration against human 5-HT2A receptor in BEK cells | 1996 | Journal 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. |
AID111333 | Relative central nervous system(CNS) activity was measured in mice; Activity in >=6 assays | 1981 | Journal 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. |
AID7783 | Unbound fraction (plasma) | 2004 | Journal 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. |
AID176735 | Dose (administered orally) inhibiting spontaneous locomotor behavior in rats | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
AID1650557 | Displacement of [3H]ifenprodil from human recombinant GluN2B expressed in mouse L(tk-) cell membranes co-expressing GluN1a incubated for 120 mins by scintillation counting method | 2020 | Bioorganic & 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. |
AID1851836 | Displacement of (+)-[3H]pentazocine from sigma-1 receptor in Sprague-Dawley rat cerebral membrane incubated for 90 mins by liquid scintillation counter analysis | 2022 | RSC medicinal chemistry, Aug-17, Volume: 13, Issue:8 | Development of tumor-targeting aza-vesamicol derivatives with high affinity for sigma receptors for cancer theranostics. |
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AID229192 | Inhibition of specific binding of [3H]NANM of sigma binding site in Guinea pig brain membranes | 1992 | Journal 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. |
AID596437 | Biodistribution 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) | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Synthesis and biological evaluation of novel 4-benzylpiperazine ligands for sigma-1 receptor imaging. |
AID113713 | Inhibition of the APO-induced stereotyped behavior in mice | 1998 | Journal 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. |
AID1686277 | Displacement of [3H]-DTG from sigma2 receptor in guinea pig brain membranes by scintillation counting | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells. |
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AID233807 | The ratio of the IC50 value of Dopamine D2 receptor to that of serotonergic 5-HT2 receptor | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16 | Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents. |
AID1213082 | Drug 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 control | 2012 | Drug 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. |
AID1449796 | Displacement of [3H]-(+)-pentazocine from sigma1 in human MDA-MB-468 cell membranes | 2017 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 27, Issue:10 | Novel small molecule guanidine Sigma1 inhibitors for advanced prostate cancer. |
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AID114233 | Salivation after subcutaneous administration in mice; nt=Not tested | 1998 | Journal 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. |
AID393361 | Selectivity ratio of Ki for rat liver sigma 2 receptor to Ki for rat liver sigma 1 receptor | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Substituted benzo[d]oxazol-2(3H)-one derivatives with preference for the sigma1 binding site. |
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AID1300809 | Displacement 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 (+)-pentazocine | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 | One-pot synthesis and sigma receptor binding studies of novel spirocyclic-2,6-diketopiperazine derivatives. |
AID234212 | Therapeutic ratio of ED50 of catalepsy to ED50 of climbing in rat models | 1987 | Journal 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. |
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AID1712206 | Displacement 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 method | 2016 | Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14 | New bifunctional antioxidant/σ1 agonist ligands: Preliminary chemico-physical and biological evaluation. |
AID223122 | Compound was evaluated for the effective dose that causes lethality in aggregated mice (group toxicity antagonism) | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Synthesis and antidopaminergic activity of some 3-(aminomethyl)tetralones as analogues of butyrophenone. |
AID229186 | Inhibition of specific binding of [125I]-PIPAG to sigma binding site in Guinea pig brain membranes | 1992 | Journal 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. |
AID1079931 | Moderate 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] | |||
AID592126 | Induction 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%) | 2011 | Journal 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. |
