| Literature DB >> 17035013 |
Dong Wook Kang1, Hyungchul Ryu, Jeewoo Lee, Krystle A Lang, Vladimir A Pavlyukovets, Larry V Pearce, Tetsurou Ikeda, Jozsef Lazar, Peter M Blumberg.
Abstract
Selected potent TRPV1 agonists (1-6) have been modified by 5- or 6-halogenation on the aromatic A-region to analyze their effects on potency and efficacy (agonism versus antagonism). The halogenation caused enhanced functional antagonism at TRPV1 compared to the corresponding prototype agonists. The analysis of SAR indicated that the antagonism was enhanced as the size of the halogen increased (I>Br>Cl) and when the 6-position was halogenated. Compounds 23c and 31b were found to be potent full antagonists with K(i) (as functional antagonist)=23.1 and 30.3 nM in rTRPV1/CHO system, respectively.Entities:
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Year: 2006 PMID： 17035013 DOI： 10.1016/j.bmcl.2006.09.059
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823