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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.
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.
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 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 ...
Studies have shown an absence of emetic side effects within the half-life of the Levonantradol administered. Other studies suggest that cannabinoid agonists can synergize opioid anti-nociception. Cannabinoid receptors are located in nociceptive pathways, and CBs can promote signal transduction in TRP channels. Although Levonantradol relieves ...
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severe psychiatric side effects including anxiety, depression, and thoughts of suicide in patients treated with the now-withdrawn rimonabant, another CB 1 antagonist that was also ...
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.