Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371788 | Bioorganic & Medicinal Chemistry Letters | 2012 | 6 Pages |
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 in a rat inflammatory pain model and limited brain exposure at analgesic doses, consistent with a lower risk of CNS-mediated tolerability issues.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Yun-Xing Cheng, Mehrnaz Pourashraf, Xuehong Luo, Sanjay Srivastava, Christopher Walpole, Dominic Salois, Stephane St-Onge, Kemal Payza, Etienne Lessard, Xiao Hong Yu, Mirosław J. Tomaszewski,