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sulpiride

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Description

Sulpiride is an atypical antipsychotic medication used to treat schizophrenia. It is a dopamine antagonist that primarily blocks D2 receptors in the mesolimbic pathway, which is thought to be involved in the positive symptoms of schizophrenia. Sulpiride is also known to have some affinity for serotonin receptors, which may contribute to its anti-anxiety and antidepressant effects. It is synthesized by a series of chemical reactions starting with 4-chloro-2-nitroaniline. Sulpiride is typically administered orally and has a relatively long half-life. It is generally well-tolerated, but common side effects include extrapyramidal symptoms, such as tremors and muscle stiffness, as well as weight gain. Sulpiride is studied because it offers an alternative treatment option for schizophrenia, particularly in cases where other antipsychotics have been ineffective or poorly tolerated. Research is ongoing to investigate the long-term effects of sulpiride and its potential role in the management of other psychiatric conditions, such as depression and anxiety.'

Sulpiride: A dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid. (From Merck Index, 11th ed) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

sulpiride : A member of the class of benzamides obtained from formal condensation between the carboxy group of 2-methoxy-5-sulfamoylbenzoic acid and the primary amino group of (1-ethylpyrrolidin-2-yl)methylamine. [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]

Cross-References

ID SourceID
PubMed CID5355
CHEMBL ID26
CHEBI ID32168
SCHEMBL ID8421
MeSH IDM0020813

Synonyms (223)

Synonym
AC-12181
neogama
levosulpirida [inn-spanish]
einecs 239-753-7
ccris 4248
enimon
sulpiride [usan:inn:ban:jan]
mariastel
normum
fidelan
eglonil
r.d. 1403
restful
kylistro
suprium
eusulpid
zemorcon
equilid
alimoral
desmenat
nufarol
psicocen
darleton
sursumid
fardalan
levosulpiridum [inn-latin]
valirem
rd 1403
pyrkappl
ozoderpin
omiryl
meresa
dresent
calmoflorine
norestran
dobren
lisopiride
dogmatyl
o-anisamide, n-((1-ethyl-2-pyrrolidinyl)methyl)-5-sulfamoyl-
benzamide, 5-(aminosulfonyl)-n-((1-ethyl-2-pyrrolidinyl)methyl)-2-methoxy-
sulpiridum [inn-latin]
eglonyl
isnamide
brn 0494008
dolmatil
sulperide
dogmatil
stamonevrol
coolspan
sulpirida [inn-spanish]
sernevin
championyl
HMS3266P12
HMS3393A08
BRD-A55272860-001-04-7
BRD-A55272860-001-03-9
KBIO1_000278
DIVK1C_000278
MLS000069434
smr000038923
(rs)-(+/-)-sulpiride
c15h23n3o4s
EU-0101050
(+)-n-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-sulfamoyl-benzamide
(+/-)-sulpiride
PRESTWICK3_000056
BIOMOL-NT_000037
PRESTWICK_431
cas-15676-16-1
LOPAC0_001050
BPBIO1_000463
OPREA1_602476
BPBIO1_000233
BPBIO1_001255
PRESTWICK2_000056
benzamide, 5-(aminosulfonyl)-n-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxy-
sulpirid
mirbanil
5-(aminosufonyl)-n-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxybenzamide
n-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-sulfamoyl-benzamide
abilit
sulpyrid
miradol
r. d. 1403
sulpiride
guastil
omperan
15676-16-1
splotin
aiglonyl
misulvan
EU-0001755
STK368596
5-(aminosulfonyl)-n-((1-ethyl-2-pyrrolidinyl)methyl)-2-methoxybenzamide
n-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-sulfamoylbenzamide
DB00391
sulpiride,(-)
sulpiride, slp
chembl26 ,
n-((1-ethyl-2-pyrrolidinyl)methyl)-5-sulfamoyl-o-anisamide
sulpiride,(+)
n-((1-ethyl-2-pyrrolidinyl)methyl)-2-methoxy-5-sulfamoylbenzamide
bdbm11638
D01226
sulpiride (jp17/usan/inn)
dogmatyl (tn)
NCGC00024852-05
NCGC00024852-04
PRESTWICK0_000056
SPBIO_002132
PRESTWICK1_000056
NINDS_000278
BIOMOL-NT_000162
BSPBIO_000211
IDI1_000278
MLS001306443
NCGC00024852-03
NCGC00024852-02
(?)-sulpiride
sulpitil
synedil
sulpor
NCGC00015966-04
( inverted question mark)-5-(aminosulfonyl)-n-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxybenzamide
S 8010 ,
( inverted question mark)-sulpiride
NCGC00015966-08
L000579
rd-1403
chebi:32168 ,
nsc-757850
n05al01
HMS500N20
FT-0652244
HMS1568K13
A809768
(2r)-1-ethyl-2-((2-methoxy-5-sulfamoylbenzamido)methyl)pyrrolidin-1-ium
AKOS004912732
HMS2095K13
HMS3263A22
7mne9m8287 ,
magnetic resonance imaging sulpiride
unii-7mne9m8287
sulpirida
5-22-08-00105 (beilstein handbook reference)
nsc 757850
sulpiridum
dtxsid1042574 ,
tox21_302205
NCGC00255813-01
dtxcid9022574
pyrikappl
CCG-205127
HMS2231K07
S4655
NCGC00015966-03
NCGC00015966-06
NCGC00015966-05
NCGC00015966-07
FT-0630504
(+-)-sulpiride
LP01050
(plusmn)-sulpiride
HMS3371P16
dl-sulpiride
HMS3372O01
gtpl5501
SCHEMBL8421
sulpiride [usan]
sulpiride [ep impurity]
sulpiride [inn]
sulpiride [mart.]
sulpiride [who-dd]
sulpiride [ep monograph]
95204-38-9
n-(1-ethyl-2-pyrrolidinylmethyl)-2-methoxy-5-sulfamidobenzamide
sulpiride [mi]
sulpiride [jan]
n-(1-ethyl-pyrrolidin-2-ylmethyl)-2-methoxy-5-sulfamoyl-benzamide
1-ethyl-2-(2-methoxy-5-sulfamoylbenzamidomethyl)pyrrolidine
NCGC00261735-01
tox21_501050
(y)-sulpiride
CS-4534
(.+/-.)-sulpiride
sulpiride, british pharmacopoeia (bp) reference standard
(rs)-(+/-)-5-aminosulfonyl-n-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxybenzamide
HY-B1019
mfcd00055061
sr-01000075402
SR-01000075402-2
HMS3651G12
sulpiride, european pharmacopoeia (ep) reference standard
sulpiride 1.0 mg/ml in methanol
SR-01000075402-6
SR-01000075402-3
HMS3712K13
Z84655412
benzamide,5-(aminosulfonyl)-n-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxy-
FT-0674703
BCP04500
(rs)-(+/-)-5-aminosulfonyl-n-[(1-ethyl -2-pyrrolidinyl)methyl]-2-methoxybenzamide
Q422418
HB1835
n-((1-ethylpyrrolidin-2-yl)methyl)-2-methoxy-5-sulfamoylbenzamide
HMS3675D18
(+/-)-n-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-sulfamoylbenzamide
BCP13871
ccris-4248
HMS3411D18
BRD-A55272860-001-08-8
STR09321
SDCCGSBI-0051020.P002
HMS3885J14
NCGC00015966-16
EN300-2010446
ps30 - sulpiride
n-(1-ethylpyrrolidin-2-ylmethyl)-2-methoxy-5-sulfamoylbenzamide
sulpiride (ep impurity)
sulpirida (inn-spanish)
sulpiridum (inn-latin)
sulpiride (ep monograph)
sulpiride (mart.)

Research Excerpts

Overview

Levosulpiride is an off-label medicine used to treat PE, but no review on its efficacy exists. Sulpiride (SPR) is a selective antagonist of central dopamine receptors but has limited clinical use due to its poor pharmacokinetics.

ExcerptReferenceRelevance
"Levosulpiride is an off-label medicine used to treat PE, but no review on its efficacy exists."( Levosulpiride for Premature Ejaculation: A Systematic Review and Meta-Analysis.
Arshad, A; Hussain, NHN; Inam, M; Irfan, M; Ismail, SB,
)
1.17
"Aminosulpiride is a benzamide used to treat acute or chronic schizophrenia Some researchers believe that early improvement of depression symptoms in patients has a certain predictive effect on the recovery of symptoms after drug treatment for schizophrenia. "( Prediction of the significance in the improvement of depression symptoms of amisulpride in the treatment of schizophrenia: an 8-week case-control study.
Ni, Y; Pan, A; Wang, G; Zheng, L; Zhou, B, 2020
)
1.07
"Sulpiride (SUL), is a selective antidopaminergic drug that had extensive biological activities. "( Precisely Fabricated Sulpiride-Loaded Nanolipospheres with Ameliorated Oral Bioavailability and Antidepressant Activity.
Abdelmonsif, DA; Aly, RG; Elgindy, NA; Mohyeldin, SM; Ragab, D; Samy, WM, 2021
)
2.38
"Sulpiride is a typical antipsychotic drug for the treatment of schizophrenia, depression and other psychological disorders. "( Multiple drug transporters mediate the placental transport of sulpiride.
Bai, M; Jiang, H; Jiang, T; Ma, Z; Sun, D; Weng, Y; Yang, X; Zheng, C, 2017
)
2.14
"Sulpiride is an old antipsychotic still frequently used in many developing countries."( The antipsychotics sulpiride induces fatty liver in rats via phosphorylation of insulin receptor substrate-1 at Serine 307-mediated adipose tissue insulin resistance.
Huang, X; Li, Y; Ren, L; Wang, C; Yu, Z; Zhou, X, 2018
)
1.53
"Sulpiride (SPR) is a selective antagonist of central dopamine receptors but has limited clinical use due to its poor pharmacokinetics. "( Synthesis, Characterisation and In Vitro Permeation, Dissolution and Cytotoxic Evaluation of Ruthenium(II)-Liganded Sulpiride and Amino Alcohol.
Choonara, YE; du Toit, LC; Kumar, P; M'bitsi-Ibouily, GC; Marimuthu, T; Modi, G; Pillay, V; Pradeep, P, 2019
)
2.17
"Levosulpiride is a newer prokinetic agent with increasingly extensive use in India by general physicians. "( Levosulpiride-Induced Dystonia: 7 Cases.
Goyal, V; Radhakrishnan, DM, 2018
)
1.6
"Sulpiride is a relatively old antipsychotic drug reputed to have a low incidence of adverse effects and an effect on the negative symptoms of schizophrenia. "( Sulpiride versus placebo for schizophrenia.
Sampson, S; Wang, J, 2014
)
3.29
"Sulpiride is an antipsychotic used in the treatment of several psychiatric disorders."( Binding of Sulpiride to Seric Albumins.
Cortez, CM; da Silva Fragoso, VM; de Morais Coura, CP; Hoppe, LY; Silva, D; Soares, MA, 2016
)
1.55
"Levosulpiride is a 5HT4 agonist/D2 antagonist prokinetic agent used to improve gastric emptying in patients with functional dyspepsia or gastroparesis. "( The effect of levosulpiride on in vitro motor patterns in the human gastric fundus, antrum, and jejunum.
Arenas, C; Clavé, P; Gallego, D; López, I; Mans, E; Ortega, O, 2016
)
1.33
"Levosulpiride (LSP) is a hydrophobic benzamide derivative used in the treatment of schizophrenia. "( Formulation, characterization, in vitro and in vivo evaluation of castor oil based self-nano emulsifying levosulpiride delivery systems.
Poorani, G; Uppuluri, KB; Uppuluri, S, 2016
)
1.2
"Sulpiride is a relatively old antipsychotic drug reputed to have low incidence of adverse effects and an effect on the negative symptoms of schizophrenia. "( Sulpiride versus placebo for schizophrenia.
Omori, IM; Wang, J, 2009
)
3.24
"Levosulpiride is a substituted benzamide that is widely used for the management of dyspepsia and emesis. "( Levosulpiride-induced movement disorders.
Chung, SJ; Kim, JS; Kim, MJ; Lee, MC; Shin, HW, 2009
)
1.47
"Sulpiride is a selective dopamine D2 antagonist."( Short-term sulpiride treatment of children and adolescents with Tourette syndrome or chronic tic disorder.
Chen, HJ; Chiu, NC; Ho, CS; Lue, HC; Shen, EY, 2009
)
1.46
"Sulpiride (SPR; L) is a substituted benzamide antipsychotic which is reported to be a selective antagonist of central dopamine receptors and claimed to have mood-elevating properties. "( Synthesis, spectroscopic and thermal characterization of sulpiride complexes of iron, manganese, copper, cobalt, nickel, and zinc salts. Antibacterial and antifungal activity.
Mohamed, GG; Soliman, MH, 2010
)
2.05
"Levosulpiride is a sulpiride isomer that exerts its prokinetic action through a dual mechanism: 1) as a D(2) dopamine receptor antagonist and 2) as a serotonin 5HT(4) receptor agonist, conferring this drug with a cholinergic effect. "( [Levosulpiride in the management of functional dyspepsia and delayed gastric emptying].
Serra, J, 2010
)
1.43
"Sulpiride is a benzamide neuroleptic used in the treatment of some psychiatric and gastroenterological disorders. "( [Toxicity of sulpiride].
Ciszowski, K; Szpak, D; Wilimowska, J, 2010
)
2.17
"Levosulpiride is a benzamide derivate D(2) dopamine antagonist with prokinetic activity that can accelerate gastric emptying and reduce discomfort in response to gastric distention. "( Levosulpiride and cisapride in the treatment of dysmotility-like functional dyspepsia: a randomized, double-masked trial.
Balboa, A; Jiménez, I; Mearin, F; Patón, C; Pérez-Mota, A; Rodrigo, L; Sebastián, JJ, 2004
)
1.44
"Sulpiride is a neuroleptic drug which is believed to block especially the non-adenylate cyclase dopaminergic receptors which are supposed to be inhibitory axoaxonic receptors on glutamatergic corticostriatal terminals."( Cerebral glutamate, neuroleptic drugs and schizophrenia: increase of cerebrospinal fluid glutamate levels and decrease of striate body glutamate levels following sulpiride treatment in rats.
Claus, D; Kim, JS; Kornhuber, HH, 1983
)
1.18
"Sulpiride is a benzamide derivative used in medical practice since 1967. "( [A major medication for autism: sulpiride (author's transl)].
Weiss, C,
)
1.86
"Sulpiride was found to be a potent dopamine antagonist in the canine exocrine pancreas."( Dopamine receptor blocking activity of sulpiride in the canine exocrine pancreas.
Honda, F; Satoh, H; Satoh, Y, 1980
)
1.25
"Sulpiride is a nonsedative neuroleptic, pharmacologically related to metoclopramide, which has previously been shown to affect various gastric functions and to exert a beneficial effect in the treatment of duodenal ulcer. "( Stimulation of pancreatic secretion by sulpiride.
Daniele, C; Ferrini, L; Gullo, L; Labó, G; Muratori, R; Nesticó, V; Priori, P, 1980
)
1.97
"Levosulpiride is an orthopramide drug that stimulates gastrointestinal motility."( The effects of levosulpiride on gastric and gall-bladder emptying in functional dyspepsia.
Arienti, V; Biagi, F; Boriani, L; Corazza, GR; Gasbarrini, G; Maconi, G; Sorge, M; Sottili, S; Ugenti, F; Van Thiel, DH, 1994
)
1.1
"Sulpiride is a substituted benzamide with selective dopaminergic blocking activity. "( Sulpiride: an antipsychotic with selective dopaminergic antagonist properties.
Caley, CF; Weber, SS, 1995
)
3.18
"Sulpiride is a safe and effective pharmacotherapeutic treatment for the acute management of schizophrenia. "( Sulpiride: an antipsychotic with selective dopaminergic antagonist properties.
Caley, CF; Weber, SS, 1995
)
3.18
"Sulpiride is a substituted benzamide with a selective action on receptors of the dopamine D2-like family, and clinical and pharmacological data suggest that it could be considered to be an atypical antipsychotic. "( A risk-benefit assessment of sulpiride in the treatment of schizophrenia.
Bitetto, A; Bravin, S; Invernizzi, G; Mauri, MC; Rudelli, R, 1996
)
2.03
"Sulpiride is a substituted benzamide with selective dopaminergic blocking activity."( Gynecomastia with sulpiride.
Fujii, A; Kaneda, Y, 2002
)
1.37
"Sulpiride is a new and chemically different neuroleptic. "( An evaluation of a unique new antipsychotic agent, sulpiride: effects on serum prolactin and growth hormone levels.
Gallant, DM; Kessler, C; Mielke, DH, 1977
)
1.95
"Sulpiride is an important tool for elucidating both the practical and heuristic aspects of subtypes of dopamine receptors and is a lead in the search for compounds that selectively affect dopaminergic mechanisms."( Sulpiride in tardive dyskinesia.
Casey, DE; Gerlach, J; Simmelsgaard, H, 1979
)
2.42
"Sulpiride, which is a regulator of autonomic nervous system function, was prescribed alone in such a case and pregnancy resulted on two occasions."( [A case of sterility treated with sulpiride (author's transl)].
Deydier-Feisthauer, C,
)
1.13
"Sulpiride is a new antipsychotic agent chemically different from recognized psychotropic compounds. "( Sulpiride: evaluation of antipsychotic activity in schizophrenic patients.
Gallant, DM; Kessler, C; Kessler, LR; Mielke, DH; Roniger, JJ, 1977
)
3.14
"Sulpiride is an antipsychotic which possesses the free sulfonamide radical. "( Studies on regional inhibition of carbonic anhydrase by sulpiride in rat brain.
Fukuda, S; Inui, M; Kaneko, Z; Konishi, H, 1979
)
1.95
"Sulpiride (Dogmatil) is a new type of drug acting on the hypothalamus resulting in a physiological increase in amplitude and frequency of gastric motor activity, reduction of signs of abnormal activity and pyloric spasm and an increase in the rate of gastric emptying. "( [Sulpiride in the management of gastroduodenal ulcers. A comparative double-blind study].
Molle, M, 1975
)
2.61
"Sulpiride is a selective D2-receptor antagonist with antipsychotic and antidepressant properties. "( Sulpiride-induced tardive dystonia.
Jankovic, J; Miller, LG, 1990
)
3.16
"L-Sulpiride is a dopamine (DA)-receptor blocker that acts as an antidepressant at low doses. "( Possible mechanism of antidepressant effect of L-sulpiride.
Collu, M; D'Aquila, PS; Forgione, A; Fratta, W; Gessa, GL; Serra, G, 1990
)
1.25
"Levo-sulpiride is a substituted benzamide with antiemetic activity 3-8 times more potent than the racemic form and the d-isomer. "( [Antiemetic properties of levo-sulpiride].
Guslandi, M, 1990
)
1.08
"L-sulpiride is an antagonist of dopamine on D2 receptors therefore inhibits the action of dopamine increasing the secretion of prolactin."( [Antiemetic effect of the levo isomer of sulpiride (L-sulpiride) in humans].
Florio, T; Forgione, A; Lombardi, G; Mastronardi, P; Mazzarella, B; Merola, B; Pinto, M; Savastano, S; Scanni, E; Schettini, G, 1989
)
1.1
"Sulpiride is a substituted benzamide which blocks selectively D-2 receptors. "( [Sulpiride in psychiatric practice].
Faltus, F; Jirák, R; Pavlovský, P, 1989
)
2.63
"Sulpiride is a potent dopamine receptor antagonist; however, it had no effect on the stomach and was ineffective in suppressing cisplatin-induced emesis."( Antagonism of cisplatin-induced emesis by metoclopramide and dazopride through enhancement of gastric motility.
Alphin, RS; Dannenburg, WN; Johnson, DN; Kinnier, WJ; Leonard, CA; Proakis, AG; Sancilio, LF; Smith, WL; Ward, JW, 1986
)
0.99

Effects

Sulpiride is a substituted benzamide antipsychotic drug playing a prominent role in the treatment of schizophrenia. Sulpiride has been claimed to be an atypical neuroleptic that might not produce tardive dyskinesia.

ExcerptReferenceRelevance
"Sulpiride, which has selective dopaminergic blocking activity, is a substituted benzamide antipsychotic drug playing a prominent role in the treatment of schizophrenia, which more selective and primarily blocks dopamine D2 and D3 receptor."( In silico Analysis of Sulpiride, Synthesis, Characterization and In vitro Studies of its Nanoparticle for the Treatment of Schizophrenia.
Akyuz, S; Bicak, B; Budama-Kilinc, Y; Cakir-Koc, R; Kaya, Z; Kecel-Gunduz, S; Kokcu, Y; Ozel, AE; Zorlu, T, 2020
)
2.32
"Sulpiride has been claimed to be an atypical neuroleptic that might not produce tardive dyskinesia."( Effect of chronic sulpiride on striatal spiperone binding.
Bannet, J; Belmaker, RH; Ebstein, RP; Gillis, S, 1980
)
1.32
"Sulpiride has the same possible side effects than classic neuroleptics."( Tardive akathisia due to sulpiride.
Arce, A; Gorospe, A; López de Munain, A; Martí Massó, JF; Poza, JJ, 1994
)
1.31
"As sulpiride has both healing effects on the ulcer and an analgesic effect against pain it can be prescribed in association with antacid mixtures for the treatment of duodenal ulcers."( [Treatment of duodenal ulcers with antacid mixtures and sulpiride. A double-blind controlled study (author's transl)].
Lai, CL; Lam, KC; Lam, SK; Wong, WS; Yam, LY; Yeung, CK,
)
0.89
"L-sulpiride has been able to control this complication very effectively."( [Antiemetic effect of the levo isomer of sulpiride (L-sulpiride) in humans].
Florio, T; Forgione, A; Lombardi, G; Mastronardi, P; Mazzarella, B; Merola, B; Pinto, M; Savastano, S; Scanni, E; Schettini, G, 1989
)
1.1
"Sulpiride, which has been utilized as an antipeptic ulcer and antidepressant in Japan, is one of the dopamine antagonists, and is considered to have anti vomiting activity. "( [Clinical evaluation of sulpiride against nausea and vomiting during cancer chemotherapy compared with domperidone--envelope method].
Kawakami, K; Kawatsu, S; Komatsu, Y; Okamoto, K; Sakata, Y; Satoh, T; Suzuki, H; Takagi, S; Tanabe, K; Yoshida, Y, 1986
)
2.02

Actions

Sulpiride may cause extrapyramidal effects, autonomic effects, tardive dyskinesia, and the neuroleptic malignant syndrome. Sulpiride caused an increase in prolactin (643 U/ml) [confidence interval (CI) 549-737]. Amisulpirides enhanced pup licking, and only at the highest dose disrupted the active components of maternal behavior such as pup retrieval and nest building.

