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raclopride

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Description

Raclopride: A substituted benzamide that has antipsychotic properties. It is a dopamine D2 receptor (see RECEPTORS, DOPAMINE D2) antagonist. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3033769
CHEMBL ID8809
CHEBI ID92070
SCHEMBL ID116054
MeSH IDM0132672

Synonyms (88)

Synonym
HMS3268I08
AB00639928-12
BRD-K04111260-001-01-9
s-(-)-raclopride
s-raclopride
gtpl94
(-)-raclopride
a-40664
BPBIO1_001215
tocris-1810
NCGC00025303-01
BIOMOL-NT_000027
PDSP1_000924
MLS001423957
raclopride
smr000449275
MLS000758220
NCGC00025303-03
(-)-(s)-3,5-dichlor-n-((1-ethyl-2-pyrrolidinyl)methyl)-6-hydroxy-o-anisamid
benzamide, 3,5-dichloro-n-((1-ethyl-2-pyrrolidinyl)methyl)-2-hydroxy-6-methoxy-, (-)-
raclopride [inn:ban]
racloprida [spanish]
(-)-(s)-3,5-dichloro-n-((1-ethyl-2-pyrrolidinyl)methyl)-6-hydroxy-o-anisamide
raclopridum [latin]
c15h20cl2n2o3
NCGC00025303-02
84225-95-6
fla 870
HMS2089C20
HMS2051C03
NCGC00025303-04
CHEMBL8809 ,
3,5-dichloro-n-[[(2s)-1-ethylpyrrolidin-2-yl]methyl]-2-hydroxy-6-methoxybenzamide
(s)3,5-dichloro-n-(1-ethyl-pyrrolidin-2-ylmethyl)-2-hydroxy-6-methoxy-benzamide
(s)-3,5-dichloro-n-(1-ethyl-pyrrolidin-2-ylmethyl)-2-hydroxy-6-methoxy-benzamide
3,5-dichloro-n-((s)-1-ethyl-pyrrolidin-2-ylmethyl)-2-hydroxy-6-methoxy-benzamide
raclopride;3,5-dichloro-n-(1-ethyl-pyrrolidin-2-ylmethyl)-2-hydroxy-6-methoxy-benzamide
(s)-3,5-dichloro-n-((1-ethylpyrrolidin-2-yl)methyl)-2-hydroxy-6-methoxybenzamide
3,5-dichloro-n-(1-ethyl-pyrrolidin-2-ylmethyl)-2-hydroxy-6-methoxy-benzamide (raclopride)
3,5-dichloro-n-(1-ethyl-pyrrolidin-2-ylmethyl)-2-hydroxy-6-methoxy-benzamide(raclopride)
bdbm50005118
NCGC00025303-05
racloprida
430k3soz7g ,
raclopridum
unii-430k3soz7g
cas-84225-95-6
dtxcid7025687
tox21_110961
dtxsid9045687 ,
HMS2232D05
AKOS015966951
CCG-100752
[3h]raclopride
gtpl3299
[3h]-raclopride
(s)-3,5-dichloro-n-((1-ethyl-2-pyrrolidinyl)methyl)-6-hydroxy-o-anisamide
raclopride [inn]
(s)-3,5-dichloro-n-((1-ethyl-2-pyrrolidinyl)methyl)-2-hydroxy-6-methoxybenzamide
raclopride [mart.]
raclopride [who-dd]
SCHEMBL116054
NC00002
tox21_110961_1
NCGC00025303-06
3,5-dichloro-n-[[(2s)-1-ethyl-2-pyrrolidinyl]methyl]-2-hydroxy-6-methoxybenzamide
(s)-3,5-dichloro-n-[(1-ethyl-2-pyrrolidinyl)methyl]-2-hydroxy-6-methoxybenzamide
R0094
SR-01000597538-1
sr-01000597538
SR-01000597538-3
CHEBI:92070
AS-73734
EX-A5252
3,5-dichloro-n-{[(2s)-1-ethylpyrrolidin-2-yl]methyl}-2-hydroxy-6-methoxybenzamide
HMS3713O20
DB12518
HMS3676J08
mfcd02179386
104953-11-9
HMS3412J08
Q7279814
BRD-K04111260-001-05-0
SDCCGSBI-0051054.P002
NCGC00025303-10
CS-0027846
D82063
HY-103414

Research Excerpts

Overview

Raclopride is a substituted benzamide with high selectivity as an antagonist of central dopaminergic D2 receptors and potential antipsychotic effects. It is a widely used positron emission tomography (PET) tracer.

ExcerptReferenceRelevance
"Raclopride is a selective antagonist of the dopamine D2 receptor. "( Development of a population pharmacokinetic model to predict brain distribution and dopamine D2 receptor occupancy of raclopride in non-anesthetized rat.
de Lange, ECM; Hartman, R; Ilkova, T; van Wijk, RC; Wong, YC, 2018
)
2.13
"11C-Raclopride is a widely used positron emission tomography (PET) tracer for measurement of striatal D2 dopamine receptor binding characteristics. "( Measurement of striatal and thalamic dopamine D2 receptor binding with 11C-raclopride.
Aalto, S; Hagelberg, N; Hietala, J; Hirvonen, J; Kajander, J; Lumme, V; Någren, K; Oikonen, V; Vilkman, H, 2003
)
1.11
"Raclopride is a substituted benzamide with high selectivity as an antagonist of central dopaminergic D2 receptors and potential antipsychotic effects. "( Behavioral profile of raclopride in agonistic encounters between male mice.
Aguilar, MA; Miñarro, J; Pérez-Iranzo, N; Simón, VM, 1994
)
2.05

Effects

11C-raclopride PET has been shown to be sensitive to changes in endogenous dopamine. 3H-Raclopride has a high affinity for the dopamine-D2 receptors (Kd = 1 nM in rat striatum)

ExcerptReferenceRelevance
"3H-Raclopride has a high affinity for the dopamine-D2 receptors (Kd = 1 nM in rat striatum) with much less affinity for any other receptor."( Raclopride, a new selective ligand for the dopamine-D2 receptors.
Farde, L; Gawell, L; Hall, H; Köhler, C; Sedvall, G, 1988
)
2.23
"11C-raclopride PET, which has been shown to be sensitive to changes in endogenous dopamine and has a high short-term test-retest reliability, can be used to investigate different regulatory states of the dopaminergic system with respect to psychiatric diseases and pharmacological influences."( Long-term stability of neurotransmitter activity investigated with 11C-raclopride PET.
Alexoff, D; Brodie, JD; Dewey, SL; Fowler, JS; Logan, J; Schlösser, R; Volkow, N; Wang, GJ; Wolf, AP, 1998
)
1.01
"3H-Raclopride has a high affinity for the dopamine-D2 receptors (Kd = 1 nM in rat striatum) with much less affinity for any other receptor."( Raclopride, a new selective ligand for the dopamine-D2 receptors.
Farde, L; Gawell, L; Hall, H; Köhler, C; Sedvall, G, 1988
)
2.23

Actions

Raclopride blocked the increase in locomotor activity produced by d-amphetamine, but did not further enhance ACh release. It did not produce any change in uptake compared to baseline or between the hemispheres.

ExcerptReferenceRelevance
"Raclopride did not produce any change in uptake compared to baseline or between the hemispheres."( Striatal adenosine A(2A) receptor-mediated positron emission tomographic imaging in 6-hydroxydopamine-lesioned rats using [(18)F]-MRS5425.
Bhattacharjee, AK; Chen, X; Jacobson, KA; Jacobson, O; Kiesewetter, DO; Lang, L; Ma, Y; Niu, G; Shinkre, B; Trenkle, WC, 2011
)
1.09
"Raclopride blocked the increase in locomotor activity produced by d-amphetamine, but did not further enhance ACh release."( Dopaminergic regulation of striatal acetylcholine release: importance of D1 and N-methyl-D-aspartate receptors.
Damsma, G; Fibiger, HC; Robertson, GS; Tham, CS, 1991
)
1

Treatment

Pretreatment with raclopride, a dopamine D2/D3 receptor antagonist, reduced the ocular hypotensive effect induced by 7-OH-DPAT in vehicle containing CAP. Pre-treatment with racLopride blocked midazolam-induced increases in mean bout duration, at doses that by themselves were ineffective.

