SR141716A is an inverse agonist at the human cannabinoid CB1 receptor

Robert S. Landsman, Thomas H. Burkey, Paul Consroe, William R. Roeske, Henry I. Yamamura

Research output: Contribution to journalArticlepeer-review

235 Scopus citations

Abstract

The effects of R(+)-[2,3-dihydro-5-methyl-3-[(morpholinyl) methyl]pyrrolo[1,2,3-de]-1,4-benzoxazin-yl]-(1-napthalenyl)methanone mesylate (WIN 55,212-2) and N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-3-pyrazole -carboxamide (SR141716A) on guanosine-5'-O-(3-[35S]thio)triphosphate ([35S]GTPγS) binding to membranes isolated from human cannabinoid CB1 receptor-transfected Chinese hamster ovary (CHO) cells were examined. WIN 55,212-2 stimulated [35S]GTPγS binding 76.3% above basal levels whereas SR141716A produced a 22.3% decrease in basal [35S]GTPγS binding. These findings demonstrate that WIN 55,212-2 is an agonist and SR141716A is an inverse agonist in this system.

Original languageEnglish (US)
Pages (from-to)R1-R2
JournalEuropean Journal of Pharmacology
Volume334
Issue number1
DOIs
StatePublished - Sep 3 1997
Externally publishedYes

Keywords

  • Cannobinoid receptor human
  • Inverse agonist
  • SR141716A

ASJC Scopus subject areas

  • Pharmacology

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