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AID5835 | Inhibitory constant was determined on 5-hydroxytryptamine 2C receptor of Bovine choroid plexus | 2002 | Journal 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. |
AID1570061 | Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
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AID624215 | Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1A | 1998 | The 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 |
AID1345615 | Human 5-HT1A receptor (5-Hydroxytryptamine receptors) | 1998 | The 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 |
AID1345718 | Human D1 receptor (Dopamine receptors) | 2009 | Journal of psychopharmacology (Oxford, England), Jan, Volume: 23, Issue:1 | Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. |
AID624222 | Antagonists at Rat 5-Hydroxytryptamine receptor 5-HT2A | 1998 | The 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. |
AID1345783 | Rat D2 receptor (Dopamine receptors) | 1990 | Nature, Sep-13, Volume: 347, Issue:6289 | Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics. |
AID1346501 | Mouse Kir3.2 (Inwardly rectifying potassium channels) | 2000 | British 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. |
AID1345235 | Rat 5-HT7 receptor (5-Hydroxytryptamine receptors) | 1993 | Proceedings 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. |
AID624218 | Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2B | 1998 | Naunyn-Schmiedeberg's archives of pharmacology, Jan, Volume: 357, Issue:1 | [3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor. |
AID1345833 | Human D3 receptor (Dopamine receptors) | 1994 | Pharmacology, biochemistry, and behavior, Nov, Volume: 49, Issue:3 | Characterization of the binding of SCH 39166 to the five cloned dopamine receptor subtypes. |
AID624223 | Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A | 2003 | Neuropsychopharmacology : 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. |
AID1345615 | Human 5-HT1A receptor (5-Hydroxytryptamine receptors) | 1997 | The 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. |
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AID624215 | Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1A | 1996 | Psychopharmacology, Mar, Volume: 124, Issue:1-2 | Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. |
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AID1345814 | Human D4 receptor (Dopamine receptors) | 1993 | European journal of pharmacology, Jun-04, Volume: 236, Issue:3 | Dopamine D4 versus D2 receptor selectivity of dopamine receptor antagonists: possible therapeutic implications. |
AID1159550 | Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening | 2015 | Nature cell biology, Nov, Volume: 17, Issue:11 | 6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling. |
AID1224817 | Assays to identify small molecules inhibitory for eIF4E expression | 2015 | Chemistry & biology, Jul-23, Volume: 22, Issue:7 | Internal Ribosome Entry Site-Based Bicistronic In Situ Reporter Assays for Discovery of Transcription-Targeted Lead Compounds. |
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AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | |||
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[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 7703 (40.57) | 18.7374 |
1990's | 4114 (21.67) | 18.2507 |
2000's | 3523 (18.56) | 29.6817 |
2010's | 2797 (14.73) | 24.3611 |
2020's | 848 (4.47) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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.
| This Compound (119.29) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 1,753 (8.62%) | 5.53% |
Trials | 0 (0.00%) | 5.53% |
Reviews | 779 (3.83%) | 6.00% |
Reviews | 0 (0.00%) | 6.00% |
Case Studies | 1,692 (8.32%) | 4.05% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 27 (0.13%) | 0.25% |
Observational | 0 (0.00%) | 0.25% |
Other | 16,079 (79.09%) | 84.16% |
Other | 13 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
Preventing ICU Subsyndromal Delirium Conversion to Delirium With Low Dose IV Haloperidol: A Double-Blind, Placebo-Controlled Pilot Study [NCT01174290] | Phase 4 | 68 participants (Actual) | Interventional | 2010-09-30 | Completed | ||
Pharmacological Modulation of Belief Salience [NCT03754062] | Phase 1 | 30 participants (Actual) | Interventional | 2017-06-01 | Completed | ||
Blood Lactate Levels in Patients Treated With Typical or Atypical Antipsychotics [NCT01139463] | 60 participants (Actual) | Observational | 2008-06-30 | Completed | |||