ExcerptReferenceRelevance
"Levosulpiride, caused an increase in the EFS-induced cholinergic contractions in the gastric antrum (+37 ± 15.18% at 100 μM, pEC50 = 4.46 ± 0.14; p < 0.05, n = 8) and jejunum (+45.4 ± 22.03% at 100 μM, pEC50 = 3.78 ± 6.81; p < 0.05, n = 5), but not in the gastric fundus. "( The effect of levosulpiride on in vitro motor patterns in the human gastric fundus, antrum, and jejunum.
Arenas, C; Clavé, P; Gallego, D; López, I; Mans, E; Ortega, O, 2016
)
1.33
"Sulpiride caused an increase in prolactin (643 U/ml) [confidence interval (CI) 549-737)."( No evidence of the usefulness of eye blinking as a marker for central dopaminergic activity.
Cohen, AF; de Kam, ML; de Waal, PP; van der Post, J; van Gerven, JM, 2004
)
1.04
"Amisulpiride at the lower doses (10 and 30 mg/kg) enhanced pup licking, and only at the highest dose disrupted the active components of maternal behavior such as pup retrieval and nest building. "( Effects of novel antipsychotics, amisulpiride and aripiprazole, on maternal behavior in rats.
Budin, R; Fleming, AS; Kapur, S; Li, M, 2005
)
1.22
"Sulpiride induces an increase in plasma prolactin and a simultaneous increase of aldosterone release in man. "( Increased aldosterone secretion induced by sulpiride.
Costa, G; de Pasquale, R; Frisina, N, 1980
)
1.97
"Sulpiride is known to produce severe cholestatic jaundice, which we believe is due to ductopenia."( Bile ductopenia following therapy with sulpiride.
Corica, F; Di Cesare, E; Longo, G; Raimondo, G; Rubino, F; Spinella, S; Villari, D, 1995
)
1.28
"Sulpiride may cause extrapyramidal effects, autonomic effects, tardive dyskinesia, and the neuroleptic malignant syndrome."( Sulpiride: an antipsychotic with selective dopaminergic antagonist properties.
Caley, CF; Weber, SS, 1995
)
2.46
"(-)-Sulpiride did not enhance DA synthesis in synaptosomes from the reserpine-treated rats.(ABSTRACT TRUNCATED AT 250 WORDS)"( Reduction of dopamine synthesis inhibition by dopamine autoreceptor activation in striatal synaptosomes with in vivo reserpine administration.
Lillgäls, MS; Tissari, AH, 1993
)
0.77
"Sulpiride augmented the increase in dopamine induced by 0.5 and 2 mg/kg amphetamine by decreasing the rate of dopamine concentration fall off in the extracellular space (P<0.05)."( Effect of dopamine D2/D3 receptor antagonist sulpiride on amphetamine-induced changes in striatal extracellular dopamine.
Gonzales, RA; Jaworski, JN; Randall, PK, 2001
)
1.29
"The sulpiride-mediated increase in [3H]DA release and the release induced by NT were additive."( Evidence that the stimulatory effect of neurotensin on dopamine release in rat nucleus accumbens slices is independent of dopamine D2-receptor activation.
Reyneke, L; Russell, VA; Taljaard, JJ, 1990
)
0.76
"(-)-Sulpiride did not produce any differential effects along the rostrocaudal axis."( A neurochemical heterogeneity of the rat striatum as measured by in vivo electrochemistry and microdialysis.
Pehek, EA; Yamamoto, BK, 1990
)
0.76
"The sulpiride group had lower metabolic rates than the controls and the schizophrenic patients later treated with chlorpromazine."( Effects of sulpiride and chlorpromazine on regional cerebral glucose metabolism in schizophrenic patients as determined by positron emission tomography.
Blomqvist, G; Greitz, T; Sjögren, I; Stone-Elander, S; Wiesel, FA; Wik, G, 1989
)
1.15
"The sulpiride-induced PRL increase was higher than that induced by TRH."( Prolactin dynamics in a patient with isolated ACTH deficiency accompanied by hyperprolactinemia.
Shibutani, Y, 1988
)
0.76

Treatment

Sulpiride treatment increased mean stereotypy scores and striatal Bmax values. It had no effect on locomotion or mesolimbic dopamine receptor density. Treatment of sulpiride intoxications is mainly symptomatic and consists of supportive care.

ExcerptReferenceRelevance
"Levosulpiride/Cimetidine treatment induced mild hyperprolactinaemia that was associated with NKC activation and Th1-type cytokine profile. "( Prolactin Induces IL-2 Associated TRAIL Expression on Natural Killer Cells from Chronic Hepatitis C Patients
Bernal, AR; Cordova, J; Garcia, AP; Hernández, J; Kershenobich, D; Luna, JS; Medel, MLH; Mummidi, S; Parra, A; Porras, LM; Reyes, GG, 2019
)
1.07
"Sulpiride treatment inhibited the incidence of uterine adenocarcinoma and precancerous lesions of atypical endometrial hyperplasia, whereas EGME had no effect on uterine carcinogenesis."( Effects of sulpiride and ethylene glycol monomethyl ether on endometrial carcinogenicity in Donryu rats.
Inoue, K; Sakamoto, Y; Takahashi, M; Taketa, Y; Taya, K; Watanabe, G; Yoshida, M, 2016
)
1.55
"Sulpiride pretreatment antagonised the effects of quinpirole."( Role of ventral pallidal D2 dopamine receptors in the consolidation of spatial memory.
Gálosi, R; Kállai, V; Karádi, Z; Kertes, E; Kovács, A; László, K; Lénárd, L; Ollmann, T; Péczely, L; Zagorácz, O, 2016
)
1.16
"Sulpiride (25 mg/kg) treatment however, once daily for 3 days with no water swimming stress, did not alter swim stress-induced antinociception (0.5, 1 and 3 min tests)."( Dopamine receptor mechanism(s) and antinociception and tolerance induced by swim stress in formalin test.
Fazli-Tabaei, S; Javid, G; Loghavi, S; Nouri, M; Yahyavi, SH; Zarrindast, MR; Zartab, H, 2006
)
1.06
"Sulpiride-treated patients with extrapyramidal side effects had significantly higher drug concentrations in serum."( Relationships between drug concentrations in serum and CSF, clinical effects and monoaminergic variables in schizophrenic patients treated with sulpiride or chlorpromazine.
Alfredsson, G; Bjerkenstedt, L; Edman, G; Härnryd, C; Oxenstierna, G; Sedvall, G; Wiesel, FA, 1984
)
1.19
"Sulpiride treatment induced (1) an increase in the serum Prl and a decrease in the serum LH, (2) an increase in the pituitary FSH and LH contents, (3) an increase in the MBH LRH concentration, and (4) an increase in the MBH dopamine (DA) turnover."( Effect of sulpiride-induced hyperprolactinaemia on catecholamine turnover and LRH concentration in the medial basal hypothalamus of rats.
Aono, T; Chatani, F; Koike, K; Kurachi, K; Tasaka, K, 1983
)
1.39
"Sulpiride treatment for 1 week caused an increase in Bmax for 3H-NPA binding, which returned to control levels at 2 and 4 weeks."( Differential alterations in striatal dopamine receptor sensitivity induced by repeated administration of clinically equivalent doses of haloperidol, sulpiride or clozapine in rats.
Hall, MD; Jenner, P; Kilpatrick, G; Marsden, CD; Rupniak, NM, 1984
)
1.19
"Sulpiride treatment induced significant (P less than 0.001) elevations of plasma PRL at 1 week [84.1 +/- 4.9 vs."( Sulpiride treatment during early human pregnancy: effect on the levels of prolactin, six steroids, and placental lactogen.
Kivinen, S; Rönnberg, L; Viinikka, L; Ylikorkala, O, 1980
)
2.43
"Levosulpiride treatment reduced the basal mean gall-bladder volume from 21.6 +/- 2.3 to 18.6 +/- 2.3 mL (P < 0.05). "( Effect of D2-dopamine receptor antagonist levosulpiride on diabetic cholecystoparesis: a double-blind crossover study.
Celle, G; Mansi, C; Mele, MR; Perilli, D; Savarino, V; Sciabà, L; Vigneri, S, 1995
)
1.11
"Sulpiride pretreatment dose-dependently reversed both the early inhibition and later activation of quinpirole-induced locomotion."( Sulpiride antagonizes the biphasic locomotor effects of quinpirole in weanling rats.
Frantz, KJ; Van Hartesveldt, C, 1995
)
2.46
"Sulpiride treatment reduced (P = .071) the LH response to GnRH on March 30; the FSH and prolactin responses to secretagogue were not altered (P > .25)."( Prolactin, gonadotropin, and hair shedding responses to daily sulpiride administration in geldings in winter.
DePew, CL; Thompson, DL, 1997
)
1.26
"Sulpiride-treated rats spent less time swimming near the trained platform location and more time in the periphery of the maze than controls, although their latency to reach the trained platform location was not significantly affected."( Involvement of the posteroventral caudate-putamen in memory consolidation in the Morris water maze.
McGaugh, JL; Setlow, B, 1999
)
1.02
"In sulpiride-pretreated rats, quinpirole induced intense head-down sniffing, grooming and object-directed oral activity."( Differential behavioural effect of quinpirole in neuroleptic-pretreated rats - role of alpha(1)-adrenoceptor.
Obuchowicz, E, 1999
)
0.82
"Sulpiride treatment appeared to antagonize partially the inhibitory effect of L-dopa on prolactin release."( Effect of sulpiride on serum growth hormone and prolactin concentrations following L-DOPA administration in man.
Kobayashi, I; Mori, M; Nemoto, T; Shimoyama, S; Uehara, T, 1977
)
1.38
"2) Sulpiride treatment (4,4 mg/kg ."( [Dopamine, catecholamine receptors, and neurohumoral regulation of renal function].
Agnoli, GC; Cacciari, M; Cariani, A; Garutti, C; Lenzi, P,
)
0.65
"When sulpiride treatment was terminated on the first day of diestrus after vaginal opening, the animals continued to show estrous cycles."( Hyperprolactinemia-induced precocious puberty in the female rat: ovarian site of action.
Advis, JP; Ojeda, SR, 1978
)
0.71
"Sulpiride treatment resulted in (P less than .05) a six- to eightfold increase in daily PRL secretion."( Plasma concentrations of cortisol, prolactin, luteinizing hormone, and follicle-stimulating hormone in stallions after physical exercise and injection of secretagogue before and after sulpiride treatment in winter.
Colborn, DR; Rahmanian, MS; Roth, TL; Thompson, DL, 1991
)
1.19
"Sulpiride treatment (1-32 mg/kg) had little effect on pilocarpine-induced penile erection while it attenuated dose-dependently the apomorphine- and amantadine-induced ones."( Septohippocampal cholinergic pathway and penile erections induced by dopaminergic and cholinergic stimulants.
Maeda, N; Matsuoka, N; Yamaguchi, I, 1990
)
1
"Sulpiride treatment increased mean stereotypy scores and striatal Bmax values, but had no effect on locomotion or mesolimbic dopamine receptor density."( Differences in the time course of dopaminergic supersensitivity following chronic administration of haloperidol, molindone, or sulpiride.
Csernansky, JG; Prosser, ES; Pruthi, R, 1989
)
1.2
"When sulpiride- or clozapine-treated guinea-pigs received cycloheximide (an inhibitor of peptide biosynthesis) there was a significant decrease of the inhibitory response, which indicates that neuroleptics produced an increase of the synthesis of opioid peptides in the ileum myenteric plexus."( Effects of chronic treatment with atypical neuroleptics on the biosynthesis and release of opioid peptides in guinea-pig ileum.
Brugger, AJ; Martínez, JA; Milanés, MV; Pérez, D; Vargas, ML, 1985
)
0.72
"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
)
0.73
"Treatment of sulpiride intoxications is mainly symptomatic and consists of supportive care."( Sulpiride intoxication: Case report of a rare intoxication.
Gawi, A; van Vliet, P; Westerman, EM; Wilms, EB; Zonneveld, S, 2021
)
2.42
"Treatment with sulpiride further probed the pharmacological basis of long-term behavioural changes."( The dopamine D2/D3 receptor agonist quinpirole increases checking-like behaviour in an operant observing response task with uncertain reinforcement: a novel possible model of OCD.
d'Angelo, LS; Day, JO; Dongelmans, ML; Eagle, DM; Mar, AC; Morein-Zamir, S; Noble, CA; Noschang, C; Robbins, TW; Theobald, DE; Urcelay, GP, 2014
)
0.74
"Treatment with sulpiride attenuated adaptive coding in both midbrain and ventral striatum, and was associated with a decrease in performance, whereas bromocriptine did not have a significant impact."( Dopamine Modulates Adaptive Prediction Error Coding in the Human Midbrain and Striatum.
Diederen, KM; Fletcher, PC; Schultz, W; Spencer, T; Vestergaard, MD; Ziauddeen, H, 2017
)
0.79
"Pretreatment of sulpiride (60 mg/kg) significantly reverted the acute stress-induced alterations, while A 68930 (0.25mg/kg) significantly restored the acute and chronic unpredictable stress-induced alterations."( Differential response of A 68930 and sulpiride in stress-induced gastric ulcers in rats.
Ahmad, A; Banu, N; Lohani, M; Mishra, V; Palit, G; Rasheed, N; Sharma, S; Singh, N; Singh, P, 2010
)
0.97
"Pre-treatment with sulpiride blocked these effects while this dopaminergic antagonist had no effect by its own."( Effects of apomorphine on rat behavior in the elevated plus-maze.
Brandão, ML; Garcia, AM; Martinez, R; Morato, S, 2005
)
0.65
"Pretreatment with sulpiride but not with yohimbine completely antagonized the inhibitory effect of pergolide."( Dopaminergic inhibition of cardiac sympathetic nerve function by pergolide.
Barrett, RJ; Lokhandwala, MF, 1982
)
0.59
"Treatment with sulpiride or chlorpromazine resulted in a significant reduction of psychotic morbidity as estimated by CPRS and global ratings."( Clinical evaluation of sulpiride in schizophrenic patients--a double-blind comparison with chlorpromazine.
Aberg-Wistedt, A; Bjerkenstedt, L; Björk, K; Gullberg, B; Härnryd, C; Oxenstierna, G; Sedvall, G; Wiesel, FA; Wik, G, 1984
)
0.92
"Pretreatment with sulpiride failed to modify the depressor action of bromocriptine on the pressor responses to vagal stimulation."( Influence of bromocriptine on the pressor responses to afferent nervous stimulation.
Gaillard-Plaza, G; Montastruc, JL; Montastruc, P,
)
0.45
"Treatment with sulpiride was associated with a significant rise in plasma prolactin level, but paradoxically these patients had significantly reduced extrapyramidal symptoms."( A clinical and pharmacodynamic evaluation of sulpiride.
Bailey, J; Bishop, M; Coppen, A; Rao, VA, 1981
)
0.86
"Treatment with sulpiride (10-320 mg/kg, p.o.) attenuated these psychological stress-induced gastric lesions in a dose-dependent manner, while it failed to suppress those induced by physical stress such as restraint water-immersion (WI) and indomethacin treatment (IND)."( Sulpiride specifically attenuates psychological stress-induced gastric lesions in rodents.
Kuratani, K; Maeda, N; Nomura, K; Yamaguchi, I, 1995
)
2.07
"Treatment with sulpiride alone also resulted in a suppressive effect during the post-implant period (P < 0.01)."( Effects of melatonin in the mediobasal hypothalamus on the secretion of gonadotrophins in sheep: role of dopaminergic pathways.
Lincoln, GA; Tortonese, DJ, 1995
)
0.63
"Treatment with sulpiride or paroxetine did not change the concentration of any of the neuropeptides measured."( Effect of sulpiride or paroxetine on cerebrospinal fluid neuropeptide concentrations in patients with chronic tension-type headache.
Bach, FW; Ekman, R; Langemark, M; Olesen, J; Rehfeld, JF; Schifter, S, 1994
)
1.03
"Pretreatment with sulpiride (32 mg/kg, p.o.) hardly affected the former two activities, but significantly reduced the anorectic activity in Zucker rats."( A screening concept based on a hypothesis led to the development of a putative cognitive enhancer that stimulates penile erection.
Arakawa, H; Maeda, N; Matsuoka, N; Ohkubo, Y; Yamaguchi, I; Yamazaki, M, 1994
)
0.61
"Pretreatment with sulpiride, a dopamine D2 receptor antagonist, blocked the induction of Fos protein in the prefrontal cortex and the core region of accumbens nucleus, but not in the medial striatum and the shell division of nucleus accumbens of rat brain."( Expression of fos protein in rat brain following administration of a nicotinic acetylcholine receptor agonist epibatidine.
Hashimoto, K; Minabe, Y; Nishimura, T; Tsunashima, K; Watanabe, K, 1998
)
0.62
"When treatment with sulpiride had been continued for more than 2 months, serum progesterone and estradiol levels fell to within the range seen in the follicular phase of the normal cycle and absence of ovulation was recognized by laparoscopy."( New hyperprolactinemia and anovulation model in common marmoset (Callithrix jacchus) and effect of cabergoline.
Inada, Y; Kojima, M; Komatsu, H; Miyata, H; Moro, M; Torii, R, 1999
)
0.62
"Treatment with sulpiride was associated with marked reductions in psychotic morbidity."( Effect of sulpiride on monoaminergic mechanisms in psychotic women.
Bjerkenstedt, L; Härnryd, C; Sedval, G, 1979
)
1
"Pretreatment with sulpiride (200 mg/kg) produced a parallel, 40-fold shift to the right of the dose-response curve for NPA."( Hypothermia in mice: D2 dopamine receptor mediation and absence of spare receptors.
Hizami, R; Kreuter, L; Meller, E, 1989
)
0.6
"pretreatment with sulpiride was more effective than i.c.v."( Central mechanisms for apomorphine-induced emesis in the dog.
Harding, RK; Hugenholtz, H; Kucharczyk, J; Lemoine, J, 1987
)
0.6

Toxicity

LD50 of sulpiride in administration into the stomach of male rats and mice is 7200 and 3400 mg/kg, for female rats and mouse - 6000 and 2300mg/kg. Haloperidol was more effective than levosulpiride injection for psychotic symptoms, aggression, and severity of agitation in acute psychosis.

ExcerptReferenceRelevance
" LD50 of sulpiride to 67% of controls."( [The relevance of anticholinesterase properties to toxicity and neuromuscular effects of sulpiride (author's transl)].
Dross, K, 1977
)
0.9
"Compared to traditional neuroleptics, most of the new antipsychotics are characterized by a low extrapyramidal side effect (EPS) liability and varying antipsychotic efficacy."( New antipsychotics: classification, efficacy, and adverse effects.
Gerlach, J, 1991
)
0.28
"Dopamine at 100 mumol L-1 was toxic when added to cultures 24 h after plating."( Toxicity of dopamine to mouse neuroblastoma x rat glioma hybrid (NG108) cells in vitro.
Wang, RG; Zhu, XZ, 1995
)
0.29
"Dopamine toxicity to NG108 cells was mainly attributed to the oxidation of dopamine and its toxic by-products, eg, H2O2."( Toxicity of dopamine to mouse neuroblastoma x rat glioma hybrid (NG108) cells in vitro.
Wang, RG; Zhu, XZ, 1995
)
0.29
" To prove whether weight gain is a relevant side effect of atypical neuroleptics, the charts of all patients admitted with DSM-III-R diagnoses of schizophrenia, schizoaffective disorder, or delusional disorder in the years 1991 to 1995 were evaluated."( Weight gain: side effect of atypical neuroleptics?
Müssigbrodt, HE; Wetterling, T, 1999
)
0.3
" Safety data collection was performed using open reporting, UKU scales or specific extrapyramidal side-effect scales; electrocardiogram recording and vital signs examination; laboratory data collection."( Safety of amisulpride (Solian): a review of 11 clinical studies.
Coulouvrat, C; Dondey-Nouvel, L, 1999
)
0.3
" A tendency towards a higher incidence of treatment-emergent adverse events with amitriptyline was observed (73% versus 64% amisulpride)."( Amisulpride in medium-term treatment of dysthymia: a six-month, double-blind safety study versus amitriptyline. AMILONG investigators.
Ravizza, L, 1999
)
0.3
" Safety was monitored by open adverse event reporting, the Simpson-Angus Scale, the Barnes Akathisia Scale and the Abnormal Involuntary Movement scale."( Safety profile of amisulpride in short- and long-term use.
Coulouvrat, C; Dondey-Nouvel, L; Rein, W, 2000
)
0.31
" Adverse events were mainly psychiatric in nature, and occurred with similar frequency in each group (amisulpride 254/370, 69%; haloperidol 82/118, 70%)."( Long-term safety and efficacy of amisulpride in subchronic or chronic schizophrenia. Amisulpride Study Group.
Colonna, L; Dondey-Nouvel, L; Rein, W; Saleem, P, 2000
)
0.31
" The tolerability evaluation was based on incidence of adverse events and routine laboratory tests."( Efficacy and safety of amisulpride 50 mg versus paroxetine 20 mg in major depression: a randomized, double-blind, parallel group study.
Cassano, GB; Jori, MC, 2002
)
0.31
" Adverse effects were acute dyskinesia (n=2) or parkinsonian syndrome, which occurred after several months or years of treatment (n=15)."( [Extrapyramidal adverse effects of veralipride (Agreal), a drug used to treat hot flushes: a propos of 17 cases].
Andréjak, M; Geslin, JM; Gras-Champel, V; Lemaire-Hurtel, AS; Masmoudi, K; Masson, H; Munier, A, 2005
)
0.33
"Although clinical trials of the antipsychotic amisulpride revealed no cardiac adverse effects, four patients with severe cardiac toxicity after overdose were reported to Australian poisons information centres in 2004-2005."( Amisulpride deliberate self-poisoning causing severe cardiac toxicity including QT prolongation and torsades de pointes.
Daly, F; Gosselin, S; Hackett, LP; Haider, T; Isbister, GK; John, S; Murray, L; O'Mullane, P, 2006
)
0.33
" Adverse effects include acute dyskinesia or Parkinsonism, which may occur after many months of treatment."( The safety of veralipride.
De Leo, V; Delia, A; Faldini, E; Morgante, G; Musacchio, MC; Petraglia, F, 2006
)
0.33
" Clinicians should select antidepressants considering their pharmacologic profiles and avoiding adverse effects."( [Review of pharmacological efficacies and side effects of antidepressants].
Ikenouchi-Sugita, A; Nakamura, J; Yoshimura, R, 2007
)
0.34
" Hitherto under-recognised toxic effects of novel chemotherapeutic agents can pose challenges for the forensic pathologist charged with performing medico-legal autopsies in cases of sudden unexpected death in young adults and particularly in those with schizophrenia."( Fatality due to amisulpride toxicity: a case report.
George, N; Gerostamoulos, D; Lynch, MJ; Woods, J, 2008
)
0.35
" Safety assessment involved adverse event reporting, physical examination, blood pressure, heart rate and ECG monitoring, and laboratory tests."( A pilot study of the safety and efficacy of amisulpride and risperidone in elderly psychotic patients.
Eich, FX; Möller, HJ; Riedel, M, 2009
)
0.35
" A total of 26 adverse events were experienced by 10 patients in the amisulpride group and five patients in the risperidone group."( A pilot study of the safety and efficacy of amisulpride and risperidone in elderly psychotic patients.
Eich, FX; Möller, HJ; Riedel, M, 2009
)
0.35
" However, increased implantation loss was observed at 10 mg/kg or more, which was considered to be caused by the adverse effect of sulpiride on oocyte development."( Collaborative work on evaluation of ovarian toxicity. 17) Two- or four-week repeated-dose studies and fertility study of sulpiride in female rats.
Adachi, T; Inoue, Y; Ishii, S; Mutai, M; Okada, M; Sugimoto, J; Ube, M; Uno, Y, 2009
)
0.77
"The main objective was to identify the occurrence of adverse events associated with amisulpride when combined with antidepressants (ADs)."( Safety of amisulpride in combination with antidepressants under common clinical practice conditions.
Ceskova, E; Priborska, Z; Suchopar, J, 2011
)
0.37
" A total of 4463 adverse events were recorded in 1624 (51%) of all treated patients."( Safety of amisulpride in combination with antidepressants under common clinical practice conditions.
Ceskova, E; Priborska, Z; Suchopar, J, 2011
)
0.37
"The advantages of AD combinations undoubtedly include administration of lower doses and a reduction of adverse events associated with higher doses of individual ADs."( Safety of amisulpride in combination with antidepressants under common clinical practice conditions.
Ceskova, E; Priborska, Z; Suchopar, J, 2011
)
0.37
"We have investigated the categorical prevalence of hyperprolactinemia and examined the relationship between prolactin levels and subjective endocrine-related adverse effects in schizophrenia patients treated with amisulpride during a 1-year period."( Relationship between prolactin levels and subjective endocrine-related adverse effects in patients with schizophrenia receiving long-term treatment with amisulpride.
Ahn, YM; Jung, DC; Kim, EY; Kim, SH; Kim, YS; Lee, NY, 2012
)
0.38
"A total of 111 patients with schizophrenia who were either started on or switched to amisulpride were assessed for prolactin levels and endocrine-related adverse effects using 6 items derived from the Liverpool University neuroleptic side-effect rating scale (LUNSERS) at baseline, 8 weeks, and 1 year."( Relationship between prolactin levels and subjective endocrine-related adverse effects in patients with schizophrenia receiving long-term treatment with amisulpride.
Ahn, YM; Jung, DC; Kim, EY; Kim, SH; Kim, YS; Lee, NY, 2012
)
0.38
" All adverse effects resolved within 24 hours."( Safety of the electroconvulsive therapy and amisulpride combination.
Gazdag, G; Iványi, Z; Takács, R; Ungvari, GS, 2013
)
0.39
" The amisulpiride-ECT combination appears to be a safe treatment option."( Safety of the electroconvulsive therapy and amisulpride combination.
Gazdag, G; Iványi, Z; Takács, R; Ungvari, GS, 2013
)
0.82
"As part of the FP7 ARITMO (Arrhythmogenic Potential of Drugs) project, we explored the publicly available US FDA Adverse Event Reporting System (FAERS) database to detect signals of torsadogenicity for antipsychotics (APs)."( Antipsychotics and torsadogenic risk: signals emerging from the US FDA Adverse Event Reporting System database.
Behr, ER; De Ponti, F; Koci, A; Moretti, U; Poluzzi, E; Raschi, E; Spina, E; Sturkenboom, M, 2013
)
0.39
" Both groups were similar in terms of the following: (a) clinical characteristics at baseline, (b) response rates, and (c) score changes in all psychopathology measures, quality of life, and all side-effect scales after 6 weeks of treatment."( Antipsychotic combination using low-dose antipsychotics is as efficacious and safe as, but cheaper, than optimal-dose monotherapy in the treatment of schizophrenia: a randomized, double-blind study.
Chen, CC; Huang, YH; Lane, HY; Lin, CH; Lin, SC; Wang, FC, 2013
)
0.39
" Incidence of adverse events in a Mexican population and drug compliance according to correct use were evaluated."( Safety of veralipride for the treatment of vasomotor symptoms of menopause.
Álvarez, IM; Arias, Mde J; Bonilla, MC; Campero, RA; Campos, ER; Escudero, RB; Flores, JB; González, CC; González, JH; Haro, SS; Marín, IH; Rodríguez, MA; Valencia, MH; Vargas, MA, 2014
)
0.4
"A total of 57 adverse events were registered during the 386-month treatment."( Safety of veralipride for the treatment of vasomotor symptoms of menopause.
Álvarez, IM; Arias, Mde J; Bonilla, MC; Campero, RA; Campos, ER; Escudero, RB; Flores, JB; González, CC; González, JH; Haro, SS; Marín, IH; Rodríguez, MA; Valencia, MH; Vargas, MA, 2014
)
0.4
" LD50 of sulpiride in administration into the stomach of male rats and mice is 7200 and 3400 mg/kg, for female rats and mice - 6000 and 2300 mg/kg."( [Toxicity assessment of sulpiride as the basis of its hygienic standardization].
Gorokhova, LG; Martynova, NA,
)
0.86
" Nine patients discontinued treatment because of adverse events."( The effectiveness and safety of amisulpride in Chinese patients with schizophrenia: An 8-week, prospective, open-label, multicenter, single-arm study.
Cao, C; Chen, Z; Deng, H; Dong, F; Gao, M; Hong, L; Li, X; Li, Y; Liang, Y; Liu, T; Lu, S; Su, L; Tang, J; Tang, M; Wang, C; Wang, X; Xie, S; Xin, L; Xu, X; Yang, F; Yu, J; Yu, X; Zhang, C; Zhang, Y; Zhu, C, 2016
)
0.43
"Haloperidol was more effective than levosulpiride injection for psychotic symptoms, aggression, and severity of agitation in acute psychosis, but extrapyramidal adverse effects were less frequent with levosulpiride as compared with those receiving haloperidol."( Efficacy and Safety of Levosulpiride Versus Haloperidol Injection in Patients With Acute Psychosis: A Randomized Double-Blind Study.
Bains, HS; Kumar, A; Lavania, S; Praharaj, SK; Sinha, V,
)
0.7
" These toxic effects were attenuated by CB1R knockout or CB1R antagonists."( Genetic or pharmacological depletion of cannabinoid CB1 receptor protects against dopaminergic neurotoxicity induced by methamphetamine in mice.
Dang, DK; Jang, CG; Jeong, JH; Kim, HC; Ledent, C; Mai, AT; Nabeshima, T; Nah, SY; Onaivi, ES; Shin, EJ; Yamamoto, T, 2017
)
0.46

Pharmacokinetics

Levosulpiride exhibited linear pharmacokinetic properties over the dose range of 25 to 100 mg by PO route and 25 to 75 mg by IM route. After iv administration, the mean +/- SD apparent elimination half-life of sulpiride was 6.7.

