This research was designed to determine the action of the novel aminoalkylindole AM630 (6-iodo-pravadoline) at the cannabinoid receptor by studying its interaction with the cannabinoid receptor agonist WIN 55,212-2 (R(+)-[2,3-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4 -benzoxazin-y1]-(1-naphthalenyl)methanone mesylate) on guanosine-5'-O-(3-[35S]thio)triphosphate ([35S]GTPγS) binding in mouse brain. WIN 55,212-2 stimulated [35S]GTPγS binding, while AM630 had no effect. AM630 antagonized WIN 55,212-2-induced [35S]GTPγS binding and shifted the WIN 55,212-2 dose-response curve to the right. These results clearly demonstrate that AM630 exerts cannabinoid receptor antagonist properties in the brain.
- Cannabinoid receptor antagonist
- [S]GTPγS binding
ASJC Scopus subject areas