Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease

…, S St-Onge, MJ Tomaszewski, M Tremblay…

Index: Plowright, Alleyn T.; Nilsson, Karolina; Antonsson, Madeleine; Amin, Kosrat; Broddefalk, Johan; Jensen, Joergen; Lehmann, Anders; Jin, Shujuan; St-Onge, Stephane; Tomaszewski, Miroslaw J.; Tremblay, Maxime; Walpole, Christopher; Wei, Zhongyong; Yang, Hua; Ulander, Johan Journal of Medicinal Chemistry, 2013 , vol. 56, # 1 p. 220 - 240

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Citation Number: 7

Abstract

Agonists of the cannabinoid receptor 1 (CB1) have been suggested as possible treatments for a range of medical disorders including gastroesophageal reflux disease (GERD). While centrally acting cannabinoid agonists are known to produce psychotropic effects, it has been suggested that the CB1 receptors in the periphery could play a significant role in reducing reflux. A moderately potent and highly lipophilic series of 2-aminobenzamides was ...