title: AM630 is a competitive cannabinoid receptor antagonist in the guinea pig brain.
abstract: AM630 has been demonstrated to be a cannabinoid receptor antagonist in the mouse brain and vas deferens. Conversely, it was recently reported that AM630 acts as a cannabinoid agonist in the guinea pig ileum. This research was designed to determine whether the difference in the action of AM630 is species specific. Studies conducted in guinea pig brain reveal that AM630 antagonizes the stimulatory effect of the cannabinoid agonist WIN 55,212-2 on [35S]GTPgammaS binding suggesting that difference in AM630 activity in different tissues is not due to species variation.
authors.affiliation: Department of Pharmacology, University of Arizona and Health Science Center, Tucson 85724, U.S.A.
authors.forename: K
authors.initials: K
authors.lastname: Hosohata
authors.forename: R M
authors.initials: RM
authors.lastname: Quock
authors.forename: Y
authors.initials: Y
authors.lastname: Hosohata
authors.forename: T H
authors.initials: TH
authors.lastname: Burkey
authors.forename: A
authors.initials: A
authors.lastname: Makriyannis
authors.forename: P
authors.initials: P
authors.lastname: Consroe
authors.forename: W R
authors.initials: WR
authors.lastname: Roeske
authors.forename: H I
authors.initials: HI
authors.lastname: Yamamura
mesh_terms: D000700:Analgesics / Q000494:pharmacology; D000818:Animals; D048588:Benzoxazines; D001667:Binding, Competitive; D001921:Brain / Q000187:drug effects* / Q000378:metabolism / Q000648:ultrastructure*; D004347:Drug Interactions; D016244:Guanosine 5'-O-(3-Thiotriphosphate) / Q000378:metabolism; D006168:Guinea Pigs; D007211:Indoles / Q000494:pharmacology*; D007700:Kinetics; D008297:Male; D009025:Morpholines / Q000494:pharmacology; D009281:Naphthalenes / Q000494:pharmacology; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug / Q000037:antagonists & inhibitors*
chemical_list: D000700:Analgesics; D048588:Benzoxazines; D007211:Indoles; D009025:Morpholines; D009281:Naphthalenes; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug; D016244:Guanosine 5'-O-(3-Thiotriphosphate); C070417:(3R)-((2,3-dihydro-5-methyl-3-((4-morpholinyl)methyl)pyrrolo-(1,2,3-de)-1,4-benzoxazin-6-yl)(1-naphthalenyl))methanone; C094023:iodopravadoline