Dopaminargics - Antagonists

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A7111 Acepromazine maleate ≥98% (HPLC) Acepromazine is a phenothiazine antipsychotic comonly used as a veterinary drug (horses, dogs and cats). The compound is an analogue antipsychotic drug chlorpromazine (#C8138). The drug is thought to block receptors of dopamine in the brain. Recently it was discover that the compound inhibits ABCG2 transported protein, which overexpression in tumors is associated with drug resistance.
 
A2729 Amisulpride ≥98% (HPLC) Amisulpride is a highly selective D2/D3 dopamine receptor antagonist and atypical antipsychotic.
Amisulpride is a substituted benzamide derivative. It has a higher affinity towards dopamine receptors in limbic structures than the striatal structures. Amisulpride has a therapeutic effect against schizophrenia.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR6(3362), HTR7(3363)
D034 (−)-Butaclamol hydrochloride solid Dopamine receptor antagonist; less active enantiomer.
 
D033 (+)-Butaclamol hydrochloride (+)-Butaclamol is a dopamine receptor antagonist; active enantiomer.
human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816)
C1671 Chlorprothixene hydrochloride D2 dopamine receptor antagonist; blocks a subset of GABAA receptors in rat cortex that is also blocked by clozapine; thioxanthine antipsychotic.
human ... DRD2(1813), DRD3(1814), HTR2A(3356), HTR2C(3358)
C6305 Clozapine Atypical antipsychotic compound. Selective antagonist for D4-dopamine receptor. Antagonist at 5-HT2A, 5-HT2C, 5-HT3, 5-HT6, and 5-HT7 serotonin receptors.
human ... ADRA1A(148), ADRA2A(150), ADRA2C(152), CHRM1(1128), DRD2(1813), DRD3(1814), DRD4(1815), HRH1(3269), HRH4(59340), HTR2A(3356), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR6(3362), HTR7(3363), KCNH1(3756), KCNH2(3757), UGT1A4(54657)
rat ... Adra1a(29412), Adra2a(25083), Adrb1(24925), Chrm1(25229), Drd1a(24316), Drd2(24318), Drd3(29238), Drd4(25432), Hrh1(24448), Htr1a(24473), Htr1b(25075), Htr2a(29595), Htr2b(29581), Htr2c(25187), Htr3a(79246), Htr7(65032), Slc6a4(25553)
D122 Domperidone powder, ≥98% (HPLC) Peripheral dopamine receptor antagonist that does not cross the blood-brain barrier; anti-emetic.
human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816), KCNH2(3757)
rat ... Drd1a(24316), Drd2(24318), Drd3(29238), Htr3a(79246)
D1414 Droperidol D1, D2 dopamine receptor antagonist; butyrophenone antipsychotic and anti-emetic.
Droperidol is a potent antagonist of dopamine subtype 2 receptor. It is an antipsychotic, which is used to treat acute behavioral anomalies. It helps to manage postoperative nausea and vomiting.
human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), HTR2A(3356), KCNH1(3756), KCNH2(3757)
E101 S-(−)-Eticlopride hydrochloride ≥98% (HPLC), powder Potent and selective D2 dopamine receptor antagonist. Eticlopride is highly specific for DAD2 receptors than pimozide or haloperidol. The gene encoding the D2 dopamine receptor (DRD2) is linked with a several disorders including Parkinson′s disease, schizophrenia, and susceptibility to alcoholism.
human ... DRD2(1813)
F4429 FAUC 213 ≥98% (HPLC), solid Highly selective D4 dopamine receptor full antagonist
human ... DRD2(1813), DRD3(1814), DRD4(1815)
F4765 Fluphenazine dihydrochloride D1/D2 dopamine receptor antagonist; phenothiazine antipsychotic; H1 histamine receptor antagonist.
human ... DRD1(1812), DRD2(1813), HRH1(3269)
F100 Fluspirilene Fluspirilene has a potential to inhibit the activity of cyclin-dependent kinase 2 (CDK2). It is an effective anti-cancer agent used for treating human hepatocellular carcinoma.
Fluspirilene is a dopamine receptor antagonist. It also acts as a calcium channel blocker. Fluspirilene is an antipsychotic agent and exhibits neuoleptic properties. It exhibits therapeutic effects against glioblastoma and Schizophrenia.
human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816)
G0544 GR 103691 ≥98% (HPLC), solid D3 dopamine receptor antagonist.
rat ... Htr1a(24473)
H1512 Haloperidol powder Haloperidol is a butyrophenone antipsychotic. It is also classified as a neuroleptic (powerful tranquilizer). Haloperidol acts as a D2, D3, and D4 dopamine receptor antagonist and thus causes Parkinson′s disorder. It also has a negative effect on the central nervous system.
human ... ABCB1(5243), ADRA1A(148), ADRA2A(150), ADRA2C(152), CHRM1(1128), DRD2(1813), DRD3(1814), DRD4(1815), EBP(10682), HRH1(3269), HTR2A(3356), HTR2C(3358), HTR7(3363), KCNH1(3756), KCNH2(3757), PRNP(5621)
rat ... Adra1a(29412), Adra2a(25083), Chrm1(25229), Chrm2(81645), Drd1a(24316), Drd2(24318), Drd3(29238), Drd4(25432), Hrh1(24448), Htr1a(24473), Htr1b(25075), Htr2a(29595), Htr2c(25187), Oprs1(29336), Slc6a3(24898), Slc6a4(25553)
SML0033 Itopride hydrochloride ≥98% (HPLC) Itopride hydrochloride enhances the gastrointestinal motility by blocking the activity of dopamine on the D2 receptors, on the post-synaptic cholinergic nerves and by inducing the liberation of acetylcholine in the myenteric plexus. It also inhibits the hydrolysis of the released acetylcholine with the help of acetylcholinesterase.
Itopride is an acetylcholinesterase (AChE) inhibitor and D2 dopamine receptor antagonist. Itopride is used as a gastroprokinetic agent.
 
