delta 9-Tetrahydrocannabinol is a partial agonist of cannabinoid receptors in mouse brain

Eur J Pharmacol. 1997 Apr 4;323(2-3):R3-4. doi: 10.1016/s0014-2999(97)00146-5.

Abstract

We measured the ability of the cannabinoid agonists delta 9-tetrahydrocannabinol and R(+)-[2,3,-dihydro-5-methyl-3- [(morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4-benzoxazin-yl]-(1-napht halenyl) methanone mesylate (WIN 55,212-2) to stimulate guanosine-5'-O-(3-[35S]thio)triphosphate ([35S]GTP gamma S) binding in mouse brain membranes. delta 9-Tetrahydrocannabinol stimulated [35S]GTP gamma S binding by about 25% as compared to WIN 55,212-2. This is the first report demonstrating that delta 9-tetrahydrocannabinol acts as a partial agonist in stimulating [35S]GTP gamma S binding in the mouse brain.

Publication types

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

MeSH terms

  • Animals
  • Benzoxazines
  • Brain / drug effects*
  • Brain / metabolism
  • Dronabinol / pharmacology*
  • Guanosine 5'-O-(3-Thiotriphosphate) / metabolism*
  • In Vitro Techniques
  • Male
  • Membranes / metabolism
  • Mice
  • Morpholines / pharmacology
  • Naphthalenes / pharmacology
  • Receptors, Cannabinoid
  • Receptors, Drug / agonists*

Substances

  • Benzoxazines
  • 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
  • Dronabinol