ExcerptReferenceRelevance
" For all drugs studied, the proposed techniques are specific, reliable and sensitive enough and can be used to perform pharmacokinetic studies in human or in animal after administration of doses in the therapeutic range."( [Quantitative determination of drugs by in situ spectrophotometry of chromatograms for pharmacokinetic studies. I. Sulpiride and other benzamides, vincamine, naftazone (author's transl)].
Bres, J; Bressolle, F; Brun, S; Rechencq, E, 1979
)
0.47
" The Cmax of the test preparation showed therapeutically relevant plasma concentrations of greater than 400 ng/ml, compared with about 300 ng/ml for the reference preparation."( The importance of pharmacokinetic data on sulpiride: results of a bioequivalence study of two sulpiride 200 mg preparations following oral administration.
Berner, G; Kieferndorf, U; Lenhard, G; Vögtle-Junkert, U; Wagener, HH, 1991
)
0.55
" The differences between the pharmacokinetic parameters of sulpiride for the 2 groups were statistically significant."( Pharmacokinetics of sulpiride after intravenous administration in patients with impaired renal function.
Brès, J; Bressolle, F; Mourad, G, 1989
)
0.84
"7) participated in a "repeated measure" design for comparing the bioavailability and pharmacokinetic behaviours of the brand-name drug of Dogmatyl and a generic sulpiride formulation."( [Comparative pharmacokinetics of two sulpiride formulations in healthy volunteers].
Chen, IJ; Ding, NC; Jang, HR; Tsay, YS; Yang, JM, 1989
)
0.75
"A pharmacokinetic study of veralipride (N-[(1-allyl-2-pyrroli dinyl)methyl]-5-sulfamoyl-o-veratramide) was performed in healthy volunteers during a chronic administration."( Pharmacokinetics of veralipride after chronic administration in humans.
Barre, J; Campistron, G; Houin, G; Jung, L; Koffell, JC; Plusquellec, Y; Rochas, MA; Staveris, S; Tillement, JP, 1988
)
0.27
"A dose-dependent pharmacokinetic study of veralipride (a new post-menopausal "hot flushes" regulator) was developed in humans after oral solution administration (100, 150, 200, and 250 mg)."( Primary dose-dependent pharmacokinetic study of veralipride.
Houin, G; Jamet, G; Jung, L; Koffel, JC; Schneider, M; Staveris, S; Tillement, JP, 1985
)
0.27
" The proposed techniques were selective, reliable and sensitive enough to be used for pharmacokinetic studies and drug monitoring."( [Determination of sulpiride and sultopride by high-performance liquid chromatography for pharmacokinetic studies].
Bres, J; Bressolle, F, 1985
)
0.6
" No significant differences between young/adult and elderly patients for the various pharmacokinetic parameters (t1/2, AUC, Cmax, Tmax, Vd and Cl), after acute and multiple dosing, were observed."( L-sulpiride in young and elderly negative schizophrenics: clinical and pharmacokinetic variables.
Altamura, CA; Coppola, MT; Leva, P; Mauri, MC, 1994
)
1.01
" For the pharmacokinetic studies of the racemic drug in man, a method of determination based on solid-phase extraction (SPE) from plasma and HPLC on a stereoselective column was developed."( Stereospecific determination of amisulpride, a new benzamide derivative, in human plasma and urine by automated solid-phase extraction and liquid chromatography on a chiral column. application to pharmacokinetics.
Ascalone, V; Malavasi, B; Ripamonti, M, 1996
)
0.29
" Two methods suitable for pharmacokinetic investigations are proposed for the determination of amisulpride in human plasma."( Determination of amisulpride, a new benzamide derivative, in human plasma and urine by liquid-liquid extraction or solid-phase extraction in combination with high-performance liquid chromatography and fluorescence detection. application to pharmacokinetic
Ascalone, V; Locatelli, M; Malavasi, B; Ripamonti, M, 1996
)
0.29
"A new procedure specific for the determination of the analytical form of the model weighting function of a complex multicomponent pharmacokinetic system with or without a shunt and time delays is described."( CXT-MAIN: a software package for determination of the analytical form of the pharmacokinetic system weighting function.
Dedík, L; Durisová, M, 1996
)
0.29
" The objectives of this study were to determine the safety and the pharmacokinetic profile of 50 mg of amisulpride administered orally as a single dose to elderly volunteers."( Safety and pharmacokinetics of a single oral dose of amisulpride in healthy elderly volunteers.
Ahtoy, P; Canal, M; Chaufour, S; Chretien, P; Deschamps, C; Hamon-Vilcot, B; Nasr, A; Piette, F; Rosenzweig, P; Zieleniuk, I, 1998
)
0.3
" The mean Cmax of the racemate amisulpride in elderly people was 64."( Safety and pharmacokinetics of a single oral dose of amisulpride in healthy elderly volunteers.
Ahtoy, P; Canal, M; Chaufour, S; Chretien, P; Deschamps, C; Hamon-Vilcot, B; Nasr, A; Piette, F; Rosenzweig, P; Zieleniuk, I, 1998
)
0.3
"A single oral dose of amisulpride was well tolerated and showed a similar pharmacokinetic profile in healthy elderly and young subjects."( Safety and pharmacokinetics of a single oral dose of amisulpride in healthy elderly volunteers.
Ahtoy, P; Canal, M; Chaufour, S; Chretien, P; Deschamps, C; Hamon-Vilcot, B; Nasr, A; Piette, F; Rosenzweig, P; Zieleniuk, I, 1998
)
0.3
" Complete pharmacokinetic profiles were obtained on days 7 and 14 for lithium and trough plasma concentrations on days 10, 12 and 14 for amisulpride."( Lack of effect of amisulpride on the pharmacokinetics and safety of lithium.
Canal, M; Coulouvrat, C; Legangneux, E; van Lier, JJ; van Vliet, AA, 2003
)
0.32
" The pharmacokinetic parameters such as AUC(0-t) (the area under the curve from zero to the time), AUC(0-infinity) (the area under the curve from zero to infinity), Cmax (maximum serum concentration), tmax (time to reach Cmax) and t1/2 (terminal half-life) were analyzed by non-compartmental analysis, and the analysis of variance (ANOVA) was carried out using logarithmically transformed AUC(0-t), AUC(0-infinity) and Cmax, and untransformed Tmax."( Pharmacokinetics and bioequivalence evaluation of 2 levosulpiride preparations after a single oral dose in healthy male Korean volunteers.
Cho, HY; Lee, YB; Moon, JD, 2004
)
0.57
"The pharmacokinetics of antipsychotic drugs has become an integral part in understanding their pharmacodynamic activity and clinical effects."( Identification of P-glycoprotein substrates and inhibitors among psychoactive compounds--implications for pharmacokinetics of selected substrates.
El Ela, AA; Härtter, S; Hiemke, C; Langguth, P; Schmitt, U; Spahn-Langguth, H, 2004
)
0.32
" These results pointed to a pharmacokinetic drug interaction between CsA and amisulpride most likely caused by inhibition of P-gp."( Cyclosporine A (CsA) affects the pharmacodynamics and pharmacokinetics of the atypical antipsychotic amisulpride probably via inhibition of P-glycoprotein (P-gp).
Abou El-Ela, A; Baron, JM; Glavinas, H; Guo, LJ; Härtter, S; Hiemke, C; Krajcsi, P; Langguth, P; Schmitt, U; Tillmann, C, 2006
)
0.33
" This method offered good precision and accuracy and was successfully applied for the pharmacokinetic and bioequivalence study of a 25 mg of levosulpiride tablet in 24 healthy Korean volunteers."( Rapid quantification of levosulpiride in human plasma using RP-HPLC-MS/MS for pharmacokinetic and bioequivalence study.
Jhee, OH; Kang, JS; Kim, HJ; Lee, MH; Lee, YS; Park, JH; Park, YS; Rhim, SY; Shaw, LM, 2009
)
0.85
"The aim of this study was to describe the double-peak plasma pharmacokinetic profile of sulpiride after oral administration to healthy volunteers based on physiological and biopharmaceutical considerations."( Therapeutic drug monitoring and pharmacokinetic compartmental analysis of sulpiride double-peak absorption profile after oral administration to human volunteers.
Helmy, SA, 2013
)
0.84
"The developed analytical method was suitable for use in pharmacokinetic studies and therapeutic drug monitoring implementation."( Therapeutic drug monitoring and pharmacokinetic compartmental analysis of sulpiride double-peak absorption profile after oral administration to human volunteers.
Helmy, SA, 2013
)
0.62
"The aim of this study was to characterize the pharmacokinetic (PK) properties and assess the safety profiles of different formulations of levosulpiride in healthy Chinese volunteers."( Tolerability and Pharmacokinetic Comparison of Oral, Intramuscular, and Intravenous Administration of Levosulpiride After Single and Multiple Dosing in Healthy Chinese Volunteers.
Chen, H; He, X; Li, H; Li, W; Ni, Y; Sattar, H; Xu, M; Zhou, Y, 2015
)
0.83
"Levosulpiride exhibited linear pharmacokinetic properties over the dose range of 25 to 100 mg by PO route and 25 to 75 mg by IM route."( Tolerability and Pharmacokinetic Comparison of Oral, Intramuscular, and Intravenous Administration of Levosulpiride After Single and Multiple Dosing in Healthy Chinese Volunteers.
Chen, H; He, X; Li, H; Li, W; Ni, Y; Sattar, H; Xu, M; Zhou, Y, 2015
)
1.19
"Current prescribing guidelines for the antipsychotic amisulpride are based largely on pharmacokinetic (PK) studies in young adults, and there is a relative absence of data on older patients, who are at greatest risk of developing adverse events."( A population approach to characterise amisulpride pharmacokinetics in older people and Alzheimer's disease.
Bertrand, J; Brownings, S; D'Antonio, F; Greaves, S; Howard, R; McLachlan, E; Nair, A; Reeves, S; Smith, A; Taylor, D, 2016
)
0.43
" Several studies about LSP in humans are present in the literature, but neither pharmacodynamic nor pharmacokinetic data of LSP is present for veterinary species."( Pharmacokinetics of levosulpiride after single-dose administration in goats (Capra hircus) by different routes of administration.
Barsotti, G; Camillo, F; Giorgi, M; Lisowski, A; Panzani, D; Poapolathep, A; Rota, A; Łebkowska-Wieruszewska, B, 2019
)
0.82

Compound-Compound Interactions

ExcerptReferenceRelevance
"1 mg/kg) in combination with fluvoxamine also caused a selective increase in extracellular DA levels in the cortex."( Sulpiride in combination with fluvoxamine increases in vivo dopamine release selectively in rat prefrontal cortex.
Ago, Y; Baba, A; Matsuda, T; Nakamura, S, 2005
)
1.77
" These results further support the previous suggestion that the cortical dopamine system plays an important role in the effects of antipsychotic drugs administered in combination with fluvoxamine."( Lack of enhanced effect of antipsychotics combined with fluvoxamine on acetylcholine release in rat prefrontal cortex.
Ago, Y; Baba, A; Matsuda, T; Nakamura, S; Sato, M, 2006
)
0.33
" The need to provide effective therapeutic interventions to patients who do not have an optimal response to clozapine is the most common reason for simultaneously prescribing a second antipsychotic drug in combination with clozapine."( Clozapine combined with different antipsychotic drugs for treatment resistant schizophrenia.
Barbui, C; Boso, M; Cipriani, A, 2009
)
0.35
"The main objective was to identify the occurrence of adverse events associated with amisulpride when combined with antidepressants (ADs)."( Safety of amisulpride in combination with antidepressants under common clinical practice conditions.
Ceskova, E; Priborska, Z; Suchopar, J, 2011
)
0.37
"The aim of this study was to explore effects on anxiety-like behavior of the D2 dopamine receptor agonist, quinpirole and of the D2 dopamine receptor antagonist, sulpiride given alone or in combination with a low dose of 17β-estradiol (17β-E2) to ovariectomized (OVX) rats."( Anxiolytic-like effect of quinpirole in combination with a low dose of 17β-estradiol in ovariectomized rats.
Fedotova, J, 2013
)
0.59
" This drug combination resulted in marked prolongation of the QT interval that triggered the electrical storm."( Citalopram and levosulpiride: a dangerous drug combination for QT prolongation.
Agosti, S; Bertero, G; Brunelli, C; Burrone, A; Casalino, L; Morelloni, S, 2013
)
0.72
" For these people, a number of treatment strategies have emerged, including the prescription of a second anti-psychotic drug in combination with clozapine."( Clozapine combined with different antipsychotic drugs for treatment-resistant schizophrenia.
Barber, S; Cipriani, A; Corsi, M; Olotu, U, 2017
)
0.46

Bioavailability

The bioavailability of levosulpiride after oral administration was poor and the absorption rate was slower compared with IM administration. This imply delayed clinical efficacy for patients with dyspepsia or neuropsychiatric disorders.

ExcerptReferenceRelevance
" Bioavailability of the oral hydrochloride solution was 85% and that of the free base suspension was 75%."( Bioavailability of 14C-sulpiride in dogs.
Alam, AS; Hagerman, LM; Imondi, AR; Udinsky, J, 1979
)
0.57
" The marked species difference in the systemic bioavailability of oral sulpiride should be taken into account when the orthopramide drugs are evaluated in pharmacological tests."( Pharmacokinetics of sulpiride after oral and intravenous administration in the rat and the dog.
Bakke, OM; Borja, L; Segura, J, 1976
)
0.81
" The third study compared the bioavailability of a 200-mg capsule dose with a 200-mg im dose in eight subjects."( Absolute bioavailability, rate of absorption, and dose proportionality of sulpiride in humans.
Brès, J; Bressolle, F; Fauré-Jeantis, A, 1992
)
0.51
"The effect of food intake on the bioavailability of sulpiride from a commercial film-coated tablet (100 mg/T) treated with polyvinylacetal diethylaminoacetate (AEA), which remains undissolved at pH above 4 approximately 5, were investigated in four healthy male subjects in the normal state or in a drug-induced achlorhydric state."( Effects of food intake on the bioavailability of sulpiride from AEA film-coated tablet having a pH-dependent dissolution characteristic in normal or drug-induced achlorhydric subjects.
Hamaguchi, T; Kobayashi, M; Mizuno, N; Shinkuma, D; Yamanaka, Y, 1991
)
0.79
"This study examined the influences of food intake on sulpiride (100 mg) bioavailability from a commercial film-coated tablet and of the meal size (small, medium or large) on sulpiride bioavailability from an aqueous solution in three healthy male volunteers."( Effects of food intake and meal size on the bioavailability of sulpiride in two dosage forms.
Hamaguchi, T; Kobayashi, M; Mizuno, N; Shinkuma, D; Yamanaka, Y, 1990
)
0.77
"The bioavailability of sulpiride taken in film-coated tablet form with sodium bicarbonate or cimetidine or with natural orange juice or diluted hydrochloric acid was studied."( The bioavailability of sulpiride taken as a film-coated tablet with sodium bicarbonate, cimetidine, natural orange juice or hydrochloric acid.
Hamaguchi, T; Kobayashi, M; Mizuno, N; Shinkuma, D; Yamanaka, Y, 1989
)
0.9
"7) participated in a "repeated measure" design for comparing the bioavailability and pharmacokinetic behaviours of the brand-name drug of Dogmatyl and a generic sulpiride formulation."( [Comparative pharmacokinetics of two sulpiride formulations in healthy volunteers].
Chen, IJ; Ding, NC; Jang, HR; Tsay, YS; Yang, JM, 1989
)
0.75
" This variation for fluphenazine may be explained by the fact that its pKa value is closer to that of piracetam, thus preventing better bioavailability of the neuroleptic, or its better affinity for DA-1 dopaminergic receptors."( Piracetam interactions with neuroleptics in psychopharmacological tests.
Bourin, M; Larousse, C; Poisson, L, 1986
)
0.27
" The absolute bioavailability after oral administration was only about 15% which was also the level after intraduodenal administration."( Gastrointestinal absorption of sulpiride in rat.
Mizuno, N; Morita, E; Nishikata, M; Shinkuma, D; Yamanaka, Y, 1986
)
0.56
" The bioavailability determined from combined plasma and urine data was only 27 +/- 9%."( The pharmacokinetics of intravenous and oral sulpiride in healthy human subjects.
Alfredsson, G; Ehrnebo, M; Sedvall, G; Wiesel, FA, 1980
)
0.52
" No correlation was obtained between in vitro dissolution rate and overall bioavailability in dogs as measured by the amounts of unchanged sulpiride excreted in the urine."( Bioavailability of sulpiride tablet and capsule in dogs.
Alam, AS; Hagerman, LM; Imondi, AR, 1980
)
0.79
"To improve the limited oral bioavailability of sulpiride, a dosage form containing sodium oleate as an absorption enhancer was developed and evaluated using gastric-emptying-controlled rabbits in a cross-over manner."( Improving the oral bioavailability of sulpiride by sodium oleate in rabbits.
Iseki, K; Kohri, N; Miyazaki, K; Naasani, I, 1995
)
0.82
" The oral bioavailability of sulpiride is poor, with estimates approximating 35%."( Sulpiride: an antipsychotic with selective dopaminergic antagonist properties.
Caley, CF; Weber, SS, 1995
)
2.03
" The effect of the number of absorption sites on absorbed amounts, on area under the curves and bioavailability is taken into account."( Pharmacokinetic compartmental model with n sites of absorption along the gastrointestinal tract.
Houin, G; Plusquellec, Y, 1994
)
0.29
" The L-DOPA was shown to hinder the absorption rate of glucose, whereas sulpiridinum was shown to suppress the main enzymes excepting snerase and alkaline phosphatase, to increase the monomeric and hydrolysate glucose transport."( [The role of dopamine in the mechanism of the regulation of the digestive-transport functions of the enterocyte membrane during stress].
Guska, NI; Razlovan, TA; Sheptitskiĭ, VA, 1993
)
0.29
"To improve the limited oral bioavailability of sulpiride, a gastric-retained form was developed and evaluated using gastric-emptying-controlled rabbits."( Improving the oral bioavailability of sulpiride by a gastric-retained form in rabbits.
Iseki, K; Kohri, N; Miyazaki, K; Naasani, I, 1996
)
0.82
" Two examples from bioavailability studies in pharmacokinetics are given."( CXT-MAIN: a software package for determination of the analytical form of the pharmacokinetic system weighting function.
Dedík, L; Durisová, M, 1996
)
0.29
" The drug concentrations were obtained by convoluting the drug absorption rate quadratic function with the drug disposition model function."( DeMonS--a new deconvolution method for estimating drug absorbed at different time intervals and/or drug disposition model parameters using a monotonic cubic spline.
Gupta, SK; Hwang, SS; Yu, Z, 1997
)
0.3
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
" The new methodology may, therefore, be used for fast bioavailability screening of virtual libraries having millions of molecules."( Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties.
Ertl, P; Rohde, B; Selzer, P, 2000
)
0.31
" The synchronous matrices increased SP bioavailability after intra-intestinal administration."( Synchronized release of sulpiride and sodium decanoate from HPMC matrices: a rational approach to enhance sulpiride absorption in the rat intestine.
Assaf, P; Baluom, M; Friedman, M; Haj-Yehia, AI; Rubinstein, A, 2000
)
0.61
"SP bioavailability after intestinal administration can be improved only if SP is released together with SD along the entire intestinal route."( Synchronized release of sulpiride and sodium decanoate from HPMC matrices: a rational approach to enhance sulpiride absorption in the rat intestine.
Assaf, P; Baluom, M; Friedman, M; Haj-Yehia, AI; Rubinstein, A, 2000
)
0.61
"The goals of this study were to examine whether formulations, capable of releasing sulpiride (SP) in synchrony with the p-Glycoprotein (P-gp) inhibitors, verapamil (Ver) or quinidine (Qn) can increase SP relative bioavailability and to suggest a rationale approach for oral administration of SP."( Improved intestinal absorption of sulpiride in rats with synchronized oral delivery systems.
Baluom, M; Friedman, M; Rubinstein, A, 2001
)
0.81
" The bioavailability of these drugs differ among different pharmaceutical preparations and even for the same preparation."( [Variance of bioavailability of pharmaceutical preparations and analysis of factors affecting it].
Hamaguchi, T; Mizuno, N; Shinkuma, D, 2003
)
0.32
" We found that RG-15 showed a good oral bioavailability (54%) and high brain levels (approx."( Subnanomolar dopamine D3 receptor antagonism coupled to moderate D2 affinity results in favourable antipsychotic-like activity in rodent models: II. behavioural characterisation of RG-15.
Agai Csongor, E; Domány, G; Elekes, O; Gémesi, LI; Gyertyán, I; Kapás, M; Kedves, R; Kiss, B; Laszy, J; Pásztor, G; Sághy, K; Szombathelyi, Z; Zájer-Balázs, M, 2008
)
0.35
"An improved HPLC method was developed and validated for the determination of concentration of amisulpride (CAS 71675-85-9) in human plasma, an attempt to compare the bioavailability of two amisulpride tablet formulations (reference and test) containing 200 mg of amisulpride."( Comparative bioavailability study of amisulpride tablets in healthy Indian volunteers.
Bhaumik, U; Bose, A; Chakrabarty, US; Chatterjee, B; Das, A; Ghosh, A; Pal, TK; Sarkar, AK, 2009
)
0.35
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
" The oral bioavailability of sulpiride is poor and it does not appear to have an extensive first-pass metabolism, nor is it extensively protein-bound."( [Toxicity of sulpiride].
Ciszowski, K; Szpak, D; Wilimowska, J, 2010
)
1.02
" They point out that the absorption rate is similar and the elimination is prorogated in sulpiride acute poisoning compared to therapeutic doses."( [Sulpiride poisoning--case report confirmed with the quantitative determination of the xenobiotic serum level].
Ciszowski, K; Groszek, B; Szpak, D; Wilimowska, J, 2011
)
1.5
"Solid lipid nanoparticles (SLN), novel drug delivery carriers, can be utilized in enhancing both intestinal permeability and dissolution of poorly absorbed drugs."( Novel sulpiride-loaded solid lipid nanoparticles with enhanced intestinal permeability.
AlOmrani, AH; Ibrahim, WM; Yassin, AE, 2014
)
0.88
" The goal was to formulate a product that is easy to use, stable, and highly bioavailable and to achieve a rapid clinical efficacy."( Pediatric suppositories of sulpiride solid dispersion for treatment of Tourette syndrome: in vitro and in vivo investigations.
Emam, SE; Ghazy, FE; Shehata, TM; Zidan, AS, 2015
)
0.71
" The bioavailability of levosulpiride via IM and PO routes was 96."( Tolerability and Pharmacokinetic Comparison of Oral, Intramuscular, and Intravenous Administration of Levosulpiride After Single and Multiple Dosing in Healthy Chinese Volunteers.
Chen, H; He, X; Li, H; Li, W; Ni, Y; Sattar, H; Xu, M; Zhou, Y, 2015
)
0.92
" The bioavailability of levosulpiride after oral administration was poor and the absorption rate was slower compared with IM administration, which imply delayed clinical efficacy for patients with dyspepsia or neuropsychiatric disorders."( Tolerability and Pharmacokinetic Comparison of Oral, Intramuscular, and Intravenous Administration of Levosulpiride After Single and Multiple Dosing in Healthy Chinese Volunteers.
Chen, H; He, X; Li, H; Li, W; Ni, Y; Sattar, H; Xu, M; Zhou, Y, 2015
)
0.92
"The aim of this study was to assess the effect of d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) on the physicochemical characterization and oral bioavailability of a novel l-sulpiride-loaded quaternary microcapsule (QMC)."( Development of a novel l-sulpiride-loaded quaternary microcapsule: Effect of TPGS as an absorption enhancer on physicochemical characterization and oral bioavailability.
Choi, HG; Choi, JS; Jin, SG; Kim, DS; Kim, DW; Kim, JO; Kim, KS; Oh, KT; Seo, YG; Yong, CS; Youn, YS, 2016
)
0.93
" Microscopy, FTIR and in vivo bioavailability studies were conducted for optimum formulation."( Formulation, characterization, in vitro and in vivo evaluation of castor oil based self-nano emulsifying levosulpiride delivery systems.
Poorani, G; Uppuluri, KB; Uppuluri, S, 2016
)
0.65
" Hence, liquid suppository system could be used for enhanced bioavailability of levosulpiride-loaded pharmaceutical products."( Development and characterisation of levosulpiride-loaded suppositories with improved bioavailability in vivo.
Khan, GM, 2019
)
1.01
" The IM mean bioavailability was 66."( Pharmacokinetics of levosulpiride after single-dose administration in goats (Capra hircus) by different routes of administration.
Barsotti, G; Camillo, F; Giorgi, M; Lisowski, A; Panzani, D; Poapolathep, A; Rota, A; Łebkowska-Wieruszewska, B, 2019
)
0.82
"To provide more efficient use of Sulpiride having a low bioavailability of the gastrointestinal tract, the nanoparticle formulation with high solubility and bioavailability was designed and synthesized for the first time in this study for the treatment of schizophrenia."( In silico Analysis of Sulpiride, Synthesis, Characterization and In vitro Studies of its Nanoparticle for the Treatment of Schizophrenia.
Akyuz, S; Bicak, B; Budama-Kilinc, Y; Cakir-Koc, R; Kaya, Z; Kecel-Gunduz, S; Kokcu, Y; Ozel, AE; Zorlu, T, 2020
)
1.15
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" However, its sparingly aqueous solubility and limited gastrointestinal permeability lead to scanty oral bioavailability which hinders its clinical efficacy."( Precisely Fabricated Sulpiride-Loaded Nanolipospheres with Ameliorated Oral Bioavailability and Antidepressant Activity.
Abdelmonsif, DA; Aly, RG; Elgindy, NA; Mohyeldin, SM; Ragab, D; Samy, WM, 2021
)
0.94
"4-fold improvement in SUL oral bioavailability together with long-circulating properties, relative to the free drug."( Precisely Fabricated Sulpiride-Loaded Nanolipospheres with Ameliorated Oral Bioavailability and Antidepressant Activity.
Abdelmonsif, DA; Aly, RG; Elgindy, NA; Mohyeldin, SM; Ragab, D; Samy, WM, 2021
)
0.94
" However, being a P-glycoprotein efflux substrate with a limited oral bioavailability imposes a challenge to its clinical efficacy."( Hybrid lipid core chitosan-TPGS shell nanocomposites as a promising integrated nanoplatform for enhanced oral delivery of sulpiride in depressive disorder therapy.
Abdelmonsif, DA; Aly, RG; Elgindy, NA; Mohyeldin, SM; Ragab, D; Samy, WM, 2021
)
0.83

