Halogenation of 4-hydroxy-3-methoxybenzyl thiourea TRPV1 agonists showed enhanced antagonism to capsaicin

…, VA Pavlyukovets, LV Pearce, T Ikeda, J Lazar…

文献索引：Kang, Dong Wook; Ryu, HyungChul; Lee, Jeewoo; Lang, Krystle A.; Pavlyukovets, Vladimir A.; Pearce, Larry V.; Ikeda, Tetsurou; Lazar, Jozsef; Blumberg, Peter M. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 1 p. 214 - 219

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被引用次数: 8

摘要

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 ...