Abstract
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-yl]-(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.
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