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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.
TM-38837 is a small molecule inverse agonist/antagonist of the CB 1 cannabinoid receptor, with peripheral selectivity. It is being developed for the treatment of obesity and metabolic disorders by 7TM Pharma. [1] The company has announced phase I clinical trials.
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.
Taranabant (codenamed MK-0364) is a cannabinoid receptor type 1 (CB 1) inverse agonist that was investigated as a potential treatment for obesity due to its anorectic effects. [1] [2] It was developed by Merck & Co.
Monlunabant (INV-202, MRI-1891, or S-MRI-1891) is a peripherally selective cannabinoid receptor 1 inverse agonist, discovered as a β-arrestin-2-biased cannabinoid receptor 1 antagonist by Dr George Kunos, Dr Resat Cinar, and Dr Malliga Iyer at the National Institutes of Health. [1] It was developed as a weight loss drug by Inversago Pharma. [2 ...
Rimonabant is an inverse agonist of the cannabinoid CB 1 receptor. Originally thought to be selective for the CB 1 receptor, rimonabant was subsequently also found to act as an antagonist of the μ-opioid receptor .
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.