AM630 is a competitive cannabinoid receptor antagonist in the guinea pig brain

Life Sci. 1997;61(9):PL115-8. doi: 10.1016/s0024-3205(97)00596-1.

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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Analgesics / pharmacology
  • Animals
  • Benzoxazines
  • Binding, Competitive
  • Brain / drug effects*
  • Brain / metabolism
  • Brain / ultrastructure*
  • Drug Interactions
  • Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
  • Guinea Pigs
  • Indoles / pharmacology*
  • Kinetics
  • Male
  • Morpholines / pharmacology
  • Naphthalenes / pharmacology
  • Receptors, Cannabinoid
  • Receptors, Drug / antagonists & inhibitors*

Substances

  • Analgesics
  • Benzoxazines
  • Indoles
  • Morpholines
  • Naphthalenes
  • Receptors, Cannabinoid
  • Receptors, Drug
  • Guanosine 5'-O-(3-Thiotriphosphate)
  • (3R)-((2,3-dihydro-5-methyl-3-((4-morpholinyl)methyl)pyrrolo-(1,2,3-de)-1,4-benzoxazin-6-yl)(1-naphthalenyl))methanone
  • iodopravadoline