Halogenation of 4-hydroxy/amino-3-methoxyphenyl acetamide TRPV1 agonists showed enhanced antagonism to capsaicin
…, AK Tao, KA Lang-Kuhs, PM Blumberg, J Lee
Index: Kang, Dong Wook; Kim, Yong Soo; Lim, Kwang Su; Kim, Myeong Seop; Pearce, Larry V.; Pavlyukovets, Vladimir A.; Tao, Andy K.; Lang-Kuhs, Krystle A.; Blumberg, Peter M.; Lee, Jeewoo Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 22 p. 8092 - 8105
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Citation Number: 5
Abstract
As an extension of our analysis of the effect of halogenation on thiourea TRPV1 agonists, we have now modified selected 4-hydroxy (or 4-amino)-3-methoxyphenyl acetamide TRPV1 agonists by 5-or 6-halogenation on the aromatic A-region and evaluated them for potency for TRPV1 binding and regulation and for their pattern of agonism/antagonism (efficacy). Halogenation shifted the functional activity at TRPV1 toward antagonism with a greater ...
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