New 1,2,3,4-tetrahydropyrrolo[3,4-b]indole derivatives as selective CB2 receptor agonists.
The preparation and evaluation of a novel class of CB2 agonists based on a 1,2,3,4-tetrahydropyrrolo[3,4-b]indole moiety are reported. They showed binding affinities up to 4.2 nM toward CB2 with sub-nanomolar EC(50) values. They also showed moderate to good (>350-fold) selectivity over the CB1 receptor.
Pagé
Daniel
D
Department of Medicinal Chemistry, AstraZeneca R&D Montreal, St-Laurent, Quebec, Canada. daniel.page@astrazeneca.com
Yang
Hua
H
Brown
William
W
Walpole
Christopher
C
Fleurent
Manon
M
Fyfe
Meredith
M
Gaudreault
François
F
St-Onge
Stéphane
S
D001667:Binding, Competitive; D004353:Drug Evaluation, Preclinical; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D011758:Pyrroles / Q000737:chemistry; D043885:Receptor, Cannabinoid, CB2 / Q000819:agonists*
D007211:Indoles; D011758:Pyrroles; D043885:Receptor, Cannabinoid, CB2