γ-Carbolines: A novel class of cannabinoid agonists with high aqueous solubility and restricted CNS penetration

…, S Srivastava, C Walpole, D Salois, S St-Onge…

Index: Cheng, Yun-Xing; Pourashraf, Mehrnaz; Luo, Xuehong; Srivastava, Sanjay; Walpole, Christopher; Salois, Dominic; St-Onge, Stephane; Payza, Kemal; Lessard, Etienne; Yu, Xiao Hong; Tomaszewski, Miroslaw J. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 4 p. 1619 - 1624

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Citation Number: 7

Abstract

An oral, peripherally restricted CB1/CB2 agonist could provide an interesting approach to treat chronic pain by harnessing the analgesic properties of cannabinoids but without the well-known central side effects. γ-Carbolines are a novel class of potent mixed CB1/CB2 agonists characterized by attractive physicochemical properties including high aqueous solubility. Optimization of the series has led to the discovery of 29, which has oral activity ...