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.

Taranabant | C27H25ClF3N3O2 | CID 11226090 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.

Two randomized, placebo-controlled clinical trials, published in the International Journal of Obesity, assessed the safety and efficacy of the cannabinoid-1 receptor (CB1R) inverse agonist...

Taranabant 是一款由 Merck 公司原研开发的一款 CB 受体小分子类反向激动剂。 据悉，Taranabant 对超重病人的临床3期研究数据表现出与Rimonabant 相似的减重效果，但由于潜在的副作用等原因，Merck 公司终止了对 Taranabant 的临床开发。

Merck & Co Inc is developing the cannabinoid receptor type 1 inverse agonist taranabant for the potential treatment of obesity and nicotine dependence. By October 2006, the drug had entered phase III trials for obesity, and by May 2008, a phase II study of taranabant as an aid to smoking cessation in chronic cigarette smokers had been completed.

2009年1月16日 · Taranabant (1) is a cannabinoid-1 receptor (CB1R) inverse agonist that was recently in late-stage clinical development for the treatment of obesity. The previously employed synthesis exhibited a number of shortcomings for continuing development, and in this paper we report an improved synthesis of the target molecule that is suitable for large ...

2009年7月14日 · Rimonabant and taranabant are two extensively studied cannabinoid-1 receptor (CB1R) inverse agonists. Their effects on in vivo peripheral tissue metabolism are generally well replicated. The...

2007年6月18日 · Taranabant is a structurally novel, highly selective, potent, orally bioavailable acyclic CB1R inverse agonist (Lin et al., 2006) that has been demonstrated to cause weight loss in rodent studies (Fong et al., 2007) at trough CNS receptor occupancy levels above 30%.

Taranabant 是一种非常有效和选择性 (比 CB2 高 900 倍) 的 CB1R 反向激动剂，其亲和力比原始先导药物高 500 倍以上。 在 cyclic-AMP 生成的功能测定中，Taranabant 被确定为反向激动剂 (EC 50 =2.4±1.4 nM) [2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Taranabant (MK-0364) 以剂量依赖性方式抑制C57BL/6N小鼠2小时和过夜的食物摄入以及过夜体重增加。

Taranabant is a novel cannabinoid CB-1 receptor (CB1R) inverse agonist in clinical development for the treatment of obesity. This double-blind, randomized, placebo-controlled, single oral dose study evaluated the safety, tolerability, pharmacokinetics, and pharmacodynamics of …