Amisulpride

Amisulpride is a dopamine D₂ and D₃ receptor antagonist (K_is = 3 and 3.5 nM, respectively).¹ It is also an antagonist of the serotonin (5-HT) receptor subtypes 5-HT_2B, 5-HT₇, and 5-HT_7A (K_is = 13, 11.5, and 135.5 nM, respectively). It is selective for these receptors over a panel of 39 additional receptors, ion channels, and transporters (K_is = >1,000 nM for all). Amisulpride increases 7-OH-DPAT-induced decreases in dopamine and acetylcholine release in electrically stimulated rat striatal slices (EC₅₀s = 2.2 and 1.2 nM, respectively).² It increases the levels of dopamine and the dopamine metabolite 3,4-dihydroxyphenylacetic acid (DOPAC) in rat striatum and nucleus accumbens when administered intraperitoneally at a dose of 10 mg/kg. Amisulpride decreases immobility time in the forced swim test in rats, as well as increases stress-induced decreases in sucrose consumption in a rat model of depression induced by chronic mild stress.³

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1. Abbas, A.I., Hedlund, P.B., Huang, X.P., et al. Amisulpride is a potent 5-HT₇ antagonist: Relevance for antidepressant actions in vivo. Psychopharmacology (Berl.) 205(1), 119-128 (2009).

2. Schoemaker, H., Claustre, Y., Fage, D., et al. Neurochemical characteristics of amisulpride, an atypical dopamine D₂/D₃ receptor antagonist with both presynaptic and limbic selectivity. J. Pharmacol. Exp. Ther. 280(1), 83-97 (1997).

3. Papp, M., and Wieronska, J. Antidepressant-like activity of amisulpride in two animal models of depression. J. Psychopharmacol. 14(1), 46-52 (2000).