Dosage Studied

A single oral dose of 50 mg sulpiride raised serum PRL levels for 12 h, with a peak level at 2 h after dosing in 7 women on the second postpartum day. 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.

ExcerptRelevanceReference
" Sultopride at low dosage also seems to have favourable effects on the agitation of the demented states and in the case of late delirante psychose."( [Sultopride: a new powerful neuroleptic (author's transl)].
Anglade, P; Baraer, J,
)
0.13
" The dosage was 3 injectable ampoules daily during the whole period of intensive care treatment."( [Prevention of stress ulcers with sulpiride (author's transl)].
Heinkelein, J,
)
0.41
" A single oral dose of 50 mg sulpiride raised serum PRL levels for 12 h, with a peak level at 2 h after dosing in 7 women on the second postpartum day."( Augmentation of puerperal lactation by oral administration of sulpiride.
Aki, T; Aono, T; Hirota, K; Kurachi, K; Nomura, A; Shioji, T, 1979
)
0.79
" The daily dosage varied from 300 to 1,200 mg Sulpiride orally and 12 to 48 mg Perphenazine."( [Study of the clinical effects of sulpiride and perphenazine in 82 schizophrenic patients by the double blind method].
Asada, S; Ishimaru, T; Kodama, H; Kubo, S; Masuda, K, 1976
)
0.79
") following dosing with Dogmatil fort tablet and 12."( [In vivo bioequivalence study of Sulpirid (GYKI-Alkaloida) and Dogmatil fort (Delagrange) 200 mg sulpiride tablets in healthy volunteers].
Mészáros, S; Past, T; Singer, J; Tomori, L; Vereczkey, L,
)
0.35
" The dose-response relation for LY171555 was bell-shaped, with a maximal effect being obtained with 10(-9) M) LY171555."( Opposing effects of dopamine D2 receptor stimulation on the spontaneous and the electrically evoked release of [3H]GABA on rat prefrontal cortex slices.
Besson, MJ; Penit-Soria, J; Rétaux, S, 1991
)
0.28
" In an intravenous cumulative dose-response study of TA-870, the plasma-free-dopamine concentration was elevated depending on the dose of TA-870."( A novel orally active dopamine prodrug TA-870. III. Positive inotropic effect and cardiorenal selectivity in anesthetized dogs.
Akimoto, Y; Nakajima, H; Nishiyama, S; Yamaguchi, I; Yoshikawa, M, 1990
)
0.28
" Pretreatment with 6-OH-dopamine resulted in a shift of the dose-response curve for apomorphine to the left, suggesting supersensitivity of D2 receptors."( Cooperation between D1- and D2-dopamine receptors in the nucleus accumbens.
Szmigielski, A; Zalewska-Kaszubska, J, 1991
)
0.28
" 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
" In patients with negative schizophrenia (4 open and 3 double-blind studies) the effective dosage of amisulpride (Solian 50) is about 150 mg/day, doses above 300 mg being ineffective or aggravating."( [Amisulpride, neuroleptic and antinegative action].
Allilaire, JF; Guérard des Lauriers, A; Lecrubier, Y; Widlöcher, D,
)
0.13
" 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
"01-1 mg/kg) increased the number of penile erections with bell-shaped dose-response curves."( Septohippocampal cholinergic pathway and penile erections induced by dopaminergic and cholinergic stimulants.
Maeda, N; Matsuoka, N; Yamaguchi, I, 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
" The cumulative urinary excretions of sulpiride for 48 h (Du48) from two dosage forms following oral administration were decreased approximately 30% by food intake."( Effects of food intake and meal size on the bioavailability of sulpiride in two dosage forms.
Hamaguchi, T; Kobayashi, M; Mizuno, N; Shinkuma, D; Yamanaka, Y, 1990
)
0.79
" 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
)
0.69
" SCH23390 (3-30 nmol), a selective D-1 DA receptor antagonist, caused a progressive parallel shift to the right in the dose-response curve for DA-induced pancreatic secretion without changes in the maximal response."( Do D-1 dopamine receptors mediate dopamine-induced pancreatic exocrine secretion in anesthetized dogs?
Chiba, S; Horiuchi, A; Iwatsuki, K; Yonekura, H, 1989
)
0.28
" There was no dose-response effect of sulpiride on serum levels of the monoamine metabolites or the amino acids."( Monoamine metabolites and amino acids in serum from schizophrenic patients before and during sulpiride treatment.
Alfredsson, G; Wiesel, FA, 1989
)
0.77
" 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
" The two high bioavailability subjects took one tablet (100 mg) with 100 ml of water (1) alone, (2) together with 1 g of sodium bicarbonate or (3) during concurrent dosing with cimetidine, 200 mg three times a day."( The bioavailability of sulpiride taken as a film-coated tablet with sodium bicarbonate, cimetidine, natural orange juice or hydrochloric acid.
Hamaguchi, T; Kobayashi, M; Mizuno, N; Shinkuma, D; Yamanaka, Y, 1989
)
0.59
" Pretreatment with sulpiride (200 mg/kg) produced a parallel, 40-fold shift to the right of the dose-response curve for NPA."( Hypothermia in mice: D2 dopamine receptor mediation and absence of spare receptors.
Hizami, R; Kreuter, L; Meller, E, 1989
)
0.61
"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
)
0.48
" These are characterized by the slope of the dose-response curve for the substances to antagonize the apomorphine-induced behavioral effects and by the effectiveness of DE gamma E in this respect."( Antipsychotic substances and dopamine in the rat brain; behavioral studies reveal distinct dopamine receptor systems.
Elands, J; Király, I; Van Ree, JM; Wolterink, G, 1989
)
0.28
" By comparing the dose-response curves of four drugs tested in the same fashion, haloperidol and sulpiride were superior to propericiazine and timiperone because they displayed a wider dose range for the maintenance treatment of remitted schizophrenic outpatients."( Prophylactic effects of neuroleptics in symptom-free schizophrenics: a comparative dose-response study of timiperone and sulpiride.
Koga, I; Nishikawa, T; Tanaka, M; Tsuda, A; Uchida, Y, 1989
)
0.7
" Each subject received a single 400-mg dose of Dogmatyl in tablet form during the first dosing period."( [Comparative pharmacokinetics of two sulpiride formulations in healthy volunteers].
Chen, IJ; Ding, NC; Jang, HR; Tsay, YS; Yang, JM, 1989
)
0.55
" 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,
)
0.13
" Whether this bipolar activity is due to the play of different kinds of receptors according to the dosage used, or is due to the dopaminergic blockade in different brain areas related to the dosage remains a problem to be solved."( [Efficacy of low doses of atypical neuroleptics (benzamides) in defect states].
Boyer, P, 1986
)
0.27
" Its dose-response curve was shifted to the right at 23 degrees C/0."( B-HT 920 and B-HT 958: presynaptic effects on electrically evoked 3H-dopamine release from slices of rat nucleus accumbens.
Cichini, G; Placheta, P; Singer, EA, 1987
)
0.27
" 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
)
0.76
" The selective DA DA1 antagonist SCH 23390 behaved as a competitive antagonist, shifting the dose-response curve to the right."( Presence of dopamine-dependent adenylate cyclase activity in human renal cortex.
Amenta, F; Baldi, E; Mannelli, M; Pupilli, C, 1988
)
0.27
" caused significant falls in blood pressure and heart rate which were maximal 5 min after dosing (-29."( B-HT 958 lowers blood pressure and heart rate in the rat through stimulation of dopamine receptors.
Brown, MJ; Harland, D, 1986
)
0.27
" The drug was injected intramuscularly in a single administration at a dosage of 600 mg."( Effect of sulpiride on chronic abstinence syndrome in addicted patients.
Drago, F; Marano, P; Nicoletti, F; Patti, F; Scapagnini, U, 1986
)
0.67
" Pretreatment of the rats with reserpine (5 mg/kg) did not produce any modification of the dose-response curve to dopamine."( Relaxant effect of dopamine on the isolated rat uterus.
Estañ, L; Martinez-Mir, I; Morales-Olivas, FJ; Rubio, E, 1988
)
0.27
") and shifted to the right the dose-response curve for agonist-induced hypothermia."( SCH 23390 antagonizes apomorphine- and ergot-induced hypothermia.
Carboni, E; Deidda, S; Di Chiara, G; Longoni, R, 1986
)
0.27
"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
)
0.69
" 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
)
0.6
" A dose-response effect was shown between 40 and 80 mg in control subjects (n = 7); in 4 hyperprolactinemics the higher dose also failed to increase PRL levels."( Effect of fenfluramine oral administration on serum prolactin levels in healthy and hyperprolactinemic women.
Adelasco, P; Brambilla, G; Cavioni, V; Ferrari, C; Mattei, AM; Scarduelli, C; Zavaglia, C, 1985
)
0.27
" 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
" The dose-response curve to dopamine was shifted to the right by both sulpiride and verapamil, indicative of competitive inhibition."( Dopamine antagonist effect of verapamil on isolated perfused rabbit ear artery.
Johnson, CE; Scriabine, A; Steinsland, OS, 1983
)
0.5
" Seven DA agonists produced U-shaped dose-response curves indicative of activity at both the autoreceptor and postsynaptic DA receptor."( Mouse locomotor activity: an in vivo test for dopamine autoreceptor activation.
Bendesky, RJ; Martin, GE, 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
"Veralipride in a daily dosage of 100 mg given twenty days each month was tested in 17 patients with hot flushes."( [Value of an novel molecule, veralipride, in the treatment of menopausal disorders].
Grall, JY, 1982
)
0.26
" Administration of meprobamate with oral sultopride in a high dosage (2 g per day) was promptly followed by an improvement in the patient's condition."( [The use of a sedative neuroleptic agent, sultopride, in posttraumatic Korsakoff syndrome in a young adult].
Cornier, P, 1983
)
0.27
"In a young patient with encephalopathy and major agitation, sultopride given in a daily dosage of two 400 mg tablets (associated with a corrector, trihexyphenidyl, CL drops nightly) ensured better vigilance, sedation of vociferations, agitation, and automutilation, and improvement of autonomy (particularly recovery of sphincter control)."( [Ambulatory treatment of agitation in encephalopathies].
de Laitre, G, 1983
)
0.27
" With a daily dosage of 150 mg, a satisfactory response was recorded in overall pathology in 76."( [Sulpiride and depression].
Lestynek, JL, 1983
)
1.18
" The present data allows the conclusion that (A) low dosed sulpiride seems to act as an antidepressant in severe and milder forms of depression, (B) a clinical progress is seen earlier than is common during treatment with tricyclics and (C) a significant increase of drive is observable."( Effect of sulpiride in endogenous depression.
Benkert, O; Holsboer, F, 1984
)
0.91
" Increasing the test-dose of apomorphine led to a biphasic effect, the spontaneous climbing behavior being decreased at low dosage and, then, both the percentage of climbing animals and the duration of the behavior were progressively increased at higher dosages."( Rat climbing behavior elicited by stimulation of cerebral dopamine receptors.
Bonnet, JJ; Costentin, J; Protais, P; Schwartz, JC, 1984
)
0.27
" Acid and pepsin secretion were inhibited in dose-response manner by dopamine in innervated mucosa, but all other effects of the compounds were different in parietal cells and chief cells and in vagally innervated and denervated mucosa."( Dopaminergic and adrenergic influence on gastric acid and pepsin secretion stimulated by food. The role of vagal innervation.
Berstad, A; Guldvog, I; Linnestad, P; Schrumpf, E, 1984
)
0.27
" Statistical evaluation of all the above parameters, determined at the three dosage levels, did not show any variations related to dose; the pharmacokinetics of sulpiride, over the dose range tested, was therefore linear and independent of dose."( Sulpiride pharmacokinetics in humans after intramuscular administration at three dose levels.
Blanchin, MD; Bres, J; Bressolle, F; Gomeni, R, 1984
)
1.91
"In DOCA-pretreated men during hypotonic polyuria Dopamine (DA) infusion in a subpressor dosage (0."( [Sulpiride (stereoisomers, racemic) and dopamine: actions and interactions on tubular reabsorption].
Agnoli, GC; Andreone, P; Cacciari, M; Garutti, C; Ikonomu, E; Lenzi, P, 1984
)
1.18
" 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
)
0.52
" Treatment of the urine from a monkey dosed orally with 14C-I by dry column chromatography and high-pressure liquid chromatography (HPLC) produced the major metabolite in pure form."( Isolation, identification, and synthesis of the major sulpiride metabolite in primates.
Brennan, JJ; Imondi, AR; Westmoreland, DG; Williamson, MJ, 1982
)
0.51
" Dose-response curves to norepinephrine in the presence of hydralazine were shifted to the right in parallel fashion at an only slight reduction of the maximum response."( Studies on the direct vasodilator effect of hydralazine in the isolated rabbit renal artery.
Gross, F; Khayyal, M; Kreye, VA, 1981
)
0.26
"To improve the limited oral bioavailability of sulpiride, a dosage form containing sodium oleate as an absorption enhancer was developed and evaluated using gastric-emptying-controlled rabbits in a cross-over manner."( Improving the oral bioavailability of sulpiride by sodium oleate in rabbits.
Iseki, K; Kohri, N; Miyazaki, K; Naasani, I, 1995
)
0.82
"01-1 mg/kg) induced penile erection in rats with bell-shaped dose-response curves."( Role of the dopaminergic, serotonergic and cholinergic link in the expression of penile erection in rats.
Maeda, N; Matsuoka, N; Yamaguchi, I, 1994
)
0.29
" In experiment 2b, a full d-amphetamine dose-response function was examined."( Isolation rearing impairs the reinforcing efficacy of intravenous cocaine or intra-accumbens d-amphetamine: impaired response to intra-accumbens D1 and D2/D3 dopamine receptor antagonists.
Everitt, BJ; Howes, SR; Phillips, GD; Robbins, TW; Whitelaw, RB, 1994
)
0.29
" Simultaneous administration of (+)-PHNO [(+)-4-propyl-9-hydroxynaphthoxazine] and CY 208-243 [(-)4,6,6a,7,8,12b-hexahydro-7-methylindolo[4,3a-b]phenan thyxidine] did not result in modification of the dose-response curve induced by each dopamine receptor agonist given alone."( Functional interaction between dopamine D1 and D2 receptors in 'MPTP' monkeys.
Guillén, J; Laguna, J; Luquin, MR; Martínez-Lage, JM; Martínez-Vila, E, 1994
)
0.29
"A within-subject dose-response analysis was conducted by locally perfusing increasing concentrations (0."( The development of D2 autoreceptor-mediated modulation of K(+)-evoked dopamine release in the neostriatum.
Andersen, SL; Gazzara, RA, 1994
)
0.29
" The compound facilitated penile erection in naive rats, and it ameliorated scopolamine-induced amnesia of rats in passive avoidance tasks with bell-shaped dose-response curves, while it dose-dependently reduced body weight gain in Zucker fatty rats."( A screening concept based on a hypothesis led to the development of a putative cognitive enhancer that stimulates penile erection.
Arakawa, H; Maeda, N; Matsuoka, N; Ohkubo, Y; Yamaguchi, I; Yamazaki, M, 1994
)
0.29
" Out of regard for the administrative and psychological advantage of the once a day dosage this form should be preferred in the treatment of major depression."( Therapeutic effects and side effects in patients with major depression treated with sulpiride once a day.
Asakura, M; Hasegawa, K; Satoh, Y; Shinozuka, T; Tsukamoto, T; Tsuneizumi, T, 1994
)
0.51
" Pregnant rats were dosed orally with cocaine hydrochloride (60 mg/kg/d) from gestational day (GD) 7-21."( Prenatal cocaine exposure revealed minimal postnatal changes in rat striatal dopamine D2 receptor sites and mRNA levels in the offspring.
Choi, HL; Stadlin, A; Tsang, D; Tsim, KW,
)
0.13
" In these four cases, dosing recommendations were not respected."( [Extrapyramidal disorders induced by veralipride (Agreal). Apropos of 5 cases].
Andréjak, M; Chetaille, E; Decocq, G; Masmoudi, K; Mizon, JP; Rosa, A,
)
0.13
" Absolute recovery of S-(-)- and R-(+)-amisulpride enantiomers from human plasma, as well as selectivity, precision and accuracy have been demonstrated to be satisfactory for pharmacokinetics in man and equivalent for both the proposed methods that have been cross-validated on real dosed human plasma samples."( Stereospecific determination of amisulpride, a new benzamide derivative, in human plasma and urine by automated solid-phase extraction and liquid chromatography on a chiral column. application to pharmacokinetics.
Ascalone, V; Malavasi, B; Ripamonti, M, 1996
)
0.29
"05, at the start and at the end of the study), while the dosage of injected insulin (0."( Chronic administration of levosulpiride and glycemic control in IDDM patients with gastroparesis.
Ciuchi, E; Giusti, R; Mansi, C; Melga, P; Prando, R; Sciaba, L, 1997
)
0.59
"In many European countries, the substituted benzamide sulpiride is used with antidepressant indication in the dosage range of 150-300 mg on an outpatient population."( The effects of sulpiride on psychomotor performance and subjective tolerance.
Gallhofer, B; Meyer-Lindenberg, A; Rammsayer, T; Ulferts, J, 1997
)
0.9
" DeMonS has been applied to (i) the griseofulvin data for estimating drug absorbed at different time intervals when the drug disposition model parameters were determined separately from intravenous data, (ii) veralipride double-peak phenomenon data to estimate simultaneously the percentage of cumulative veralipride absorbed and the veralipride disposition model parameters without reference intravenous data, (iii) a comparative bioequivalence study of gastrointestinal therapeutic system (GITS) pseudoephedrine HCI (PeHCI) controlled-release oral dosage forms when the drug disposition model parameters were not available, and (iv) estimation of both drug disposition model parameters and the absorption rate of drug from Testoderm (testosterone transdermal system) in the presence of endogenous testosterone production."( DeMonS--a new deconvolution method for estimating drug absorbed at different time intervals and/or drug disposition model parameters using a monotonic cubic spline.
Gupta, SK; Hwang, SS; Yu, Z, 1997
)
0.3
" The drug had only a limited effect in reducing negative symptoms, which were relatively stable, enduring phenomena in this sample, despite dosage reduction."( One-year, low-dose neuroleptic study of in-patients with chronic schizophrenia characterised by persistent negative symptoms. Amisulpride v. haloperidol.
Alberts, JL; Barnes, TR; Curson, DA; Pantelis, C; Speller, JC, 1997
)
0.3
" The present experiments extend these findings by investigating: (a) interactions between isolation rearing and repeated handling/testing on presynaptic DA function in the NAC using in vivo microdialysis: (b) the dose-response curve for the effects of d-amphetamine, and the responses elicited by high potassium, using in vivo microdialysis, and (c) postsynaptic function in isolates as indexed by DA receptor-linked cAMP production."( Isolation rearing in rats: pre- and postsynaptic changes in striatal dopaminergic systems.
Hall, FS; Humby, T; Inglis, W; Kendall, DA; Marsden, CA; Robbins, TW; Wilkinson, LS, 1998
)
0.3
" Extrapyramidal tolerability was better in the ASP group, as demonstrated by smaller increases in the Simpson-Angus Scale, the AIMS, and the Barnes Akathisia Scale in ANCOVA analyses with dosage as covariate."( Amisulpride versus flupentixol in schizophrenia with predominantly positive symptomatology -- a double-blind controlled study comparing a selective D2-like antagonist to a mixed D1-/D2-like antagonist. The Amisulpride Study Group.
Adler, G; Benkert, O; Gattaz, WF; Gründer, G; Hillert, A; Philipp, M; Rein, W; Sauer, H; Schröder, J; Wetzel, H, 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
)
0.3
" However, these findings should be confirmed after multiple dosing in a larger population in order to establish the lack of need of dosage adjustment in this elderly population."( Safety and pharmacokinetics of a single oral dose of amisulpride in healthy elderly volunteers.
Ahtoy, P; Canal, M; Chaufour, S; Chretien, P; Deschamps, C; Hamon-Vilcot, B; Nasr, A; Piette, F; Rosenzweig, P; Zieleniuk, I, 1998
)
0.3
" The patients received amisulpride with flexible dosage between 600 and 1,200 mg/d during a 3-month period (792 mg/d +/- 318)."( [Evaluation of efficacy and tolerance of amisulpride in treatment of schizophrenic psychoses].
Chabannes, JP; Farah, S; Gerard, D; Pelissolo, A,
)
0.13
" 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
)
1.21
" The method is reproducible and convenient for quantitative analysis and purity control of sulpiride in its raw material and in its dosage forms."( Quantitative analysis of sulpiride and impurities of 2-aminomethyl-1-ethylpyrrolidine and methyl-5-sulphamoyl-2-methoxybenzoate in pharmaceuticals by high-performance thin-layer chromatography and scanning densitometry.
Agbaba, D; Marinkovic, V; Miljkovic, T; Vladimirov, S; Zivanov-Stakic, D,
)
0.66
" The CNS profile of multiple doses of a low dosage regimen of amisulpride (50 mg once daily for 4 days) was assessed in a randomised, double-blind, 3-way crossover, placebo-controlled study carried out in 12 young sleep-deprived (for 36 h) subjects, using EEG and various measures of psychomotor and cognitive functions."( Effects of 50mg amisulpride on EEG, psychomotor and cognitive functions in healthy sleep-deprived subjects.
Allain, H; Gandon, JM; Miget, N; Patat, A; Rosenzweig, P, 1999
)
0.3
" Thus, the inhibitory dose-response effects of a D2-preferring [sulpride], a D3-preferring [U 99194A] and combination of varying doses of these antagonists [sulpride + U 99194A] were evaluated on the ability of the cited agonists to produce vomiting."( The role of D2 and D3 dopamine receptors in the mediation of emesis in Cryptotis parva (the least shrew).
Ahmad, B; Darmani, NA; Zhao, W, 1999
)
0.3
" A dose-response effect was observed."( Behavioural motor effects of MK-801 and DNQX parenteral administration in adult cats: dose-response analysis. Modulatory role of dopaminergic D1 and D2 antagonists on MK-801 induced motor behaviours.
Gonzalez, M; Infante, C; Motles, E, 2000
)
0.31
" 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
)
0.31
" In Experiment 3, LH infusion by reverse microdialysis of the D(2) receptor blocker sulpiride released ACh in the LH in a dose-response manner."( Dopamine-acetylcholine interaction in the rat lateral hypothalamus in the control of locomotion.
De Parada, MP; Hernandez, L; Hoebel, BG; Parada, MA; Rada, P, 2000
)
0.53
" 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
)
0.31
" This appeared to be a clear-cut reversed dose-response relationship for both substituted benzamides, being the dose potency 1 mg/kg>5 mg/kg>10 mg/kg."( Effects of acute or chronic administration of substituted benzamides in experimental models of depression in rats.
Arezzi, A; Drago, F; Virzì, A, 2000
)
0.31
" In an open pilot study, we investigated 26 inpatients (13 female, 13 male) with schizophrenic or depressive disorder treated with SULP (mean daily dosage 64-1062 mg) administered orally, either as a monotherapy or as an add-on treatment to a stable and unchanged medication for 3-60 days."( Serum levels of sulpiride enantiomers after oral treatment with racemic sulpiride in psychiatric patients: a pilot study.
Härtter, S; Hiemke, C; Köhler, D; Müller, MJ, 2001
)
0.66
"80 SD, were treated with clomipramine at a mean dosage of 57."( A single blind comparison of amisulpride, fluoxetine and clomipramine in the treatment of restricting anorectics.
Cavagnini, F; Clemente, A; Ferrari, VM; Laini, V; Lugo, F; Mantero, M; Mauri, MC; Redaelli, G; Ruggiero, GM; Zappulli, D, 2001
)
0.31
"Ten adolescent cases are presented with regard to the efficacy, side effects and dosage of amisulpride."( [Initial experiences with amisulpride, an in Germany novel, atypical neuroleptic drug in treatment of adolescents with psychiatric disorders].
Göpel, C; Marcus, A, 2001
)
0.31
" In patients with acute exacerbations of schizophrenia, the recommended dosage of amisulpride is 400 to 800 mg/day, although dosages < or =1200 mg/day may be administered."( Amisulpride: a review of its use in the management of schizophrenia.
Curran, MP; Perry, CM, 2001
)
0.31
" Consequently, the dosage of amisulpride that is recommended in patients with acute exacerbations of schizophrenia is 400 to 800 mg/day, although dosages < or =1200 mg/day may be administered."( Amisulpride: a review of its use in the management of schizophrenia.
Curran, MP; Perry, CM, 2001
)
0.31
" In patients with acute exacerbations of schizophrenia, the recommended dosage of amisulpride is 400 to 800 mg/day, although dosages < or = 1200 mg/day may be administered."( Spotlight on amisulpride in schizophrenia.
Curran, MP; Perry, CM, 2002
)
0.31
" Consequently, the dosage of amisulpride that is recommended in patients with acute exacerbations of schizophrenia is 400 to 800 mg/day, although dosages < or = 1200 mg/day may be administered."( Spotlight on amisulpride in schizophrenia.
Curran, MP; Perry, CM, 2002
)
0.31
