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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 ...
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.
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]
Zevaquenabant (S-MRI-1867, INV-101, or MRI-1867) is an investigational small-molecule drug, discovered by Dr George Kunos, Dr Resat Cinar, and Dr Malliga iyer at the National Institutes of Health. Zevaquenabant was described as a third generation cannabinoid receptor 1 (CB1R) antagonist due to its peripheral selectivity and polypharmacology . [ 1 ]
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.
Drinabant reached phase IIb clinical trials for this purpose in the treatment of obesity but was shortly thereafter discontinued, [4] likely due to the observation of severe psychiatric side effects including anxiety, depression, and thoughts of suicide in patients treated with the now-withdrawn rimonabant, another CB 1 antagonist that was also ...
JD5037 is an antiobesity drug candidate which acts as a peripherally-restricted cannabinoid inverse agonist at CB 1 receptors.It is very selective for the CB 1 subtype, with a Ki of 0.35nM, >700-fold higher affinity than it has for CB 2 receptors.
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 ...
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