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The carbonate analogues of 5'-halogenated resiniferatoxin as TRPV1 ligands.

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 TRPV1. 5-Halogenation converted the agonists to partial agonists or full antagonists and the extent of antagonism reflected the order of I>Br>Cl>F, with a somewhat greater extent of antagonism for the derivatives of the 4-amino RTX surrogates compared to the corresponding derivatives of RTX itself. The carbonate analogues of I-RTX (60) and 5-bromo-4-amino-RTX (66) were potent and full antagonists with Ki(ant)=2.23 and 2.46 nM, respectively, for rat TRPV1, which were ca. 5-fold more potent than I-RTX (2) under our conditions. The conformational analysis of the I-RTX-carbonate (60) indicated that its bent conformation was similar to that of I-RTX, consistent with compound 60 and I-RTX showing comparable potent antagonism.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Lim KS,Lee H,Kim SE,Ha TH,Ann J,Son K,Choi S,Sun W,Pearce LV,DeAndrea-Lazarus IA,Blumberg PM,Lee J

doi

10.1016/j.ejmech.2013.07.042

subject

Has Abstract

pub_date

2013-10-01 00:00:00

pages

233-43

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(13)00491-1

journal_volume

68

pub_type

杂志文章

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