" Analyses of CFA-derived factor scores showed that ASP was significantly superior to FPX regarding the latent 'depressive' dimension, independent of baseline scores, dosage and changes in akinesia."( Differential effects of high-dose amisulpride versus flupentixol on latent dimensions of depressive and negative symptomatology in acute schizophrenia: an evaluation using confirmatory factor analysis.
Benkert, O; Müller, MJ; Wetzel, H, 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
" twice, 30 min before each dosing of dopamine."( Dopamine-induced protection against indomethacin-evoked intestinal lesions in rats--role of anti-intestinal motility mediated by D2 receptors.
Kato, S; Matsumoto, M; Miyazawa, T; Takeuchi, K, 2003
)
0.32
" It includes concepts of human neurobiology and neuropharmacology and their application to clinical medicine, as well as the presentation of the clinical evidence on the therapeutic efficacy and safety of amisulpride in schizophrenia, highlighting dosage issues."( Dopaminergic deficit and the role of amisulpride in the treatment of schizophrenia.
Kasper, S, 2002
)
0.31
" However, no correlation between prolactin levels and dosage could be found."( [Plasma prolactin level and incidence of adverse endocrinologic effects during therapy with atypical neuroleptics].
Fric, M; Laux, G, 2003
)
0.32
" The objectives of this study were to determine (1) the dose-response effects for the self-administration of EtOH into the VTA of male Wistar rats, and (2) the involvement of VTA DA neurons in the reinforcing actions of EtOH within the VTA."( Intracranial self-administration of ethanol within the ventral tegmental area of male Wistar rats: evidence for involvement of dopamine neurons.
Bell, RL; Kuc, KA; McBride, WJ; Melendez, RI; Murphy, JM; Rodd, ZA; Zhang, Y, 2004
)
0.32
" This allows the dosage to be adjusted and the treatment tailored to various clinical situations."( Dosage finding and outcome in the treatment of schizophrenic inpatients with amisulpride. Results of a drug utilization observation study.
Linden, M; Scheel, T; Xaver Eich, F, 2004
)
0.32
" Dosage was significantly influenced by the severity of the illness."( Dosage finding and outcome in the treatment of schizophrenic inpatients with amisulpride. Results of a drug utilization observation study.
Linden, M; Scheel, T; Xaver Eich, F, 2004
)
0.32
" In contrast, reliable in vitro permeability data in combination with in vitro release data collected in biorelevant media led to successful prediction of the human input profile; regardless of the dosage form, simulated and actual mean input profiles differed by less than 20%."( Canine versus in vitro data for predicting input profiles of L-sulpiride after oral administration.
Fotaki, N; Reppas, C; Symillides, M, 2005
)
0.57
" Forty patients with delirium were randomly assigned to either AMSP or QTP groups, with a flexible dosing schedule."( Amisulpride versus quetiapine for the treatment of delirium: a randomized, open prospective study.
Bahk, WM; Kweon, YS; Lee, CT; Lee, HK; Lee, KU; Pae, CU; Won, WY, 2005
)
0.33
" Apomorphine induced a biphasic dose-response relationship, low doses producing hyperalgesia and high doses inducing antinociception."( Biphasic effect of apomorphine on rat nociception and effect of dopamine D2 receptor antagonists.
Constandil, L; Eschalier, A; Hernandez, A; Laurido, C; Pelissier, T, 2006
)
0.33
" No significant correlation was detected between prolactin levels and either amisulpride dosage or duration of administration."( Amisulpride-induced hyperprolactinemia is reversible following discontinuation.
Liappas, J; Mourikis, I; Paparrigopoulos, T; Soldatos, C; Tzavellas, E, 2007
)
0.34
"Amisulpride has a pronounced prolactin-elevating effect which appears to be independent of dosage and duration of administration."( Amisulpride-induced hyperprolactinemia is reversible following discontinuation.
Liappas, J; Mourikis, I; Paparrigopoulos, T; Soldatos, C; Tzavellas, E, 2007
)
0.34
"One hundred six consecutive cancer outpatients with depressive symptoms were treated in a prospective, intention to treat, 4-week study, and were evaluated in single-blind with Montgomery Asberg rating scale for depression (MADRS), clinical global impression (CGI) and dosage record treatment emergent symptom scale (DOTES) to assess side effects of treatment."( Amisulpride in the short-term treatment of depressive and physical symptoms in cancer patients during chemotherapies.
Berra, C; Binaschi, L; Borio, R; Torta, R, 2007
)
0.34
"The trial was a prospective, open-label, single-center one with a flexible dosing of SGAs."( Differences in the effect of second-generation antipsychotics on prolactinaemia: six weeks open-label trial in female in-patients.
Cejpková, A; Rodáková, I; Svestka, J; Synek, O; Tomanová, J, 2007
)
0.34
"Four different stability-indicating procedures are described for determination of tiapride in pure form, dosage form, and human plasma."( Stability-indicating methods for determination of tiapride in pure form, pharmaceutical preparation, and human plasma.
Abdelkawy, M; Abdelwahab, NS; Metwally, FH,
)
0.13
" anticholinergics and antiparkinsonian agents) until the effective dosage has been reached."( Practical issues with amisulpride in the management of patients with schizophrenia.
Alptekin, K; Kontaxakis, VP; Pani, L; Villagrán, JM, 2008
)
0.35
"To find the appropriate dosing period to detect ovarian toxicity, sulpiride, a D2 antagonist was orally dosed to female rats at dose levels of 1, 10, and 100 mg/kg/day daily for 2 or 4 weeks in repeated-dose toxicity studies."( Collaborative work on evaluation of ovarian toxicity. 17) Two- or four-week repeated-dose studies and fertility study of sulpiride in female rats.
Adachi, T; Inoue, Y; Ishii, S; Mutai, M; Okada, M; Sugimoto, J; Ube, M; Uno, Y, 2009
)
0.8
"Although clozapine has been shown to be the treatment of choice in people with schizophrenia that are resistant to treatment, one third to two thirds of people still have persistent positive symptoms despite clozapine monotherapy of adequate dosage and duration."( Clozapine combined with different antipsychotic drugs for treatment resistant schizophrenia.
Barbui, C; Boso, M; Cipriani, A, 2009
)
0.35
"To measure behavioral and brain functional markers of drug-related attentional bias in stimulant-dependent individuals studied repeatedly after short-term dosing with dopamine D(2)/D(3) receptor antagonist and agonist challenges."( Influence of compulsivity of drug abuse on dopaminergic modulation of attentional bias in stimulant dependence.
Abbott, S; Barnes, A; Bullmore, ET; Craig, KJ; Ersche, KD; Merlo-Pich, EV; Müller, U; Ooi, C; Robbins, TW; Sahakian, BJ; Shabbir, SS; Suckling, J, 2010
)
0.36
"We report on 6 cases with partial response of psychotic positive symptoms to QTP despite sufficient dosage (mean, 783 mg/d) and serum levels (mean, 405 μg/L)."( Quetiapine combined with amisulpride in schizophrenic patients with insufficient responses to quetiapine monotherapy.
Englisch, S; Enning, F; Grosshans, M; Marquardt, L; Waltereit, R; Zink, M,
)
0.13
" At a dosage of 25mg three times daily, levosulpiride accelerates gastric and gallbladder emptying."( [Levosulpiride in the management of functional dyspepsia and delayed gastric emptying].
Serra, J, 2010
)
1.14
"OCS were significantly more prevalent and severe in group I, in which OCS severity correlated with dosage of clozapine and duration of treatment."( Antiserotonergic antipsychotics are associated with obsessive-compulsive symptoms in schizophrenia.
Englisch, S; Esslinger, C; Meyer-Lindenberg, A; Rausch, F; Schirmbeck, F; Zink, M, 2011
)
0.37
" To project the comparison in a sensible way, the methods are used for the stability indicating quantitative analysis of mixtures of mebeverine hydrochloride and sulpiride in binary mixtures as a case study in presence of their reported impurities and degradation products (summing up to 6 components) in raw materials and pharmaceutical dosage form via handling the UV spectral data."( Support vector regression and artificial neural network models for stability indicating analysis of mebeverine hydrochloride and sulpiride mixtures in pharmaceutical preparation: a comparative study.
Darwish, HW; Naguib, IA, 2012
)
0.78
"The mean dosage of amisulpride was 195."( Hyperprolactinemia induced by low-dosage amisulpride in Korean psychiatric patients.
Kang, SG; Kim, TW; Lee, BH; Lee, HJ; Park, YM; Yoon, HK, 2012
)
0.38
" After bilaterally implantation of cannulae into the CA1 and/or VTA in adult male Wistar rats weighing 210-310 g, dose-response effects of different doses of intra-VTA morphine (0."( Role of D1/D2 dopamine receptors in the CA1 region of the rat hippocampus in the rewarding effects of morphine administered into the ventral tegmental area.
Esmaeili, MH; Haghparast, A; Kermani, M; Parvishan, A, 2012
)
0.38
" There were 386 treatment cycles; 272 were assigned to dosing schedule 1, which included 20 days of treatment with 10 days of suspension, and 114 were assigned to dosing schedule 2, which included 5 days of treatment and 2 days of suspension."( Safety of veralipride for the treatment of vasomotor symptoms of menopause.
Álvarez, IM; Arias, Mde J; Bonilla, MC; Campero, RA; Campos, ER; Escudero, RB; Flores, JB; González, CC; González, JH; Haro, SS; Marín, IH; Rodríguez, MA; Valencia, MH; Vargas, MA, 2014
)
0.4
" For the 20 × 10 dosing schedule, the highest incidence was observed for anxiety (2."( Safety of veralipride for the treatment of vasomotor symptoms of menopause.
Álvarez, IM; Arias, Mde J; Bonilla, MC; Campero, RA; Campos, ER; Escudero, RB; Flores, JB; González, CC; González, JH; Haro, SS; Marín, IH; Rodríguez, MA; Valencia, MH; Vargas, MA, 2014
)
0.4
"Both dosing schedules show acceptable safety profiles for up to 6 months of use when used according to the contraindications in the current prescribing information for standard use (2012) and recent medical literature."( Safety of veralipride for the treatment of vasomotor symptoms of menopause.
Álvarez, IM; Arias, Mde J; Bonilla, MC; Campero, RA; Campos, ER; Escudero, RB; Flores, JB; González, CC; González, JH; Haro, SS; Marín, IH; Rodríguez, MA; Valencia, MH; Vargas, MA, 2014
)
0.4
" D1-like receptor activation produced an inverted U-shaped dose-response curve on plasticity induced by both facilitatory tDCS and PAS."( Nonlinear dose-dependent impact of D1 receptor activation on motor cortex plasticity in humans.
Fresnoza, S; Kuo, MF; Nitsche, MA; Paulus, W, 2014
)
0.4
" Exposure to amisulpride (D2/3 receptor antagonist) induced a biphasic dose-response in total distance travelled and in angular velocity."( Differential effects of dopamine D1 and D 2/3 receptor antagonism on motor responses.
Gerlai, R; Muraleetharan, A; Nowicki, M; Tran, S, 2015
)
0.42
" On day 8, the amisulpride dosage was increased to 800 mg orally daily and his manic symptoms worsened."( Amisulpride-associated mania in a young adult with schizophrenia and cerebral disease.
Chen, CY; Chen, TY; Chuang, WC; Kuo, SC; Yeh, YW, 2014
)
0.4
" Sulpiride SD-incorporated witepsol H15 formulation showed acceptable in vitro characteristics with a bioavailability of 117% relative to oral dosing, which excel that in humans (27% after dosing of oral product)."( Pediatric suppositories of sulpiride solid dispersion for treatment of Tourette syndrome: in vitro and in vivo investigations.
Emam, SE; Ghazy, FE; Shehata, TM; Zidan, AS, 2015
)
1.62
" The method was validated and was finally applied to determine the enantiomeric purity of S-SUL in pharmaceutical dosage forms."( Quality by design in the chiral separation strategy for the determination of enantiomeric impurities: development of a capillary electrophoresis method based on dual cyclodextrin systems for the analysis of levosulpiride.
Del Bubba, M; Furlanetto, S; Orlandini, S; Pasquini, B; Pinzauti, S, 2015
)
0.6
" Although our study suggests the prescription dosage and duration of antipsychotic treatment decreased significantly after FDA warning in 2005, the duration of treatment was still long."( Dosage and duration of antipsychotic treatment in demented outpatients with agitation or psychosis.
Chiang, HL; Hwang, TJ; Hwu, HG; Lin, YT; Shan, JC; Sheu, YH, 2015
)
0.42
" Brain exposure at microdosing agreed with pharmacological dosing conditions for the investigated drugs."( Large Variation in Brain Exposure of Reference CNS Drugs: a PET Study in Nonhuman Primates.
Amini, N; Farde, L; Finnema, SJ; Halldin, C; Lundquist, S; Nakao, R; Schou, M; Takano, A; Varnäs, K, 2015
)
0.42
" There was no support for a dose-response relationship for any drug combination."( Skating on thin ice: pragmatic prescribing for medication refractory schizophrenia.
Joyce, DW; Mateos Fernandez, MJ; Sarkar, SN; Shergill, SS; Tracy, DK, 2015
)
0.42
"Levosulpiride was administered to 42 healthy male and female (1:1) subjects in tablet (PO) and injectable (IM and IV) dosage forms."( Tolerability and Pharmacokinetic Comparison of Oral, Intramuscular, and Intravenous Administration of Levosulpiride After Single and Multiple Dosing in Healthy Chinese Volunteers.
Chen, H; He, X; Li, H; Li, W; Ni, Y; Sattar, H; Xu, M; Zhou, Y, 2015
)
1.19
"Six weeks of individually dosed amisulpride treatment."( Striatal Reward Activity and Antipsychotic-Associated Weight Change in Patients With Schizophrenia Undergoing Initial Treatment.
Ebdrup, BH; Glenthøj, B; Nielsen, MØ; Rostrup, E; Wulff, S, 2016
)
0.43
"Across the two studies, 689 patients were randomized and dosed with study medication, of whom 626 were evaluable per protocol."( Intravenous Amisulpride for the Prevention of Postoperative Nausea and Vomiting: Two Concurrent, Randomized, Double-blind, Placebo-controlled Trials.
Bergese, SD; Candiotti, KA; Chassard, D; Diemunsch, P; Eberhart, L; Fox, G; Gan, TJ; Kovac, AL; Kranke, P; Leiman, DG; Melson, TI; Minkowitz, HS; Motsch, J, 2017
)
0.46
"S-SNEDDS can be a very useful approach for providing patient acceptable dosage forms with improved oral dissolution and biovailability."( Development of novel amisulpride-loaded solid self-nanoemulsifying tablets: preparation and pharmacokinetic evaluation in rabbits.
Fahmy, RH; Gamal, W; Mohamed, MI, 2017
)
0.46
" Therefore, drug monitoring is necessary for appropriate dosage adjustments."( Chromatographic determination of zonisamide, topiramate and sulpiride in plasma by a fluorescent 'turn-on' chemosensor.
Barary, MA; El-Yazbi, AF; Ibrahim, FA; Wagih, MM, 2017
)
0.7
" Model predictions were used to simulate dose-response and dose-EPS."( A Population Approach to Guide Amisulpride Dose Adjustments in Older Patients With Alzheimer's Disease.
Bertrand, J; Brownings, S; D'Antonio, F; Dunn, JT; Greaves, S; Howard, R; Kessler, R; Marsden, P; McLachlan, E; Nair, A; Reeves, S; Smith, A; Taylor, D; Uchida, H, 2017
)
0.46
" Participants received 400 mg of amisulpride or two matching placebo capsules for the first 4 weeks, after which there was a clinical option to titrate the dosage of amisulpride up to 800 mg or four matching placebo capsules for the remaining 8 weeks."( Amisulpride augmentation in clozapine-unresponsive schizophrenia (AMICUS): a double-blind, placebo-controlled, randomised trial of clinical effectiveness and cost-effectiveness.
Amos, T; Bagalkote, H; Barnes, TR; Davies, L; Fitzgerald, Z; Fridrich, P; Haddad, PM; Husni, M; Iqbal, K; Keown, P; Kumar, R; Leeson, VC; Marston, L; Osborn, D; Paton, C; Singh, V; Whittaker, W; Zafar, R, 2017
)
0.46
" Oral dosing of LSP in goats is probably not viable as its oral bioavailability was very low."( Pharmacokinetics of levosulpiride after single-dose administration in goats (Capra hircus) by different routes of administration.
Barsotti, G; Camillo, F; Giorgi, M; Lisowski, A; Panzani, D; Poapolathep, A; Rota, A; Łebkowska-Wieruszewska, B, 2019
)
0.82
" A set of core outcomes to standardise infant weight and milk volume measurement is also needed, as well as a strong basis for the dose and dosage form used."( Oral galactagogues (natural therapies or drugs) for increasing breast milk production in mothers of non-hospitalised term infants.
Foong, SC; Foong, WC; Ho, JJ; Marasco, LA; Ong, JH; Tan, ML, 2020
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
antidepressantAntidepressants are mood-stimulating drugs used primarily in the treatment of affective disorders and related conditions.
antiemeticA drug used to prevent nausea or vomiting. An antiemetic may act by a wide range of mechanisms: it might affect the medullary control centres (the vomiting centre and the chemoreceptive trigger zone) or affect the peripheral receptors.
antipsychotic agentAntipsychotic drugs are agents that control agitated psychotic behaviour, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect.
dopaminergic antagonistA drug that binds to but does not activate dopamine receptors, thereby blocking the actions of dopamine or exogenous agonists.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
N-alkylpyrrolidine
sulfonamideAn amide of a sulfonic acid RS(=O)2NR'2.
benzamides
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (66)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
acetylcholinesteraseHomo sapiens (human)Potency31.70550.002541.796015,848.9004AID1347395
thioredoxin reductaseRattus norvegicus (Norway rat)Potency0.56230.100020.879379.4328AID588453
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency7.76063.189029.884159.4836AID1224846
RAR-related orphan receptor gammaMus musculus (house mouse)Potency54.48270.006038.004119,952.5996AID1159521
ATAD5 protein, partialHomo sapiens (human)Potency3.26290.004110.890331.5287AID493107
GLS proteinHomo sapiens (human)Potency3.54810.35487.935539.8107AID624146
Microtubule-associated protein tauHomo sapiens (human)Potency8.91250.180013.557439.8107AID1468
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency16.29210.000657.913322,387.1992AID1259377; AID1259378
progesterone receptorHomo sapiens (human)Potency19.33120.000417.946075.1148AID1346795
regulator of G-protein signaling 4Homo sapiens (human)Potency0.26650.531815.435837.6858AID504845
EWS/FLI fusion proteinHomo sapiens (human)Potency26.92360.001310.157742.8575AID1259253; AID1259256
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency54.94100.000214.376460.0339AID720692
retinoid X nuclear receptor alphaHomo sapiens (human)Potency43.64120.000817.505159.3239AID1159527
arylsulfatase AHomo sapiens (human)Potency4.77551.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency41.85310.035520.977089.1251AID504332
aryl hydrocarbon receptorHomo sapiens (human)Potency74.80630.000723.06741,258.9301AID743085; AID743122
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.00160.540617.639296.1227AID2364; AID2528
D(1A) dopamine receptorHomo sapiens (human)Potency8.21810.02245.944922.3872AID488982; AID488983
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency10.00000.01789.637444.6684AID588834
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency35.48130.251215.843239.8107AID504327
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency19.01150.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Carbonic anhydrase Astrosclera willeyanaKi0.37800.03201.51729.6000AID644379
Carbonic anhydrase Sulfurihydrogenibium sp. YO3AOP1Ki0.06740.00450.16240.8760AID1268964
Carbonic anhydrase Stylophora pistillataKi0.43000.00000.686710.0000AID436565; AID552130
Carbonic anhydraseStylophora pistillataKi0.41500.00000.50715.7100AID552131
Carbonic anhydraseHelicobacter pylori 26695Ki0.19150.02000.54864.3600AID261581; AID263638
Carbonic anhydrase 12Homo sapiens (human)Ki0.00390.00021.10439.9000AID1067227; AID238316; AID770582
Bile salt export pumpRattus norvegicus (Norway rat)IC50 (µMol)1,000.00000.40002.75008.6000AID1209456
Bile salt export pumpHomo sapiens (human)IC50 (µMol)638.10000.11007.190310.0000AID1209455; AID1449628
Carbonic anhydrase 1Homo sapiens (human)IC50 (µMol)1.20000.00582.14107.9000AID50344
Carbonic anhydrase 1Homo sapiens (human)Ki4.21830.00001.372610.0000AID1067230; AID1142833; AID1188134; AID1190063; AID1194024; AID1195369; AID1262263; AID1268962; AID1275913; AID1287517; AID1434427; AID1453412; AID1628036; AID1799591; AID238276; AID261579; AID263636; AID271172; AID275807; AID349605; AID367820; AID369271; AID414955; AID427125; AID436563; AID552127; AID577526; AID612725; AID644380; AID725955; AID743515; AID764719; AID770586
Carbonic anhydrase 2Homo sapiens (human)IC50 (µMol)0.04000.00021.10608.3000AID47748
Carbonic anhydrase 2Homo sapiens (human)Ki0.31700.00000.72369.9200AID1061069; AID1067229; AID1142834; AID1188135; AID1190064; AID1194025; AID1195370; AID1240217; AID1262264; AID1268963; AID1275912; AID1278409; AID1287518; AID1434428; AID1453413; AID1628037; AID1796771; AID1799591; AID238300; AID256963; AID261580; AID263637; AID271173; AID275808; AID349606; AID367821; AID369272; AID414956; AID427124; AID436564; AID437749; AID552128; AID577527; AID612726; AID644381; AID669115; AID725956; AID743514; AID764718; AID770585
Carbonic anhydrase 3Homo sapiens (human)Ki10.60000.00022.010210.0000AID301578
Alpha-2A adrenergic receptorHomo sapiens (human)IC50 (µMol)2.01900.00001.44217.3470AID625201
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.75700.00010.807410.0000AID625201
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)50.00000.00002.800510.0000AID1210069
D(2) dopamine receptorHomo sapiens (human)IC50 (µMol)0.08580.00000.74728.0000AID1607338; AID597452; AID625253
D(2) dopamine receptorHomo sapiens (human)Ki0.06590.00000.651810.0000AID1916460; AID238699; AID625253
DRattus norvegicus (Norway rat)Ki1.60000.00010.610010.0000AID63020
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki1.60000.00010.25675.8000AID63020
D(4) dopamine receptorHomo sapiens (human)Ki2.10000.00000.436210.0000AID238274
Carbonic anhydrase 6Homo sapiens (human)Ki2.00720.00011.47109.9200AID1799591; AID275806; AID369273; AID552129
D(1B) dopamine receptorRattus norvegicus (Norway rat)Ki1.60000.00020.24622.0000AID63020
D(4) dopamine receptorRattus norvegicus (Norway rat)Ki1.60000.00020.18872.0000AID63020
Delta-type opioid receptorMus musculus (house mouse)Ki0.62000.00000.53939.4000AID1188134; AID1188135
Delta-type opioid receptorRattus norvegicus (Norway rat)Ki0.04000.00000.60689.2330AID1188135
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki1.20000.00000.38458.6000AID1188134
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki3.00000.00030.380610.0000AID1916455
Carbonic anhydrase 5A, mitochondrialHomo sapiens (human)Ki0.17400.00001.27259.9000AID256964
D(3) dopamine receptorHomo sapiens (human)IC50 (µMol)0.26510.00011.01788.7960AID597446; AID597453; AID625254
D(3) dopamine receptorHomo sapiens (human)Ki0.06170.00000.602010.0000AID238350; AID625254; AID65133
Carbonic anhydrase 7Homo sapiens (human)Ki2.42120.00021.37379.9000AID1060765; AID764717; AID770584
Cytochrome P450 2J2Homo sapiens (human)IC50 (µMol)50.00000.01202.53129.4700AID1210069
Carbonic anhydraseSaccharomyces cerevisiae S288CKi0.12400.08200.56098.7000AID367822
D(2) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)0.22150.00010.54948.4000AID64295; AID64609
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki1.60000.00000.437510.0000AID63020
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.04000.00000.27869.0000AID1188135
Beta-carbonic anhydrase 1Mycobacterium tuberculosis H37RvKi2.30000.00483.38419.8400AID349607
Carbonic anhydrase 2Mycobacterium tuberculosis H37RvKi0.26600.00902.20969.8400AID437750
Carbonic anhydrase 9Homo sapiens (human)Ki0.04090.00010.78749.9000AID1067228; AID1796771; AID271174; AID275809; AID369274; AID770583
Carbonic anhydrase, alpha family Hydrogenovibrio crunogenus XCL-2Ki0.87300.00250.32341.1000AID1268965
Carbonic anhydrase Cryptococcus neoformans var. grubiiKi0.81200.01000.73648.3470AID669116
Carbonic anhydraseCandida albicans SC5314Ki0.76000.01051.44448.3470AID427122; AID669117
Carbonic anhydrase Anopheles gambiae (African malaria mosquito)Ki0.02950.00980.51174.3600AID1195371
Delta carbonic anhydraseConticribra weissflogiiKi0.25900.04960.99789.2000AID1061066
Carbonic anhydrase Nakaseomyces glabratus CBS 138Ki0.11300.00701.21749.1700AID744415
Carbonic anhydrase 4Bos taurus (cattle)IC50 (µMol)0.62000.02100.20600.6200AID48112
Carbonic anhydrase 15Mus musculus (house mouse)Ki0.07300.00091.884610.0000AID369275
D(2) dopamine receptorCanis lupus familiaris (dog)IC50 (µMol)0.20000.20000.20000.2000AID62570
Carbonic anhydrase 5B, mitochondrialHomo sapiens (human)Ki0.01800.00001.34129.9700AID256965
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
D(2) dopamine receptorHomo sapiens (human)Kd0.00280.00000.64599.5000AID1484195
D(3) dopamine receptorHomo sapiens (human)Kd0.03980.00000.07480.3162AID1484181
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Carbonic anhydrase Brucella suis 1330Kinact0.01900.01700.86285.8700AID459696
Carbonic anhydrase 1Homo sapiens (human)Kinact1.20000.01000.93878.6000AID293811; AID299242
Carbonic anhydrase 2Homo sapiens (human)Kinact0.04000.00300.794610.0000AID293812; AID299243
D(2) dopamine receptorHomo sapiens (human)Kb0.00300.00041.654910.0000AID1484185
D(3) dopamine receptorHomo sapiens (human)K0.00810.00810.00810.0081AID1916467
D(3) dopamine receptorHomo sapiens (human)Kb0.04000.00141.584310.0000AID1484186
Carbonic anhydrase 9Homo sapiens (human)Kinact0.03100.00500.31976.6700AID293813
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (219)

