D₂ Receptor Antagonist

A 80426 is an orally active serotonin (5-HT uptake) inhibitor (IC₅₀ = 13 nM; K_i = 3.8 nM) and α₂-Adrenoceptor receptor antagonist (K_i = 2 nM). A 80426 shows weak antagonistic effect to dopamine D₁ receptor (K_i = 744 nM) and D₂ receptor (K_i = 52 nM). A 80426 upregulates the expression and activity of TRPV1, activates the NF-κB and PI3K pathways, and reduces the levels of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α. A 80426 can be used in research related to inflammatory pain and depression.

Dopamine D2 receptor antagonist-3 (Example 17) is an orally active and selective dopamine D2 receptor antagonist with a pIC₅₀ of 5.52. Dopamine D2 receptor antagonist-3 exhibits antipsychotic activity in the Apomorphine (HY-12723) induced agitation in rats. Dopamine D2 receptor antagonist-3 can be used for psychiatric and neurological disorders research.

1192U90 is an antipsychotic agent, dopamine D₂ receptor antagonist as well as serotonin 5-HT_1a receptor agonist. 1192U90 reduces the number of spontaneously firing neurons in the limbic dopamine system.

BRL 34778 is a potent, selective and orally active dopamine D2 receptor antagonist with a K_i of 2.14 nM. BRL 34778 exhibits antipsychotic activity with low activity for extrapyramidal effects and sedation. BRL 34778 can be used for the research of neurological disease, such as schizophrenia.

Tefludazine is an orally active antagonist of dopamine D₂ receptor with an IC₅₀ of 8.8 nM and 5-HT₂ receptor with an IC₅₀ of 8.6 nM. Tefludazine moderately inhibits the uptake of dopamine, norepinephrine and serotonin in rat brain synaptosomes, with IC₅₀ values of 520 nM, 660 nM and 7000 nM, respectively. Tefludazine exhibits long-acting antipsychotic activity, lacks anticholinergic activity, shows Clozapine (HY-14539)-like effects at low doses and Haloperidol (HY-14538)-like effects at high doses. Tefludazine can be used for the research of psychotic disorders.

Risperidone mesylate(R 64 766 mesylate) 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.

Blonanserin-d₅ (AD-5423-d₅) is a deuterium labeled Blonanserin (HY-13575). Blonanserin is a dopamine D2/5-HT2 receptor antagonist and an atypical antipsychotic.

Methopromazine maleate is a dopamine D2 receptor (Dopamine D2 receptor) antagonist belonging to the phenothiazine class of compounds, with an LD₅₀ of 366 mg/kg in mouse studies. Methopromazine maleate competitively binds to and blocks G-protein coupled receptors (GPCR) in the central nervous system, thereby inhibiting downstream signal transduction. Methopromazine maleate can be used in research on chronic schizophrenia.

Metopimazine-d₆ (EXP999-d₆; RP9965-d₆) is the deuterium labeled Metopimazine (HY-116578). Metopimazine (EXP999; RP9965) is a phenothiazine, orally available, selective dopamine D2 receptor antagonist that does not penetrate the blood-brain barrier. Metopimazine blocks dopamine D2 receptors in the chemoreceptor trigger zone and the periphery, thereby inhibiting nausea and vomiting. Metopimazine is indicated for chemotherapy-induced nausea and vomiting, and has low central side effects due to its poor brain penetration. The use of metopimazine in acute gastroenteritis may have potential risks.

Melperone (Standard) is the analytical standard of Melperone (HY-B2169). This product is intended for research and analytical applications. Melperone is a butyrophenone with atypical antipsychotic properties. Melperone is a multireceptor antagonist with K_ds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with K_d values ​​of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone is also a CYP2D6 inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly.

Melperone-d₄ hydrochloride is the deuterium labeled Melperone hydrochloride (HY-103109). Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with K_ds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with K_d values ​​of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly.

Iloperidone hydrochloride (HP 873 hydrochloride) is a D₂/5-HT₂ receptor antagonist. Iloperidone hydrochloride is an atypical antipsychotic for the schizophrenia symptoms.

Haloperidol-d₄ N-Oxide is the deuterium labeled Haloperidol. Haloperidol is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic.

ADX-10061 (compound NNC 687) is a dopamine D1 receptor antagonist with the K_i values of 9.1 nM, 5.8 nM, > 10 000 nM and 355 nM for adenylyl cyclase, D1, D2 and 5-HT₂ receptor, respectively. ADX-10061 can be used for study of schizophrenia.

BRD5814 is a D2R antagonist. BRD5814 can be used in schizophrenia research.

Biriperone is a D₁, D₂, and 5-HT_2A receptor antagonist with pK_i values of 6.372, 7.88 and 7.619. Biriperone blocks amphetamine-induced hyperactivity and stereotypy in rodents. Biriperone blocks secondary conditioned avoidance responses in rodents. Biriperone can be used for the research of schizophrenia.

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

Abaperidone is a potent antagonist of 5-HT_2A receptor and dopamine D₂ receptor with IC₅₀s of 6.2 and 17 nM.

(S)-Remoxipride ((-)-Remoxipride) hydrochloride hydrate ((S)-Remoxipride hydrochloride hydrate) is a selective dopamine D₂-receptor antagonist with an IC₅₀ value of 1.57 μM. (S)-Remoxipride hydrochloride hydrate can be used for the research of psychotic disorder.

Desethoxy Quetiapine dihydrochloride (Compound 28) is an antagonist for dopamine D2 receptor with an IC₅₀ of 1330 nM. Desethoxy Quetiapine dihydrochloride antagonises Apomorphine (HY-12723)-induced climbing and swimming disruption in mouse models.