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 1 | 24 participants (Anticipated) | Interventional | 2011-02-28 | Enrolling 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) | Interventional | 2023-09-01 | Not yet recruiting | |||
TREC-Lebanon Trial: A Randomised Controlled Trial for Rapid Tranquilisation for Agitated Patients in the Emergency Setting [NCT03639558] | Phase 4 | 100 participants (Actual) | Interventional | 2018-08-28 | Completed | ||
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 3 | 60 participants (Anticipated) | Interventional | 2016-01-31 | Recruiting | ||
Feasibility of Prophylactic Haldol to Prevent Delirium in Cancer Patients [NCT03489551] | Phase 4 | 17 participants (Actual) | Interventional | 2011-11-30 | Completed | ||
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 4 | 66 participants (Actual) | Interventional | 2014-02-28 | Terminated(stopped due to PI lapsed institutional training) | ||
Strategies for Persistent Agitated Delirium in Palliative Care [NCT03743649] | Phase 2/Phase 3 | 206 participants (Anticipated) | Interventional | 2019-07-17 | Recruiting | ||
A Comparison of Haloperidol 5mg IM vs Droperidol 2.5mg and Ondansetron for the Treatment of Hyperemesis in Cannabis Hyperemesis Syndrome [NCT05065567] | Phase 2 | 38 participants (Actual) | Interventional | 2021-08-30 | Terminated(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) | Observational | 2009-03-31 | Completed | |||
Outcomes of Antipsychotic Medication Use in the Emergency Department: A Retrospective Comparison Study [NCT02504450] | 93 participants (Actual) | Observational | 2015-04-30 | Completed | |||
Neuroendocrine, Metabolite Substrates, Clinical Symptoms and Cognitive Function in Schizophrenia [NCT02423096] | 200 participants (Anticipated) | Observational [Patient Registry] | 2013-12-31 | Recruiting | |||
Intramuscular Olanzapine Versus Haloperidol or Midazolam for the Management of Acute Agitation in the Emergency Department - a Multicentre Randomised Clinical Trial [NCT02380118] | Phase 4 | 167 participants (Actual) | Interventional | 2014-12-31 | Terminated(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) | Observational | 2014-02-28 | Completed | |||
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 4 | 60 participants (Actual) | Interventional | 2021-04-01 | Completed | ||
Haloperidol Versus Ondansetron for Cannabis Hyperemesis Syndrome (HaVOC): A Randomized Controlled Trial [NCT03056482] | Phase 4 | 33 participants (Actual) | Interventional | 2017-05-21 | Completed | ||
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 4 | 21 participants (Actual) | Interventional | 2015-02-01 | Completed | ||
Clozapine and Olanzapine in the Treatment of Violence in Schizophrenic Patients [NCT01123408] | 110 participants (Actual) | Interventional | 1999-06-30 | Completed | |||
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 3 | 3 participants (Actual) | Interventional | 2010-05-31 | Terminated(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 3 | 337 participants (Actual) | Interventional | 2015-07-08 | Completed | ||
A Randomized Double-blind Multicenter Double-dummy Non-inferiority Trial of Inhaled Loxapine and Intramuscular Haloperidol + Lorazepam for the Reduction of Agitation [NCT03110900] | Phase 4 | 2 participants (Actual) | Interventional | 2017-09-30 | Terminated(stopped due to Sponsor Withdrawal) | ||
Effects of Aripiprazole and Haloperidol on Mesolimbic System Functioning: A Pharmacological fMRI Study [NCT01161277] | Phase 4 | 54 participants (Actual) | Interventional | 2010-08-31 | Completed | ||
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 4 | 149 participants (Actual) | Interventional | 2010-02-28 | Completed | ||
Early Clinical Evaluation of the Pharmacokinetics and Mechanism Based Pharmacodynamics of Haloperidol Using Positron Emission Tomography in Healthy Volunteers [NCT01193621] | Phase 1 | 12 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
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 3 | 460 participants (Actual) | Interventional | 2005-07-01 | Completed | ||
Intravenous Haloperidol Versus Ondansetron for Treatment of Established Nausea and Vomiting in Patients Undergoing Surgery With General Anesthesia: A Randomized Clinical Trial [NCT02143531] | Phase 4 | 120 participants (Actual) | Interventional | 2008-09-30 | Completed | ||
Haldol/Diphenhydramine Versus Metoclopramide/Diphenhydramine for Treatment of Acute Headache in the Emergency Department: A Randomized Controlled Trial [NCT02098499] | Phase 4 | 68 participants (Actual) | Interventional | 2013-06-30 | Completed | ||