ExcerptReferenceRelevance
"Raclopride treatment enhanced depressive-like symptoms in several tasks, and the MFB DBS partially reversed the depressive-like phenotype."( Deep Brain Stimulation of the Medial Forebrain Bundle in a Rodent Model of Depression: Exploring Dopaminergic Mechanisms with Raclopride and Micro-PET.
Braun, F; Coenen, VA; Döbrössy, MD; Meyer, PT; Sörensen, A; Thiele, S; Weis, J, 2020
)
1.49
"Raclopride-treated mice had reduced f(R) and V compared with saline-treated mice during steady states, but showed a similar increase in f(R) and V at exercise onset."( Dopaminergic modulation of exercise hyperpnoea via D(2) receptors in mice.
Homma, I; Iwase, M; Izumizaki, M; Tsuchiya, N, 2012
)
1.1
"Raclopride-treated subjects showed a slightly reduced level of climbing scores at the beginning of the first session, but persisted in emitting this costly behavioural response up to the end of the session, while no effects were observed in the second session."( Possible role of dopamine D1-like and D2-like receptors in behavioural activation and evaluation of response efficacy in the forced swimming test.
D'Aquila, PS; Galistu, A, 2012
)
1.1
"Raclopride treatment elevated striatal binding of 3H-nemonapride and 3H-spiperone to a lesser extent, and did not alter 3H-raclopride binding."( Dopamine receptor subtypes: differential regulation after 8 months treatment with antipsychotic drugs.
Creese, I; Florijn, WJ; Tarazi, FI, 1997
)
1.02
"Raclopride-treated rats also exhibited delayed reentry times to the white chamber compared to control rats (p < 0.01) and spent significantly less time in the white chamber (p < 0.05)."( Effects of SCH23390 and raclopride on anxiety-like behavior in rats tested in the black-white box.
Costall, B; Smythe, JW; Timothy, C, 1999
)
1.33
"Pretreatment with raclopride, a dopamine D2/D3 receptor antagonist, reduced the ocular hypotensive effect induced by 7-OH-DPAT in vehicle containing CAP thereby supporting the role for dopamine D2/D3 receptors in modulating IOP."( Biodegradable calcium phosphate nanoparticles as a new vehicle for delivery of a potential ocular hypotensive agent.
Chu, TC; He, Q; Potter, DE, 2002
)
0.64
"Pretreatment with raclopride blocked the increments, but raclopride alone did not alter baseline values of k*."( D-Amphetamine stimulates D2 dopamine receptor-mediated brain signaling involving arachidonic acid in unanesthetized rats.
Bazinet, RP; Bhattacharjee, AK; Chang, L; Rapoport, SI; White, L, 2006
)
0.66
"Pretreatment with raclopride blocked the enhancement of startle by SKF 82958 at the low intensities and attenuated the enhancement at the high intensities."( Enhancement of the acoustic startle response in rats by the dopamine D1 receptor agonist SKF 82958.
Davis, M; Meloni, EG, 1999
)
0.63
"Pre-treatment with raclopride blocked midazolam-induced increases in mean bout duration, at doses that by themselves were ineffective, but did not reverse the decrease in intrabout lick rate."( The effect of the dopamine D2 receptor antagonist raclopride on the pattern of licking microstructure induced by midazolam in the rat.
Cooper, SJ; Higgs, S, 2000
)
0.88
"Pretreatment with raclopride significantly increased PPI in the DAT (-/-) mice, whereas SCH23390 had no significant effect."( Prepulse inhibition deficits and perseverative motor patterns in dopamine transporter knock-out mice: differential effects of D1 and D2 receptor antagonists.
Caron, MG; Fumagalli, F; Geyer, MA; Paulus, MP; Ralph, RJ, 2001
)
0.63
"Pretreatment with raclopride resulted in decreased intake in independent ingestion (II) tests, but not in oral catheter (OC) tests on PN 7, 14, and 21."( Raclopride decreases sucrose intake of rat pups in independent ingestion tests.
Gayle, C; Smith, GP; Tyrka, A, 1992
)
2.05

Toxicity

ExcerptReferenceRelevance
"We examined the relationship between antipsychotic-associated mental side effects and dopamine D2 receptor occupancy in striatal subdivisions using high-resolution positron emission tomography with [11C]raclopride to better characterize the neurochemical mechanism underlying these adverse effects."( Antipsychotic-associated mental side effects and their relationship to dopamine D2 receptor occupancy in striatal subdivisions: a high-resolution PET study with [11C]raclopride.
Cho, SE; Cho, ZH; Kim, HK; Kim, JH; Kim, YB; Lee, SY; Son, YD, 2011
)
0.75
" To examine the roles of each of these proteins in methylone-induced toxic effects, we used SERT and DAT knockout (KO) mice and assessed the hyperthermic and lethal effects caused by a single administration of methylone."( Methylone-induced hyperthermia and lethal toxicity: role of the dopamine and serotonin transporters.
Goda, Y; Hall, FS; Ito, M; Kikura-Hanajiri, R; Lesch, KP; Moriya, Y; Murphy, DL; Ohara, A; Piao, YS; Sora, I; Uhl, GR, 2015
)
0.42

Pharmacokinetics

The pharmacokinetic and pharmacodynamic properties of raclopride, a new antipsychotic, were investigated in 16 healthy men. The linear 1-compartment open model with zero-order absorption was the most appropriate pharmacokinetics model.

ExcerptReferenceRelevance
"The pharmacokinetic and pharmacodynamic properties of raclopride, a new antipsychotic, were investigated in 16 healthy men."( Pharmacokinetics of raclopride formulations. Influence of prolactin and tolerability in healthy male volunteers.
Farde, L; Hammarlund-Udenaes, M; Movin-Osswald, G; Nordström, AL; Wahlén, A, 1992
)
0.86
" The linear 1-compartment open model with zero-order absorption was the most appropriate pharmacokinetic model describing the raclopride plasma concentration profile after a single 8 mg dose of raclopride ER capsules."( An open study of tolerability and pharmacokinetics of raclopride extended release capsules in psychiatric patients: a Canadian study.
Bloom, D; Gendron, A; Movin-Osswald, G; Nair, NP; Sirois, G; Uppfeldt, G, 1995
)
0.75
" In pharmacokinetic analysis of time-activity curves (TAC), such averaging over heterogeneous tissues may introduce a systematic error (heterogeneity error) but may also improve the accuracy and precision of parameter estimation."( Non-invasive assessment of distribution volume ratios and binding potential: tissue heterogeneity and interindividually averaged time-activity curves.
Bares, R; Becker, GA; Dohmen, BM; Mueller-Schauenburg, W; Reimold, M; Reischl, G, 2004
)
0.32
"'Choice of weights' is important in pharmacokinetic neuroreceptor quantification with the SRTM."( Evaluation of non-uniform weighting in non-linear regression for pharmacokinetic neuroreceptor modelling.
Buchert, R; Thiele, F, 2008
)
0.35
" This novel method was applied to a pharmacokinetic study of S-RCP in rats."( A highly sensitive LC-MS/MS method for the determination of S-raclopride in rat plasma: application to a pharmacokinetic study in rats.
Dixit, A; Giri, S; Gupta, M; Mullangi, R; Punde, RR; Rajagopal, S; Suresh, PS, 2011
)
0.61
" To this aim, the 1-h phase during which imaging-data are acquired was evaluated by using a pharmacokinetic approach."( Pharmacokinetic analysis of plasma curves obtained after i.v. injection of the PET radioligand [11C] raclopride provides a likely explanation for rapid radioligand metabolism.
Castagnoli, A; Farde, L; Halldin, C; Mansi, L; Sestini, S, 2012
)
0.59
" The aims of this study were to comprehensively evaluate its pharmacokinetic (PK) profiles in different brain compartments and to establish a PK-RO model that could predict the brain distribution and RO of raclopride in the freely moving rat using a LC-MS based approach."( Development of a population pharmacokinetic model to predict brain distribution and dopamine D2 receptor occupancy of raclopride in non-anesthetized rat.
de Lange, ECM; Hartman, R; Ilkova, T; van Wijk, RC; Wong, YC, 2018
)
0.88

Compound-Compound Interactions

The effects of dopamine release manipulated by drugs on the in vivo binding of [11C]raclopride in the striatum were evaluated in conscious monkeys. The effects of topiramate on glutamatergic neurotransmission in the rat mPFC were investigated.

