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利瑞喹尼

维基百科,自由的百科全书
利瑞喹尼
臨床資料
ATC碼
  • 未分配
识别信息
  • 10-chloro-1-[(3S)-3-ethoxypyrrolidine-1-carbonyl]-3-phenyl-6,7-dihydrobenzo[a]quinolizin-4-one
CAS号143943-73-1  checkY
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
化学信息
化学式C26H25ClN2O3
摩尔质量448.95 g·mol−1
3D模型(JSmol英语JSmol
  • CCO[C@H]1CCN(C1)C(=O)C2=C3C4=C(CCN3C(=O)C(=C2)C5=CC=CC=C5)C=CC(=C4)Cl
  • InChI=1S/C26H25ClN2O3/c1-2-32-20-11-12-28(16-20)25(30)23-15-22(17-6-4-3-5-7-17)26(31)29-13-10-18-8-9-19(27)14-21(18)24(23)29/h3-9,14-15,20H,2,10-13,16H2,1H3/t20-/m0/s1 ☒N
  • Key:CBSWRAUYCIIUEI-FQEVSTJZSA-N ☒N

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]

活性代谢物Ro41-3290

参考资料

[编辑]
  1. ^ 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. 
  2. ^ 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. 
  3. ^ 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. 
  4. ^ 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. 
  5. ^ US Patent 5561233 Process for the preparation of an intermediate of a benzo[a]quinolizinone derivative