L135 L-741,626 ≥98% (HPLC) Selective D2 dopamine receptor antagonist.
human ... DRD2(1813), DRD3(1814), DRD4(1815)
L131 L-745,870 hydrochloride Selective D4 dopamine receptor antagonist.
human ... DRD4(1815)
L106 Loxapine succinate salt solid D2/D4 dopamine receptor antagonist; 5-HT2A/2B, 5-H7 serotonin receptor antagonist; dibenzoxazepine antipsychotic agent.
human ... DRD2(1813), DRD3(1814), DRD4(1815), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR7(3363)
M4068 Mesoridazine benzenesulfonate ≥98% (HPLC), powder Mesoridazine benzenesulfonate is a D2 dopamine receptor antagonist; antipsychotic.
human ... DRD2(1813), HTR2A(3356)
M0763 Metoclopramide hydrochloride solid D2 antagonist; 5-HT3 antagonist; antipsychotic; anti-emetic.
human ... DRD2(1813), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360)
SML0066 NGB 2904 hydrochloride ≥98% (HPLC) Inhibition of dopamine D3 receptor function by NGB 2904 increases spontaneous locomotor activity in rodents.
NGB 2904 is a potent and selective dopamine D3 receptor antagonist with a D3/D2 ratio of 800 for rat and high binding affinity (1.4 nM) at the hD3 receptor with 150-fold selectivity for primate D3 receptors over primate D2L receptors. It attenuates the rewarding effects of cocaine and methamphetamine.
 
O111 Octoclothepin maleate salt solid D2 dopamine receptor antagonist; 5-HT2 serotonin receptor antagonist.
human ... DRD2(1813), HTR2A(3356), HTR2B(3357), HTR2C(3358)
O1141 Olanzapine ≥98% (HPLC) Olanzapine is a 5-HT2 serotonin and D1/D2 dopamine receptor antagonist.
human ... DRD2(1813), DRD3(1814), DRD4(1815), HTR2A(3356), HTR2C(3358)
P6402 Perphenazine D2 dopamine receptor antagonist; α-adrenergic receptor antagonist and σ-receptor agonist; phenothiazine antipsychotic. Inhibits glutamate dehydrogenase in vitro.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152), DRD2(1813), OPRS1(10280)
P1793   Pimozide D2 dopamine receptor antagonist; binds with high affinity to the cloned 5-HT7 receptor; Ca2+ channel antagonist; antipsychotic
human ... ABCB1(5243), CACNA1G(8913), CYP3A4(1576), DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816), HTR2A(3356), HTR7(3363), KCNH1(3756), KCNH2(3757), OPRD1(4985)
mouse ... Abcb1a(18671), Abcb1b(18669)
rat ... Scnn1g(24768)
P3246 Pipamperone dihydrochloride ~99% (HPLC), powder D2 dopamine receptor antagonist; 5-HT2 serotonin receptor antagonist; antipsychotic.
Pipamperone, a butyrophenone derivative is a pharmacological chaperone and is a membrane-permeable dopamine receptor D4 (DRD4) antagonist. The affinity of pipamperone is higher for DRD4 and 5-hydroxytryptamine 2A receptor (5-HT2A) in comparison with DRD2. It may be useful therapeutic in treating behavioral disorders and psychomotor agitation symptoms.
 
