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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 ...
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 ]
Ibipinabant (SLV319, BMS-646,256) is a drug used in scientific research which acts as a potent and highly selective CB 1 antagonist. [1] It has potent anorectic effects in animals, [2] and was researched for the treatment of obesity, although CB 1 antagonists as a class have now fallen out of favour as potential anorectics following the problems seen with rimonabant, and so ibipinabant is now ...
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.
[19] [31] For drugs recently sold on the market, drugs have information pages (monographs) that provide information on any potential interaction between a medication and grapefruit juice. [19] Because there is a growing number of medications that are known to interact with citrus, [ 1 ] patients should consult a pharmacist or physician before ...
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.
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.