Antagonists

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D034 (−)-Butaclamol hydrochloride solid Dopamine receptor antagonist; less active enantiomer.
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
D033 (+)-Butaclamol hydrochloride (+)-Butaclamol is a dopamine receptor antagonist; active enantiomer.
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.
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.
C1671 Chlorprothixene hydrochloride D2 dopamine receptor antagonist; blocks a subset of GABAA receptors in rat cortex that is also blocked by clozapine; thioxanthine antipsychotic.
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.
D122 Domperidone powder, ≥98% (HPLC) Peripheral dopamine receptor antagonist that does not cross the blood-brain barrier; anti-emetic.
D1414 Droperidol D1, D2 dopamine receptor antagonist; butyrophenone antipsychotic and anti-emetic.
SML1350 EPPTB ≥95% (HPLC) EPPTB is a selective antagonist of the trace amine-associated receptor 1 (TAAR1), a G protein-coupled receptor (GPCR) activated by endogenous trace amines (tyramine, tryptamine, synephrine, octopamine, β)-phenylethylamine), which are chemically similar to monoaminergic neurotransmitters (epinephrine, norepinephrine, dopamine). TAAR1 is considered a promising target for the treatment of neuropsychiatric disorders, however study of TAAR1 has hampered by the fact that selective ligands have not been available. EPPTB is the first potent and selective TAAR1 antagonist with an IC50 of 28 nM at mouse TAAR1. EPPTB is less selective for rat and human with IC50 values of 4539 and 7487 nM, respectively.
F4429 FAUC 213 ≥98% (HPLC), solid Highly selective D4 dopamine receptor full antagonist
F4765 Fluphenazine dihydrochloride D1/D2 dopamine receptor antagonist; phenothiazine antipsychotic; H1 histamine receptor antagonist.
F100 Fluspirilene Dopamine receptor antagonist; antipsychotic; calcium channel blocker.
G0544 GR 103691 ≥98% (HPLC), solid D3 dopamine receptor antagonist.
H3041 Halopemide ≥98% (HPLC) Halopemide is a dopamine receptor antagonist and a phospholipase D2 inhibitor. Halopemide may be used as a screen to identify inhibitors of human PLD2 using an in vitro biochemical assay. It is also inhibitory at benzodiazepine binding sites.
H1512 Haloperidol powder Butyrophenone antipsychotic; D2, D3, and D4 dopamine receptor antagonist.
SML0033 Itopride hydrochloride ≥98% (HPLC) 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.
L131 L-745,870 hydrochloride Selective D4 dopamine receptor antagonist.
L133 L-750,667 trihydrochloride solid Selective D4 dopamine receptor antagonist.
L106 Loxapine succinate salt solid D2/D4 dopamine receptor antagonist; 5-HT2A/2B, 5-H7 serotonin receptor antagonist; dibenzoxazepine antipsychotic agent.
M4068 Mesoridazine benzenesulfonate ≥98% (HPLC), powder Mesoridazine benzenesulfonate is a D2 dopamine receptor antagonist; antipsychotic.
M0763 Metoclopramide hydrochloride solid D2 antagonist; 5-HT3 antagonist; antipsychotic; anti-emetic.
M1818 Molindone hydrochloride ≥98% (HPLC), solid D2 dopamine receptor antagonist; MAO inhibitor.
N140 N-(p-Isothiocyanatophenethyl)spiperone hydrochloride Selective irreversible D2 dopamine receptor antagonist.
S128 N-Methylspiperone hydrochloride solid D2 dopamine receptor antagonist.
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.
PZ0354 PF-04363467 hydrochloride ≥98% (HPLC) PF-4363467 hydrochloride is a Dopamine D3/D2 receptor antagonist. PF-4363467 has 100-fold selectivity for D3 with a Ki value of 3.1 nM for D3R compared to a Ki value of 692 nM for D2R and high selectivity for D3R compared to other biogenic amine receptors. PF-4363467 attenuated opioid drug-seeking behavior in a rat model of addiction without causing the extrapyramidal symptoms often associated with D2R antagonism.