ExcerptReferenceRelevance
"The effects of dopamine release manipulated by drugs on the in vivo binding of [11C]raclopride in the striatum were evaluated in conscious monkeys combined with microdialysis."( Is synaptic dopamine concentration the exclusive factor which alters the in vivo binding of [11C]raclopride?: PET studies combined with microdialysis in conscious monkeys.
Harada, N; Kakiuchi, T; Nishiyama, S; Ohba, H; Sato, K; Tsukada, H, 1999
)
0.75
"The effects of ketamine, a noncompetitive antagonist of NMDA receptors, on the striatal dopaminergic system were evaluated multiparametrically in the monkey brain using high-resolution positron emission tomography (PET) in combination with microdialysis."( Ketamine decreased striatal [(11)C]raclopride binding with no alterations in static dopamine concentrations in the striatal extracellular fluid in the monkey brain: multiparametric PET studies combined with microdialysis analysis.
Fukumoto, D; Harada, N; Kakiuchi, T; Nishiyama, S; Ohba, H; Sato, K; Tsukada, H, 2000
)
0.58
" Here, using intracellular recording in vitro, we investigated the effects of topiramate on glutamatergic neurotransmission in the rat mPFC, both when given alone and in combination with raclopride or clozapine."( Differential effects of topiramate on prefrontal glutamatergic transmission when combined with raclopride or clozapine.
Jardemark, KE; Konradsson, A; Marcus, MM; Schilström, B; Svensson, TH, 2009
)
0.76

Bioavailability

ExcerptReferenceRelevance
"5 L/kg; mean absolute bioavailability was 65 to 67% following the oral solution and the ER formulations."( Pharmacokinetics of raclopride formulations. Influence of prolactin and tolerability in healthy male volunteers.
Farde, L; Hammarlund-Udenaes, M; Movin-Osswald, G; Nordström, AL; Wahlén, A, 1992
)
0.61
"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
"Intranasal drug delivery is a noninvasive drug delivery route that can enhance systemic delivery of therapeutics with poor oral bioavailability by exploiting the rich microvasculature within the nasal cavity."( Positron Emission Tomography Assessment of the Intranasal Delivery Route for Orexin A.
Alving, K; Dharanipragada, R; Giovanni, A; Gupta, A; Hoekman, J; Hooker, JM; Hurst, W; Rowe, W; Van de Bittner, GC; Van de Bittner, KC; Wey, HY; Ying, X, 2018
)
0.48
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

The PK-RO model could facilitate the selection of optimal dose and dosing time when raclopride is used as tracer or as pharmacological blocker in various rat studies.

ExcerptRelevanceReference
" However, the area under the prolactin level curve was similar after administration of all dosage forms."( Pharmacokinetics of raclopride formulations. Influence of prolactin and tolerability in healthy male volunteers.
Farde, L; Hammarlund-Udenaes, M; Movin-Osswald, G; Nordström, AL; Wahlén, A, 1992
)
0.61
" The atypical antipsychotic clozapine exhibited an "inverted-U" shaped dose-response curve, reversing the apomorphine-induced loss of PPI at low doses but not at high doses."( Effects of spiperone, raclopride, SCH 23390 and clozapine on apomorphine inhibition of sensorimotor gating of the startle response in the rat.
Braff, DL; Geyer, MA; Keith, VA; Swerdlow, NR, 1991
)
0.6
" Both 23390 and raclopride, which were used at low dosage (0."( Antagonism of EEGraphic and behavioural effects of methamphetamine by selective receptor blockers (SCH 23390 and raclopride) in the rabbit.
Albergati, A; Bo, P; Dallocchio, C; Marchioni, E; Savoldi, F, 1991
)
0.84
" When milk intake was stable, dose-response functions were determined for cocaine (4."( Attenuation of the effects of cocaine on milk consumption in rats by dopamine antagonists.
Rapoza, D; Woolverton, WL, 1991
)
0.28
" The dose-response curves for both agonists were shifted to the left in the hypothyroid rats compared to water-treated controls."( The hypothyroid rat as a model of increased sensitivity to dopamine receptor agonists.
Cameron, DL; Crocker, AD, 1990
)
0.28
" For remoxipride, the dose-response curve for antagonism of GBL-reversal was superimposable over that for antagonism of apomorphine-induced stereotypies, with an ED50 value about 12 times higher than that for antagonism of apomorphine-induced hyperactivity."( Comparison of the effects of haloperidol, remoxipride and raclopride on "pre"- and postsynaptic dopamine receptors in the rat brain.
Fowler, CJ; Magnusson, O; Mohringe, B; Ogren, SO; Wijkström, A, 1988
)
0.52
" The administration of repeated doses of raclopride showed linear pharmacokinetics based on parameter values which are either constant (effective elimination half-life, total plasma clearance, and dose-normalized area under the plasma concentration-time curve) or varying proportionally (trough plasma concentration, peak plasma concentration, average plasma concentration and the area under the plasma concentration-time curve for a dosage interval at steady state) with the doses."( An open study of tolerability and pharmacokinetics of raclopride extended release capsules in psychiatric patients: a Canadian study.
Bloom, D; Gendron, A; Movin-Osswald, G; Nair, NP; Sirois, G; Uppfeldt, G, 1995
)
0.81
" This shift in the cocaine dose-response curve was apparent when conditioning commenced either 3 or 7, but not 14, days after the cessation of cocaine pretreatment."( Sensitization to the conditioned rewarding effects of cocaine: pharmacological and temporal characteristics.
Heidbreder, C; Shippenberg, TS, 1995
)
0.29
" In anaesthetized dogs (n = 5), dose-response curves were obtained by intravenous infusion of increasing doses of dopexamine (5-20 micrograms kg-1 min-1)."( Cardiovascular actions of dopexamine in anaesthetized and conscious dogs.
Abdul-Hussein, N; Chang, DH; Einstein, R; Matthews, R; Richardson, DP; Wong, TW, 1994
)
0.29
" An adequate test of the theory that preference for hippocampal dopamine D2 receptors with afford a good therapeutic ratio requires an alternative dosing regimen."( Savoxepine: striatal dopamine-D2 receptor occupancy in human volunteers measured using positron emission tomography (PET).
Ametamey, S; Antonini, A; Beer, HF; Gerebtzoff, A; Gut, A; Leenders, KL; Locher, JT; Maître, L; Thomann, R; Weinreich, R, 1993
)
0.29
" Dopamine depletion with reserpine did increase the striatum/cerebellum ratio at a low dosage of [11C]APO (10 nmol/kg)."( Synthesis and in vivo distribution in the rat of a dopamine agonist: N-([11C]methyl)norapomorphine.
Korf, J; Vaalburg, W; van der Worp, H; Visser, GM; Wiegman, T; Zijlstra, S, 1993
)
0.29
" The dose-response curves at which each drug produced vacuous jaw movements are presented and discussed in terms of their predictive capabilities of early onset extrapyramidal side effects."( The effects of raclopride on vacuous jaw movements in rats following acute administration.
Harrington, A; Kaczmarek, HJ; Steinpreis, RE, 1996
)
0.65
" With increasing time between dosing and PET scanning there was a curvilinear increase in BP, so that all studies performed at or after 18 h post-dose gave BPs in the normal range (mean +/- 2 SD)."( The time course of binding to striatal dopamine D2 receptors by the neuroleptic ziprasidone (CP-88,059-01) determined by positron emission tomography.
Bench, CJ; Boyce, M; Brannick, LY; Dolan, RJ; Frackowiak, RS; Grasby, PM; Gunn, KP; Lammertsma, AA; Warrington, SJ, 1996
)
0.29
" The baseline stability will also serve as a necessary reference for further dose-response studies and investigations of subchronical pharmacological interventions."( Long-term stability of neurotransmitter activity investigated with 11C-raclopride PET.
Alexoff, D; Brodie, JD; Dewey, SL; Fowler, JS; Logan, J; Schlösser, R; Volkow, N; Wang, GJ; Wolf, AP, 1998
)
0.53
" The shift to the left in the dose-response curve of quinpirole in isolated A/J mice indicated that D2-like dopamine receptor functions can be altered by social experience."( D2-like dopamine receptor mediation of social-emotional reactivity in a mouse model of anxiety: strain and experience effects.
Gariépy, JL; Gendreau, PL; Lewis, MH; Petitto, JM, 1998
)
0.3
" Results following bolus administration of these drugs were consistent with the cumulative dosing procedure, although of smaller magnitude and higher variability."( The effects of dopaminergic agents on reaction time in rhesus monkeys.
Gold, LH; Weed, MR, 1998
)
0.3
" A steady-state treatment condition was ensured by dosing the patients with 750 mg quetiapine daily during 3 weeks followed by a period of tapering off the dose."( N-[11C]methylspiperone PET, in contrast to [11C]raclopride, fails to detect D2 receptor occupancy by an atypical neuroleptic.
Bergström, M; Gefvert, O; Hagberg, G; Långström, B; Lindström, L; Wiesel, FA; Wieselgren, IM, 1998
)
0.56
", 30 min) were administered to rats for 4 weeks in a between-groups dosing design."( Haloperidol, raclopride, and eticlopride induce microcatalepsy during operant performance in rats, but clozapine and SCH 23390 do not.
Fowler, SC; Liou, JR, 1998
)
0.67
"The objective of the present study was to demonstrate an enhancement of the acoustic startle response by dopamine D1 receptor agonists and to characterize this effect pharmacologically in terms of dose-response and selective antagonism at both the dopamine D1 and D2 receptor using a varied range of startle-eliciting intensities."( Enhancement of the acoustic startle response in rats by the dopamine D1 receptor agonist SKF 82958.
Davis, M; Meloni, EG, 1999
)
0.3
" Among 18 dopaminergic ligands studied dopamine, NPA, apomorphine and quinpirole were full agonists in activation of [(35)S]GTPgammaS binding, while seven ligands were partial agonists with efficacies from 16 to 69% of the effect of dopamine and seven ligands were antagonists having no effect on the basal level of [(35)S]GTPgammaS binding, but inhibited dopamine-dependent activation in a dose-response manner."( Modulation of [(35)S]GTPgammaS binding to chinese hamster ovary cell membranes by D(2(short)) dopamine receptors.
Ferré, S; Finnman, UB; Fuxe, K; Owman, C; Rinken, A; Terasmaa, A, 2000
)
0.31
" We exemplify how this dosing confounder could lead to inappropriate conclusions."( Are animal studies of antipsychotics appropriately dosed? Lessons from the bedside to the bench.
Kapur, S; Remington, G; Wadenberg, ML, 2000
)
0.31
"Quetiapine shows a transiently high D2 occupancy, which decreases to very low levels by the end of the dosing interval."( A positron emission tomography study of quetiapine in schizophrenia: a preliminary finding of an antipsychotic effect with only transiently high dopamine D2 receptor occupancy.
Jones, C; Kapur, S; Remington, G; Seeman, P; Shammi, CS; Zipursky, R, 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
" Daily dosing with A-77636 rapidly produced complete tolerance, as previously observed, whereas coadministration of the D2 agonist quinpirole plus A-77636 failed to either delay or prevent tolerance."( Dinapsoline: characterization of a D1 dopamine receptor agonist in a rat model of Parkinson's disease.
Gulwadi, AG; Korpinen, CD; Mailman, RB; Nichols, DE; Sit, SY; Taber, MT, 2001
)
0.31
"A dose-response relationship between dopamine D(2) occupancy and acute extrapyramidal symptoms (EPS) has been well established."( The relationship between dopamine D2 receptor occupancy and the vacuous chewing movement syndrome in rats.
Kapur, S; Nobrega, JN; Remington, G; Turrone, P, 2003
)
0.32
" One consistent aspect of STN stimulation is the ability to reduce the dosage of dopaminergic medications; sometimes they can be eliminated altogether."( Stimulation of the subthalamic nucleus in Parkinson's disease does not produce striatal dopamine release.
Abosch, A; Houle, S; Hussey, D; Kapur, S; Lang, AE; Lozano, AM; Miyasaki, J; Sime, E, 2003
)
0.32
