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Vol. 292, Issue 3, 886-894, March 2000
Department of Pharmacology and Toxicology, Virginia Commonwealth
University, Richmond, Virginia
Many of the pharmacological effects of
9-tetrahydrocannabinol are mediated through
CB1 and CB2 cannabinoid receptors. However, with the discovery of endogenous cannabinoids, some discrepancies have
arisen. Furthermore, unlike the CB1 receptor, the sequences of the mouse and human CB2 receptor are divergent, raising
the possibility of species specificity. The gene for the rat
CB2 receptor was cloned, expressed, and its properties
compared with those of mouse and human CB2 receptors.
Sequence analysis of the coding region of the rat CB2
genomic clone indicates 90% nucleic acid identity (93% amino acid
identity) between rat and mouse and 81% nucleic acid identity (81%
amino acid identity) between rat and human. The rat CB2
receptor was stably expressed in human embryonic kidney-293 cells to
examine its pharmacology. The rat CB2 showed low affinity
for anandamide, an endogenous ligand shown to act at the
CB1 receptor. In contrast, high-affinity binding for
SR144528 (CB2-selective antagonist) as well as several
cannabinoid receptor agonists was observed. Coupling to adenylate
cyclase was observed. Aspects of the pharmacology of
palmitoylethanolamide were also examined. It bound to CB1
and CB2 receptors with low affinity and stimulated GTP
S
binding in the cerebellum and CB2-expressing cell lines
with low potency. The data in this study suggest that the discrepancies
in affinities between rat and human may represent species differences.
The rat CB2 receptor genomic clone will be a useful tool
for studying the function and regulation of CB2 in rats.
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