泰伦那班
化合物
泰伦那班(英语:Taranabant;研发代号:MK-0364)是一种大麻素受体1反向激动剂,由于其厌食作用而被研究作为一种潜在的肥胖治疗方法。[1][2]它是由默克公司发现的。
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臨床資料 | |
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给药途径 | 口服 |
ATC碼 | |
法律規範狀態 | |
法律規範 |
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识别信息 | |
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CAS号 | 701977-09-5 ![]() |
PubChem CID | |
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CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.207.983 |
化学信息 | |
化学式 | C27H25ClF3N3O2 |
摩尔质量 | 515.96 g·mol−1 |
3D模型(JSmol) | |
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2008年10月,由于中枢神经系统的严重副作用(主要是抑郁和焦虑),默克公司停止了该药物的III期临床试验。[3][4][5][6]
参见
参考资料
- ^ Armstrong HE, Galka A, Lin LS, Lanza TJ Jr, Jewell JP, Shah SK; et al. Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists. Bioorganic & Medicinal Chemistry Letters. 2007, 17 (8): 2184–7. PMID 17293109. doi:10.1016/j.bmcl.2007.01.087.
- ^ Fong TM, Guan XM, Marsh DJ, Shen CP, Stribling DS, Rosko KM, et al. Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-5-(trifluoromethyl)pyridin-2-yl]oxy]propanamide (MK-0364), in rodents. Journal of Pharmacology and Experimental Therapeutics. Jun 2007, 321 (3): 1013–22. PMID 17327489. S2CID 20001781. doi:10.1124/jpet.106.118737.
- ^ Press release by Merck. [4 October 2008]. (原始内容存档于2009-09-21).
- ^ Aronne LJ, Tonstad S, Moreno M, Gantz I, Erondu N, Suryawanshi S, Molony C, Sieberts S, Nayee J, Meehan AG, Shapiro D, Heymsfield SB, Kaufman KD, Amatruda JM. A clinical trial assessing the safety and efficacy of taranabant, a CB1R inverse agonist, in obese and overweight patients: a high-dose study. International Journal of Obesity. May 2010, 34 (5): 919–35. PMID 20157323. doi:10.1038/ijo.2010.21 .
- ^ Kipnes MS, Hollander P, Fujioka K, Gantz I, Seck T, Erondu N, Shentu Y, Lu K, Suryawanshi S, Chou M, Johnson-Levonas AO, Heymsfield SB, Shapiro D, Kaufman KD, Amatruda JM. A one-year study to assess the safety and efficacy of the CB1R inverse agonist taranabant in overweight and obese patients with type 2 diabetes. Diabetes, Obesity & Metabolism. June 2010, 12 (6): 517–31. PMID 20518807. S2CID 23886192. doi:10.1111/j.1463-1326.2009.01188.x .
- ^ Proietto J, Rissanen A, Harp JB, Erondu N, Yu Q, Suryawanshi S, Jones ME, Johnson-Levonas AO, Heymsfield SB, Kaufman KD, Amatruda JM. A clinical trial assessing the safety and efficacy of the CB1R inverse agonist taranabant in obese and overweight patients: low-dose study. International Journal of Obesity. August 2010, 34 (8): 1243–54. PMID 20212496. doi:10.1038/ijo.2010.38 .