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Updated: Jan 1, 2026

Intracerebroventricular Treatment with Resiniferatoxin and Pain Tests in Mice
Published on: September 2, 2020
Discovery of indane propanamides as potent and selective TRPV1 antagonists
Songyeon Ahn1, Yong Soo Kim1, Myeong Seup Kim1
1Laboratory of Medicinal Chemistry, College of Pharmacy, Seoul National University, Seoul 08826, Republic of Korea.
Abstract:
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.
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