利瑞喹尼

利瑞喹尼
臨床資料
ATC碼	未分配;
识别信息
	IUPAC命名法 10-chloro-1-[(3S)-3-ethoxypyrrolidine-1-carbonyl]-3-phenyl-6,7-dihydrobenzo[a]quinolizin-4-one; ;
CAS号	143943-73-1
PubChem CID	3045375;
ChemSpider	2308119 ;
UNII	2VUW1087AD;
ChEMBL	ChEMBL2105118;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID80162579 ;
化学信息
化学式	C26H25ClN2O3
摩尔质量	448.95 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES CCO[C@H]1CCN(C1)C(=O)C2=C3C4=C(CCN3C(=O)C(=C2)C5=CC=CC=C5)C=CC(=C4)Cl;
	InChI 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 ; Key:CBSWRAUYCIIUEI-FQEVSTJZSA-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GABA_A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

^ 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

[pmid8522640-1] 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.

[pmid8848532-2] 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.

[pmid11095577-3] 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.

[pmid11307042-4] 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

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利瑞喹尼

参考资料

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