A Double Blinded Randomized Trial of Ketamine Versus Haloperidol for Severe Prehospital Agitation [NCT02103881] | Phase 4 | 0 participants (Actual) | Interventional | 2014-04-30 | Withdrawn | ||
Meth-OD: A Phase 2a Study of IXT-m200 in Patients With Toxicity From Methamphetamine Overdose [NCT04715230] | Phase 2 | 20 participants (Actual) | Interventional | 2021-06-30 | Terminated(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 3 | 25 participants (Actual) | Interventional | 2013-08-31 | Completed | ||
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 3 | 240 participants (Anticipated) | Interventional | 2009-02-28 | Completed | ||
How Does the Brain Learn About Positive and Negative Things? [NCT06014606] | 150 participants (Actual) | Interventional | 2021-03-01 | Completed | |||
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 4 | 335 participants (Actual) | Interventional | 2005-01-31 | Terminated(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 2 | 46 participants (Actual) | Interventional | 2007-08-15 | Terminated | ||
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 3 | 376 participants (Actual) | Interventional | 2008-09-30 | Completed | ||
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 1 | 60 participants (Anticipated) | Interventional | 2020-03-12 | Recruiting | ||
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 4 | 212 participants (Actual) | Interventional | 2011-05-31 | Completed | ||
Atypical Antipsychotics and Hyperglycemic Emergencies: Multicentre, Retrospective Cohort Study of Administrative Data [NCT02582736] | 725,489 participants (Actual) | Observational | 2012-04-30 | Completed | |||
Treatment of Clozapine-resistant Schizophrenia : Comparison Between Augmentation With Haloperidol and Electroconvulsive Therapy [NCT00753051] | 18 participants (Actual) | Interventional | 2008-06-30 | Completed | |||
Methylphenidate, Rivastigmine or Haloperidol in Hypoactive Delirium in Intensive Care Patients: a Randomized, Mono-blind Pilot Trial [NCT00599287] | Phase 3 | 80 participants (Anticipated) | Interventional | 2008-02-29 | Terminated(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 4 | 11 participants (Actual) | Interventional | 2004-10-31 | Terminated(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) | Interventional | 2005-03-31 | Completed | |||
Metabolic Effects of Subchronic Dopamine D2 Receptor Blockade by Antipsychotic Drugs in Healthy Humans [NCT00625170] | 11 participants (Actual) | Interventional | 2004-05-31 | Completed | |||
A Comparison of Long-Acting Injectable Medications for Schizophrenia [NCT01136772] | Phase 4 | 311 participants (Actual) | Interventional | 2011-03-31 | Completed | ||
MIND-USA Study: Modifying the Impact of ICU-Associated Neurological Dysfunction [NCT01211522] | Phase 3 | 566 participants (Actual) | Interventional | 2011-12-14 | Completed | ||
Study of Evaluating Quetiapine in Improving Sleep Quality of Schizophrenia [NCT00642369] | 60 participants (Actual) | Interventional | 2008-03-31 | Completed | |||
GiSAS Trial: Aripiprazole, Olanzapine, and Haloperidol in the Long Term Treatment of Schizophrenia. [NCT01052389] | Phase 4 | 300 participants (Actual) | Interventional | 2007-07-31 | Completed | ||
[NCT00631722] | 80 participants (Actual) | Interventional | 2007-05-31 | Completed | |||
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 3 | 318 participants (Anticipated) | Interventional | 2023-03-28 | Not yet recruiting | ||
Intravenous Haloperidol for the Treatment of Headache in the Emergency Department [NCT02747511] | Phase 4 | 118 participants (Actual) | Interventional | 2015-10-31 | Completed | ||
An Open-Label, Single-Dose, Crossover Study to Determine the Bioequivalency of Generic Haloperidol Tablets vs. Haldol in Normal Volunteers. [NCT00946491] | Phase 1 | 30 participants (Actual) | Interventional | 1987-04-30 | Completed | ||
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) | Observational | 2019-05-06 | Completed | |||
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) | Observational | 2015-07-24 | Completed | |||
[NCT00838032] | Phase 4 | 70 participants (Anticipated) | Interventional | 2008-08-31 | Recruiting | ||
Compare Efficacy and Safety Between Quetiapine and Haloperidol in Treatment Delirium [NCT00954603] | Phase 3 | 52 participants (Actual) | Interventional | 2009-06-30 | Terminated(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 4 | 198 participants (Actual) | Interventional | 2008-08-31 | Completed | ||
