Amisulpride hydrochloride  (Synonyms: 氨磺必利盐酸盐; DAN 2163 hydrochloride)

Amisulpride hydrochloride is a dopamine D₂/D₃ receptor antagonist with K_is of 2.8 and 3.2 nM for human dopamine D₂ and D₃, respectively.

Ki: 2.8 nM (D₂ receptor), 3.2 nM (D₃ receptor)

Amisulpride hydrochloride is an atypical dopamine D₂/D₃ receptor antagonist with K_is of 2.8 and 3.2 nM for human dopamine D₂ and D₃, respectively. Amisulpride hydrochloride (100 nM) inhibits quinpirole-elicited [³H]thymidine incorporation with an IC₅₀ value of 22±3 nM (n=3). Amisulpride hydrochloride slightly but significantly increases [³H]dopamine release from slices of the rat striatum (S₂/S₁=0.88±0.04 under control conditions, n=6; 1.04±0.08 in the presence of 100 nM Amisulpride hydrochloride,n=4; P<0.05) and opposes the inhibitory effects of 7-OH-DPAT in both brain areas^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Only the highest dose of Amisulpride hydrochloride (100 mg/kg) significantly reduces dopamine levels in the striatum or limbic system. Amisulpride hydrochloride significantly increases the synthesis of dopamine in the rat striatum and limbic system at doses of 20 and 100 mg/kg. Amisulpride hydrochloride (0.5 to 75 mg/kg) fails to provoke an additional increase in dopa accumulation in the striatum but slightly accelerates, at 75 mg/kg, dopamine synthesis in the limbic system. In comparison with vehicle-treated controls, Amisulpride hydrochloride (10 mg/kg) increases extracellular dopamine levels. The administration of Amisulpride hydrochloride (0.5 to 15 mg/kg s.c.) provokes a time- and dose-dependent increase in the stimulation-evoked dopamine release. Amisulpride hydrochloride decreases striatal ACh levels significantly at 30 and 100 mg/kg (87.5% and 56.3% of control levels, respectively)^[1]. In both acute study, Amisulpride hydrochloride (70 mg/kg, p.o.) significantly increases the duration of swimming behavior [F(3,28)=45.90, p<0.01]^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

405.94

C₁₇H₂₈ClN₃O₄S

81342-13-4

氨磺必利盐酸盐

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Schoemaker H, et al. Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity. J Pharmacol Exp Ther. 1997 Jan;280(1):83-97.  [Content Brief]

  [2]. Pawar GR, et al. Evaluation of antidepressant like property of amisulpride per se and its comparison with fluoxetine and olanzapine using forced swimming test in albino mice. Acta Pol Pharm. 2009 May-Jun;66(3):327-31.  [Content Brief]