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Identification of an endogenous 2-monoglyceride, present in canine gut, that binds to cannabinoid receptors.
Upon intravenous administration to mice, 2-Ara-Gl caused the typical tetrad of effects produced by THC: antinociception, immobility, reduction of spontaneous activity, and lowering of the rectal temperature. Expand
Cannabinoid-induced mesenteric vasodilation through an endothelial site distinct from CB1 or CB2 receptors.
It is suggested that Abn-cbd and cannabidiol are a selective agonist and antagonist, respectively, of an as-yet-unidentified endothelial receptor for anandamide, activation of which elicits NO-independent mesenteric vasodilation, possibly by means of the release of an endothelium-derived hyperpolarizing factor (EDHF). Expand
Evaluation of binding in a transfected cell line expressing a peripheral cannabinoid receptor (CB2): identification of cannabinoid receptor subtype selective ligands.
Although most of the chosen compounds did not discriminate between CB1 and CB2, several ligands were identified that showed selectivity and can now serve as a basis for the design of compounds with even greater selectivity. Expand
Behavioral, biochemical, and molecular modeling evaluations of cannabinoid analogs
The structural diversity and wide-ranging potencies of the analogs described herein provide the opportunity to develop a pharmacophore for the cannabinoids using molecular modeling techniques. Expand
Cannabinoid structure-activity relationships: correlation of receptor binding and in vivo activities.
High correlations were demonstrated between binding affinity and in vivo potency in both the rat drug discrimination model and for psychotomimetic activity in humans, and the structure-activity relationship indicated the importance of side chain structure to high-affinity binding. Expand
In vivo characterization of a specific cannabinoid receptor antagonist (SR141716A): inhibition of delta 9-tetrahydrocannabinol-induced responses and apparent agonist activity.
It is not clear whether this pharmacological activity represents an uncharacterized action of SR141716A, or an index of tonic activity of an endogenous cannabinergic system, but it will be useful in establishing the biochemical events responsible for the in vivo effects of exogenous cannabinoids, as well as inestablishing the existence of a putative endogenous cannabinoidergic system. Expand
Aminoalkylindole analogs: cannabimimetic activity of a class of compounds structurally distinct from delta 9-tetrahydrocannabinol.
Six novel aminoalkylindole analogs, related structurally to the dual cyclooxygenase inhibitor and nonopioid analgesic pravadoline, were evaluated in the mouse to determine whether theirExpand
Cannabinoid-induced hypotension and bradycardia in rats mediated by CB1-like cannabinoid receptors.
Similar rank orders of potency, stereoselectivity and sensitivity to blockade by SR141716A indicate the involvement of CB1-like receptors in the hypotensive and bradycardic actions of cannabinoids, whereas the mechanism of the pressor effect of THC and anandamide remains unclear. Expand
The pharmacological activity of anandamide, a putative endogenous cannabinoid, in mice.
It is demonstrated that anandamide produces effects in a tetrad of tests used to predict cannabimimetic activity and supports the contention of its role as an endogenous cannabinoid ligand. Expand
Structure-activity relationships of indole- and pyrrole-derived cannabinoids.
A series of indole- and pyrrole-derived cannabinoids was developed, in which the morpholinoethyl group was replaced with another cyclic structure or with a carbon chain that more directly corresponded to the side chain of Delta9-THC and were tested for CB1 binding affinity and in a battery of in vivo tests. Expand