The carbonate analogues of 5′-halogenated resiniferatoxin as TRPV1 ligands

…, IA DeAndrea-Lazarus, PM Blumberg, J Lee

Index: Lim, Kwang Su; Lee, Hobin; Kim, Sung Eun; Ha, Tae-Hwan; Ann, Jihyae; Son, Karam; Choi, Sun; Sun, Wei; Pearce, Larry V.; Deandrea-Lazarus, Ian A.; Blumberg, Peter M.; Lee, Jeewoo European Journal of Medicinal Chemistry, 2013 , vol. 68, p. 233 - 243

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Abstract

Abstract A series of carbonate analogues of 5′-halogenated RTX have been investigated in order to examine the effect of the carbonate group as a linker and the role of halogens in the reversal of activity from agonism to antagonism for rat and human TRPV1 heterologously expressed in Chinese hamster ovary cells. The carbonate analogues showed similar activities to the corresponding RTX derivatives in rat TRPV1 but lower potency in human ...

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