Melperone-d₄is intended for use as an internal standard for the quantification of melperone by GC- or LC-MS. Melperone is an atypical antipsychotic.¹It binds to α₁- and α₂-adrenergic and dopamine D₂receptors (K_ds = 180, 150, and 180 nM, respectively), as well as the serotonin (5-HT) receptor subtype 5-HT_2A(K_d= 102 nM). It is selective for these receptors over histamine H₁, muscarinic, 5-HT_1A, 5-HT_1D, and 5-HT_2Creceptors (K_ds = 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)