Processvia Protein(s)Taxonomy
estrous cycleCarbonic anhydrase 12Homo sapiens (human)
chloride ion homeostasisCarbonic anhydrase 12Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 12Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 1Homo sapiens (human)
morphogenesis of an epitheliumCarbonic anhydrase 2Homo sapiens (human)
positive regulation of synaptic transmission, GABAergicCarbonic anhydrase 2Homo sapiens (human)
positive regulation of cellular pH reductionCarbonic anhydrase 2Homo sapiens (human)
angiotensin-activated signaling pathwayCarbonic anhydrase 2Homo sapiens (human)
regulation of monoatomic anion transportCarbonic anhydrase 2Homo sapiens (human)
secretionCarbonic anhydrase 2Homo sapiens (human)
regulation of intracellular pHCarbonic anhydrase 2Homo sapiens (human)
neuron cellular homeostasisCarbonic anhydrase 2Homo sapiens (human)
positive regulation of dipeptide transmembrane transportCarbonic anhydrase 2Homo sapiens (human)
regulation of chloride transportCarbonic anhydrase 2Homo sapiens (human)
carbon dioxide transportCarbonic anhydrase 2Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 2Homo sapiens (human)
response to bacteriumCarbonic anhydrase 3Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 3Homo sapiens (human)
positive regulation of cytokine productionAlpha-2A adrenergic receptorHomo sapiens (human)
DNA replicationAlpha-2A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
Ras protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
Rho protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2A adrenergic receptorHomo sapiens (human)
actin cytoskeleton organizationAlpha-2A adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell migrationAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
cellular response to hormone stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2A adrenergic receptorHomo sapiens (human)
vasodilationAlpha-2A adrenergic receptorHomo sapiens (human)
glucose homeostasisAlpha-2A adrenergic receptorHomo sapiens (human)
fear responseAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of potassium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAP kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion-dependent exocytosisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2A adrenergic receptorHomo sapiens (human)
intestinal absorptionAlpha-2A adrenergic receptorHomo sapiens (human)
thermoceptionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of lipid catabolic processAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of uterine smooth muscle contractionAlpha-2A adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
phospholipase C-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of wound healingAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transmembrane transporter activityAlpha-2A adrenergic receptorHomo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasisD(2) dopamine receptorHomo sapiens (human)
response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein phosphorylationD(2) dopamine receptorHomo sapiens (human)
response to amphetamineD(2) dopamine receptorHomo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressureD(2) dopamine receptorHomo sapiens (human)
regulation of heart rateD(2) dopamine receptorHomo sapiens (human)
regulation of sodium ion transportD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(2) dopamine receptorHomo sapiens (human)
positive regulation of neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
positive regulation of receptor internalizationD(2) dopamine receptorHomo sapiens (human)
autophagyD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
neuron-neuron synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
axonogenesisD(2) dopamine receptorHomo sapiens (human)
synapse assemblyD(2) dopamine receptorHomo sapiens (human)
sensory perception of smellD(2) dopamine receptorHomo sapiens (human)
long-term memoryD(2) dopamine receptorHomo sapiens (human)
grooming behaviorD(2) dopamine receptorHomo sapiens (human)
locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
adult walking behaviorD(2) dopamine receptorHomo sapiens (human)
protein localizationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell population proliferationD(2) dopamine receptorHomo sapiens (human)
associative learningD(2) dopamine receptorHomo sapiens (human)
visual learningD(2) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(2) dopamine receptorHomo sapiens (human)
response to light stimulusD(2) dopamine receptorHomo sapiens (human)
response to toxic substanceD(2) dopamine receptorHomo sapiens (human)
response to iron ionD(2) dopamine receptorHomo sapiens (human)
response to inactivityD(2) dopamine receptorHomo sapiens (human)
Wnt signaling pathwayD(2) dopamine receptorHomo sapiens (human)
striatum developmentD(2) dopamine receptorHomo sapiens (human)
orbitofrontal cortex developmentD(2) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(2) dopamine receptorHomo sapiens (human)
adenohypophysis developmentD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell migrationD(2) dopamine receptorHomo sapiens (human)
peristalsisD(2) dopamine receptorHomo sapiens (human)
auditory behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of synaptic transmission, GABAergicD(2) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(2) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
response to histamineD(2) dopamine receptorHomo sapiens (human)
response to nicotineD(2) dopamine receptorHomo sapiens (human)
positive regulation of urine volumeD(2) dopamine receptorHomo sapiens (human)
positive regulation of renal sodium excretionD(2) dopamine receptorHomo sapiens (human)
positive regulation of multicellular organism growthD(2) dopamine receptorHomo sapiens (human)
response to cocaineD(2) dopamine receptorHomo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleepD(2) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(2) dopamine receptorHomo sapiens (human)
drinking behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(2) dopamine receptorHomo sapiens (human)
response to morphineD(2) dopamine receptorHomo sapiens (human)
pigmentationD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(2) dopamine receptorHomo sapiens (human)
negative regulation of innate immune responseD(2) dopamine receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IID(2) dopamine receptorHomo sapiens (human)
negative regulation of insulin secretionD(2) dopamine receptorHomo sapiens (human)
acid secretionD(2) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(2) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(2) dopamine receptorHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityD(2) dopamine receptorHomo sapiens (human)
response to axon injuryD(2) dopamine receptorHomo sapiens (human)
branching morphogenesis of a nerveD(2) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(2) dopamine receptorHomo sapiens (human)
epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(2) dopamine receptorHomo sapiens (human)
release of sequestered calcium ion into cytosolD(2) dopamine receptorHomo sapiens (human)
dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of synapse structural plasticityD(2) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(2) dopamine receptorHomo sapiens (human)
excitatory postsynaptic potentialD(2) dopamine receptorHomo sapiens (human)
positive regulation of growth hormone secretionD(2) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeD(2) dopamine receptorHomo sapiens (human)
regulation of locomotion involved in locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
negative regulation of cellular response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor productionD(2) dopamine receptorHomo sapiens (human)
positive regulation of long-term synaptic potentiationD(2) dopamine receptorHomo sapiens (human)
hyaloid vascular plexus regressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of neuron migrationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(2) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAP kinase activityD(4) dopamine receptorHomo sapiens (human)
behavioral fear responseD(4) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(4) dopamine receptorHomo sapiens (human)
response to amphetamineD(4) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(4) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
adult locomotory behaviorD(4) dopamine receptorHomo sapiens (human)
positive regulation of sodium:proton antiporter activityD(4) dopamine receptorHomo sapiens (human)
positive regulation of kinase activityD(4) dopamine receptorHomo sapiens (human)
response to histamineD(4) dopamine receptorHomo sapiens (human)
social behaviorD(4) dopamine receptorHomo sapiens (human)
regulation of dopamine metabolic processD(4) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(4) dopamine receptorHomo sapiens (human)
fear responseD(4) dopamine receptorHomo sapiens (human)
regulation of circadian rhythmD(4) dopamine receptorHomo sapiens (human)
positive regulation of MAP kinase activityD(4) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(4) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(4) dopamine receptorHomo sapiens (human)
rhythmic processD(4) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(4) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(4) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(4) dopamine receptorHomo sapiens (human)
inhibitory postsynaptic potentialD(4) dopamine receptorHomo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalizationD(4) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(4) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerD(4) dopamine receptorHomo sapiens (human)
chemical synaptic transmissionD(4) dopamine receptorHomo sapiens (human)
detection of chemical stimulus involved in sensory perception of bitter tasteCarbonic anhydrase 6Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 6Homo sapiens (human)
smooth muscle contraction5-hydroxytryptamine receptor 7Homo sapiens (human)
circadian rhythm5-hydroxytryptamine receptor 7Homo sapiens (human)
blood circulation5-hydroxytryptamine receptor 7Homo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 7Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 7Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
response to ethanolD(3) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(3) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
learning or memoryD(3) dopamine receptorHomo sapiens (human)
learningD(3) dopamine receptorHomo sapiens (human)
locomotory behaviorD(3) dopamine receptorHomo sapiens (human)
visual learningD(3) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(3) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(3) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(3) dopamine receptorHomo sapiens (human)
response to histamineD(3) dopamine receptorHomo sapiens (human)
social behaviorD(3) dopamine receptorHomo sapiens (human)
response to cocaineD(3) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(3) dopamine receptorHomo sapiens (human)
response to morphineD(3) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(3) dopamine receptorHomo sapiens (human)
positive regulation of mitotic nuclear divisionD(3) dopamine receptorHomo sapiens (human)
acid secretionD(3) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(3) dopamine receptorHomo sapiens (human)
negative regulation of oligodendrocyte differentiationD(3) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(3) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(3) dopamine receptorHomo sapiens (human)
musculoskeletal movement, spinal reflex actionD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(3) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(3) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(3) dopamine receptorHomo sapiens (human)
positive regulation of dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(3) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(3) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(3) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(3) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(3) dopamine receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicCarbonic anhydrase 7Homo sapiens (human)
positive regulation of cellular pH reductionCarbonic anhydrase 7Homo sapiens (human)
neuron cellular homeostasisCarbonic anhydrase 7Homo sapiens (human)
regulation of chloride transportCarbonic anhydrase 7Homo sapiens (human)
regulation of intracellular pHCarbonic anhydrase 7Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 7Homo sapiens (human)
fatty acid metabolic processCytochrome P450 2J2Homo sapiens (human)
icosanoid metabolic processCytochrome P450 2J2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2J2Homo sapiens (human)
regulation of heart contractionCytochrome P450 2J2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2J2Homo sapiens (human)
linoleic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
organic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
response to hypoxiaCarbonic anhydrase 9Homo sapiens (human)
morphogenesis of an epitheliumCarbonic anhydrase 9Homo sapiens (human)
response to xenobiotic stimulusCarbonic anhydrase 9Homo sapiens (human)
response to testosteroneCarbonic anhydrase 9Homo sapiens (human)
secretionCarbonic anhydrase 9Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 9Homo sapiens (human)
synaptic transmission, dopaminergicD(2) dopamine receptorCanis lupus familiaris (dog)
hyaloid vascular plexus regressionD(2) dopamine receptorCanis lupus familiaris (dog)
response to bacteriumCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (58)

Processvia Protein(s)Taxonomy
zinc ion bindingCarbonic anhydrase 12Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 12Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
arylesterase activityCarbonic anhydrase 1Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 1Homo sapiens (human)
protein bindingCarbonic anhydrase 1Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 1Homo sapiens (human)
hydro-lyase activityCarbonic anhydrase 1Homo sapiens (human)
cyanamide hydratase activityCarbonic anhydrase 1Homo sapiens (human)
arylesterase activityCarbonic anhydrase 2Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 2Homo sapiens (human)
protein bindingCarbonic anhydrase 2Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 2Homo sapiens (human)
cyanamide hydratase activityCarbonic anhydrase 2Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 3Homo sapiens (human)
protein bindingCarbonic anhydrase 3Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 3Homo sapiens (human)
nickel cation bindingCarbonic anhydrase 3Homo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein kinase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-1B adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-2C adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
thioesterase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
heterotrimeric G-protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
norepinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2A adrenergic receptorHomo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(2) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(2) dopamine receptorHomo sapiens (human)
protein bindingD(2) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(2) dopamine receptorHomo sapiens (human)
dopamine bindingD(2) dopamine receptorHomo sapiens (human)
ionotropic glutamate receptor bindingD(2) dopamine receptorHomo sapiens (human)
identical protein bindingD(2) dopamine receptorHomo sapiens (human)
heterocyclic compound bindingD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(2) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(4) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(4) dopamine receptorHomo sapiens (human)
protein bindingD(4) dopamine receptorHomo sapiens (human)
potassium channel regulator activityD(4) dopamine receptorHomo sapiens (human)
SH3 domain bindingD(4) dopamine receptorHomo sapiens (human)
dopamine bindingD(4) dopamine receptorHomo sapiens (human)
identical protein bindingD(4) dopamine receptorHomo sapiens (human)
metal ion bindingD(4) dopamine receptorHomo sapiens (human)
epinephrine bindingD(4) dopamine receptorHomo sapiens (human)
norepinephrine bindingD(4) dopamine receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityD(4) dopamine receptorHomo sapiens (human)
neurotransmitter receptor activityD(4) dopamine receptorHomo sapiens (human)
serotonin bindingD(4) dopamine receptorHomo sapiens (human)
zinc ion bindingCarbonic anhydrase 6Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 6Homo sapiens (human)
protein binding5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 7Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 7Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
zinc ion bindingCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(3) dopamine receptorHomo sapiens (human)
protein bindingD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(3) dopamine receptorHomo sapiens (human)
zinc ion bindingCarbonic anhydrase 7Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 7Homo sapiens (human)
monooxygenase activityCytochrome P450 2J2Homo sapiens (human)
iron ion bindingCytochrome P450 2J2Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
isomerase activityCytochrome P450 2J2Homo sapiens (human)
linoleic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
hydroperoxy icosatetraenoate isomerase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 5,6-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
heme bindingCytochrome P450 2J2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2J2Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 9Homo sapiens (human)
protein bindingCarbonic anhydrase 9Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 9Homo sapiens (human)
molecular function activator activityCarbonic anhydrase 9Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 4Bos taurus (cattle)
carbonate dehydratase activityCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
zinc ion bindingCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (52)

Processvia Protein(s)Taxonomy
plasma membraneCarbonic anhydrase 12Homo sapiens (human)
membraneCarbonic anhydrase 12Homo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 12Homo sapiens (human)
apical plasma membraneCarbonic anhydrase 12Homo sapiens (human)
plasma membraneCarbonic anhydrase 12Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
cytosolCarbonic anhydrase 1Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 1Homo sapiens (human)
cytoplasmCarbonic anhydrase 2Homo sapiens (human)
cytosolCarbonic anhydrase 2Homo sapiens (human)
plasma membraneCarbonic anhydrase 2Homo sapiens (human)
myelin sheathCarbonic anhydrase 2Homo sapiens (human)
apical part of cellCarbonic anhydrase 2Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 2Homo sapiens (human)
cytoplasmCarbonic anhydrase 2Homo sapiens (human)
plasma membraneCarbonic anhydrase 2Homo sapiens (human)
apical part of cellCarbonic anhydrase 2Homo sapiens (human)
cytosolCarbonic anhydrase 3Homo sapiens (human)
cytosolCarbonic anhydrase 3Homo sapiens (human)
cytoplasmCarbonic anhydrase 3Homo sapiens (human)
cytoplasmAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
basolateral plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
neuronal cell bodyAlpha-2A adrenergic receptorHomo sapiens (human)
axon terminusAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic active zone membraneAlpha-2A adrenergic receptorHomo sapiens (human)
dopaminergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
postsynaptic density membraneAlpha-2A adrenergic receptorHomo sapiens (human)
glutamatergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
GABA-ergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
receptor complexAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
Golgi membraneD(2) dopamine receptorHomo sapiens (human)
acrosomal vesicleD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
ciliumD(2) dopamine receptorHomo sapiens (human)
lateral plasma membraneD(2) dopamine receptorHomo sapiens (human)
endocytic vesicleD(2) dopamine receptorHomo sapiens (human)
axonD(2) dopamine receptorHomo sapiens (human)
dendriteD(2) dopamine receptorHomo sapiens (human)
synaptic vesicle membraneD(2) dopamine receptorHomo sapiens (human)
sperm flagellumD(2) dopamine receptorHomo sapiens (human)
dendritic spineD(2) dopamine receptorHomo sapiens (human)
perikaryonD(2) dopamine receptorHomo sapiens (human)
axon terminusD(2) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(2) dopamine receptorHomo sapiens (human)
ciliary membraneD(2) dopamine receptorHomo sapiens (human)
non-motile ciliumD(2) dopamine receptorHomo sapiens (human)
dopaminergic synapseD(2) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(2) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(2) dopamine receptorHomo sapiens (human)
presynaptic membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
centrosomeD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(4) dopamine receptorHomo sapiens (human)
membraneD(4) dopamine receptorHomo sapiens (human)
postsynapseD(4) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(4) dopamine receptorHomo sapiens (human)
dendriteD(4) dopamine receptorHomo sapiens (human)
extracellular regionCarbonic anhydrase 6Homo sapiens (human)
extracellular spaceCarbonic anhydrase 6Homo sapiens (human)
cytosolCarbonic anhydrase 6Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 6Homo sapiens (human)
extracellular spaceCarbonic anhydrase 6Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
trans-Golgi network membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
synapse5-hydroxytryptamine receptor 7Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 7Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
mitochondrial matrixCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
mitochondrionCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
cytoplasmCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
mitochondrionCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
synapseD(3) dopamine receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
cytosolCarbonic anhydrase 7Homo sapiens (human)
cytoplasmCarbonic anhydrase 7Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2J2Homo sapiens (human)
extracellular exosomeCytochrome P450 2J2Homo sapiens (human)
cytoplasmCytochrome P450 2J2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2J2Homo sapiens (human)
nucleolusCarbonic anhydrase 9Homo sapiens (human)
plasma membraneCarbonic anhydrase 9Homo sapiens (human)
membraneCarbonic anhydrase 9Homo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 9Homo sapiens (human)
microvillus membraneCarbonic anhydrase 9Homo sapiens (human)
plasma membraneCarbonic anhydrase 9Homo sapiens (human)
side of membraneCarbonic anhydrase 4Bos taurus (cattle)
Golgi membraneD(2) dopamine receptorCanis lupus familiaris (dog)
mitochondrionCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
mitochondrial matrixCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
mitochondrionCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
cytoplasmCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (390)

