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A series of indane-type acetamide and propanamide analogues were investigated as TRPV1 antagonists. The analysis of structure-activity relationship indicated that indane A-region analogues exhibited better antagonism than did the corresponding 2,3-dihydrobenzofuran and 1,3-benzodioxole surrogates. Among them, antagonist 36 exhibited potent and selective antagonism toward capsaicin for hTRPV1 and mTRPV1. Further, in vivo studies indicated that antagonist 36 showed excellent analgesic activity in both phases of the formalin mouse pain model and inhibited the pain behavior completely at a dose of 1 mg/kg in the 2nd phase. Copyright © 2019. Published by Elsevier Ltd.


Songyeon Ahn, Yong Soo Kim, Myeong Seup Kim, Jihyae Ann, Heejin Ha, Young Dong Yoo, Young Ho Kim, Peter M Blumberg, Robert Frank-Foltyn, Gregor Bahrenberg, Hannelore Stockhausen, Thomas Christoph, Jeewoo Lee. Discovery of indane propanamides as potent and selective TRPV1 antagonists. Bioorganic & medicinal chemistry letters. 2020 Feb 01;30(3):126838

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PMID: 31864799

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