P9178 Prochlorperazine dimaleate salt Phenothiazine antipsychotic; D2 dopamine receptor antagonist; antispasmodic
Prochlorperazine is an anti-nausea and neuroleptic agent. It is known to cause neuropsychiatric side effects. Prochlorperazine inhibits the action of dopamine in the central nervous system. It acts as an antiemetic drug and prevents vomiting and stimulates sleep. Prochlorperazine is useful as a tranquilizer in the treatment of schizophrenia and nonpsychotic anxiety.
human ... DRD2(1813)
P6656 Promazine hydrochloride D2 dopamine receptor antagonist; phenothiazine antipsychotic.
human ... DRD2(1813), DRD3(1814), DRD4(1815), HTR2A(3356)
P7780 Propionylpromazine hydrochloride Phenothiazine antipsychotic; D2 dopamine receptor antagonist.
human ... DRD2(1813)
D041 S(+)-Propylnorapomorphine hydrochloride solid Limbic-selective dopamine antagonist.
 
Q3638 Quetiapine hemifumarate salt ≥98% (HPLC) Quetiapine hemifumarate is an atypical antipsychotic, a combined serotonin (5HT2) and dopamine (D2) receptor antagonist.
Quetiapine promotes oligodendrogenesis in vitro. It is used in treating depressive disorders.
human ... DRD2(1813), HTR2A(3356), HTR2C(3358)
R121 S(−)-Raclopride (+)-tartrate salt >97%, solid Selective D2 dopamine receptor antagonist.
human ... DRD2(1813)
PZ0174 Sonepiprazole hydrate ≥98% (HPLC) Sonepiprazole (U-101387) is a selective D4 dopamine antagonist. Ki = 10 nM for the dopamine D4.2 receptor.
 
S7395 Spiperone solid Selective D2 dopamine receptor antagonist; α1B-adrenoceptor antagonist; mixed 5-HT2A/5-HT1 serotonin receptor antagonist; antipsychotic.
human ... ADRA1B(147), DRD2(1813), DRD3(1814), HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356)
rat ... Adra1a(29412), Adra1b(24173), Adra1d(29413), Adra2a(25083), Drd1a(24316), Drd2(24318), Drd3(29238), Htr1a(24473), Htr2a(29595), Htr2c(25187), Htr7(65032)
S7771 (S)-(−)-Sulpiride ≥98% (titration) (S)-(−)-Sulpiride or Levosulpiride blocks the inhibitory enteric D2 receptors (neuronal and muscular). It has prokinetic activity and is effective in the treatment of functional dyspepsia and gastroparesis in insulin-dependent diabetes mellitus patients.7,8 Since dopamine controls human sexual function, (S)-(−)-Sulpiride is reportedly effective in treatment of erectile dysfunctions.9
D2 dopamine receptor antagonist; antipsychotic.
human ... DRD2(1813), DRD3(1814)
rat ... Adra1a(29412), Drd2(24318), Drd3(29238), Htr1a(24473), Htr2a(29595)
S8010 (±)-Sulpiride (±)-Sulpiride is a D2 dopamine antagonist and an effective treatment for schizophrenia when used in combination with clozapine, a relatively weak D2-dopaminergic antagonist. It is an antipsychotic agent and also exhibits neuroleptic properties but poorly penetrates the central nervous system.45,46
human ... CA1(759), CA2(760), CA4(762), CA5A(763), CA5B(11238), CA9(768), DRD2(1813)
T9025 Thioridazine hydrochloride ≥99% D2 dopamine receptor antagonist; phenothazine antipsychotic with reduced extrapyramidal side effects; Ca2+ channel blocker.
human ... DRD2(1813), DRD3(1814), DRD4(1815), HTR2A(3356), HTR2C(3358)
T103 Trifluperidol hydrochloride Trifluperidol is a dopamine receptor antagonist with antipsychotic effects used in the treatment of schizophrenia. This neuroleptic penetrates the brain and also affects the glial cells leading to increased release of proinflammatory cytokines. It also alters the metabolism of carbohydrates and amino acids in the brain cortex.
human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816)
U116 U-99194 maleate salt ≥98% (HPLC), solid U-99194 is a putative D3 antagonist with a 30-fold preference for the dopamine D3 vs. D2 receptor.
human ... DRD3(1814)
F114 cis-(Z)-Flupenthixol dihydrochloride ≥98% (HPLC), solid Antipsychotic; neuroleptic agent; dopamine receptor antagonist. cis-(Z)-Flupenthixol dihydrochloride (FLU) is used to treat schizophrenia and anxiolytic and depressive disorders Dopamine D1 plays a major role in lung fluid homeostasis. It controls the airway smooth muscle tone by producing adenylyl cyclase/cAMP, that would favor airway relaxation in asthmatics. Dopamine in the lung, serves as a neurotransmitter and noradrenaline precursor.
human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816)