溴乙那班
化合物
溴乙那班（英語：Surinabant；開發代號：SR147778），也譯作舒立納班或速利那班，是一種大麻素受體1拮抗劑，由賽諾菲開發。[1]它正在被研究作為尼古丁成癮的潛在治療方法，以幫助戒煙。它也可能被開發為一種有助於減肥的厭食藥物，但是市場上已經有幾種大麻素受體1拮抗劑或反向激動劑或為了該應用而正在開發這的藥物，[2]因此溴乙那班目前主要被開發為一種抗吸煙藥物，[3]可能應用於治療其他成癮性疾病，如酗酒。[4][5]該藥物也有其他潛在的應用，例如治療注意力不足過動症。[6]
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| CAS號 | 288104-79-0  |
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| 化學資訊 | |
| 化學式 | C23H23BrCl2N4O |
| 摩爾質量 | 522.27 g·mol−1 |
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在2012年對戒煙進行了劑量範圍研究；[7]它沒有提高成功率，但減少了體重的增加。在20毫克和60毫克時觀察到四氫大麻酚對心率的抑制作用，但在5毫克時沒有。[8]
參見
參考資料
- ^ Rinaldi-Carmona M, Barth F, Congy C, Martinez S, Oustric D, Pério A, et al. SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization. The Journal of Pharmacology and Experimental Therapeutics. September 2004, 310 (3): 905–14. PMID 15131245. S2CID 25640461. doi:10.1124/jpet.104.067884.
- ^ Doggrell SA. Will the new CB1 cannabinoid receptor antagonist SR-147778 have advantages over rimonabant?. Expert Opinion on Investigational Drugs. March 2005, 14 (3): 339–42. PMID 15833065. S2CID 33937749. doi:10.1517/13543784.14.3.339.
- ^ Lamota L, Bermudez-Silva FJ, Marco EM, Llorente R, Gallego A, Rodríguez de Fonseca F, Viveros MP. Effects of adolescent nicotine and SR 147778 (Surinabant) administration on food intake, somatic growth and metabolic parameters in rats. Neuropharmacology. January 2008, 54 (1): 194–205. PMID 17720206. S2CID 22293050. doi:10.1016/j.neuropharm.2007.07.004.
- ^ Gessa GL, Serra S, Vacca G, Carai MA, Colombo G. Suppressing effect of the cannabinoid CB1 receptor antagonist, SR147778, on alcohol intake and motivational properties of alcohol in alcohol-preferring sP rats. Alcohol and Alcoholism. 2005, 40 (1): 46–53. PMID 15582988. doi:10.1093/alcalc/agh114
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- ^ Lallemand F, De Witte P. SR147778, a CB1 cannabinoid receptor antagonist, suppresses ethanol preference in chronically alcoholized Wistar rats. Alcohol. July 2006, 39 (3): 125–34. PMID 17127132. doi:10.1016/j.alcohol.2006.08.001.
- ^ Louis C, Terranova JP, Decobert M, Bizot JC, Françon D, Alonso R, Cohen C, Griebel G. Surinabant, a new CB1 receptor antagonist, displays efficacy in animal models of attention deficit/hyperactivity disorder. Behavioural Pharmacology. 2005, 16: S42. doi:10.1097/00008877-200509001-00133.
- ^ Tonstad S, Aubin HJ. Efficacy of a dose range of surinabant, a cannabinoid receptor blocker, for smoking cessation: a randomized controlled clinical trial. Journal of Psychopharmacology. July 2012, 26 (7): 1003–9. PMID 22219220. S2CID 39145361. doi:10.1177/0269881111431623.
- ^ Klumpers LE, Roy C, Ferron G, Turpault S, Poitiers F, Pinquier JL, et al. Surinabant, a selective cannabinoid receptor type 1 antagonist, inhibits Δ9-tetrahydrocannabinol-induced central nervous system and heart rate effects in humans. British Journal of Clinical Pharmacology. July 2013, 76 (1): 65–77. PMC 3703229 . PMID 23278647. doi:10.1111/bcp.12071.
