Ontology highlight
ABSTRACT:
SUBMITTER: Dixon DD
PROVIDER: S-EPMC3445631 | biostudies-literature | 2012 Aug
REPOSITORIES: biostudies-literature
Bioorganic & medicinal chemistry letters 20120615 16
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 K(i) 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 ...[more]