Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371272 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
Abstract
A series of tricyclic cannabinoids incorporating a heteroaroyl group at C3 were prepared as probes to explore the binding site(s) of the CB1 and CB2 receptors. This relatively unexplored structural motif is shown to be CB2 selective with Ki values at low nanomolar concentrations when the heteroaromatic group is 3-benzothiophenyl (41) or 3-indolyl (50). When photoactivated, the lead compound 41 was shown to successfully label the CB2 receptor through covalent attachment at the active site while 50 failed to label. The benzothiophenone moiety may be a photoactivatable moiety suitable for selective labeling.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Darryl D. Dixon, Marcus A. Tius, Ganesh A. Thakur, Han Zhou, Anna L. Bowman, Vidyanand G. Shukla, Yan Peng, Alexandros Makriyannis,