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Zevaquenabant was described as a third generation cannabinoid receptor 1 (CB1R) antagonist due to its peripheral selectivity and polypharmacology. [1] It acts as a peripherally selective inverse agonist of the cannabinoid receptor 1 and an inducible nitric oxide synthase (iNOS) inhibitor.
A cannabinoid receptor antagonist, also known simply as a cannabinoid antagonist or as an anticannabinoid, is a type of cannabinoidergic drug that binds to cannabinoid receptors (CBR) and prevents their activation by endocannabinoids. They include antagonists, inverse agonists, and antibodies of CBRs.
An example of a receptor site that possesses basal activity and for which inverse agonists have been identified is the GABA A receptors.Agonists for GABA A receptors (such as muscimol) create a relaxant effect, whereas inverse agonists have agitation effects (for example, Ro15-4513) or even convulsive and anxiogenic effects (certain beta-carbolines).
The mechanism of action is through activation of the CB 2 receptor leading to production of specialized proresolving eicosanoids such as lipoxin A4 and prostaglandin J2. Studies in animals at doses up to 40 mg/kg show minimal psychoactivity of lenabasum, compared to that produced by tetrahydrocannabinol . [ 6 ]
2-Arachidonoylglycerol (2-AG) is an endocannabinoid, an endogenous agonist of the CB 1 receptor and the primary endogenous ligand for the CB2 receptor. [1] [2] It is an ester formed from the omega-6 fatty acid arachidonic acid and glycerol. It is present at relatively high levels in the central nervous system, with cannabinoid neuromodulatory ...
GPR55 is activated by the plant cannabinoids Δ 9-THC [12] and the endocannabinoids anandamide, 2-AG and noladin ether in the low nanomolar range. Exocannabinoids such as the synthetic cannabinoid CP-55940 are also able to activate the receptor [12] while the structurally unrelated cannabinoid mimic WIN 55,212-2 fails to activate the receptor. [10]
CP 55,940 is 45 times more potent than Δ 9-THC, and fully antagonized by rimonabant (SR141716A). [2] It is considered a full agonist at both CB 1 and CB 2 receptors and has K i values of 0.58 nM and 0.68 nM respectively, but is an antagonist at GPR55, the putative "CB 3" receptor. [3]
AM-251 is an inverse agonist at the CB 1 cannabinoid receptor. AM-251 is structurally very close to rimonabant; both are biarylpyrazole cannabinoid receptor antagonists.In AM-251, the p-chloro group attached to the phenyl substituent at C-5 of the pyrazole ring is replaced with a p-iodo group.