SML0018 PG01037 dihydrochloride hydrate ≥98% (HPLC) PG01037 dihydrochloride is a selective dopamine D3 receptor antagonist. It is more selective for D3 receptors than other D3 antagonists that are currently available with a D2/D3 selectivity ratio of 867and a D4/D3 selectivity ratio of 13,000.
Selective dopamine D3 receptor antagonist
P6402 Perphenazine D2 dopamine receptor antagonist; α-adrenergic receptor antagonist and σ-receptor agonist; phenothiazine antipsychotic. Inhibits glutamate dehydrogenase in vitro.
P1793   Pimozide D2 dopamine receptor antagonist; binds with high affinity to the cloned 5-HT7 receptor; Ca2+ channel antagonist; antipsychotic
P3246 Pipamperone dihydrochloride ~99% (HPLC), powder D2 dopamine receptor antagonist; 5-HT2 serotonin receptor antagonist; antipsychotic.
P9178 Prochlorperazine dimaleate salt Phenothiazine antipsychotic; D2 dopamine receptor antagonist; antispasmodic
P6656 Promazine hydrochloride D2 dopamine receptor antagonist; phenothiazine antipsychotic.
P7780 Propionylpromazine hydrochloride Phenothiazine antipsychotic; D2 dopamine receptor antagonist.
Q3638 Quetiapine hemifumarate salt ≥98% (HPLC) Quetiapine hemifumarate is an atypical antipsychotic, a combined serotonin (5HT2) and dopamine (D2) receptor antagonist.
S159 R(−)-SCH-12679 maleate salt solid SCH-12679 is a benzazepine compound and a psychoactive drug that antagonizes D1-dopamine receptor. It reduces the D1-induced locomotor activity and self-mutilation in rats. SCH-12679 decreased aggressiveness and hyperactive behavior in mentally deficient patients.
D054 R(+)-SCH-23390 hydrochloride ≥98% (HPLC), solid R(+)-SCH-23390 hydrochloride is a selective D1 dopamine receptor antagonist.
D206 S(−)-DS 121 hydrochloride solid Dopamine autoreceptor antagonist with some selectivity for the D3 dopamine receptor.
R121 S(−)-Raclopride (+)-tartrate salt >97%, solid Selective D2 dopamine receptor antagonist.
D041 S(+)-Propylnorapomorphine hydrochloride solid Limbic-selective dopamine antagonist.
E101 S-(−)-Eticlopride hydrochloride ≥98% (HPLC), powder Potent and selective D2 dopamine receptor antagonist.
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.
SML1924 T1AM ≥98% (HPLC) New T1AM (3-Iodothyronamine) is an endogenous biogenic amine derived from thyroid hormone. T1AM is a potent agonist of trace amine-associated receptor TAAR1 (TAR1, TA1), a GPCR primarily found in the brain.
T9025 Thioridazine hydrochloride ≥99% D2 dopamine receptor antagonist; phenothazine antipsychotic with reduced extrapyramidal side effects; Ca2+ channel blocker.
T0410 Tiapride hydrochloride Tiapride, an atypical neuroleptic agent, antagonizes D2 and D3 dopamine receptors. It exhibits anti-dyskinetic and anxiolytic activities. It is effective in the management of alcohol withdrawal and treatment of tic disease in children.
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.
U115 U-101958 maleate salt solid U-101958 maleate salt is a selective D4 dopamine receptor antagonist. Studies have reported that U-101958 maleate cannot inhibit bromocriptine-mediated [3H]thymidine incorporation in opossum kidney (OK) cells.
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.
F114 cis-(Z)-Flupenthixol dihydrochloride ≥98% (HPLC), solid Antipsychotic; neuroleptic agent; dopamine receptor antagonist.