Periciazine

Periciazine is a typical antipsychotic.¹ It binds to the dopamine D₁ receptor and androgen receptor (K_is = 0.01 and 3 µM, respectively).^1,2 Periciazine is an α₁-adrenergic receptor (α₁-AR) antagonist (IC₅₀ = 0.0041 µM in rat forebrain homogenates), as well as an α₂-AR antagonist (IC₅₀ = 2 µM 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 µM.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.

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1. Kanba, S., Suzuki, E., Nomura, S., et al. Affinity of neuroleptics for D₁ receptor of human brain striatum. J. 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 drugs. Proc. Natl. Acad. Sci. USA 104(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 antagonists. Eur. 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-2. ACS Med. Chem. Lett. 11(12), 2526-2533 (2020).

5. Cechin, E.M., Quevedo, J., Barichello, T., et al. Dose-related effects of propericiazine in rats. Braz. J. Med. Biol. Res. 36(2), 227-231 (2003).