D₂ Receptor Antagonist

Haloperidol is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic agent. Haloperidol can be used in the study of schizophrenia, tics in Tourette syndrome, mania in bipolar disorder, delirium, agitation, acute psychosis, and hallucinations from alcohol withdrawal.

Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a K_i of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with K_is of 9.5 nM and 4 nM, respectively. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC₅₀=11 nM).

Risperidone is a serotonin 5-HT₂ receptor blocker, P-Glycoprotein inhibitor and potent dopamine D₂ receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively.

cis-Flupenthixol is an orally active dopamine receptor antagonist, with a K_i value of 1.4 nM for the Dopamine D-1 receptor and 0.74 nM for the Dopamine D-2 receptor. cis-Flupenthixol blocks dopamine receptors in the medial preoptic area and striatum, impairs male mating behavior, and reduces the concentrations of striatal dopamine metabolites. cis-Flupenthixol alters striatal acetylcholine concentrations in a time-dependent manner and enhances Apomorphine (HY-12723)-induced stereotyped behaviors. cis-Flupenthixol inhibits exploratory locomotor activity and triggers a compensatory increase in dopamine turnover in the striatum and limbic regions. cis-Flupenthixol can be used in studies related to tardive dyskinesia.

Sulpiride is an orally active dopamine D2/D3 receptor antagonist. Sulpiride is an atypical antipsychotic agent of the benzamide family. Sulpiride can be used in research into anxiety, depression and breast cancer.

Raclopride is a dopamine D₂/D₃ receptor antagonist with potential antipsychotic effects. Raclopride binds to D₂ and D₃ receptors with K_is of 1.8 nM and 3.5 nM, respectively.

Buspirone is an orally active 5-HT1A receptor agonist, and a dopamine D2 autoreceptorsant antagonist. Buspirone is an anxiolytic agent, and can be used for the generalized anxiety disorder research.

Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia.

Ziprasidone (CP-88059), an orally active antipsychotic agent, is a combined 5-HT and dopamine receptor antagonist. Ziprasidone mesylate trihydrate has affinities for Rat D₂ (K_i=4.8 nM), 5-HT_2A (K_i=0.42 nM) and 5-HT_1A (K_i=3.4 nM).

Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with K_i values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation.

Prochlorperazine dimaleate is an orally active phenothiazine-type dopamine D2 receptor (D2R) antagonist. Prochlorperazine exhibits anti-cancer activity in vitro against various cancer cell lines. Prochlorperazine dimaleate exhibits IC₅₀ values of 6.4 μM, 4.5 μM and 2.3 μM for NOX1, NOX2 and NOX5, respectively. Prochlorperazine dimaleate has antedesmosidic activity against dengue virus (DENV). Prochlorperazine dimaleate can be used for research on nausea, vomiting, migraine, and schizophrenia.

Lurasidone (SM-13496) is an antagonist of both dopamine D₂ and 5-HT₇ with IC₅₀s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT_1A receptor with an IC₅₀ of 6.75 nM.

Amisulpride ((Rac)-Aramisulpride) is a racemic (50:50) mixture of the R-Amisulpride (HY-109167) and S-Amisulpride (HY-126068). Amisulpride is a dopamine D₂/D₃ receptor antagonist with K_i values of 2.8 and 3.2 nM for human dopamine b>D₂ and b>D₃, respectively. Amisulpride is a 5-HT₇ receptor antagonist with a K_i of 44 nM. Amisulpride can be used in psychiatric research.

Metoclopramide is a potent antagonist of 5-HT₃ and dopamine D2 receptor, with IC₅₀s of 308 nM and 483 nM, respectively. Metoclopramide can be used for the research of nausea and vomiting, gastro-oesophageal reflux, and gastroparesis.

Eticlopride hydrochloride, a selective dopamine D2‐like receptor antagonist, exhibits high affinity for dopamine D2, α1-adrenergic, α2-adrenergic, 5HT1, 5HT2 receptors with K_is of 0.09, 112, 699, 6220, and 830 nM, respectively. Eticlopride hydrochloride is an antipsychotic agent.

Rotundine is an antagonist of dopamine D1, D2 and D3 receptors with IC₅₀s of 166 nM, 1.4 μM and 3.3 μM, respectively. Rotundine is also an antagonist of 5-HT_1A with an IC₅₀ of 370 nM.

Blonanserin (AD-5423) is a potent and orally active 5-HT_2A (K_i=0.812 nM) and dopamine D2 receptor (K_i =0.142 nM) antagonist. Blonanserin is usually acts as an atypical antipsychotic agent and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension.

Flunarizine dihydrochloride is a potent dual Na⁺/Ca²⁺ channel (T-type) blocker. Flunarizine dihydrochloride is a D₂ dopamine receptor antagonist. Flunarizine dihydrochloride shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects.

Ecopipam (SCH 39166) hydrochloride is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with K_is of 1.2 nM and 2.0 nM, respectively. Ecopipam hydrochloride shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (K_i=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam hydrochloride can be used for the research of schizophrenia and obesity.

Pridopidine, a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist. Pridopidine exerts high affinity towards sigma 1 receptor (S1R) with K_i between 70 and 80 nM, which is ~100× higher than its affinity toward D2R.