D₂ Receptor Antagonist

Moperone (R 1658) is an antagonist for D2 dopamine receptor and D3 dopamine receptor, with IC₅₀ of 1.0 nM and 1.0 nM.

Ecopipam (SCH 39166) hydrobromide 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 hydrobromide 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 hydrobromide can be used for the research of schizophrenia and obesity.

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

Risperidone-d₄ is the deuterium labeled Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.

Lurasidone metabolite 14326 hydrochloride is a minor active metabolite of Lurasidone (HY-B0032A) generated via metabolism by CYP3A4. Lurasidone metabolite 14326 hydrochloride shares similar receptor-binding properties with Lurasidone, acting as an antagonist of the dopamine D2 receptor (dopamine D2 receptor), an antagonist of the serotonin 5-HT2A and 5-HT7 receptors (5-HT2A and 5-HT7 receptor), and a partial agonist of the serotonin 5-HT1A receptor. Lurasidone metabolite 14326 hydrochloride can be used in the research of schizophrenia and bipolar depression.

Zuclopenthixol ((Z)-Clopenthixol) dihydrochloride is a thioxanthene derivative which acts as a mixed dopamine D1/D2 receptor antagonist. Zuclopenthixol dihydrochloride is used in the study of schizophrenia.

MLS6357 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist. MLS6357 exhibits antagonist activity in the D3R-mediated and the BRET-based β-arrestin recruitment assay with IC₅₀s of 13 and 14 μM, and no activity for other DAR subtypes (D1R/D2R/D4R/D5R) (IC₅₀ > 100 μM). MLS6357 is also an antagonist in the D3R-mediated Go-BRET assay with an IC₅₀ of 17 μM. MLS6357 can be used for the study of neuropsychiatric disorders, including substance use disorder.

FAUC 213 is an orally active and highly selective dopamine D₄ receptor complete antagonist with a K_i of 2.2 nM for hD_4.4. FAUC 213 has less activity on D₂ and D₃ receptors (K_is of 3.4 μM, 5.3 μM for hD₂, hD₃, respectively). FAUC 213 can cross the blood-brain barrier (BBB). FAUC 213 exhibits atypical antipsychotic characteristic.

N-Methylspiroperidol is a D2 receptor antagonist. N-Methylspiroperidol can be labeled as [18F]N-Methylspiroperidol and used in PET (Positron Emission Tomography) to study how it binds to the 5-HT2C receptor and the competition and effects of neurotransmitters like dopamine on these receptors.

S-14506 hydrochloride is a potent 5-HT1A agonist, as well as 5-HT_2A/2C antagonist. S-14506 hydrochloride displays dopamine antagonist properties by blocking dopamine D2 receptors. S-14506 hydrochloride inhibits the in vivo binding of [3H]raclopride in striatum and olfactory bulbs. S-14506 hydrochloride has the potential for the research of anxiolytic agent.

D3/5-HT receptor modulator-1 (compound 5i) is a selective dopamine D3 receptor and 5-HT2A receptor antagonist and a partial 5-HT1A receptor agonist. D3/5-HT receptor modulator-1 shows K_i values of 4.5 nM, 11.9 nM, and 15.3 nM for dopamine D3, 5-HT2A, and 5-HT2A receptors. D3/5-HT receptor modulator-1 has a low affinity for dopamine D2 receptors, 5-HT2C receptors, and hERG channels. D3/5-HT receptor modulator-1 has an atypical antipsychotic profile.

Mosapramine (Clospipramine) is an orally active antipsychotic agent and one of the metabolites of Clocapramine (HY-B2073) after oral absorption. Mosapramine exerts its effects by specifically binding to striatal dopamine D2 receptors and frontal lobe 5-HT2 receptors, with a D2/5-HT2 receptor occupancy ratio of 7.4. Mosapramine induces typical neuropharmacological responses in rat brain regions, including extrapyramidal symptoms, hyperprolactinemia, increased salivation, constipation, and upregulated Fos protein expression. Mosapramine also features a reduced incidence of weight loss. Mosapramine is applicable to research related to schizophrenia.

Spiramide (AMI-193) is a potent and selective antagonist of 5-HT₂ and dopamine D2 receptor, with K_is of 2 nM and 3 nM, respectively. Spiramide has >2000-fold selectivity for 5-HT₂ versus 5-HT_1C (K_i=4300 nM) receptors. Spiramide exhibits antipsychotic activity.

Risperidone hydrochloride (R 64 766 hydrochloride) 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.

Zuclopenthixol-d₄ succinate is the deuterium labeled Zuclopenthixol. Zuclopenthixol is a thioxanthene derivative which acts as a mixed dopamine D1/D2 receptor antagonist.

Risperidone-d6 (R 64 766-d6) is the deuterium labeled Risperidone (HY-11018). 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.

Ziprasidone (CP-88059) mesylate trihydrate is an orally active 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).

Clocapramine is an antagonist of the D₂, 5-HT_2A receptors.

Propionylpromazine-d₆ (hydrochloride) is the deuterium labeled Propionylpromazine hydrochloride. Propionylpromazine hydrochloride (Propiopromazine hydrochloride), a dopamine receptor D2 (DRD2) antagonist, can be used in the research of Parkinson disease.

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