Treatment of Behavioral Symptoms in Alzheimer's Disease [NCT00009217] | Phase 4 | 44 participants (Actual) | Interventional | 1999-01-31 | Completed | ||
Placebo- and Haloperidol-Controlled Double-Blind Trial of Olanzapine in Patients With Manic or Mixed Episode of Bipolar I Disorder [NCT00129220] | Phase 3 | 224 participants (Actual) | Interventional | 2005-07-31 | Completed | ||
Combination of Haloperidol and Magnesium for Delirium Prevention in Critically Ill Elderly Patients After Elective Major Surgery [NCT06168773] | Phase 2/Phase 3 | 135 participants (Actual) | Interventional | 2022-11-01 | Completed | ||
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 1 | 32 participants (Actual) | Interventional | 2019-11-15 | Completed | ||
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 1 | 32 participants (Actual) | Interventional | 2019-11-15 | Completed | ||
Delirium in the ICU: a Prospective, Randomized, Trial of Placebo vs. Haloperidol vs. Ziprasidone [NCT00096863] | Phase 2 | 102 participants (Actual) | Interventional | 2004-12-31 | Completed | ||
A Comparison of Risperidone and Haloperidol for Prevention of Relapse in Subjects With Schizophrenia and Schizoaffective Disorders [NCT00253110] | Phase 4 | 396 participants (Actual) | Interventional | 1996-05-31 | Completed | ||
Optimization of Acute Treatment in First Episode Schizophrenic Patients by New Pharmacological Treatments [NCT00157378] | Phase 4 | 300 participants | Interventional | 2000-11-30 | Active, not recruiting | ||
Drug Interactions With Risk of QT-prolongation in a General Hospital: an Epidemiological Point Prevalence Study [NCT02043912] | 222 participants (Actual) | Observational | 2013-07-31 | Completed | |||
CSP #451 - The Clinical and Economic Impact of Olanzapine in the Treatment of Schizophrenia [NCT00007774] | Phase 4 | 600 participants (Anticipated) | Interventional | 1998-03-31 | Completed | ||
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 2 | 114 participants (Anticipated) | Interventional | 2020-11-26 | Recruiting | ||
Longitudinal Comparative Effectiveness of Bipolar Disorder Therapies [NCT02893371] | 1,037,352 participants (Actual) | Observational | 2016-09-30 | Completed | |||
Topical Haloperidol: Evidence of Absorption After Topical Administration [NCT01684969] | Early Phase 1 | 0 participants (Actual) | Interventional | 2012-03-31 | Withdrawn(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) | Interventional | 2008-06-30 | Terminated | |||
Intravenous Immunoglobulins as Effective Treatment in Sydenham's Chorea [NCT00615797] | 20 participants (Actual) | Interventional | 2002-05-31 | Completed | |||
Intramuscular Clozapine in the Management of Aggression in Schizophrenic Patients [NCT00189995] | Phase 3 | 0 participants (Actual) | Interventional | Withdrawn | |||
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 4 | 360 participants | Interventional | 2003-08-31 | Completed | ||
A Comparison of Midazolam or Haloperidol Premedication Versus Placebo for Reducing Ketamine Induced Agitation After Adult Procedural Sedation in the Emergency Department [NCT02909465] | Phase 4 | 185 participants (Actual) | Interventional | 2016-07-31 | Completed | ||
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 3 | 67 participants (Actual) | Interventional | 2006-07-31 | Completed | ||
Safety and Efficacy of Four Intramuscular Interventions for the Management of Acute Psychomotor Agitation [NCT01485692] | 120 participants (Actual) | Interventional | 2009-02-28 | Completed | |||
[NCT00000179] | Phase 3 | 0 participants | Interventional | Completed | |||
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 3 | 300 participants | Interventional | 2005-09-30 | Completed | ||
A Double-Blind Randomized Comparison of the Efficacy and Safety of Intramuscular Olanzapine and Intramuscular Haloperidol in Acutely Agitated Patients With Schizophrenia [NCT00485901] | Phase 3 | 50 participants (Actual) | Interventional | 2004-07-31 | Completed | ||
Pharmacokinetics of Understudied Drugs Administered to Children Per Standard of Care [NCT01431326] | 3,520 participants (Actual) | Observational | 2011-11-30 | Completed | |||
Metabolic Profile and Anthropometric Changes in Schizophrenia [NCT00534183] | 2,006 participants (Actual) | Interventional | 2006-06-30 | Completed | |||
A Multicenter, Randomized, Double-Blind, Placebo Controlled Study of Aripiprazole Monotherapy in the Treatment of Acutely Manic Patients With Bipolar I Disorder [NCT00097266] | Phase 3 | 615 participants | Interventional | 2004-12-31 | Completed | ||