" The current study describes a rodent model of amphetamine-induced [11C]raclopride reduction, which allowed the characterisation of the dose-response and temporal dynamics of this reduction over a 24-h time course."( Temporal characterisation of amphetamine-induced dopamine release assessed with [11C]raclopride in anaesthetised rodents.
Goggi, JL; Grasby, PM; Hirani, E; Houston, GC; Hume, SP, 2004
)
0.78
" A potential issue with these studies is that the same challenge dose is used in sensitized and control conditions even though that dose may occupy different positions on the respective dose-response curves."( Ability of dopamine antagonists to inhibit the locomotor effects of cocaine in sensitized and non-sensitized C57BL/6 mice depends on the challenge dose.
Colpaert, FC; Kleven, MS; Koek, W; Prinssen, EP, 2004
)
0.32
"We have previously reported that repeated dosing with the selective serotonin reuptake inhibitor (SSRI) citalopram decreases striatal [11C]raclopride binding in healthy volunteers."( Effects of fluoxetine on dopamine D2 receptors in the human brain: a positron emission tomography study with [11C]raclopride.
Aalto, S; Hietala, J; Hirvonen, J; Ilonen, T; Kajander, J; Någren, K; Penttilä, J; Syvälahti, E, 2004
)
0.74
" According to response, dosage was then adjusted to a maximum dosage of 20 mg daily of either drug."( Treatment response to olanzapine and haloperidol and its association with dopamine D receptor occupancy in first-episode psychosis.
Christensen, BK; Daskalakis, Z; Epstein, I; Furimsky, I; Kapur, S; Roy, P; Sanger, T; Zipursky, RB, 2005
)
0.33
" When patients were rescanned following dosage adjustment, mean D2 receptor occupancies were greater than 70% in both groups."( Treatment response to olanzapine and haloperidol and its association with dopamine D receptor occupancy in first-episode psychosis.
Christensen, BK; Daskalakis, Z; Epstein, I; Furimsky, I; Kapur, S; Roy, P; Sanger, T; Zipursky, RB, 2005
)
0.33
" In contrast, SCH23390 caused no differential strain effect with respect to dosage whether sucrose was real or sham fed."( Dopamine D2 receptors contribute to increased avidity for sucrose in obese rats lacking CCK-1 receptors.
Covasa, M; De Jonghe, BC; Hajnal, A, 2007
)
0.34
" Half maximal effective concentration values were consistently higher in striatal than in extrastriatal regions (temporal cortex: 39 ng/mL; putamen: 64 ng/mL), irrespective of the time between last dosing and scan."( Striatal and extrastriatal D2/D3-receptor-binding properties of ziprasidone: a positron emission tomography study with [18F]Fallypride and [11C]raclopride (D2/D3-receptor occupancy of ziprasidone).
Bartenstein, P; Boy, C; Bröcheler, A; Buchholz, HG; Cumming, P; Fellows, C; Gründer, G; Hiemke, C; Janouschek, H; Landvogt, C; Rösch, F; Schäfer, W; Spreckelmeyer, K; Vernaleken, I; Veselinovic, T; Wong, DF, 2008
)
0.55
" This finding has important implications for dosing of antipsychotics in older patients with schizophrenia."( Sensitivity of older patients to antipsychotic motor side effects: a PET study examining potential mechanisms.
Graff-Guerrero, A; Kapur, S; Mamo, DC; Mulsant, BH; Pollock, BG; Uchida, H, 2009
)
0.35
" On the other hand, we found a gene dosage effect for mouse Sp4 gene in the modulation of sensorimotor gating, a putative endophenotype for both schizophrenia and bipolar disorder."( Transcription factor SP4 is a susceptibility gene for bipolar disorder.
Geyer, MA; Greenwood, TA; Guo, S; He, L; Kelsoe, JR; Tang, W; Zhou, X, 2009
)
0.35
" The 32 mg dose of BL-1020 resulted in an average D(2) RO of 44% at 4-6 h post dosing (pd), which declined to 33% at 24 h pd."( BL-1020, a novel antipsychotic candidate with GABA-enhancing effects: D2 receptor occupancy study in humans.
Antoni, G; Appel, L; Eriksson, C; Geffen, Y; Heurling, K; Kapur, S, 2009
)
0.35
" This single dosage may be sufficient for the treatment of schizophrenia and might be useful as a new dosing schedule choice."( Dopamine D2 receptor occupancy by perospirone: a positron emission tomography study in patients with schizophrenia and healthy subjects.
Arakawa, R; Ito, H; Okubo, Y; Okumura, M; Suhara, T; Takahashi, H; Takano, A; Takano, H, 2010
)
0.36
"The goal of the present investigation was to study a full dose-response of quinpirole in production of species-specific 50 kHz ultrasonic vocalizations in rats, and to study involvement of D2 and D3 dopamine receptors in this response."( Quinpirole-induced 50 kHz ultrasonic vocalization in the rat: role of D2 and D3 dopamine receptors.
Brudzynski, SM; Komadoski, M; St Pierre, J, 2012
)
0.38
"5 mg/kg), an average tissue concentration of approximately 60 nM was detected compared to 15 nM when the drug was dosed at 2 mg/kg, indicating a linear response between dose and detected abundance."( Qualitative and quantitative MALDI imaging of the positron emission tomography ligands raclopride (a D2 dopamine antagonist) and SCH 23390 (a D1 dopamine antagonist) in rat brain tissue sections using a solvent-free dry matrix application method.
Andren, PE; Farde, L; Goodwin, RJ; Harrison, DJ; Iverson, SL; Mackay, CL; Nilsson, A, 2011
)
0.59
"Population pharmacokinetics can predict antipsychotic blood concentrations at a given time point prior to a dosage change."( Dopamine D2/3 Receptor Occupancy Following Dose Reduction Is Predictable With Minimal Plasma Antipsychotic Concentrations: An Open-Label Clinical Trial.
Bies, RR; Caravaggio, F; Gerretsen, P; Graff-Guerrero, A; Mamo, DC; Mar, W; Mulsant, BH; Nakajima, S; Plitman, E; Pollock, BG; Suzuki, T; Uchida, H, 2016
)
0.43
"D2/3R occupancy levels can be predicted from blood drug concentrations collected prior to dosage change."( Dopamine D2/3 Receptor Occupancy Following Dose Reduction Is Predictable With Minimal Plasma Antipsychotic Concentrations: An Open-Label Clinical Trial.
Bies, RR; Caravaggio, F; Gerretsen, P; Graff-Guerrero, A; Mamo, DC; Mar, W; Mulsant, BH; Nakajima, S; Plitman, E; Pollock, BG; Suzuki, T; Uchida, H, 2016
)
0.43
" Prolactin levels could assist in the determination of appropriate antipsychotic dosing to minimize adverse effects."( Threshold of Dopamine D2/3 Receptor Occupancy for Hyperprolactinemia in Older Patients With Schizophrenia.
Caravaggio, F; Chung, JK; Gerretsen, P; Graff-Guerrero, A; Iwata, Y; Mamo, DC; Mar, W; Mulsant, BH; Nakajima, S; Plitman, E; Pollock, BG; Rajji, TK; Suzuki, T; Uchida, H, 2016
)
0.43
" The PK-RO model could facilitate the selection of optimal dose and dosing time when raclopride is used as tracer or as pharmacological blocker in various rat studies."( Development of a population pharmacokinetic model to predict brain distribution and dopamine D2 receptor occupancy of raclopride in non-anesthetized rat.
de Lange, ECM; Hartman, R; Ilkova, T; van Wijk, RC; Wong, YC, 2018
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
salicylamides
[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 (24)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency44.56250.140911.194039.8107AID2451
Chain A, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency28.37090.177814.390939.8107AID2147
LuciferasePhotinus pyralis (common eastern firefly)Potency12.58930.007215.758889.3584AID411
GALC proteinHomo sapiens (human)Potency0.707928.183828.183828.1838AID1159614
GLS proteinHomo sapiens (human)Potency14.12540.35487.935539.8107AID624170
pregnane X nuclear receptorHomo sapiens (human)Potency27.48410.005428.02631,258.9301AID1346982; AID1346985
cytochrome P450 2D6Homo sapiens (human)Potency13.80290.00108.379861.1304AID1645840
arylsulfatase AHomo sapiens (human)Potency1.34591.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency26.67950.035520.977089.1251AID504332
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency12.58930.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency1.25890.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency7.94330.00636.904339.8107AID883
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency35.48130.010323.856763.0957AID2662
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency9.07430.005612.367736.1254AID624032
lethal factor (plasmid)Bacillus anthracis str. A2012Potency31.62280.020010.786931.6228AID912
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency7.94330.00638.235039.8107AID883
[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)
D(2) dopamine receptorHomo sapiens (human)IC50 (µMol)0.05200.00000.74728.0000AID1547948; AID1547952
D(2) dopamine receptorHomo sapiens (human)Ki0.01490.00000.651810.0000AID1142394; AID1143583; AID1629121; AID309290; AID309291
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki0.00930.00010.25675.8000AID65625
D(4) dopamine receptorHomo sapiens (human)Ki3.10000.00000.436210.0000AID309293
D(3) dopamine receptorHomo sapiens (human)Ki0.01140.00000.602010.0000AID1143582; AID1629120; AID309292; AID65135
D(2) dopamine receptorMus musculus (house mouse)IC50 (µMol)0.03200.00090.47332.4310AID64280
D(2) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)0.02790.00010.54948.4000AID64280; AID64285; AID64299; AID64596; AID64610
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.00780.00000.437510.0000AID65260; AID65268; AID65269; AID65409; AID65562; AID65723; AID65747
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (124)

