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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.
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.
Rimonabant is a selective CB 1 receptor blocker and was discovered and developed by Sanofi-Aventis. [6]On 21 June 2006, the European Commission approved the sale of rimonabant in the then-25-member European Union as a prescription drug for use in conjunction with diet and exercise for patients with a body mass index (BMI) greater than 30 kg/m 2, or patients with a BMI greater than 27 kg/m 2 ...
In 2006, it was discovered that H4CBD has a binding affinity of 145 nM at the CB1 receptor and potential anti-inflammatory effects independent of its cannabinoid receptor action. [2] In contrast, CBD has been found to bind to the CB1 receptor as an inverse agonist/antagonist with a K i ranging from 3.3 to 4.8 mM. [3] [4]
Cannabinoid receptor 1 (CB1), is a G protein-coupled cannabinoid receptor that in humans is encoded by the CNR1 gene. [5] And discovered, by determination and characterization in 1988, [6] and cloned in 1990 for the first time.
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.
CID16020046 is a compound which acts as an inverse agonist at the former orphan receptor GPR55, [1] and may be the first selective inverse agonist characterised for this receptor. It was found to block a number of GPR55 mediated responses such as wound healing and activation of immune system T-cells and B-cells, as well as showing inverse ...
SR144528 is a drug that acts as a potent and highly selective CB 2 receptor inverse agonist, with a K i of 0.6 nM at CB 2 and 400 nM at the related CB 1 receptor.