Kobayashi, Jun-ichi et al. published their research in Bioorganic & Medicinal Chemistry in 2021 |CAS: 1459793-02-2

The Article related to trpm8 antagonist adverse event, cyp3a4 induction, oab, phenylglycinamide, reactive metabolite, trpm8, trpm8 antagonist, Pharmacology: Drug Interactions and General Pharmacology and other aspects.Recommanded Product: 1459793-02-2

On January 15, 2021, Kobayashi, Jun-ichi; Hirasawa, Hideaki; Fujimori, Yoshikazu; Nakanishi, Osamu; Kamada, Noboru; Ikeda, Tetsuya; Yamamoto, Akitoshi; Kanbe, Hiroki published an article.Recommanded Product: 1459793-02-2 The title of the article was Identification of N-acyl-N-indanyl-α-phenylglycinamides as selective TRPM8 antagonists designed to mitigate the risk of adverse effects. And the article contained the following:

Transient receptor potential melastatin 8 (TRPM8), a temperature-sensitive ion channel responsible for detecting cold, is an attractive mol. target for the treatment of pain and other disorders. We have previously discovered a selective TRPM8 antagonist, KPR-2579, which inhibited bladder afferent hyperactivity induced by acetic acid instillation into the bladder. However, addnl. studies have revealed potential adverse effects with KPR-2579, such as the formation of a reactive metabolite, CYP3A4 induction, and convulsions. In this report, we describe the optimization of α-phenylglycinamide derivatives to mitigate the risk of these adverse effects. The optimal compound 13x exhibited potent inhibition against icilin-induced wet-dog shakes and cold-induced frequent voiding in rats, with a wide safety margin against the potential side effects. The experimental process involved the reaction of (S)-2,3-Dihydrobenzofuran-3-amine hydrochloride(cas: 1459793-02-2).Recommanded Product: 1459793-02-2

The Article related to trpm8 antagonist adverse event, cyp3a4 induction, oab, phenylglycinamide, reactive metabolite, trpm8, trpm8 antagonist, Pharmacology: Drug Interactions and General Pharmacology and other aspects.Recommanded Product: 1459793-02-2

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem