Dopamine Receptor Antagonist

Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (K_i=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (K_i=11 to 31 nM), muscarinic M1-5 (K_i=1.9-25 nM), and adrenergic α1 receptor (K_i=19 nM). Olanzapine is an atypical antipsychotic.

Droperidol (Dehydrobenzperidol) is a butyrophenone pamine-2 receptor antagonist that inhibits the activation of GABA(A) and neuronal nicotinic receptors (nAChR), with IC₅₀ values of 12.6 nM and 5.8 μM. Droperidol has anesthetic and sedative properties.

Levomepromazine (Methotrimeprazine) is an orally active antipsychotic compound and Ca²⁺ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca²⁺ levels. Levomepromazine has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine can induce adaptive ER stress and autophagy. In addition, Levomepromazine has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine can be used in the study psychiatric disorders and relieving nausea and vomiting.

Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).

Piperacetazine is an orally active dopamine receptor antagonist and phenothiazine antipsychotic. Piperacetazine can directly bind to the PAX3::FOXO1 fusion protein and inhibit its transcriptional activity. Piperacetazine also exhibits antitumor activity with an IC₅₀ of 7.627 μM against PANC-1 cells. Piperacetazine can be used for the research of diseases such as schizophrenia and pancreatic cancer and other tumors.

Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2.

Levosulpiride (RV-12309) is the (S)-enantiomer of sulpiride, which is a D2 receptor a antagonist, an atypical antipsychotic agent of the benzamide class.

Azaperone is an antagonist of dopamine D2 receptor (Dopamine D2 Receptor) and α-adrenergic receptor (AR). Azaperone reduces vasomotor tone, mean arterial pressure, hematocrit, hemoglobin concentration, and etorphine-induced duration; induces transient tachycardia followed by bradycardia, splenic uptake of red blood cells, and sedation; alters animal behaviors; and produces sedation with distinct onset and duration in foals. Azaperone is used for sedation and tranquilization in various animals to reduce stress and aggressive behaviors, and serves as a preanesthetic agent.

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

Alizapride is a potent antiemetic, acting as a dopamine receptor antagonist. Alizapride also used in human digestive disorders.

Clozapine-d₄ is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors.

Clebopride malate is an orally active dopamine Receptor antagonist. Clebopride malate acts on dopamine D2 receptors and has antiemetic and prokinetic effects. Clebopride malate can be used in the study of functional gastrointestinal disorders.

SB269652 is the first drug-like allosteric modulator of the dopamine D2 receptor (D2R); a new chemical probe that can differentiate D2R monomers from dimers or oligomers depending on the observed pharmacology.

Lenperone (AHR 2277 free base) has antipsychotic effect. Lenperone improves depressive symptoms.

Haloperidol (Standard) is the analytical standard of Haloperidol. This product is intended for research and analytical applications. Haloperidol is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic.

(S)-SCH-23390 hydrochloride is the S-enantiomer of SCH-23390 (HY-19545). SCH-23390 is a dopamine D1-like receptor antagonist (with K_i values of 0.2 nM and 0.3 nM for the D1 and D5 receptor subtypes, respectively).

Sultopride hydrochloride (LIN-1418 hydrochloride) is a selective antagonist of dopamine D2 receptor.

Haloperidol decanoate is a depot preparation of haloperidol, a commonly used butyrophenone derivative with antipsychotic activity. Haloperidol decanoate can increase the striatal D₂ receptor in rat. Haloperidol decanoate can improve conditions of psychoses (mainly schizophrenia). Haloperidol decanoate can lead to increased accumulation of the dopamine metabolites homo-vanillic acid. Haloperidol decanoate can reduce intestinal transport, increase gastric emptying and reduce acid output in rat model.

Levomepromazine maleate (Methotrimeprazine maleate) is an orally active antipsychotic compound and Ca²⁺ release inducer. Levomepromazine maleate inhibits SERCA pump and induces an increase in cytoplasmic Ca²⁺ levels. Levomepromazine maleate has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine maleate can induce adaptive ER stress and autophagy. In addition, Levomepromazine maleate has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine maleate can be used in the study psychiatric disorders and relieving nausea and vomiting.

JNJ-37822681 dihydrochloride is a potent, specific, centrally active, fast-dissociating dopamine D₂ receptor antagonist with a moderate binding affinity for the dopamine D_2L receptor (K_i =158 nM), which has potential for the treatment of schizophrenia and bipolar disorder.