Relative efficacies of cannabinoid CB1 receptor agonists in the mouse brain

Thomas H. Burkey, Raymond M. Quock, Paul Consroe, Frederick J. Ehlert, Yoshiaki Hosohata, William R. Roeske, Henry I. Yamamura

Research output: Contribution to journalArticlepeer-review

75 Scopus citations

Abstract

We measured (-)-5-(1,1-dimethylheptyl)-2-[5-hydroxy-2-(3-hydroxypropyl)cyclohexyl]-phenol (CP 55,940)-, (-)11-OH-Δ8-tetrahydrocannabinol-dimethylheptyl (HU-210)-, anandamide- and Δ9-tetrahydrocannabinol-stimulated G protein activation in mouse brain using the [35S]GTPγS functional assay. The K(i) values for these drugs were determined by agonist competition binding with the cannabinoid CB, receptor antagonist [3H] N-(piperidin-1-yl-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H -pyrazole-3-carboxamidehydrochloride ([3H]SR141716A). This information was used to calculate the efficacy for drug stimulation of G protein activity, The rank order of efficacy was CP 55,940 > HU-210 > anandamide > Δ9-tetrahydrocannabinol with the latter two drugs being partial agonists. Since efficacy values relate receptor occupancy to functional responses, we believe efficacy values are a better measure of drug-mediated functional responses compared with measurements of drug potency.

Original languageEnglish (US)
Pages (from-to)295-298
Number of pages4
JournalEuropean Journal of Pharmacology
Volume336
Issue number2-3
DOIs
StatePublished - Oct 8 1997
Externally publishedYes

Keywords

  • Brain
  • Cannabinoid receptor
  • Cannnbinoid
  • Drug efficacy
  • Mouse
  • Partial agonist
  • Tetrahydrocannabinol

ASJC Scopus subject areas

  • Pharmacology

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