AM630 is an inverse agonist at the human cannabinoid CB1 receptor

Life Sci. 1998;62(9):PL109-13. doi: 10.1016/s0024-3205(97)01187-9.

Abstract

The present investigation examines WIN 55,212-2 and AM630 at the cloned human cannabinoid CB1 receptor stably expressed in Chinese hamster ovary (CHO) cells. The effect of various concentrations of WIN 55,212-2 and AM630 on basal [35S]GTPgammaS binding to cell membranes was determined. WIN 55,212-2 (100 microM) stimulated basal [35S]GTPgammaS binding 77.9% with an EC50 value of 0.36 microM. Conversely, AM630 (100 microM) inhibited basal [35S]GTPgammaS binding by 20.9% with an EC50 value of 0.90 microM. These results show that WIN 55,212-2 is an agonist and AM630 is an inverse agonist in this system.

Publication types

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

MeSH terms

  • Animals
  • Benzoxazines
  • CHO Cells
  • Cell Membrane / drug effects
  • Cell Membrane / metabolism
  • Cricetinae
  • Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
  • Humans
  • Indoles / pharmacology*
  • Morpholines / pharmacology
  • Naphthalenes / pharmacology
  • Receptors, Cannabinoid
  • Receptors, Drug / antagonists & inhibitors*
  • Recombinant Proteins / antagonists & inhibitors

Substances

  • Benzoxazines
  • Indoles
  • Morpholines
  • Naphthalenes
  • Receptors, Cannabinoid
  • Receptors, Drug
  • Recombinant Proteins
  • Guanosine 5'-O-(3-Thiotriphosphate)
  • Win 55212-2
  • iodopravadoline