Amisulpride Inhibitor CAS No. 71675-85-9

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KI0913	Amisulpride	50 mg	$154

Chemical Characteristic

Product Name	Amisulpride
Synonyms	Solian
CAS No.	71675-85-9
Molecular Weight	369.48
Formula	C₁₇H₂₇N₃O₄S
Chemical Name	4-amino-N-((1-ethylpyrrolidin-2-yl)methyl)-5-(ethylsulfonyl)-2-methoxybenzamide
Smiles	C(=O)(c1c(cc(c(c1)S(=O)(=O)CC)N)OC)NCC1N(CCC1)CC
Chemical Structure

Biological activities

Amisulpride is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder. In vitro, amisulpride has high affinity and selectivity for the human dopamine D2 and D3 receptors with Ki values of 2.8 and 3.2 nM, respectively. Amisulpride antagonizes D3 and both pre- and postsynaptic D2-like dopamine receptors of the rat striatum or nucleus accumbens in vitro. At low doses amisulpride (??0 mg/kg) preferentially blocks presynaptic dopamine autoreceptors that control dopamine synthesis and release in the rat, whereas at higher doses amisulpride (40-80 mg/kg) postsynaptic dopamine D2 receptor occupancy and antagonism is apparent.^[1] Furthermore, in mice, amisulpride antagonizes hypothermia induced by apomorphine, quinpirole or (?) 7-hydroxy-2-(di-n-propylamino)-tetralin. Amisulpride (54 mg/kg i.p.) blocks grooming behavior observed after a short period in water, a D1 receptor-mediated behavior. Amisulpride (100 mg/kg i.p.) only partially inhibits apomorphine-induced stereotypies (gnawing) and has no effect on stereotypies induced by d-amphetamine.^[2] In the mouse tail-flick assay, amisulpride potently inhibits antinociceptor with an ED50 value of 36.6 mg/kg.^[3]

Protocols

In vivo: Amisulpride is dissolved in ethanol 70% and saline in 30:70 ratios.^[3]

References

[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, 280(1): 83-97. [2] Perrault G, et al. Psychopharmacological profile of amisulpride: an antipsychotic drug with presynaptic D2/D3 dopamine receptor antagonist activity and limbic selectivity. J Pharmacol Exp Ther. 1997, 280(1): 73-82. [3] Weizman T, et al. The antinociceptive effect of amisulpride in mice is mediated through opioid mechanisms. Eur J Pharmacol. 2003, 478(2-3): 155-159.

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