Randomised Double-blind Placebo-controlled Study of Post-operative Haloperidol Versus Placebo for Prevention of Post-operative Delirium After Acute Hip Surgery [NCT00250237] | Phase 3 | 220 participants (Actual) | Interventional | 2005-11-30 | Completed | ||
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 4 | 19 participants (Actual) | Interventional | 2003-01-31 | Terminated(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 2 | 20 participants (Anticipated) | Interventional | 2005-12-31 | Completed | ||
One Year Maintenance Treatment With Low Dose Haloperidol vs. Risperidone in First-Episode Schizophrenia [NCT00159081] | Phase 4 | 159 participants (Actual) | Interventional | 2000-11-30 | Completed | ||
A Randomised Open Label Pilot Study of the Efficacy of Dexmedetomidine and Haloperidol in Ventilated Patients With ICU-associated Agitation and Delirium [NCT00505804] | Phase 2 | 20 participants (Actual) | Interventional | 2005-01-31 | Completed | ||
Clozapine or Haloperidol in First Episode Schizophrenia [NCT00169091] | Phase 4 | 32 participants (Actual) | Interventional | 1996-03-31 | Terminated | ||
Early Pharmacological Intervention to Prevent Delirium: Haloperidol Prophylaxis in Older Emergency Department Patients [NCT01530308] | Phase 4 | 242 participants (Actual) | Interventional | 2012-11-30 | Completed | ||
Early Recognition and Optimal Treatment of Delirium in Patients With Advanced Cancer [NCT01539733] | 101 participants (Actual) | Interventional | 2010-03-31 | Completed | |||
5HT3 Antagonism and Auditory Gating in Schizophrenia [NCT00018850] | 0 participants | Interventional | 1998-06-30 | Completed | |||
Predicting the Optimal Pharmacotherapy for Outpatients With Schizophrenia [NCT00018642] | 0 participants | Interventional | 1997-04-30 | Completed | |||
A Comparison of Two Different Treatments for Major Depression With Psychotic Features: Ziprasidone vs. Combined Sertraline and Haloperidol [NCT00340379] | Phase 2/Phase 3 | 72 participants (Actual) | Interventional | 2003-04-30 | Completed | ||
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) | Observational | 2017-06-15 | Completed | |||
Haloperidol and/or Chlorpromazine for Refractory Agitated Delirium in the Palliative Care Unit [NCT03021486] | Phase 2/Phase 3 | 70 participants (Actual) | Interventional | 2017-06-05 | Active, 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) | Interventional | 2011-11-30 | Completed | |||
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 4 | 12 participants (Actual) | Interventional | 2017-09-01 | Terminated(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 3 | 56 participants (Actual) | Interventional | 2012-12-31 | Completed | ||
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 3 | 104 participants (Anticipated) | Interventional | 2012-11-30 | Recruiting | ||
Prophylactic Haloperidol Use for Delirium in ICU Patients; a Randomized Placebo-controlled Double-blind Multicentre Trial [NCT01785290] | Phase 4 | 1,800 participants (Actual) | Interventional | 2013-06-30 | Completed | ||
Randomized Controlled Trial Comparing Haloperidol, Quetiapine and Placebo in the Pharmacological Treatment of Delirium : The Haloquet Trial [NCT01811459] | Phase 3 | 107 participants (Actual) | Interventional | 2013-02-28 | Completed | ||
Preventing Post-Operative Delirium in Pneumonectomy, Esophagectomy and Thoracotomy Patients [NCT02213900] | Phase 4 | 135 participants (Actual) | Interventional | 2013-09-30 | Completed | ||
Correlation Between Cognitive Function and Relapse of Schizophrenia Regarding Dose Reduction in Patients Undergoing High-dose Antipsychotic Therapy [NCT03019887] | 139 participants (Actual) | Interventional | 2011-04-30 | Completed | |||
Valproic Acid for Treatment of Hyperactive or Mixed Delirium in ICU [NCT02343575] | Phase 4 | 3 participants (Actual) | Interventional | 2015-01-31 | Terminated(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 2 | 80 participants (Anticipated) | Interventional | 2021-09-01 | Recruiting | ||
Managing Agitated Delirium With Neuroleptics and Anti-Epileptics as a Neuroleptic Sparing Strategy [NCT05431595] | Phase 2/Phase 3 | 150 participants (Anticipated) | Interventional | 2022-07-19 | Enrolling 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 3 | 187 participants (Actual) | Interventional | 2005-09-30 | Completed | ||
"Absorption of ABH Gel (Ativan®, Lorazepam; Benadryl®, Diphenhydramine; and Haldol®, Haloperidol Gel) From the Skin of Normal Volunteers" [NCT01204255] | 11 participants (Actual) | Interventional | 2010-11-15 | Completed | |||
