4-amino-5-ethylsulfonyl-2-methoxy-N-[[1-(1,1,2,2,2-pentadeuterioethyl)pyrrolidin-2-yl]methyl]benzamide

Description

Amisulpride-d₅ is intended for use as an internal standard for the quantification of amisulpride by GC- or LC-MS. Amisulpride is a dopamine D₂ and D₃ receptor antagonist (K_is = 3 and 3.5 nM, respectively). 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). 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 reduces stress-induced decreases in sucrose consumption in a rat model of depression induced by chronic mild stress.

Uses

Labelled Amisulpride (A633250). Amisulpride is a neuroleptic agent, an analogue of Sulpiride (S689145). Amisulpride is used as an antipsychotic. Amisulpride is a dopamine receptor antagonist.

IC 50

D₃ Receptor

References

[1] ATHEIR I ABBAS. Amisulpride is a potent 5-HT7 antagonist: relevance for antidepressant actions in vivo.[J]. Psychopharmacology, 2009: 119-128. DOI: 10.1007/s00213-009-1521-8
[2] H SCHOEMAKER. Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity.[J]. Journal of Pharmacology and Experimental Therapeutics, 1997, 280 1: 83-97.
[3] M PAPP  J W. Antidepressant-like activity of amisulpride in two animal models of depression.[J]. Journal of Psychopharmacology, 2000, 14 1: 46-52. DOI: 10.1177/026988110001400106