Perphenazine-d4 is intended for use as an internal standard for the quantification of perphenazine by GC- or LC-MS. Perphenazine is a typical antipsychotic.1 It binds to dopamine D2, α1A-, α2A-, α2B-, and α2C-adrenergic, M3 muscarinic, and histamine H1 receptors (Kis = 1.4, 10, 1,848, 104.9, 85.2, 810.5 and 8 nM, respectively), as well as the serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7 (Kis = 421, 5.6, 132, 17, and 23 nM, respectively). Perphenazine (1, 5, and 10 mg/kg) enhances morphine-induced analgesia in the tail-flick and hot plate tests in rats.2 It reduces cannibalism in female mice when administered at doses of 2 and 4 mg/kg.3 Formulations containing perphenazine have been used in the treatment of schizophrenia and psychosis.
1.Kroeze, W.K., Hufeisen, S.J., Popadak, B.A., et al.H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugsNeuropsychopharmacology28(3)519-526(2003) 2.Ozdemir, E., Bagcivan, I., and Gursoy, S.Role of D?/D? dopamin receptors antagonist perphenazine in morphine analgesia and tolerance in ratsBosn. J. Basic Med. Sci.13(2)119-125(2013) 3.Carter, D.B., Kennett, M.J., and Franklin, C.L.Use of perphenazine to control cannibalism in DBA/1 miceComp. Med.52(5)452-455(2002)