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Melperone-d4 is intended for use as an internal standard for the quantification of melperone by GC- or LC-MS. Melperone is an atypical antipsychotic.1 It binds to α1- and α2-adrenergic and dopamine D2 receptors (Kds = 180, 150, and 180 nM, respectively), as well as the serotonin (5-HT) receptor subtype 5-HT2A (Kd = 102 nM). It is selective for these receptors over histamine H1, muscarinic, 5-HT1A, 5-HT1D, and 5-HT2C receptors (Kds = 580, >10,000, 2,200, 3,400, and 2,100 nM, respectively). Melperone (2 mg/kg per day) increases basal, but not amphetamine-induced, extracellular dopamine levels in the rat nucleus accumbens.2

1.Richelson, E., and Souder, T.Binding of antipsychotic drugs to human brain receptors: Focus on newer generation compoundsLife Sci.68(1)29-39(2000) 2.Ichikawa, J., and Meltzer, H.Y.The effect of chronic atypical antipsychotic drugs and haloperidol on amphetamine-induced dopamine release in vivoBrain Res.574(1-2)98-104(1992)

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