Assay IDTitleYearJournalArticle
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID47748Inhibitory activity of compound against human carbonic anhydrase II2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the antipsychotic drug sulpiride.
AID1278409Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by CO2 hydrase stopped flow assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea.
AID238300Ki value against human carbonic anhydrase II (hCA II)2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs?
AID263639Selectivity for Helicobacter pylori recombinant CA over human recombinant CA22006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Carbonic anhydrase inhibitors: cloning and sulfonamide inhibition studies of a carboxyterminal truncated alpha-carbonic anhydrase from Helicobacter pylori.
AID597453Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID176655Subcutaneous dose to inhibit apomorphine-induced stereotyped behavior in 50% of rats1981Journal of medicinal chemistry, Oct, Volume: 24, Issue:10
Synthesis and neuroleptic activity of benzamides. Cis-N-(1-benzyl-2-methylpyrrolidin-3-yl)-5-chloro-2-methoxy-4-(methylamino)benzamide and related compounds.
AID242944Ratio of dopamine receptor D2 long and D3 ki values2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.
AID12234881-Octanol-water distribution coefficient, log D of the compound at pH 7.42012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Predicting phenolic acid absorption in Caco-2 cells: a theoretical permeability model and mechanistic study.
AID1209456Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID644381Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration assay2012Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
Cloning, characterization and sulfonamide inhibition studies of an α-carbonic anhydrase from the living fossil sponge Astrosclera willeyana.
AID236914Permeability Coefficient in hexadecane membranes model2005Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
Exploring the role of different drug transport routes in permeability screening.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID414961Inhibition of Mycobacterium tuberculosis H37Rv recombinant beta-carbonic anhydrase 1 expressed in Escherichia coli BL21 by stopped flow CO2 hydration method2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate.
AID1278412Inhibition of Pseudoalteromonas haloplanktis gamma carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea.
AID64438Inhibition of 0.1 nM of [125I]- (S)-N-(1-Ethyl-pyrrolidin-2-ylmethyl)-5-iodo-2-methoxy-benzamide binding in striatal homogenates of rat brain1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
(S)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-[125I]iodo- 2-methoxybenzamide hydrochloride, a new selective radioligand for dopamine D-2 receptors.
AID1067230Inhibition of human cytosolic carbonic anhydrase 1 by stopped-flow CO2 hydration assay2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties.
AID678712Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID19419Partition coefficient (logD7.4)1998Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7
Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes.
AID552129Inhibition of human recombinant CA6 by stopped-flow CO2 hydration assay2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata.
AID770581Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for human carbonic anhydrase 92013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID238316Ki value against human carbonic anhydrase XII (hCA XII)2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs?
AID1268965Inhibition of recombinant Thiomicrospira crunogena XCL-2 carbonic anhydrase by stopped flow CO2 hydrase assay2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Sulfonamide inhibition studies of the α-carbonic anhydrase from the gammaproteobacterium Thiomicrospira crunogena XCL-2, TcruCA.
AID293812Inhibition of human recombinant CA2 by stopped flow CO2 hydrase assay2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Carbonic anhydrase inhibitors: inhibition of cytosolic/tumor-associated isoforms I, II, and IX with iminodiacetic carboxylates/hydroxamates also incorporating benzenesulfonamide moieties.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1453410Inhibition of Francisella tularensis beta-carbonic anhydrase assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay
AID1916455Binding affinity to 5-HT7R (unknown origin) assessed as inhibition constant2021Bioorganic & medicinal chemistry letters, 10-01, Volume: 49Chemical update on the potential for serotonin 5-HT
AID1142836Inhibition of Legionella pneumophilia subsp. Pneumophila strain Philadelphia-1 carbonic anhydrase-1 assessed as CO2 hydrase activity by stopped-flow assay2014Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11
Sulfonamide inhibition studies of two β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila.
AID467613Volume of distribution at steady state in human2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID453203Lipophilicity, log D of the compound2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
Development of an in silico model for human skin permeation based on a Franz cell skin permeability assay.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID597458Displacement of [125I]DOI from 5HT2A receptor2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity.
AID1726079Inhibition of Vibrio cholerae beta carbonic anhydrase pre-incubated for 15 mins prior to testing by phenol red-based stopped-flow CO2 hydration assay2020ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
In Silico-Guided Identification of New Potent Inhibitors of Carbonic Anhydrases Expressed in
AID597455Displacement of [3H]8-OH-DPAT from 5HT1A receptor2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity.
AID1268964Inhibition of recombinant Sulfurihydrogenibium yellowstonense YO3AOP1 carbonic anhydrase by stopped flow CO2 hydrase assay2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Sulfonamide inhibition studies of the α-carbonic anhydrase from the gammaproteobacterium Thiomicrospira crunogena XCL-2, TcruCA.
AID349607Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase 1 encoded by Rv1284 by stopped flow CO2 hydration assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
AID238699Binding affinity for human dopamine receptor D2 long2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.
AID293813Inhibition of human recombinant CA9 by stopped flow CO2 hydrase assay2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Carbonic anhydrase inhibitors: inhibition of cytosolic/tumor-associated isoforms I, II, and IX with iminodiacetic carboxylates/hydroxamates also incorporating benzenesulfonamide moieties.
AID256964Inhibitory activity against human recombinant mitochondrial isozyme CA VA2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors.
AID156204Binding to POPC/GMI liposomes using biosensor system2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
SPR biosensor studies of the direct interaction between 27 drugs and a liposome surface: correlation with fraction absorbed in humans.
AID644380Inhibition of human recombinant carbonic anhydrase 1 after 15 mins by stopped flow CO2 hydration assay2012Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
Cloning, characterization and sulfonamide inhibition studies of an α-carbonic anhydrase from the living fossil sponge Astrosclera willeyana.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1194027Inhibition of recombinant Porphyromonas gingivalis gamma-carbonic anhydrase by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic cyanobacterium Nostoc commune.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1060765Inhibition of human recombinant carbonic anhydrase 7 preincubated for 15 mins by stopped flow CO2 hydration assay2014European journal of medicinal chemistry, Jan, Volume: 71Structure-based screening for the discovery of new carbonic anhydrase VII inhibitors.
AID369275Inhibition of mouse recombinant carbonic anhydrase 15 by stopped flow CO2 hydrase assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
AID678713Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID28925Highest effective permeability across hexadecane membrane (pH 4-8)2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes.
AID678714Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID552130Inhibition of Stylophora pistillata carbonic anhydrase by stopped-flow CO2 hydration assay2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata.
AID1262263Inhibition of human CA1 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23
Anion and sulfonamide inhibition studies of an α-carbonic anhydrase from the Antarctic hemoglobinless fish Chionodraco hamatus.
AID367821Inhibition of human recombinant CA2 by stopped-flow CO2 hydrase assay2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Carbonic anhydrase inhibitors: inhibition of the beta-class enzyme from the yeast Saccharomyces cerevisiae with sulfonamides and sulfamates.
AID64439Inhibition of [3H](S)-sulpiride binding in striatal homogenates of rat brain1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
(S)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-[125I]iodo- 2-methoxybenzamide hydrochloride, a new selective radioligand for dopamine D-2 receptors.
AID237585Tested for fraction of oral dose absorbed orally in humans2005Journal 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).
AID1194026Inhibition of recombinant Methanosarcina thermophila gamma-carbonic anhydrase by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic cyanobacterium Nostoc commune.
AID1453413Inhibition of human carbonic anhydrase-2 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay
AID678717Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1434427Inhibition of recombinant human carbonic anhydrase 1 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis
AID1215122Percentage unbound in solid supported porcine brain membrane vesicles at 5 uM by TRANSIL assay2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID299249Inhibition of Helicobacter pylori alpha carbonic anhydrase by stopped-flow CO2 hydrase assay2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors.
AID1194024Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic cyanobacterium Nostoc commune.
AID29844Fraction absorbed after oral administration in humans2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Experimental and computational screening models for the prediction of intestinal drug absorption.
AID293811Inhibition of human recombinant CA1 by stopped flow CO2 hydrase assay2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Carbonic anhydrase inhibitors: inhibition of cytosolic/tumor-associated isoforms I, II, and IX with iminodiacetic carboxylates/hydroxamates also incorporating benzenesulfonamide moieties.
AID725956Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Cloning, characterization, and sulfonamide and thiol inhibition studies of an α-carbonic anhydrase from Trypanosoma cruzi, the causative agent of Chagas disease.
AID367820Inhibition of human recombinant CA1 by stopped-flow CO2 hydrase assay2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Carbonic anhydrase inhibitors: inhibition of the beta-class enzyme from the yeast Saccharomyces cerevisiae with sulfonamides and sulfamates.
AID271175Selectivity for human recombinant carbonic anhydrase 9 over carbonic anhydrase 22006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX.
AID238274Binding affinity for Dopamine receptor D42005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.
AID612731Inhibition of Salmonella Typhimurium recombinant carbonic anhydrase 1 at pH 8.3 by stopped flow CO2 hydration assay2011Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates.
AID552131Inhibition of Stylophora pistillata carbonic anhydrase 2 by stopped-flow CO2 hydration assay2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata.
AID231333Ratio of [(apical to basal)/(basal to apical)] (Caco-2 cell monolayer)2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Experimental and computational screening models for the prediction of intestinal drug absorption.
AID1916460Binding affinity to D2R (unknown origin) assessed as inhibition constant2021Bioorganic & medicinal chemistry letters, 10-01, Volume: 49Chemical update on the potential for serotonin 5-HT
AID261582Selectivity ratio for human carbonic anhydrase 2 over Helicobacter pylori carbonic anhydrase2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs.
AID29812Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID242945Ratio of dopamine receptor D2 long and D4 ki values2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.
AID1190065Inhibition of Plasmodium falciparum Eta-carbonic anhydrase pre-incubated for 15 mins before CO2 substrate addition by stopped-flow CO2 hydration assay2015Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
Sulfonamide inhibition studies of the η-class carbonic anhydrase from the malaria pathogen Plasmodium falciparum.
AID436563Inhibition of human recombinant CA1 by stopped-flow CO2 assay2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Carbonic anhydrase inhibitors. Inhibition studies of a coral secretory isoform by sulfonamides.
AID65423Compound was tested for its ability to displace [3H]- spiperone from Dopamine receptor D2 in rat striatal membranes1989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
Synthesis and D2 dopaminergic activity of pyrrolidinium, tetrahydrothiophenium, and tetrahydrothiophene analogues of sulpiride.
AID678721Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1262266Inhibition of weddell seal alphaCA incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23
Anion and sulfonamide inhibition studies of an α-carbonic anhydrase from the Antarctic hemoglobinless fish Chionodraco hamatus.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID743515Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by CO2 hydration stopped-flow assay2013Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6
The alpha-carbonic anhydrase from the thermophilic bacterium Sulfurihydrogenibium yellowstonense YO3AOP1 is highly susceptible to inhibition by sulfonamides.
AID1188135Inhibition of human recombinant Carbonic anhydrase 2 compound preincubated for 15 mins by stopped flow CO2 hydrase assay method2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID28679Partition coefficient (logD6.8)2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes.
AID694812Binding affinity bovine carbonic anhydrase2010ACS medicinal chemistry letters, Sep-09, Volume: 1, Issue:6
Labeled Ligand Displacement: Extending NMR-Based Screening of Protein Targets.
AID597452Antagonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity.
AID271173Inhibition of human recombinant carbonic anhydrase 2 by stopped-flow CO2 hydrase assay2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID177972Compound was evaluated in vivo its antagonist activity against apomorphine induced behavioral syndrome such as Stereotypy in rat after intraperitoneal administration; activity value ranges from 198-2381985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Potential neuroleptic agents. 3. Chemistry and antidopaminergic properties of substituted 6-methoxysalicylamides.
AID612732Inhibition of Salmonella Typhimurium recombinant carbonic anhydrase 2 at pH 8.3 by stopped flow CO2 hydration assay2011Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates.
AID1061068Inhibition of Leishmania donovani chagasi recombinant beta-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Sulfonamide inhibition studies of the δ-carbonic anhydrase from the diatom Thalassiosira weissflogii.
AID1262264Inhibition of human CA2 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23
Anion and sulfonamide inhibition studies of an α-carbonic anhydrase from the Antarctic hemoglobinless fish Chionodraco hamatus.
AID1142834Inhibition of human carbonic anhydrase-2 by stopped-flow CO2 hydration assay2014Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11
Sulfonamide inhibition studies of two β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila.
AID271174Inhibition of human recombinant carbonic anhydrase 9 by stopped-flow CO2 hydrase assay2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX.
AID28924Effective permeability (Pe) across a hexadecane membrane (pH 6.8)2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes.
AID678722Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1067225Selectivity ratio of Ki for human transmembrane carbonic anhydrase 2 to Ki for human cytosolic carbonic anhydrase 122014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1240215Inhibition of Pseudoalteromonas haloplanktis gamma carbonic anhydrase by CO2 hydration assay2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis.
AID275815Selectivity for human CA VI over human CA II2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors.
AID1291363Inhibition of recombinant Vibrio cholerae gamma-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8
Comparison of the sulfonamide inhibition profiles of the α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae.
AID311934Dissociation constant, pKa of the compound2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID261580Inhibition of human recombinant carbonic anhydrase 2 by stopped-flow CO2 hydrase assay2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID711212Inhibition of recombinant Vibrio cholerae carbonic anhydrase expressed in Escherichia coli (DE3) preincubated for 15 mins by stopped-flow CO2 hydrase assay2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
DNA cloning, characterization, and inhibition studies of an α-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae.
AID63414Compound was evaluated for its ability to inhibit the potassium -induced release of [3H]- acetylcholine release in mouse striatal membranes by stimulating Dopamine receptor D21989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
Synthesis and D2 dopaminergic activity of pyrrolidinium, tetrahydrothiophenium, and tetrahydrothiophene analogues of sulpiride.
AID1484186Allosteric antagonist activity at D3 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of dopamine induced beta-arrestin recruitment after 90 mins by DiscoveRx PathHunter assay
AID669119Inhibition of GST-tagged Malassezia globosa ATCC 96807/CBS 7966 MG-CA expressed in Escherichia coli BL21(DE3) cells preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target.
AID1275912Inhibition of human Carbonic anhydrase2 using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Sulfonamide inhibition studies of the β-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae.
AID612725Inhibition of human recombinant carbonic anhydrase 1 at pH 7.5 by stopped flow CO2 hydration assay2011Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates.
AID770584Inhibition of human cytosolic carbonic anhydrase 7 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID467612Fraction unbound in human plasma2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID669115Inhibition of human carbonic anhydrase 2 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target.
AID349606Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID669116Inhibition of Cryptococcus neoformans Can2 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target.
AID275816Selectivity for human CA VI over human CA I2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors.
AID1278413Inhibition of recombinant Colwellia psychrerythraea gamma carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea.
AID236916Percentage of mass balance in hexadecane membranes model2005Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
Exploring the role of different drug transport routes in permeability screening.
AID744415Inhibition of recombinant full length Candida glabrata NCE103 expressed in Escherichia coli BL21 preincubated for 15 mins by stopped-flow CO2 hydrase assay2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Carbonic anhydrase inhibitors: inhibition of the β-class enzyme from the pathogenic yeast Candida glabrata with sulfonamides, sulfamates and sulfamides.
AID699934Inverse agonist activity at human D2S receptor expressed in HEK293T cells coexpressing GalphaoA-91-Rluc8 and mVenus-Gbeta1gamma2 after 2 mins by bioluminescence resonance energy transfer assay relative to dopamine2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
Molecular determinants of selectivity and efficacy at the dopamine D3 receptor.
AID1190064Inhibition of human recombinant carbonic anhydrase 2 by stopped-flow CO2 hydration assay2015Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
Sulfonamide inhibition studies of the η-class carbonic anhydrase from the malaria pathogen Plasmodium falciparum.
AID577526Inhibition of human carbonic anhydrase I by spectrophotometry at pH 7.52011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
A new β-carbonic anhydrase from Brucella suis, its cloning, characterization, and inhibition with sulfonamides and sulfamates, leading to impaired pathogen growth.
AID1204106Inhibition of recombinant Streptococcus mutans UA159 beta-carbonic anhydrase expressed in Escherichia coli Arctic cells preincubated for 15 mins by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
Sulfonamide inhibition study of the β-class carbonic anhydrase from the caries producing pathogen Streptococcus mutans.
AID156202Binding to POPC (palmitoyl-oleolyl-phosphatidyl-choline) liposomes using biosensor system2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
SPR biosensor studies of the direct interaction between 27 drugs and a liposome surface: correlation with fraction absorbed in humans.
AID1195371Inhibition of Anopheles gambiae carbonic anhydrase pre-incubated for 15 mins by stopped-flow CO2 hydration assay2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
The β-carbonic anhydrase from the malaria mosquito Anopheles gambiae is highly inhibited by sulfonamides.
AID1453411Inhibition of Burkholderia pseudomallei beta-carbonic anhydrase assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay
AID577527Inhibition of human carbonic anhydrase II by spectrophotometry at pH 7.52011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
A new β-carbonic anhydrase from Brucella suis, its cloning, characterization, and inhibition with sulfonamides and sulfamates, leading to impaired pathogen growth.
AID427122Inhibition of Candida albicans recombinant Nce103 by stopped-flow CO2 hydration assay2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides.
AID743513Inhibition of Helicobacter pylori recombinant alpha carbonic anhydrase preincubated for 15 mins by CO2 hydration stopped-flow assay2013Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6
The alpha-carbonic anhydrase from the thermophilic bacterium Sulfurihydrogenibium yellowstonense YO3AOP1 is highly susceptible to inhibition by sulfonamides.
AID1413588Displacement of [3H]-sulpiride from human D3 receptor expressed in HEK293 cells at 100 nM after 150 mins by liquid scintillation counting method relative to control2018MedChemComm, Sep-01, Volume: 9, Issue:9
Design, synthesis, and evaluation of bitopic arylpiperazine-phthalimides as selective dopamine D
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1061067Inhibition of Porphyromonas gingivalis recombinant gamma-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Sulfonamide inhibition studies of the δ-carbonic anhydrase from the diatom Thalassiosira weissflogii.
AID275808Inhibition of human recombinant cytosolic isozyme CA II by stopped-flow CO2 hydrase method2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors.
AID1188138Inhibition of Porphyromonas gingivalis Gamma-carbonic anhydrase compound preincubated for 15 mins by stopped flow CO2 hydrase assay method2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes.
AID1275910Inhibition of Vibrio cholerae beta-carbonic anhydrase using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Sulfonamide inhibition studies of the β-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae.
AID28399Cellular permeability (Pc) (Caco-2 cell monolayer)2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Experimental and computational screening models for the prediction of intestinal drug absorption.
AID60018Inhibition of apomorphine induced emesis in dogs following p.o. administration.1984Journal of medicinal chemistry, Sep, Volume: 27, Issue:9
Synthesis and neuroleptic activity of N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxy-5-sulfonamidobenzamide s.
AID764717Inhibition of human cytosolic carbonic anhydrase 7 preincubated for 15 mins by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Carbonic anhydrase inhibitors: Synthesis and inhibition of the cytosolic mammalian carbonic anhydrase isoforms I, II and VII with benzene sulfonamides incorporating 4,5,6,7-tetrachlorophthalimide moiety.
AID252345Amount of cGMP level in rat neostriatal membranes after incubation at 1.0 uM2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Preparation and pharmacological characterization of trans-2-amino-5(6)-fluoro-6(5)-hydroxy-1-phenyl-2,3-dihydro-1H-indenes as D2-like dopamine receptor agonists.
AID1067229Inhibition of human cytosolic carbonic anhydrase 2 by stopped-flow CO2 hydration assay2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties.
AID770583Inhibition of human membrane bound carbonic anhydrase 9 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID644379Inhibition of GST-tagged astrosclera willeyana Astrosclerin-3 expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay2012Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
Cloning, characterization and sulfonamide inhibition studies of an α-carbonic anhydrase from the living fossil sponge Astrosclera willeyana.
AID1067227Inhibition of human transmembrane carbonic anhydrase 12 by stopped-flow CO2 hydration assay2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties.
AID1240216Inhibition of Methanosarcina thermophila recombinant gamma carbonic anhydrase by stopped flow CO2 hydrase assay method2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis.
AID455986Permeability across human Caco-2 cells2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain.
AID1061066Inhibition of Thalassiosira weissflogii delta carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Sulfonamide inhibition studies of the δ-carbonic anhydrase from the diatom Thalassiosira weissflogii.
AID436564Inhibition of human recombinant CA2 by stopped-flow CO2 assay2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Carbonic anhydrase inhibitors. Inhibition studies of a coral secretory isoform by sulfonamides.
AID597446Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity.
AID414955Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration method2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate.
AID467611Dissociation constant, pKa of the compound2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1067226Selectivity ratio of Ki for human transmembrane carbonic anhydrase 2 to Ki for human cytosolic carbonic anhydrase 92014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties.
AID1434428Inhibition of human carbonic anhydrase 2 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis
AID1061170Inhibition of Porphyromonas gingivalis gamma-carbonic anhydrase expressed in Escherichia coli preincubated for 15 mins by stopped flow CO2 hydration assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the oral pathogen Porphyromonas gingivalis.
AID1209455Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID369272Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydrase assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID299243Inhibition of human carbonic anhydrase 2 by stopped-flow CO2 hydrase assay2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors.
AID367822Inhibition of Saccharomyces cerevisiae recombinant CA expressed in Escherichia coli by stopped-flow CO2 hydrase assay2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Carbonic anhydrase inhibitors: inhibition of the beta-class enzyme from the yeast Saccharomyces cerevisiae with sulfonamides and sulfamates.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1061069Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Sulfonamide inhibition studies of the δ-carbonic anhydrase from the diatom Thalassiosira weissflogii.
AID62570The IC50 value was reported as apparent, since [3H]NCA was purported to be irreversible (dopamine receptor from Canine striatal membranes). Result indicates the mean of two separate experiments, each performed in triplicate.1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
Aporphines. 58. N-(2-chloroethyl) [8,9-2H]norapomorphine, an irreversible ligand for dopamine receptors: synthesis and application.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID770582Inhibition of human membrane bound carbonic anhydrase 12 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID669117Inhibition of Candida albicans CaNce103 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target.
AID311933Inhibition of ASM in rat PC12 cells assessed as residual activity at 10 uM2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID1484195Competitive antagonist activity at D2 long receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of dopamine induced beta-arrestin recruitment after 90 mins by DiscoveRx PathHunter assay
AID1194028Inhibition of recombinant Nostoc commune gamma-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic cyanobacterium Nostoc commune.
AID1262267Inhibition of Chionodraco hamatus alphaCA incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23
Anion and sulfonamide inhibition studies of an α-carbonic anhydrase from the Antarctic hemoglobinless fish Chionodraco hamatus.
AID437750Inhibition of full length Mycobacterium tuberculosis H37Rv recombinant carbonic anhydrase 2 encoded by RV3588c by stopped flow CO2 hydration assay2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Carbonic anhydrase inhibitors. Characterization and inhibition studies of the most active beta-carbonic anhydrase from Mycobacterium tuberculosis, Rv3588c.
AID597456Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity.
AID1223490Apparent permeability across human differentiated Caco2 cells2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Predicting phenolic acid absorption in Caco-2 cells: a theoretical permeability model and mechanistic study.
AID567091Drug absorption in human assessed as human intestinal absorption rate2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Prediction of drug intestinal absorption by new linear and non-linear QSPR.
AID1287517Inhibition of human carbonic anhydrase 1 incubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Sulfonamide inhibition studies of the β-carbonic anhydrase from the newly discovered bacterium Enterobacter sp. B13.
AID18847Percent of drug absorbed by human intestine after oral administration2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties.
AID64789Affinity constant of compound was evaluated in rat striatum tissue preparation.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Dopamine D-2 receptor imaging radiopharmaceuticals: synthesis, radiolabeling, and in vitro binding of (R)-(+)- and (S)-(-)-3-iodo-2-hydroxy-6-methoxy-N- [(1-ethyl-2-pyrrolidinyl)methyl]benzamide.
AID552128Inhibition of human recombinant CA2 by stopped-flow CO2 hydration assay2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata.
AID1275911Inhibition of Vibrio cholerae alpha-carbonic anhydrase using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Sulfonamide inhibition studies of the β-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae.
AID612726Inhibition of human recombinant carbonic anhydrase 2 at pH 7.5 by stopped flow CO2 hydration assay2011Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID48112Inhibitory activity of compound against bovine carbonic anhydrase IV2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the antipsychotic drug sulpiride.
AID1628036Inhibition of full length human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stop flow CO2 hydrase assay2016Bioorganic & medicinal chemistry letters, 09-01, Volume: 26, Issue:17
Cloning, expression, purification and sulfonamide inhibition profile of the complete domain of the η-carbonic anhydrase from Plasmodium falciparum.
AID238276Ki value against human carbonic anhydrase I (hCA I)2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs?
AID770585Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID29845Estimation of fraction absorbed (Fa) in the human intestine using biosensor technology.2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
SPR biosensor studies of the direct interaction between 27 drugs and a liposome surface: correlation with fraction absorbed in humans.
AID1188134Inhibition of human recombinant Carbonic anhydrase 1 compound preincubated for 15 mins by stopped flow CO2 hydrase assay method2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes.
AID28234% absorbed in human GI-tract2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes.
AID64609Tested in vitro for inhibition of [3H]spiperone binding to dopamine receptor D21993Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22
Conformationally restricted analogues of remoxipride as potential antipsychotic agents.
AID369271Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydrase assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID271172Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydrase assay2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1240214Inhibition of Nostoc commune gamma carbonic anhydrase by CO2 hydration assay2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis.
AID50344Inhibitory activity of compound against human carbonic anhydrase I2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the antipsychotic drug sulpiride.
AID1215126Ratio of fraction unbound in Wistar rat brain homogenate at 5 uM after 5 hrs by equilibrium dialysis method to fraction unbound in solid supported porcine brain membrane vesicles at 5 uM by TRANSIL assay2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID1215121Fraction unbound in Wistar rat brain homogenate at 5 uM after 5 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID369273Inhibition of human full length recombinant carbonic anhydrase 6 by stopped flow CO2 hydrase assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
AID436565Inhibition of cloned Stylophora pistillata alpha-CA expressed in human HEK293 cells by stopped-flow CO2 assay2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Carbonic anhydrase inhibitors. Inhibition studies of a coral secretory isoform by sulfonamides.
AID743514Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by CO2 hydration stopped-flow assay2013Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6
The alpha-carbonic anhydrase from the thermophilic bacterium Sulfurihydrogenibium yellowstonense YO3AOP1 is highly susceptible to inhibition by sulfonamides.
AID28392Apparent permeability coefficient (Papp) (Caco-2 cell monolayer)2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Experimental and computational screening models for the prediction of intestinal drug absorption.
AID699932Competitive antagonist activity at human D2S receptor expressed in HEK293T cells coexpressing GalphaoA-91-Rluc8 and mVenus-Gbeta1gamma2 assessed as rightward shift in dopamine-induced effect at 100 nM after 2 mins by bioluminescence resonance energy trans2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
Molecular determinants of selectivity and efficacy at the dopamine D3 receptor.
AID427124Inhibition of Helicobacter pylori beta-carbonic anhydrase by stopped-flow CO2 hydration assay2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides.
AID61052The dissociation constant for the inhibition of agonist effect on the K+ evoked release of [3H]- acetylcholine in mouse striatal membranes1989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
Synthesis and D2 dopaminergic activity of pyrrolidinium, tetrahydrothiophenium, and tetrahydrothiophene analogues of sulpiride.
AID20050Human absorption A (%)1998Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7
Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes.
AID252344Amount of cGMP level in rat neostriatal membranes after incubation at 0.1 uM2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Preparation and pharmacological characterization of trans-2-amino-5(6)-fluoro-6(5)-hydroxy-1-phenyl-2,3-dihydro-1H-indenes as D2-like dopamine receptor agonists.
AID131391Inhibition of apomorphine induced climbing in mice following p.o. administration.1984Journal of medicinal chemistry, Sep, Volume: 27, Issue:9
Synthesis and neuroleptic activity of N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxy-5-sulfonamidobenzamide s.
AID349608Inhibition of full length Mycobacterium tuberculosis H37Rv recombinant carbonic anhydrase 3 expressed in Escherichia coli BL21 by stopped flow CO2 hydration assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID743512Inhibition of Sulfurihydrogenibium yellowstonense YO3AOP1 recombinant carbonic anhydrase preincubated for 15 mins by CO2 hydration stopped-flow assay2013Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6
The alpha-carbonic anhydrase from the thermophilic bacterium Sulfurihydrogenibium yellowstonense YO3AOP1 is highly susceptible to inhibition by sulfonamides.
AID1268962Inhibition of recombinant human carbonic anhydrase-1 by stopped flow CO2 hydrase assay2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Sulfonamide inhibition studies of the α-carbonic anhydrase from the gammaproteobacterium Thiomicrospira crunogena XCL-2, TcruCA.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID261579Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydrase assay2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs.
AID539464Solubility of the compound in 0.1 M phosphate buffer at 600 uM at pH 7.4 after 24 hrs by LC/MS/MS analysis2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.
AID256963Inhibitory activity against human recombinant cytosolic CA22005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors.
AID414956Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration method2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate.
AID1484181Competitive antagonist activity at D3 receptor (unknown origin) expressed in CHOK1 cells assessed as induction of rightward shift in the dopamine dose response curve for beta-arrestin recruitment after 90 mins by DiscoveRx PathHunter assay
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1142837Inhibition of Legionella pneumophilia subsp. Pneumophila strain Philadelphia-1 carbonic anhydrase-2 assessed as CO2 hydrase activity by stopped-flow assay2014Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11
Sulfonamide inhibition studies of two β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila.
AID577530Inhibition of Brucella suis carbonic anhydrase II by spectrophotometry at pH 8.32011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
A new β-carbonic anhydrase from Brucella suis, its cloning, characterization, and inhibition with sulfonamides and sulfamates, leading to impaired pathogen growth.
AID678716Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID263636Inhibition of human recombinant CA12006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Carbonic anhydrase inhibitors: cloning and sulfonamide inhibition studies of a carboxyterminal truncated alpha-carbonic anhydrase from Helicobacter pylori.
AID1188137Inhibition of Porphyromonas gingivalis Beta-carbonic anhydrase compound preincubated for 15 mins by stopped flow CO2 hydrase assay method2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes.
AID299250Inhibition of Helicobacter pylori beta carbonic anhydrase by stopped-flow CO2 hydrase assay2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors.
AID1210069Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID299242Inhibition of human carbonic anhydrase 1 by stopped-flow CO2 hydrase assay2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors.
AID1628038Inhibition of recombinant Plasmodium falciparum eta-carbonic anhydrase (181 to 538 residues) expressed in Escherichia coli artic express (DE3) preincubated for 15 mins by stop flow CO2 hydrase assay2016Bioorganic & medicinal chemistry letters, 09-01, Volume: 26, Issue:17
Cloning, expression, purification and sulfonamide inhibition profile of the complete domain of the η-carbonic anhydrase from Plasmodium falciparum.
AID459696Inhibition of Brucella suis CA1 expressed in Escherichia coli BL21(DE3) by stopped-flow CO2-hydration assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Cloning, characterization, and inhibition studies of a beta-carbonic anhydrase from Brucella suis.
AID1268963Inhibition of recombinant human carbonic anhydrase-2 by stopped flow CO2 hydrase assay2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Sulfonamide inhibition studies of the α-carbonic anhydrase from the gammaproteobacterium Thiomicrospira crunogena XCL-2, TcruCA.
AID369274Inhibition of human recombinant carbonic anhydrase 9 catalytic domain by stopped flow CO2 hydrase assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
AID15120Percent of the drug absorbed after administration to humans was determined1999Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
Molecular hashkeys: a novel method for molecular characterization and its application for predicting important pharmaceutical properties of molecules.
AID1061169Inhibition of recombinant Methanosarcina thermophila gamma-CA CAM by stopped flow CO2 hydration assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the oral pathogen Porphyromonas gingivalis.
AID770586Inhibition of human cytosolic carbonic anhydrase 1 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID229193Inhibition of specific binding of [3H]NANM of sigma receptor in Guinea pig brain membranes1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites.
AID1194025Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic cyanobacterium Nostoc commune.
AID177799Compound was evaluated in vivo for antagonist activity against apomorphine induced behavioral syndrome such as Hyperactivity in rat after intraperitoneal administration; activity value ranges from 62.7-68.51985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Potential neuroleptic agents. 3. Chemistry and antidopaminergic properties of substituted 6-methoxysalicylamides.
AID275817Selectivity for human CA VI over human CA IX2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors.
AID65133Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybrid pharmacophore- and structure-based database searching approach.
AID1195370Inhibition of human carbonic anhydrase 2 pre-incubated for 15 mins by stopped-flow CO2 hydration assay2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
The β-carbonic anhydrase from the malaria mosquito Anopheles gambiae is highly inhibited by sulfonamides.
AID1067228Inhibition of human transmembrane carbonic anhydrase 9 by stopped-flow CO2 hydration assay2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties.
AID1434429Inhibition of Burkholderia pseudomallei Gamma-carbonic anhydrase assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis
AID256967Selectivity ratio for human CA VB over human CA VA2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors.
AID1190063Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydration assay2015Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
Sulfonamide inhibition studies of the η-class carbonic anhydrase from the malaria pathogen Plasmodium falciparum.
AID238350Binding affinity for human dopamine receptor D32005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID62467Compound was evaluated for the competitive binding of [3H]NCA to dopamine receptor from Canine striatal membranes1984Journal 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.
AID243011Selectivity ratio against human carbonic anhydrases II and XII2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs?
AID1142838Inhibition of Helicobacter pylori carbonic anhydrase by stopped-flow CO2 hydration assay2014Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11
Sulfonamide inhibition studies of two β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila.
AID293814Selectivity for human recombinant CA9 over human recombinant CA22007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Carbonic anhydrase inhibitors: inhibition of cytosolic/tumor-associated isoforms I, II, and IX with iminodiacetic carboxylates/hydroxamates also incorporating benzenesulfonamide moieties.
AID261581Inhibition of Helicobacter pylori recombinant carbonic anhydrase by stopped-flow CO2 hydrase assay2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs.
AID778725Inhibition of recombinant Leishmania donovani chagasi beta-carbonic anhydrase expressed in baculovirus infected insect Sf9 cells incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Leishmania donovani chagasi, the protozoan parasite responsible for leishmaniasis.
AID349605Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
AID275806Inhibition of full length human recombinant CA VI2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID427123Inhibition of Cryptococcus neoformans recombinant Can2 by stopped-flow CO2 hydration assay2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides.
AID63020In vitro ability to displace [3H]spiroperidol from rat dopamine receptor1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
2-Amino-6-chloro-4-(N-methylpiperazino)pyrimidines, inhibitors of spiroperidol binding.
AID64295In vitro binding affinity at Dopamine receptor D2 in rat by displacing [3H]- spiperone from rat striatal membrane1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Potential neuroleptic agents. 3. Chemistry and antidopaminergic properties of substituted 6-methoxysalicylamides.
AID764718Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Carbonic anhydrase inhibitors: Synthesis and inhibition of the cytosolic mammalian carbonic anhydrase isoforms I, II and VII with benzene sulfonamides incorporating 4,5,6,7-tetrachlorophthalimide moiety.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID311935Partition coefficient, log P of the compound2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID1287520Inhibition of recombinant Enterobacter sp. B13 beta carbonic anhydrase incubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Sulfonamide inhibition studies of the β-carbonic anhydrase from the newly discovered bacterium Enterobacter sp. B13.
AID476929Human intestinal absorption in po dosed human2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
AID236268Fraction absorbed in human intestine after oral administration compound was measured2005Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
Exploring the role of different drug transport routes in permeability screening.
AID427125Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydrase method2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides.
AID1278410Inhibition of Porphyromonas gingivalis gamma carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea.
AID256966Selectivity ratio for human CA VB over human CA22005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors.
AID699933Inverse agonist activity at human D3R receptor expressed in HEK293T cells coexpressing GalphaoA-91-Rluc8 and mVenus-Gbeta1gamma2 after 2 mins by bioluminescence resonance energy transfer assay relative to dopamine2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
Molecular determinants of selectivity and efficacy at the dopamine D3 receptor.
AID1413589Displacement of [3H]-sulpiride from human D2 receptor expressed in HEK293 cells at 100 nM after 150 mins by liquid scintillation counting method relative to control2018MedChemComm, Sep-01, Volume: 9, Issue:9
Design, synthesis, and evaluation of bitopic arylpiperazine-phthalimides as selective dopamine D
AID699931Competitive antagonist activity at human D3 receptor expressed in HEK293T cells coexpressing GalphaoA-91-Rluc8 and mVenus-Gbeta1gamma2 assessed as rightward shift in dopamine-induced effect at 100 nM after 2 mins by bioluminescence resonance energy transf2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
Molecular determinants of selectivity and efficacy at the dopamine D3 receptor.
AID1240217Inhibition of human recombinant carbonic anhydrase-2 by stopped flow CO2 hydrase assay method2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis.
AID592681Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID275807Inhibition of human recombinant cytosolic isozyme CA I by stopped-flow CO2 hydrase method2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors.
AID678715Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1278411Inhibition of Nostoc commune gamma carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea.
AID65253Binding affinity which represents concentration giving half-maximal inhibition of [3H]spiperone (Dopamine receptor D2) binding to rat tissue homogenate1998Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20
New antipsychotic agents with serotonin and dopamine antagonist properties based on a pyrrolo[2,1-b][1,3]benzothiazepine structure.
AID552127Inhibition of human recombinant CA1 by stopped-flow CO2 hydration assay2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata.
AID725955Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Cloning, characterization, and sulfonamide and thiol inhibition studies of an α-carbonic anhydrase from Trypanosoma cruzi, the causative agent of Chagas disease.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID437749Inhibition of human recombinant CA2 by stopped-flow hydration assay2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Carbonic anhydrase inhibitors. Characterization and inhibition studies of the most active beta-carbonic anhydrase from Mycobacterium tuberculosis, Rv3588c.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1434430Inhibition of Vibrio cholerae Gamma-carbonic anhydrase assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis
AID1190066Selectivity index, ratio of Ki for Trypanosoma cruzi carbonic anhydrase to Ki for Plasmodium falciparum Eta-carbonic anhydrase2015Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
Sulfonamide inhibition studies of the η-class carbonic anhydrase from the malaria pathogen Plasmodium falciparum.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID577531Inhibition of Brucella suis carbonic anhydrase I by spectrophotometry at pH 8.32011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
A new β-carbonic anhydrase from Brucella suis, its cloning, characterization, and inhibition with sulfonamides and sulfamates, leading to impaired pathogen growth.
AID1916467Binding affinity to D3R (unknown origin) assessed as inhibition constant2021Bioorganic & medicinal chemistry letters, 10-01, Volume: 49Chemical update on the potential for serotonin 5-HT
AID1188136Inhibition of Helicobacter pylori Beta-carbonic anhydrase compound preincubated for 15 mins by stopped flow CO2 hydrase assay method2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes.
AID176324In vivo blocking of apomorphine induced stereotypies following 1 mg/kg i.p. in rats after 60 min.1982Journal of medicinal chemistry, Nov, Volume: 25, Issue:11
Potential neuroleptic agents. 2,6-Dialkoxybenzamide derivatives with potent dopamine receptor blocking activities.
AID236913Permeability Coefficient in Caco-2 cell culture model2005Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
Exploring the role of different drug transport routes in permeability screening.
AID1607338Antagonist activity at human D2R expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 120 mins by beta-galactosidase based PathHunter assay2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D
AID1275913Inhibition of human Carbonic anhydrase1 using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Sulfonamide inhibition studies of the β-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae.
AID453204Permeability in human skin after 48 hrs by Franz cell permeability assay2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
Development of an in silico model for human skin permeation based on a Franz cell skin permeability assay.
AID1287518Inhibition of human carbonic anhydrase 2 incubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Sulfonamide inhibition studies of the β-carbonic anhydrase from the newly discovered bacterium Enterobacter sp. B13.
AID1484185Antagonist activity at D2 long receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of dopamine induced beta-arrestin recruitment after 90 mins by DiscoveRx PathHunter assay
AID1209457Unbound Cmax in human plasma2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID134562Toxicity in mice following p.o. administration.1984Journal of medicinal chemistry, Sep, Volume: 27, Issue:9
Synthesis and neuroleptic activity of N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxy-5-sulfonamidobenzamide s.
AID176323In vivo blocking of apomorphine induced hyperactivity following 1 mg/kg i.p. in rats after 60 min.1982Journal of medicinal chemistry, Nov, Volume: 25, Issue:11
Potential neuroleptic agents. 2,6-Dialkoxybenzamide derivatives with potent dopamine receptor blocking activities.
AID764719Inhibition of human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Carbonic anhydrase inhibitors: Synthesis and inhibition of the cytosolic mammalian carbonic anhydrase isoforms I, II and VII with benzene sulfonamides incorporating 4,5,6,7-tetrachlorophthalimide moiety.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID229187Inhibition of specific binding of [125I]PIPAG to sigma receptor in Guinea pig brain membranes1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites.
AID1195369Inhibition of human carbonic anhydrase 1 pre-incubated for 15 mins by stopped-flow CO2 hydration assay2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
The β-carbonic anhydrase from the malaria mosquito Anopheles gambiae is highly inhibited by sulfonamides.
AID252343Amount of cGMP level in rat neostriatal membranes after incubation at 10 uM2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Preparation and pharmacological characterization of trans-2-amino-5(6)-fluoro-6(5)-hydroxy-1-phenyl-2,3-dihydro-1H-indenes as D2-like dopamine receptor agonists.
AID180891The dosage at which 50% of the animals were cataleptic was measured after (ip) administration in male Sprague-Dawley rats1982Journal of medicinal chemistry, Nov, Volume: 25, Issue:11
Potential neuroleptic agents. 2,6-Dialkoxybenzamide derivatives with potent dopamine receptor blocking activities.
AID256965Inhibitory activity against human recombinant mitochondrial isozyme CA VB2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors.
AID1142833Inhibition of human carbonic anhydrase-1 by stopped-flow CO2 hydration assay2014Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11
Sulfonamide inhibition studies of two β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila.
AID1453412Inhibition of human carbonic anhydrase-1 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay
AID726232Inhibition of Trypanosoma cruzi CL Brener recombinant alpha-carbonic anhydrase expressed in insect Sf9 cell Baculovirus system by stopped flow CO2 hydration assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Cloning, characterization, and sulfonamide and thiol inhibition studies of an α-carbonic anhydrase from Trypanosoma cruzi, the causative agent of Chagas disease.
AID263637Inhibition of human recombinant CA22006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Carbonic anhydrase inhibitors: cloning and sulfonamide inhibition studies of a carboxyterminal truncated alpha-carbonic anhydrase from Helicobacter pylori.
AID263638Inhibition of Helicobacter pylori recombinant CA2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Carbonic anhydrase inhibitors: cloning and sulfonamide inhibition studies of a carboxyterminal truncated alpha-carbonic anhydrase from Helicobacter pylori.
AID1628037Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins by stop flow CO2 hydrase assay2016Bioorganic & medicinal chemistry letters, 09-01, Volume: 26, Issue:17
Cloning, expression, purification and sulfonamide inhibition profile of the complete domain of the η-carbonic anhydrase from Plasmodium falciparum.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID301578Inhibition of human recombinant CA 3 assessed as CO2 hydration by stopped flow kinetic assay2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
Carbonic anhydrase inhibitors: cloning, characterization, and inhibition studies of the cytosolic isozyme III with sulfonamides.
AID1287519Inhibition of Vibrio cholerae beta carbonic anhydrase incubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Sulfonamide inhibition studies of the β-carbonic anhydrase from the newly discovered bacterium Enterobacter sp. B13.
AID236912Permeability Coefficient in 2/4/A1 cell model2005Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
Exploring the role of different drug transport routes in permeability screening.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID275809Inhibition of catalytic domain of human recombinant CA IX2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors.
AID242943Ratio of dopamine receptor D3 and D4 ki values2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1346210Human carbonic anhydrase 12 (4.2.1.1 Carbonate dehydratases)2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs?
AID1345788Human D2 receptor (Dopamine receptors)1995Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Jul, Volume: 12, Issue:4
Lack of discrimination by agonists for D2 and D3 dopamine receptors.
AID1345833Human D3 receptor (Dopamine receptors)1995Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Jul, Volume: 12, Issue:4
Lack of discrimination by agonists for D2 and D3 dopamine receptors.
AID1346202Human carbonic anhydrase 7 (4.2.1.1 Carbonate dehydratases)2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID1345928Human carbonic anhydrase 1 (4.2.1.1 Carbonate dehydratases)2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs?
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1799591Enzyme Inhbition Assay from Article 10.1111/j.1747-0285.2009.00902.x: \\Carbonic anhydrase inhibitors: glycosylsulfanilamides act as subnanomolar inhibitors of the human secreted isoform VI.\\2009Chemical biology & drug design, Dec, Volume: 74, Issue:6
Carbonic anhydrase inhibitors: glycosylsulfanilamides act as subnanomolar inhibitors of the human secreted isoform VI.
AID1796771CA Inhibition Assay from Article 10.1021/jm050333c: \\Carbonic anhydrase inhibitors: stacking with Phe131 determines active site binding region of inhibitors as exemplified by the X-ray crystal structure of a membrane-impermeant antitumor sulfonamide compl2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Carbonic anhydrase inhibitors: stacking with Phe131 determines active site binding region of inhibitors as exemplified by the X-ray crystal structure of a membrane-impermeant antitumor sulfonamide complexed with isozyme II.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (3,886)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901406 (36.18)18.7374
1990's960 (24.70)18.2507
2000's796 (20.48)29.6817
2010's623 (16.03)24.3611
2020's101 (2.60)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 83.92

