利瑞喹尼
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| 臨床資料 | |
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| 识别信息 | |
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| CAS号 | 143943-73-1  |
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| CompTox Dashboard (EPA) | |
| 化学信息 | |
| 化学式 | C26H25ClN2O3 |
| 摩尔质量 | 448.95 g·mol−1 |
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利瑞喹尼（英语：Lirequinil，开发代号：Ro41-3696）是一种非苯二氮䓬类催眠药，可与GABAA受体上的苯二氮䓬位点结合。在人体临床试验中，利瑞喹尼被发现具有与唑吡坦相似的疗效，但笨拙和记忆障碍等副作用较少。然而，它的作用也比唑吡坦慢得多，口服给药后2.5小时才达到血浆峰值浓度，其O-去乙基代谢物Ro41-3290也具有活性，半衰期为8小时。[1][2][3][4]这意味着虽然作为催眠药有效，但由于产生更多的次日镇静作用，利瑞喹尼未能证明优于唑吡坦，因此它尚未被用于临床。它是由罗氏的一个团队在1990年代开发的。[5]
参考资料
[编辑]- ^ Dingemanse J, Bury M, Roncari G, Zell M, Gieschke R, Gaillard AW, Odink J, van Brummelen P. Pharmacokinetics and pharmacodynamics of Ro 41-3696, a novel nonbenzodiazepine hypnotic. Journal of Clinical Pharmacology. August 1995, 35 (8): 821–9. PMID 8522640. S2CID 20456430. doi:10.1002/j.1552-4604.1995.tb04126.x.
- ^ Dingemanse J, Bury M, Bock J, Joubert P. Comparative pharmacodynamics of Ro 41-3696, a new hypnotic, and zolpidem after night-time administration to healthy subjects. Psychopharmacology. November 1995, 122 (2): 169–74. PMID 8848532. S2CID 11960902. doi:10.1007/BF02246091.
- ^ Dingemanse J, Bury M, Hussain Y, van Giersbergen P. Comparative tolerability, pharmacodynamics, and pharmacokinetics of a metabolite of a quinolizinone hypnotic and zolpidem in healthy subjects. Drug Metabolism and Disposition. December 2000, 28 (12): 1411–6. PMID 11095577.
- ^ Dingemanse J, Pedrazzetti E, van Giersbergen PL. Multiple-dose tolerability, pharmacodynamics, and pharmacokinetics of the quinolizinone hypnotic Ro 41-3696 in elderly subjects. Clinical Neuropharmacology. 2001, 24 (2): 82–90. PMID 11307042. S2CID 21588500. doi:10.1097/00002826-200103000-00003.
- ^ US Patent 5561233 Process for the preparation of an intermediate of a benzo[a]quinolizinone derivative