910798-30-0Relevant 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.
NOVEL TETRAHYDRO-1H-PYRIDO [4,3-b] INDOLE DERIVATIVES AS CB1’ RECEPTOR LIGANDS
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, (2010/11/24)
Compounds of Formulae I, or pharmaceutically acceptable salts thereof: wherein R1, R2 and R3 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.