Pericyazine

Periciazine is a typical antipsychotic.¹ It binds to the dopamine D₁ receptor and androgen receptor (K_is = 0.01 and 3 ?M, respectively).^1,2 Periciazine is an α₁-adrenergic receptor (α₁-AR) antagonist (IC₅₀ = 0.0041 ?M in rat forebrain homogenates), as well as an α₂-AR antagonist (IC₅₀ = 2 ?M in rat cortical homogenates).³ It also inhibits severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (M^pro) activity by 55% when used at a concentration of 100 ?M.⁴ Periciazine (0.075 mg/kg) increases the number of entries into, and the percentage of time spent in, the open arms of the elevated plus maze in rats, indicating anxiolytic-like activity.⁵ Formulations containing periciazine have been used in the treatment of schizophrenia and psychosis.

1.Kanba, S., Suzuki, E., Nomura, S., et al.Affinity of neuroleptics for D1 receptor of human brain striatumJ. Psychiatry Neurosci.19(4)265-269(1994) 2.Bisson, W.H., Cheltsov, A.V., Bruey-Sedano, N., et al.Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugsProc. Natl. Acad. Sci. USA104(29)11927-11932(2007) 3.Megens, A.A.H.P., Leysen, J.E., Awouters, F.H.L., et al.Further validation of in vivo and in vitro pharmacological procedures for assessing the ɑ2/ɑ1-selectivity of test compounds: (1) ɑ-adrenoceptor antagonistsEur. J. Pharmacol.129(1-2)49-55(1986) 4.Ghahremanpour, M.M., Tirado-Rives, J., Deshmukh, M., et al.Identification of 14 known drugs as inhibitors of the main protease of SARS-CoV-2ACS Med. Chem. Lett.11(12)2526-2533(2020) 5.Cechin, E.M., Quevedo, J., Barichello, T., et al.Dose-related effects of propericiazine in ratsBraz. J. Med. Biol. Res.36(2)227-231(2003)