Processvia Protein(s)Taxonomy
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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (18)

Processvia Protein(s)Taxonomy
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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (25)

Processvia Protein(s)Taxonomy
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)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
synapseD(3) dopamine receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (165)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
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.
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.
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.
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.
AID309291Displacement of [3H]spiperone from dopamine D2long receptor in CHO cells2007Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D(2)-like dopamine receptors.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID726714Unbound fraction in rat plasma at 1000 ng/g after 5 hrs by equilibrium dialysis method2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Discovery of novel α₁-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands.
AID1142394Displacement of [3H]spiperone from human D2 receptor transfected in HEK cells2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Shuttle-cargo fusion molecules of transport peptides and the hD2/3 receptor antagonist fallypride: a feasible approach to preserve ligand-receptor binding?
AID1487392Antagonist activity at human D2L receptor expressed in CHO cell membranes assessed as dissociation rate constant2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID63369In vivo inhibitory activity against dopamine (D1) receptor in rat caudate-putamen tissue2003Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22
Synthesis and affinity of a possible byproduct of electrophilic radiolabeling of [123I]IBZM.
AID62003In vitro inhibition of [3H]spiperone binding to Dopamine receptor D2 in Macaca nemestrina striatal membranes1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
N-fluoroalkylated and N-alkylated analogues of the dopaminergic D-2 receptor antagonist raclopride.
AID309296Displacement of [3H]prazosin from adrenergic-alpha-1 receptor in pig striatal membrane2007Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D(2)-like dopamine receptors.
AID178322In vivo inhibition of apomorphine induced stereotypy in rats.1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Potential neuroleptic agents. 4. Chemistry, behavioral pharmacology, and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides.
AID309297Lipophilicity, log D at pH 7.42007Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D(2)-like dopamine receptors.
AID29813Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
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]
AID64610The affinity for the Dopamine receptor D2 was assessed by the inhibition of [3H]-spiperone binding in rat striatal membranes in vitro.1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Potential antipsychotic agents. 7. Synthesis and antidopaminergic properties of the atypical highly potent (S)-5-bromo-2,3-dimethoxy-N-[(1-ethyl-2-pyrrolidinyl)methyl]benzamide and related compounds. A comparative study.
AID65409Inhibition constant against dopamine receptor D2 in rat1993Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2
Fluorinated and iodinated dopamine agents: D2 imaging agents for PET and SPECT.
AID1547949Antagonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Functional-Selectivity Relationship Studies of Novel Apomorphine Analogs to Develop D1R/D2R Biased Ligands.
AID1487361Antagonist activity at human D2L receptor expressed in CHO cell membranes assessed as residence time after 30 mins by liquid scintillation counting method2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID726709Ratio of drug level in brain to plasma in rat at 1 hr2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Discovery of novel α₁-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands.
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]
AID517794Apparent permeability across human Caco-2 cells2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for α(1)-adrenoceptors.
AID517795Ratio of permeability in human Caco-2 cells2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for α(1)-adrenoceptors.
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]
AID1547952Antagonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Functional-Selectivity Relationship Studies of Novel Apomorphine Analogs to Develop D1R/D2R Biased Ligands.
AID62727Antidopamine activity in vitro by ability to displace [3H]spiperone from rat brain striatal preparations.1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Potential neuroleptic agents. 4. Chemistry, behavioral pharmacology, and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides.
AID62004In vitro inhibition of [3H]-Spiperone binding to Dopamine receptor D2 in Macaca nemestrina striatal membranes (using L-tartrate salt of authentic raclopride)1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
N-fluoroalkylated and N-alkylated analogues of the dopaminergic D-2 receptor antagonist raclopride.
AID1212341Cytotoxicity against human Fa2N-4 cells by lactate dehydrogenase assay2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells).
AID226638Hill coefficient value.1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Synthesis of (R,S)-2'-trans-7-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'- propenyl)-amino]tetralin (trans-7-OH-PIPAT): a new D3 dopamine receptor ligand.
AID65260Compound was evaluated for binding affinity towards DA D-2 receptor using radioligand [3H]SPI1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
Conformational analysis of dopamine D-2 receptor antagonists of the benzamide series in relation to a recently proposed D-2 receptor-interaction model.
AID309290Displacement of [3H]spiperone from dopamine D2short receptor in CHO cells2007Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D(2)-like dopamine receptors.
AID64299In vitro binding affinity for Dopamine D2 receptor of rat using [3H]YM-09151 as radioligand2002Journal of medicinal chemistry, Oct-10, Volume: 45, Issue:21
Synthesis and pharmacological evaluation of 1-[(1,2-diphenyl-1H-4-imidazolyl)methyl]-4-phenylpiperazines with clozapine-like mixed activities at dopamine D(2), serotonin, and GABA(A) receptors.
AID726716Efflux ratio of apparent permeability from basolateral to apical side over apical to basolateral side in human Caco2 cells at 1 to 20 uM2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Discovery of novel α₁-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID176588Hyperactivity by regression analysis, through intraperitoneal route of administration1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Potential antipsychotic agents. 7. Synthesis and antidopaminergic properties of the atypical highly potent (S)-5-bromo-2,3-dimethoxy-N-[(1-ethyl-2-pyrrolidinyl)methyl]benzamide and related compounds. A comparative study.
AID64436In vivo inhibitory activity against dopamine (D2) receptor in rat caudate-putamen tissue2003Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22
Synthesis and affinity of a possible byproduct of electrophilic radiolabeling of [123I]IBZM.
AID1629120Binding affinity to dopamine D3 receptor (unknown origin)2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
Highly Selective Dopamine D3 Receptor (D3R) Antagonists and Partial Agonists Based on Eticlopride and the D3R Crystal Structure: New Leads for Opioid Dependence Treatment.
AID65135Compound was measured for its ability to compete with [3H]spiperone binding to the human Dopamine receptor D3 transfected 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.
AID63409Affinity constant of compound was evaluated in human brain1988Journal 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.
AID64596Inhibitory concentration required for displacing radioligand [3H]SPI from DA D-2 receptor1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
Conformational analysis of dopamine D-2 receptor antagonists of the benzamide series in relation to a recently proposed D-2 receptor-interaction model.
AID309294Displacement of [3H]8HO-DPAT from serotonin 5-HT1A receptor in pig striatal membrane2007Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D(2)-like dopamine receptors.
AID176476Catalepsy interval defined as the time required for both fore limbs to be removed from the bar when administered intraperitoneally1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds.
AID63408Affinity constant of compound was evaluated in human brain1988Journal 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.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
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]
AID180163The catalepsy was measured in rat by using bar test1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Potential antipsychotic agents. 9. Synthesis and stereoselective dopamine D-2 receptor blockade of a potent class of substituted (R)-N-[(1-benzyl-2-pyrrolidinyl)methyl]benzamides. Relations to other side chain congeners.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID65268Displacement of [3H]- spiperone from dopamine receptor D2 of striatal membranes without sodium chloride1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Synthesis and in vitro evaluation of 2,3-dimethoxy-5-(fluoroalkyl)-substituted benzamides: high-affinity ligands for CNS dopamine D2 receptors.
AID1243903Displacement of [3H]raclopride from dopamine D2 receptor in Sprague-Dawley rat striatal membranes after 30 mins2015European journal of medicinal chemistry, Aug-28, Volume: 101Bifunctional compounds targeting both D2 and non-α7 nACh receptors: design, synthesis and pharmacological characterization.
AID309292Displacement of [3H]spiperone from dopamine D3 receptor in CHO cells2007Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D(2)-like dopamine receptors.
AID517796Distribution coefficient, log D of the compound2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for α(1)-adrenoceptors.
AID1487393Antagonist activity at human D2L receptor expressed in CHO cell membranes assessed as residence time2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
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]
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.
AID65723In vitro binding affinity against dopamine receptor D2 in rat striata; value ranges from 1.8-3.0 nM1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
N-fluoroalkylated and N-alkylated analogues of the dopaminergic D-2 receptor antagonist raclopride.
AID184626Compound was tested for its acute toxicity in rat after ip administration1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Potential neuroleptic agents. 4. Chemistry, behavioral pharmacology, and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides.
AID65269Compound was evaluated for binding affinity towards dopamine receptor D2 in striatal membranes, using [3H]- spiperone as radioligand in the presence of sodium chloride1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Synthesis and in vitro evaluation of 2,3-dimethoxy-5-(fluoroalkyl)-substituted benzamides: high-affinity ligands for CNS dopamine D2 receptors.
AID176650Stereotypies was scored by regression analysis, through intraperitoneal route of administration1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Potential antipsychotic agents. 7. Synthesis and antidopaminergic properties of the atypical highly potent (S)-5-bromo-2,3-dimethoxy-N-[(1-ethyl-2-pyrrolidinyl)methyl]benzamide and related compounds. A comparative study.
