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March 15, 2024Pharmacology Research & PerspectivesOpen Access

Preclinical metabolism and the disposition of vornorexant/TS‐142, a novel dual orexin 1/2 receptor antagonist for the treatment of insomnia

Yoshihiro Konno Shunsuke Kamigaso Hidetoh Toki Shuichi Terasaka Hirohiko Hikichi Hiromi Endo Junichi Yamaguchi Akiko Mizuno‐Yasuhira

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Abstract

We investigated the metabolism and disposition of vornorexant, a novel dual orexin receptor antagonist, in rats and dogs, and clarified in vitro metabolite profiles in humans. Furthermore, we investigated the pharmacokinetics of active metabolites in rats and dogs and their CNS distribution in rats to elucidate its contribution to drug efficacy. [

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Konno et al. (2024) studied this question.

synapsesocial.com/papers/68e73cccb6db6435876b69f6 https://doi.org/10.1002/prp2.1183

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