Perphenazine | Antipsychotic agent

Perphenazine (58-39-9) is a clinically useful typical antipsychotic drug. The therapeutic mode of action is not well understood but it binds to a wide variety of receptors including serotonin, histamine, dopamine, and a-adrenergic.¹ Perphenazine is an inhibitor of acid sphingomyelinase(ASM)² and positively affected xenografted tumor growth via perturbation of intracellular cholesterol transport through ASM³. It has also been shown to be an inhibitor of glutamate dehydrogenase.⁴

References/Citations

1) Kroeze et al. (2003), H1-Histamine Receptor Affinity Predicts Short-Term Weight Gain for Typical and Atypical Antipsychotic Drugs; Neuropharmacology, 28 519
2) Kornhuber et al. (2011), Identification of Novel Functional Inhibitors of Acid Sphingomyelinase; PLoS One, 6 e23852
3) Kuzu et al. (2017), Modulating cancer cell survival by targeting intracellular cholesterol transport; Br. J. Cancer, epub ahead of print
4) Couee and Tipton (1990), Inhibition of ox brain glutamate by perphenazine; Biochem. Pharmacol. 39 1167