阿达色林

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阿达色林
臨床資料
ATC碼
  • 未分配
识别信息
  • N-[2-(4-pyrimidin-2-ylpiperazin-1-yl)ethyl]adamantane-1-carboxamide
CAS号127266-56-2  ☒N
PubChem CID
ChemSpider
UNII
ChEMBL
化学信息
化学式C21H31N5O
摩尔质量369.51 g·mol−1
3D模型(JSmol英语JSmol
  • O=C(NCCN2CCN(c1ncccn1)CC2)C35CC4CC(CC(C3)C4)C5
  • InChI=1S/C21H31N5O/c27-19(21-13-16-10-17(14-21)12-18(11-16)15-21)22-4-5-25-6-8-26(9-7-25)20-23-2-1-3-24-20/h1-3,16-18H,4-15H2,(H,22,27) checkY
  • Key:HPFLVTSWRFCPCV-UHFFFAOYSA-N checkY

阿达色林INN:adatanserin;开发代号:WY-50,324SEB-324)是一种混合的5-HT1A受体部分激动剂以及5-HT2A5-HT2C受体拮抗剂。[1][2][3]惠氏公司试图将其开发为抗抑郁药,但最终没有得到推广。[3][4]

阿达色林已被证明对缺血引起的谷氨酸兴奋毒性具有神经保护作用,这种作用似乎是通过阻断5-HT2A受体介导的。[5]

参见[编辑]

参考资料[编辑]

  1. ^ Singh A, Lucki I. Antidepressant-like activity of compounds with varying efficacy at 5-HT1A receptors. Neuropharmacology. April 1993, 32 (4): 331–40. PMID 8497336. S2CID 38611829. doi:10.1016/0028-3908(93)90153-T. 
  2. ^ Kleven MS, Koek W. Pharmacological characterization of in vivo properties of putative mixed 5-HT1A agonist/5-HT2A/2C antagonist anxiolytics. I. Antipunishment effects in the pigeon. The Journal of Pharmacology and Experimental Therapeutics. February 1996, 276 (2): 388–97. PMID 8632301. 
  3. ^ 3.0 3.1 Abou-Gharbia MA, Childers WE, Fletcher H, et al. Synthesis and SAR of adatanserin: novel adamantyl aryl- and heteroarylpiperazines with dual serotonin 5-HT(1A) and 5-HT(2) activity as potential anxiolytic and antidepressant agents. Journal of Medicinal Chemistry. December 1999, 42 (25): 5077–94. PMID 10602693. doi:10.1021/jm9806704. 
  4. ^ Stahl, S. M. Essential psychopharmacology: neuroscientific basis and practical application需要免费注册. Cambridge, UK: Cambridge University Press. 2000: 262. ISBN 0-521-64615-4. adatanserin. 
  5. ^ Dawson LA, Galandak J, Djali S. Attenuation of ischemic efflux of endogenous amino acids by the novel 5-HT(1A)/5-HT(2) receptor ligand adatanserin. Neurochemistry International. March 2002, 40 (3): 203–9. PMID 11741003. S2CID 24104458. doi:10.1016/S0197-0186(01)00082-1.