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 journalArticle

71 Citations (Scopus)

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

Fingerprint

Cannabinoid Receptor Agonists
Dronabinol
Brain
rimonabant
Pharmaceutical Preparations
GTP-Binding Proteins
Cannabinoid Receptor Antagonists
Phenol

Keywords

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

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

Burkey, T. H., Quock, R. M., Consroe, P., Ehlert, F. J., Hosohata, Y., Roeske, W. R., & Yamamura, H. I. (1997). Relative efficacies of cannabinoid CB1 receptor agonists in the mouse brain. European Journal of Pharmacology, 336(2-3), 295-298. https://doi.org/10.1016/S0014-2999(97)01255-7

Relative efficacies of cannabinoid CB1 receptor agonists in the mouse brain. / Burkey, Thomas H.; Quock, Raymond M.; Consroe, Paul; Ehlert, Frederick J.; Hosohata, Yoshiaki; Roeske, William R; Yamamura, Henry I.

In: European Journal of Pharmacology, Vol. 336, No. 2-3, 08.10.1997, p. 295-298.

Research output: Contribution to journalArticle

Burkey, TH, Quock, RM, Consroe, P, Ehlert, FJ, Hosohata, Y, Roeske, WR & Yamamura, HI 1997, 'Relative efficacies of cannabinoid CB1 receptor agonists in the mouse brain', European Journal of Pharmacology, vol. 336, no. 2-3, pp. 295-298. https://doi.org/10.1016/S0014-2999(97)01255-7
Burkey, Thomas H. ; Quock, Raymond M. ; Consroe, Paul ; Ehlert, Frederick J. ; Hosohata, Yoshiaki ; Roeske, William R ; Yamamura, Henry I. / Relative efficacies of cannabinoid CB1 receptor agonists in the mouse brain. In: European Journal of Pharmacology. 1997 ; Vol. 336, No. 2-3. pp. 295-298.
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