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

MetricThis Compound (vs All)
Research Demand Index83.92 (24.57)
Research Supply Index8.43 (2.92)
Research Growth Index4.39 (4.65)
Search Engine Demand Index154.83 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (83.92)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials427 (10.28%)5.53%
Reviews180 (4.34%)6.00%
Case Studies307 (7.39%)4.05%
Observational4 (0.10%)0.25%
Other3,234 (77.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (15)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
The Role of Dopamine, Reward Learning and Prefrontal Activity in Expectation-induced Mood Enhancement [NCT05208294]296 participants (Anticipated)Interventional2022-01-31Recruiting
Neuroendocrine, Metabolite Substrates, Clinical Symptoms and Cognitive Function in Schizophrenia [NCT02423096]200 participants (Anticipated)Observational [Patient Registry]2013-12-31Recruiting
Evaluation of the Necessity of Long-term Pharmacological Treatment With Antipsychotics for the Prevention of Relapse in Long-term Stabilized Schizophrenic Patients: a Randomized, Single-blind, Longitudinal Trial [NCT02307396]Phase 421 participants (Actual)Interventional2015-02-01Completed
Effectiveness of Antipsychotic Combination With Psychosocial Intervention on Outcome of Patients With Schizophrenia:One-Year Follow up. [NCT00654576]Phase 41,400 participants (Anticipated)Interventional2005-02-28Completed
A Randomized Blind Parallel Intramuscular Haloperidol-Controlled Multicenter Clinical Trial to Evaluate the Efficacy and Safety of Intramuscular Levosulpiride in the Treatment of Chinese Patients With Agitation Of Schizophrenia [NCT00866645]Phase 2/Phase 3240 participants (Anticipated)Interventional2009-02-28Completed
The Effect of Antiemetics on Bowel Preparation Before Colonoscopy [NCT04583111]Phase 4200 participants (Anticipated)Interventional2020-03-01Recruiting
Dopaminergic Mechanisms of Gating Working Memory, Learning and Motivation: a Pharmaco-fMRI Study [NCT05884671]47 participants (Actual)Interventional2021-09-23Completed
Sulpiride Versus Placebo for Reducting Hot Flushes During Climacteric: a Double-blind Randomized Clinical Trial [NCT02749747]Phase 328 participants (Actual)Interventional2014-06-30Completed
Safety and Efficacy of Intrathecally Administered Magnesium Sulfate Added to Morphine and Local Anesthetics for Major Abdominal Cancer Surgery [NCT03459417]90 participants (Actual)Interventional2018-01-01Completed
Dopaminergic Modulation of Choroidal Blood Flow Changes During Dark/Light Transitions [NCT00280501]21 participants (Actual)Interventional2005-08-31Completed
Randomized Multicentric Open-label Phase III Clinical Trial to Evaluate the Efficacy of Continual Treatment Versus Discontinuation Based in the Presence of Prodromes in a First Episode of Non-affective Psychosis. [NCT01765829]Phase 3104 participants (Anticipated)Interventional2012-11-30Recruiting
Therapeutic Drug Monitoring and Pharmacokinetic Compartmental Analysis of Sulpiride [NCT01777685]16 participants (Actual)Interventional2013-01-31Completed
Efficacy of Interpersonal Psychotherapy in Treatment Resistant Depression [NCT01896349]74 participants (Anticipated)Interventional2013-04-30Recruiting
Pharmacovigilance in Gerontopsychiatric Patients [NCT02374567]Phase 3407 participants (Actual)Interventional2015-01-31Terminated
Clinical Trial to Evaluate the Safety and Efficacy of Levosulpiride to Improve Retinal Alterations in Patients With Diabetic Retinopathy and Diabetic Macular Edema. [NCT03161652]Phase 2120 participants (Anticipated)Interventional2017-05-24Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]