910801-35-3Relevant articles and documents
γ-Carbolines: A novel class of cannabinoid agonists with high aqueous solubility and restricted CNS penetration
Cheng, Yun-Xing,Pourashraf, Mehrnaz,Luo, Xuehong,Srivastava, Sanjay,Walpole, Christopher,Salois, Dominic,St-Onge, Stephane,Payza, Kemal,Lessard, Etienne,Yu, Xiao Hong,Tomaszewski, Miros?aw J.
, p. 1619 - 1624 (2012/04/04)
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.