溴乙那班
化合物
溴乙那班（英语：Surinabant；开发代号：SR147778），也译作舒立纳班或速利那班，是一种大麻素受体1拮抗剂，由赛诺菲开发。[1]它正在被研究作为尼古丁成瘾的潜在治疗方法，以帮助戒烟。它也可能被开发为一种有助于减肥的厌食药物，但是市场上已经有几种大麻素受体1拮抗剂或反向激动剂或为了该应用而正在开发这的药物，[2]因此溴乙那班目前主要被开发为一种抗吸烟药物，[3]可能应用于治疗其他成瘾性疾病，如酗酒。[4][5]该药物也有其他潜在的应用，例如治疗注意力不足过动症。[6]
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| CAS号 | 288104-79-0  |
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| 化学式 | C23H23BrCl2N4O |
| 摩尔质量 | 522.27 g·mol−1 |
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在2012年对戒烟进行了剂量范围研究；[7]它没有提高成功率，但减少了体重的增加。在20毫克和60毫克时观察到四氢大麻酚对心率的抑制作用，但在5毫克时没有。[8]
参见
参考资料
- ^ 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.
