Receptor activity and conformational analysis of 5′-halogenated resiniferatoxin analogs as TRPV1 ligands

…, SG Park, S Choi, LV Pearce, PM Blumberg…

Index: Lim, Kwang Su; Kang, Dong Wook; Kim, Yong Soo; Kim, Myeong Seop; Park, Seul-Gi; Choi, Sun; Pearce, Larry V.; Blumberg, Peter M.; Lee, Jeewoo Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 1 p. 299 - 302

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Citation Number: 5

Abstract

A series of 5′-halogenated resiniferatoxin analogs have been investigated in order to examine the effect of halogenation in the A-region on their binding and the functional pattern of agonism/antagonism for rat TRPV1 heterologously expressed in Chinese hamster ovary cells. Halogenation at the 5-position in the A-region of RTX and of 4-amino RTX shifted the agonism of parent compounds toward antagonism. The extent of antagonism was greater ...