"目录号: HY-14545A
GPCR/G ProteinNeuronal Signaling-
Amisulpride(DAN 2163)盐酸盐是多巴胺拮抗剂，对D2和D3受体的Ki分别为2.8 nM和3.2 nM。
Dopamine Receptor
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Chlorpromazine hydrochloride-Brexpiprazole-Haloperidol-Cabergoline-Clozapine-Cariprazine hydrochloride-L-DOPA-Perphenazine-Dopamine hydrochloride-Oxidopamine hydrobromide-Sertindole-B-HT 920-Azaperone-Fluphenazine dihydrochloride-Iloperidone-
生物活性
Description
Amisulpride Hcl(DAN 2163 Hcl) is an antipsychotic drug, which is a selective dopamine antagonist (Ki=2.8 nM D2 receptor; Ki=3.2 nM D3 receptor).Target: D2/D3 receptorAmisulpride hydrochloride is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder. In small doses it is also used to treat depression. Amisulpride hydrochloride functions primarily as a D2 and D3 receptor antagonist. It has high affinity for these receptors with dissociation constants of 2.8 nM and 3.2 nM, respectively [1]. At low doses (< or = 10 mg/kg) amisulpride hydrochloride preferentially blocks presynaptic dopamine autoreceptors that control dopamine synthesis and release in the rat, whereas at higher doses (40-80 mg/kg) postsynaptic dopamine D2 receptor occupancy and antagonism is apparent. In contrast, haloperidol is active in all of these paradigms within the same dose range. Amisulpride hydrochloride preferentially inhibits in vivo binding of the D2/D3 antagonist [3H]raclopride to the limbic system (ID50 = 17 mg/kg) in comparison to the striatum (ID50 = 44 mg/kg) of the rat, increases striatal and limbic tissue 3,4-dihydroxyphenylacetic acid levels with similar potency and efficacy, and preferentially increases extracellular 3,4-dihydroxyphenylacetic acid levels in the nucleus accumbens when compared to the striatum [1]. Clinical indications: Schizophrenia; Bipolar disorder; Dysthymia; FDA Approved Date: February 2002Toxicity: Insomnia; Hypersalivation; Hyperprolactinaemia; Nausea; Vomiting [2]
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Phase 4
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Phase 4
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