Discovery of novel 6, 6-heterocycles as transient receptor potential vanilloid (TRPV1) antagonists

…, T Caldwell, X Zheng, R Bakthavatchalam…

Index: Blum, Charles A.; Caldwell, Timothy; Zheng, Xiaozhang; Bakthavatchalam, Rajagopal; Capitosti, Scott; Brielmann, Harry; De Lombaert, Stephane; Kershaw, Mark T.; Matson, David; Krause, James E.; Cortright, Daniel; Crandall, Marci; Martin, William J.; Murphy, Beth Ann; Boyce, Susan; Jones, A. Brian; Mason, Glenn; Rycroft, Wayne; Perrett, Helen; Conley, Rachael; Burnaby-Davies, Nicola; Chenard, Bertrand L.; Hodgetts, Kevin J. Journal of Medicinal Chemistry, 2010 , vol. 53, # 8 p. 3330 - 3348

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Citation Number: 18

Abstract

The transient receptor potential cation channel, subfamily V, member 1 (TRPV1) is a nonselective cation channel that can be activated by a wide range of noxious stimuli, including capsaicin, acid, and heat. Blockade of TRPV1 activation by selective antagonists is under investigation in an attempt to identify novel agents for pain treatment. The design and synthesis of a series of novel TRPV1 antagonists with a variety of different 6, 6- ...