Background:

Amisulpride is an atypical antagonist of dopamine D2/D3 receptor with Ki values of 2.8±0.4nM and 3.2±0.3nM for D2 and D3 receptor subtypes, respectively [1].

Amisulpride has shown high affinity to the cloned and stably transfected human dopamine D2 with Ki values of 2.8±0.4nM and 3.2±0.3nM for D2 and D3 receptor subtypes, respectively. Amisulpride has been reported to inhibit radioligand binding to native dopamine D2 receptor in membranes from the rat striatum with an IC50 value of 21nM. Besides, Amisulpride has been revealed to displace [3H]raclopride binding in vivo with an ED50 value of 17.3±1.86mg/kg in the rat limbic system. In addition, Amisulpride has been noted to inhibit quinpirole-induced [3H]thymidine with an IC50 value of 22±3nM [1].

参考文献:
[1] Schoemaker H1, Claustre Y, Fage D, Rouquier L, Chergui K, Curet O, Oblin A, Gonon F, Carter C, Benavides J, Scatton B. 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.