AID64280Inhibition of [3H]spiperone binding to rat striatal dopamine receptor D2 was determined in vitro1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Potential antipsychotic agents. 9. Synthesis and stereoselective dopamine D-2 receptor blockade of a potent class of substituted (R)-N-[(1-benzyl-2-pyrrolidinyl)methyl]benzamides. Relations to other side chain congeners.
AID726708Ratio of drug level in brain to plasma at steady state in rat at 1000 ng/g after 5 hrs2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Discovery of novel α₁-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands.
AID65747Inhibition of [3H]raclopride binding to rat striatal dopamine receptor D21991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Potential antipsychotic agents. 9. Synthesis and stereoselective dopamine D-2 receptor blockade of a potent class of substituted (R)-N-[(1-benzyl-2-pyrrolidinyl)methyl]benzamides. Relations to other side chain congeners.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID30174Percent of zwitter ion formed, was determined at pH 7.41993Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2
Effects of solvation on the ionization and conformation of raclopride and other antidopaminergic 6-methoxysalicylamides: insight into the pharmacophore.
AID1487360Antagonist activity at human D2L receptor expressed in CHO cell membranes assessed as dissociation rate constant after 30 mins by liquid scintillation counting method2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID309293Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells2007Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D(2)-like dopamine receptors.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID65562Inhibition of [3H]spiperone binding to rat striatal membrane Dopamine receptor D21990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds.
AID176414Evaluated in vitro for antipsychotic activity (stereotypies) for the block of apomorphine induced response after ip administration 60 min prior to apomorphine (1 mg/kg sc)1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID176317Block of apomorphine-induced response measured as stereotypies injected ip 60 min prior to apomorphine hydrochloride(1 mg/kg, sc)1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Potential antipsychotic agents. 9. Synthesis and stereoselective dopamine D-2 receptor blockade of a potent class of substituted (R)-N-[(1-benzyl-2-pyrrolidinyl)methyl]benzamides. Relations to other side chain congeners.
AID1547953Antagonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay relative to control2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Functional-Selectivity Relationship Studies of Novel Apomorphine Analogs to Develop D1R/D2R Biased Ligands.
AID1143584Selectivity ratio of Ki for human dopamine D2 receptor expressed in HEK293 cells to Ki for human dopamine D3 receptor expressed in HEK293 cells2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Tranylcypromine substituted cis-hydroxycyclobutylnaphthamides as potent and selective dopamine D₃ receptor antagonists.
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
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID176601In vitro antipsychotic activity was determined block of apomorphine induced response after ip administration 60 min prior to apomorphine (1 mg/kg sc)1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds.
AID64285In vitro ability to inhibit the binding of [3H]spiperone to dopamine receptor D2 in rat striatal membranes.1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds.
AID28390Dissociation constants determined by potentiometry at 25 degree celsius (phenolic group)1993Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2
Effects of solvation on the ionization and conformation of raclopride and other antidopaminergic 6-methoxysalicylamides: insight into the pharmacophore.
AID17656Dissociation constant of the compound; value ranges from 0.81-1.2 nM1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
N-fluoroalkylated and N-alkylated analogues of the dopaminergic D-2 receptor antagonist raclopride.
AID592682Apparent permeability from apical to basolateral side of human Caco2 cells after 2 hrs by LC/MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID196438Inhibition constant on radiolabeled [125I]FIDA2 binding to rat striatal membranes1993Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2
Fluorinated and iodinated dopamine agents: D2 imaging agents for PET and SPECT.
AID65625Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells.1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Synthesis of (R,S)-2'-trans-7-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'- propenyl)-amino]tetralin (trans-7-OH-PIPAT): a new D3 dopamine receptor ligand.
AID1547948Antagonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Functional-Selectivity Relationship Studies of Novel Apomorphine Analogs to Develop D1R/D2R Biased Ligands.
AID309289Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane2007Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D(2)-like dopamine receptors.
AID1629121Binding affinity to dopamine D2 receptor (unknown origin)2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
Highly Selective Dopamine D3 Receptor (D3R) Antagonists and Partial Agonists Based on Eticlopride and the D3R Crystal Structure: New Leads for Opioid Dependence Treatment.
AID65751Competitive binding assay against Dopamine receptor D2 in rat striatal membranes and [125I]-IBF radioligand1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Synthesis and characterization of iodobenzamide analogues: potential D-2 dopamine receptor imaging agents.
AID28391Dissociation constants determined by potentiometry at 25 degree celsius (Amino group)1993Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2
Effects of solvation on the ionization and conformation of raclopride and other antidopaminergic 6-methoxysalicylamides: insight into the pharmacophore.
AID176943Dose which blocks the hypothermic effect of apomorphine by 50% against Sprague-Dawley rats when administered intraperitoneally1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds.
AID23473Partition coefficient (logP)1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
N-fluoroalkylated and N-alkylated analogues of the dopaminergic D-2 receptor antagonist raclopride.
AID726710Unbound fraction in rat brain at 1000 ng/g after 5 hrs by equilibrium dialysis method2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Discovery of novel α₁-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands.
AID1143583Displacement of [3H]N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Tranylcypromine substituted cis-hydroxycyclobutylnaphthamides as potent and selective dopamine D₃ receptor antagonists.
AID29131The isoelectric point (pI) as the arithmetic mean of pKa1 and pKa21993Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2
Effects of solvation on the ionization and conformation of raclopride and other antidopaminergic 6-methoxysalicylamides: insight into the pharmacophore.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID197731Block of apomorphine-induced response measured as hyperactivity injected ip 60 min prior to apomorphine hydrochloride(1 mg/kg, sc)1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Potential antipsychotic agents. 9. Synthesis and stereoselective dopamine D-2 receptor blockade of a potent class of substituted (R)-N-[(1-benzyl-2-pyrrolidinyl)methyl]benzamides. Relations to other side chain congeners.
AID196437Inhibition constant on radiolabeled [125I]FIDA1 binding to rat striatal membranes1993Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2
Fluorinated and iodinated dopamine agents: D2 imaging agents for PET and SPECT.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID176315Block of apomorphine-induced response measured as hypothermia injected ip 30 min prior to apomorphine hydrochloride(1 mg/kg, sc)1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Potential antipsychotic agents. 9. Synthesis and stereoselective dopamine D-2 receptor blockade of a potent class of substituted (R)-N-[(1-benzyl-2-pyrrolidinyl)methyl]benzamides. Relations to other side chain congeners.
AID592683Apparent permeability from basolateral side to apical side of human Caco2 cells by LC/MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID178320In vivo inhibition of apomorphine induced hyperactivity in rats.1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Potential neuroleptic agents. 4. Chemistry, behavioral pharmacology, and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides.
AID309295Displacement of [3H]ketanserin from serotonin 5-HT2 receptor in pig striatal membrane2007Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D(2)-like dopamine receptors.
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.
AID726771Apparent permeability across apical to basolateral side in human Caco2 cells at 1 to 20 uM by LC-MS/MS analysis2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Discovery of novel α₁-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
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.
AID1212314Drug uptake in lysosomes of human Fa2N-4 cells assessed as inhibition of LysoTracker Red fluorescence after 30 mins2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells).
AID1143582Displacement of [3H]N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Tranylcypromine substituted cis-hydroxycyclobutylnaphthamides as potent and selective dopamine D₃ receptor antagonists.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
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.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
AID1345783Rat D2 receptor (Dopamine receptors)2000Molecular pharmacology, Jan, Volume: 57, Issue:1
Nonconserved residues in the second transmembrane-spanning domain of the D(4) dopamine receptor are molecular determinants of D(4)-selective pharmacology.
AID1347024Rat D4 receptor (Dopamine receptors)2000Molecular pharmacology, Jan, Volume: 57, Issue:1
Nonconserved residues in the second transmembrane-spanning domain of the D(4) dopamine receptor are molecular determinants of D(4)-selective pharmacology.
AID1345783Rat D2 receptor (Dopamine receptors)1990Nature, Sep-13, Volume: 347, Issue:6289
Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.
AID1345833Human D3 receptor (Dopamine receptors)1995The Journal of pharmacology and experimental therapeutics, Nov, Volume: 275, Issue:2
Functional correlates of dopamine D3 receptor activation in the rat in vivo and their modulation by the selective antagonist, (+)-S 14297: 1. Activation of postsynaptic D3 receptors mediates hypothermia, whereas blockade of D2 receptors elicits prolactin
AID1345788Human D2 receptor (Dopamine receptors)1995The Journal of pharmacology and experimental therapeutics, Nov, Volume: 275, Issue:2
Functional correlates of dopamine D3 receptor activation in the rat in vivo and their modulation by the selective antagonist, (+)-S 14297: 1. Activation of postsynaptic D3 receptors mediates hypothermia, whereas blockade of D2 receptors elicits prolactin
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)1998European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3
Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study.
AID624215Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1A1998European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3
Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study.
AID1345898Rat D3 receptor (Dopamine receptors)1990Nature, Sep-13, Volume: 347, Issue:6289
Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
AID1345783Rat D2 receptor (Dopamine receptors)1985Biochemical pharmacology, Jul-01, Volume: 34, Issue:13
Specific in vitro and in vivo binding of 3H-raclopride. A potent substituted benzamide drug with high affinity for dopamine D-2 receptors in the rat brain.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,761)

