泽奎替奈

化合物

泽奎替奈INN:zelquistinel;开发代号:GATE-251AGN-241751)是一种口服活性小分子NMDA受体调节剂英语NMDA receptor modulator。Gate Neurosciences正在开发该药物以用于治疗重度抑郁症,该药物此前由艾尔建开发。[1][2][3]

泽奎替奈
临床资料
给药途径口服
药物类别英语Drug classNMDA受体调节剂英语NMDA receptor modulator
识别信息
  • tert-butyl (4S)-2-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-3-oxo-2,5-diazaspiro[3.4]octane-5-carboxylate
CAS号2151842-64-5
PubChem CID
ChemSpider
UNII
化学信息
化学式C15H25N3O5
摩尔质量327.38 g·mol−1
3D模型(JSmol英语JSmol
  • C[C@H]([C@@H](C(=O)N)N1C[C@]2(C1=O)CCCN2C(=O)OC(C)(C)C)O
  • InChI=1S/C15H25N3O5/c1-9(19)10(11(16)20)17-8-15(12(17)21)6-5-7-18(15)13(22)23-14(2,3)4/h9-10,19H,5-8H2,1-4H3,(H2,16,20)/t9-,10+,15+/m1/s1
  • Key:ABAPCYNTEPGBNJ-FTGAXOIBSA-N

泽奎替奈通过NMDA受体上的独特结合位点(独立于甘氨酸位点)发挥作用,以调节受体活性并增强NMDA受体介导的突触可塑性。[4][5]作用机制雷帕替奈相似。然而,与雷帕替奈不同的是,泽奎替奈具有口服生物利用度、更高的效力和改进的药物特性。[2][3][5]

2018年7月23日,美国食品药品监督管理局授予泽奎替奈开发快速通道英语Fast track (FDA)资格,作为重度抑郁症的研究性新疗法。[6]截至2019年8月,该药物已完成IIa期临床试验。[1][3][7]

参见

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参考资料

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  1. ^ 1.0 1.1 NMDA receptor modulators - AdisInsight. adisinsight.springer.com. 
  2. ^ 2.0 2.1 Home - Gate Neurosciences. [2022-05-12]. (原始内容存档于2023-09-05) (美国英语). 
  3. ^ 3.0 3.1 3.2 Aptinyx Inc. Allergan Exercises Option to Acquire Compound from Aptinyx Discovery Platform Under Ongoing Research Collaboration. www.prnewswire.com (新闻稿). [2024-05-09]. (原始内容存档于2024-05-20). 
  4. ^ Donello JE, Banerjee P, Li YX, Guo YX, Yoshitake T, Zhang XL, et al. Positive N-Methyl-D-Aspartate Receptor Modulation by Rapastinel Promotes Rapid and Sustained Antidepressant-Like Effects. The International Journal of Neuropsychopharmacology. March 2019, 22 (3): 247–259. PMC 6403082 . PMID 30544218. doi:10.1093/ijnp/pyy101. 
  5. ^ 5.0 5.1 Pothula S, Liu RJ, Wu M, Sliby AN, Picciotto MR, Banerjee P, Duman RS. Positive modulation of NMDA receptors by AGN-241751 exerts rapid antidepressant-like effects via excitatory neurons. Neuropsychopharmacology. March 2021, 46 (4): 799–808. PMC 8027594 . PMID 33059355. doi:10.1038/s41386-020-00882-7. 
  6. ^ plc, Allergan. Allergan Receives FDA Fast Track Designation for AGN-241751 for the Treatment of Major Depressive Disorder (MDD). www.prnewswire.com (新闻稿). [2022-05-16] (英语). 
  7. ^ Clinical trial number NCT03586427 for "A Double-Blind, Placebo-Controlled, Fixed-Dose Study of AGN-241751 in Adult Participants With Major Depressive Disorder" at ClinicalTrials.gov

外部链接

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