Alizapride-13C-d3 is intended for use as an internal standard for the quantification of alizapride by GC- or LC-MS. Alizapride is a dopamine D2 receptor antagonist (Ki = 66-340 nM in radioligand binding assays).1 It is selective for dopamine D2 over α1-, α2-, and β-adrenergic receptors (IC50s = >10 µM for all). It reduces decreases in gastrointestinal transit induced by dopamine , apomorphine, or bromocriptine in rats when administered at a dose of 5 mg/kg.2 Formulations containing alizapride have been used in the treatment of pre- and postoperative nausea.
1.Chivers, J.K., Gommeren, W., Leysen, J.E., et al.Comparison of the in-vitro receptor selectivity of substituted benzamide drugs for brain neurotransmitter receptorsJ. Pharm. Pharmacol.40(6)415-421(1988) 2.Dhasmana, K.M., VillalÓn, C.M., Zhu, Y.N., et al.The role of dopamine (D2), α and β-adrenoceptor receptors in the decrease in gastrointestinal transit induced by dopamine and dopamine-related drugs in the ratPharmacol. Res.27(4)335-347(1993)