1: Eur J Pharm Sci. 2004 Nov;23(3):233-43. 

Comparison of cannabinoid ligands affinities and efficacies in murine tissues
and in transfected cells expressing human recombinant cannabinoid receptors.

Govaerts SJ, Hermans E, Lambert DM.

Unite de Chimie Pharmaceutique et de Radiopharmacie, Ecole de Pharmacie,
Universite catholique de Louvain, 73 Avenue E.Mounier, B-1200 Brussels, Belgium.

Affinities and efficacies of several reference cannabinoid ligands were
investigated at central and peripheral cannabinoid receptors in three different
species (rat, mouse, and human). The tested compounds belong to different
chemical classes such as classical and non-classical terpene derivatives
(Delta(8)-THC, Delta(9)-THC, HU 210, CP 55,940, CP 55,244, CP 55,243 and CP
47,947), aminoalkylindole (WIN 55,212-2, WIN 55,212-3) and diarylpyrazole
cannabinoids (SR 141716A, SR 144528). As cannabinoid receptors have been shown
to be mainly coupled to Gi/o type G- proteins, and by using the
[(35)S]-GTPgammaS nucleotide binding modulation, we characterized the functional
activity of these ligands which can act as agonists (positive intrinsic
activity), partial agonists (partial positive intrinsic activity), antagonists
(no intrinsic activity), or inverse agonists (negative intrinsic activity). To
our knowledge, some derivatives (Delta(8)-THC, WIN 55,212-3, CP 55,243 and CP
47,947) have never been characterized in [(35)S]-GTPgammaS binding assays and up
to now, this study represents the largest survey of reference cannabinoids
performed in unique experimental conditions and in the same laboratory.

PMID: 15489124 [PubMed - in process]