TimeframeStudies, This Drug (%)All Drugs %
pre-199070 (3.98)18.7374
1990's554 (31.46)18.2507
2000's660 (37.48)29.6817
2010's418 (23.74)24.3611
2020's59 (3.35)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 37.41

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index37.41 (24.57)
Research Supply Index7.57 (2.92)
Research Growth Index5.34 (4.65)
Search Engine Demand Index56.78 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (37.41)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials132 (7.33%)5.53%
Reviews27 (1.50%)6.00%
Case Studies12 (0.67%)4.05%
Observational0 (0.00%)0.25%
Other1,631 (90.51%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (11)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Brain Dopaminergic Signaling in Opioid Use Disorders (OUD) [NCT03190954]Early Phase 1300 participants (Anticipated)Interventional2017-08-17Recruiting
Neuroimaging Studies of Reward Processing in Depression [NCT03026036]123 participants (Actual)Observational2016-04-30Completed
Examining the Effects of Estradiol on Neural and Molecular Response to Rewards in Perimenopausal-Onset Anhedonia and Psychosis [NCT05282277]Phase 4103 participants (Anticipated)Interventional2022-04-20Recruiting
Imaging of Dopamine Systems in Anorexia Nervosa [NCT00670293]50 participants (Actual)Observational2008-07-31Completed
An Open Label, 1-sequence Cross-over, Positron Emission Tomography (PET) Study With [11C]Raclopride to Determine Central D2 Dopamine Receptor Occupancy of Quetiapine Fumarate Immediate Release (SEROQUEL®) With Quetiapine Fumarate Extended Release (SEROQUE [NCT00832221]Phase 110 participants (Anticipated)Interventional2009-01-31Completed
Imaging Dopamine D2 Agonist Binding Sites in Schizophrenia [NCT03999190]0 participants (Actual)Observational2019-07-31Withdrawn(stopped due to investigational radiotracer was not approved)
Brain Dopamine Function in Human Obesity [NCT03648892]Early Phase 161 participants (Actual)Interventional2018-09-21Completed
Motor Memory: Study of the Role of Dopamine in Healthy Subjects and Patients With Parkinson's Disease Using PET and EEG [NCT00032812]64 participants Observational2002-03-31Completed
Neural Basis of Decision Making Deficits in Traumatic Brain Injury [NCT02169310]Phase 180 participants (Anticipated)Interventional2014-11-18Recruiting
[NCT02152670]1 participants (Actual)Interventional2014-05-31Terminated(stopped due to Study drug became unaffordable for the purposes of the research.)
Monoamine Contributions to Neurocircuitry in Eating Disorders [NCT02020408]Phase 488 participants (Actual)Interventional2011-05-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT02020408 (2) [back to overview]5-HT Transporter Binding as Measured During the PET Scan
NCT02020408 (2) [back to overview]Dopamine D2/D3 Receptor Binding as Measured During the PET Scan After Amphetamine Administration
NCT03648892 (7) [back to overview]Associations Between Brain Metabolite GABA Via MRS and Striatal D2BP Via [18F]Fallypride
NCT03648892 (7) [back to overview]Change in Striatal Dopamine D2BP After a Palatable Meal
NCT03648892 (7) [back to overview]Correlation Between Change in Striatal Dopamine D2BP After a Palatable Meal and BMI
NCT03648892 (7) [back to overview]Correlation Between Striatal D2 Receptor Binding Potential (D2BP) as Measured by [18F]Fallypride and [11C]Raclopride Time-activity Curves
NCT03648892 (7) [back to overview]Associations Between ad Libitum Meal Consumption and Striatal D2 Receptor (D2R)
NCT03648892 (7) [back to overview]Associations Between Behavioral Performance on Food Go/No Go Computer Task and Striatal D2BP
NCT03648892 (7) [back to overview]Relationship Between Striatal D2BP and BMI is Quadratic or Linear

5-HT Transporter Binding as Measured During the PET Scan

"Use PET and [11C]DASB to explore 5-HTT receptor binding potential midbrain and striatal regions of interest in eating disorder subtypes.~The Binding Potential (BP) was calculated as BP Non Displaceable (ND) = (VT/VND) -1. [VT = distribution volume in tissue; VND = non-displaceable distribution volume]. The binding of the 5-HTT on PET presumably reflects 5-HTT density and/or affinity." (NCT02020408)
Timeframe: 90 minute PET scan

,,,
Interventionbinding potential (BPND) (Mean)
[11C]DASB BPND anteroventral striatum[11C]DASB BPND post dorsal caudate[11C]DASB BPND posterior putamen[11C]DASB BPND predorsal caudate[11C]DASB BPND anterior putamen[11C]DASB BPND midbrain
[11C]DASB Binding Potential Control Women1.680.441.361.081.702.21
[11C]DASB Binding Potential in REC AN1.540.351.270.991.592.06
[11C]DASB Binding Potential in REC ANBN1.460.391.170.991.491.98
[11C]DASB Binding Potential in REC BN1.600.371.320.981.572.17

[back to top]

Dopamine D2/D3 Receptor Binding as Measured During the PET Scan After Amphetamine Administration

Use PET and [11C]raclopride to explore Dopamine D2/D3 receptor binding potential (BPND) in striatal regions of interest in eating disorder subtypes after amphetamine administration. The Binding Potential (BP) was calculated as BP Non Displaceable (ND) = (VT/VND) -1. [VT = distribution volume in tissue; VND = non-displaceable distribution volume]. (NCT02020408)
Timeframe: 90 min PET scan

,,
Interventionbinding potential (BPND) (Mean)
[11C]raclopride BPND anteroventral striatum[11C]raclopride BPND post dorsal caudate[11C]raclopride BPND anterior putamen[11C]raclopride BPND posterior putamen[11C]raclopride BPND predorsal caudate
[11C]Raclopride Binding Potential Control Women2.091.692.712.532.48
[11C]Raclopride Binding Potential in REC AN2.011.622.652.462.40
[11C]Raclopride Binding Potential in REC ANBN1.941.692.602.472.47

[back to top]

Associations Between Brain Metabolite GABA Via MRS and Striatal D2BP Via [18F]Fallypride

"Exploratory analyses of correlations between brain metabolite GABA via magnetic resonance spectroscopy (MRS) and striatal D2BP via [18F]Fallypride.~Pearson's correlation coefficient is used with a possible range between -1 to 1 indicating strong association in the same direction as correlation is closer to 1, strong association in opposite direction as correlation is closer to -1, and no association as correlation is closer to 0." (NCT03648892)
Timeframe: assessed at Days 2-5

InterventionCorrelation Coefficiant (Number)
Dopamine D2/3 Receptor Antagonists-0.254

[back to top]

Change in Striatal Dopamine D2BP After a Palatable Meal

To determine the effect of palatable meal consumption on striatal D2BP using [11C]Raclopride (NCT03648892)
Timeframe: assessed at Days 2-5

InterventionBinding Potential (Mean)
Dopamine D2/3 Receptor Antagonists-0.0164

[back to top]

Correlation Between Change in Striatal Dopamine D2BP After a Palatable Meal and BMI

To determine association between change in striatal dopamine D2BP after a palatable meal consumption and BMI. Binding potential estimates will be estimated within subjects using [11C]Raclopride (NCT03648892)
Timeframe: assessed at Days 2-5

InterventionCorrelation Coefficient (Number)
Dopamine D2/3 Receptor Antagonists0.276

[back to top]

Correlation Between Striatal D2 Receptor Binding Potential (D2BP) as Measured by [18F]Fallypride and [11C]Raclopride Time-activity Curves

"Correlations between striatal D2BP via [18F]Fallypride and striatal D2BP via [11C]Raclopride is obtained.~Pearson's correlation coefficient is used with a possible range between -1 to 1 indicating strong association in the same direction as correlation is closer to 1, strong association in opposite direction as correlation is closer to -1, and no association as correlation is closer to 0." (NCT03648892)
Timeframe: assessed at Days 2-5

InterventionCorrelation Coefficient (Number)
Dopamine D2/3 Receptor Antagonists0.468

[back to top]

Associations Between ad Libitum Meal Consumption and Striatal D2 Receptor (D2R)

Exploratory analyses of correlations between eating behavior measured by ad libitum food intake at a single meal and striatal D2R via [18F]Fallypride and via [11C]Raclopride (NCT03648892)
Timeframe: assessed at Days 2-5

InterventionCorrelation Coefficient (Number)
D2R Via [18F]FallyprideD2R Via [11C]Raclopride
Dopamine D2/3 Receptor Antagonists-0.037-0.118

[back to top]

Associations Between Behavioral Performance on Food Go/No Go Computer Task and Striatal D2BP

"Exploratory analyses of correlations between behavioral performance on Food Go/No Go computer task measured by No Go accuracy as commission errors and striatal D2BP via [18F]Fallypride and via [11C]Raclopride.~Pearson's correlation coefficient is used with a possible range between -1 to 1 indicating strong association in the same direction as correlation is closer to 1, strong association in opposite direction as correlation is closer to -1, and no association as correlation is closer to 0." (NCT03648892)
Timeframe: assessed at Days 2-5

InterventionCorrelation Coefficient (Number)
D2BP Via [18F]FallyprideD2BP Via [11C]Raclopride
Dopamine D2/3 Receptor Antagonists0.1560.047

[back to top]

Relationship Between Striatal D2BP and BMI is Quadratic or Linear

Coefficient estimate of the quadratic term of BMI in quadratic regression is obtained and Coefficient estimate of the linear term of BMI in simple linear regression is obtained. (NCT03648892)
Timeframe: assessed at Days 2-5

InterventionCoefficient estimate (Number)
Coefficeint of quadratic determination with D2BP Via [18F]FallyprideCoefficient of quadratic determination with D2BP Via [11C]RacloprideCoefficient of linear determination with D2BP Via [18F]FallyprideCoefficient of linear determination with D2BP Via [11C]Raclopride
Dopamine D2/3 Receptor Antagonists-0.022-0.001-0.032-0.027

[back to top]