AM630 is an inverse agonist at the human cannabinoid CB1 receptor

Robert S. Landsman, Alexandros Makriyannis, Hongfeng Deng, Paul Consroe, William R. Roeske, Henry I. Yamamura

Research output: Contribution to journalArticle

49 Scopus citations

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]GTPγS binding to cell membranes was determined. WIN 55,212-2 (100 μM) stimulated basal [35S]GTPγS binding 77.9% with an EC50 value of 0.36 μM. Conversely, AM630 (100 μM) inhibited basal [35S]GTPγS binding by 20.9% with an EC50 value of 0.90 μM. These results show that WIN 55,212-2 is an agonist and AM630 is an inverse agonist in this system.

Original languageEnglish (US)
Pages (from-to)PL109-PL113
JournalLife Sciences
Volume62
Issue number9
DOIs
StatePublished - Jan 23 1998
Externally publishedYes

Keywords

  • AM630
  • CHO cells
  • GTPγS
  • Human cannabinoid CB receptor
  • Inverse agonism
  • Inverse agonist
  • Negative intrinsic activity
  • WIN 55,212-2

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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    Landsman, R. S., Makriyannis, A., Deng, H., Consroe, P., Roeske, W. R., & Yamamura, H. I. (1998). AM630 is an inverse agonist at the human cannabinoid CB1 receptor. Life Sciences, 62(9), PL109-PL113. https://doi.org/10.1016/S0024-3205(97)01187-9