Phase 4 Study of Optimal Dose of Haloperidol [NCT01639599] | 150 participants (Actual) | Interventional | 2012-03-31 | Completed | |||
ORIC-I: Optimizing Recovery From Intensive Care: Mechanical Ventilation and Delirium [NCT00300391] | Phase 3 | 40 participants (Actual) | Interventional | 2006-03-31 | Terminated(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 2 | 100 participants (Anticipated) | Interventional | 2017-06-30 | Not 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) | Interventional | 2010-06-30 | Completed | |||
Agents Intervening Against Delirium in Intensive Care Unit (AID-ICU) A Randomized, Blinded, Placebo-controlled Trial [NCT03392376] | Phase 4 | 1,000 participants (Anticipated) | Interventional | 2018-06-13 | Active, 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 2 | 60 participants (Actual) | Interventional | 2009-09-30 | Completed | ||
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 2 | 93 participants (Actual) | Interventional | 2014-01-31 | Active, not recruiting | ||
Real-time Decision Support for Postoperative Nausea and Vomiting (PONV) Prophylaxis [NCT02625181] | 27,034 participants (Actual) | Interventional | 2016-07-31 | Completed | |||
Reducing the Burden of Chronic Psychotic Disorders in Tanzania [NCT04327843] | Phase 3 | 22 participants (Actual) | Interventional | 2019-11-05 | Completed | ||
Study of add-on Ramelteon Therapy on Sleep and Circadian Rhythm Disruption in Patients With Schizophrenia [NCT03075657] | Phase 4 | 120 participants (Actual) | Interventional | 2017-05-01 | Completed | ||
Baden PRIDe Trial - Baden Prevention and Reduction of Incidence of Postoperative Delirium Trial [NCT02433041] | Phase 4 | 200 participants (Actual) | Interventional | 2013-07-31 | Completed | ||
Pharmacovigilance in Gerontopsychiatric Patients [NCT02374567] | Phase 3 | 407 participants (Actual) | Interventional | 2015-01-31 | Terminated | ||
Haloperidol Compared to Dexamethasone in Lowering Postoperative Nausea and Vomiting and Pain in Adult After Laparoscopy [NCT05246631] | Phase 4 | 80 participants (Actual) | Interventional | 2020-01-01 | Completed | ||
The Impact of Genetic Variation In Nicotinic Cholinergic Receptors on Functional Brain Networks Underlying Addiction Susceptibility [NCT01924468] | Phase 1 | 76 participants (Actual) | Interventional | 2013-08-14 | Completed | ||
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 2 | 356 participants (Actual) | Interventional | 2002-07-31 | Completed | ||
Quetiapine Versus Haloperidol in the Management of Hyperactive Delirium [NCT05690698] | Phase 3 | 100 participants (Actual) | Interventional | 2023-04-09 | Completed | ||
A Comparison Study of the Efficacy of a Rapid Titration of Quetiapine and Haloperidol in Agitated Adults in an Emergency Setting. [NCT00457366] | Phase 4 | 72 participants (Actual) | Interventional | 2006-05-31 | Completed | ||
[NCT02493192] | Phase 4 | 110 participants (Anticipated) | Interventional | 2015-07-31 | Not yet recruiting | ||
Pharmacological Management of Delirium [NCT00842608] | 551 participants (Actual) | Interventional | 2009-02-28 | Completed | |||
Lurasidone Effects on Tissue Glutamate in Schizophrenia [NCT02199743] | Phase 4 | 35 participants (Actual) | Interventional | 2013-02-28 | Completed | ||
Haloperidol vs Conventional Therapy for Gastroparesis [NCT02057549] | Phase 4 | 36 participants (Actual) | Interventional | 2012-11-30 | Terminated(stopped due to PI left institution) | ||
Prospective Evaluation of Symptoms and Open Label Haloperidol in Cannabinoid Hyperemesis Syndrome (HALO) [NCT04176055] | Phase 4 | 4 participants (Actual) | Interventional | 2020-10-13 | Completed | ||
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) | Interventional | 2014-05-31 | Completed | |||
Rapid Agitation Control With Ketamine in the Emergency Department (RACKED): a Randomized Controlled Trial [NCT03375671] | Phase 2 | 81 participants (Actual) | Interventional | 2018-05-29 | Completed | ||
Delirium: Is Prophylactic Drug Therapy Useful in High Risk Patients as Defined by the Delirium Risk Prediction Model? [NCT03199950] | Phase 4 | 1,366 participants (Anticipated) | Interventional | 2017-06-23 | Recruiting | ||
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 3 | 142 participants (Actual) | Interventional | 2018-02-22 | Terminated(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) | Interventional | 2012-03-31 | Completed | |||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |