来索吡琼

来索吡琼INN:lesopitron;开发代号:E-4424)是5-HT1A受体的选择性完全激动剂,其结构与阿扎匹隆相关。[1]2001 年,Esteve将其开发作为抗焦虑药,用于治疗广泛性焦虑症[2][3]它进入了II期临床试验,但开发进度已停止,因为此后没有出现关于来索吡琼的新消息。[2][3]

来索吡琼
臨床資料
给药途径口服给药
ATC碼
  • 未分配
法律規範狀態
法律規範
  • 不受管制
识别信息
  • 2-{4-[4-(4-chloro-1H-pyrazol-1-yl)butyl]piperazin-1-yl}pyrimidine
CAS号132449-46-8
PubChem CID
ChemSpider
UNII
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
化学信息
化学式C15H21ClN6
摩尔质量320.83 g·mol−1
3D模型(JSmol英语JSmol
  • Clc1cn(nc1)CCCCN3CCN(c2ncccn2)CC3

参见

参考资料

  1. ^ Haj-Dahmane S, Jolas T, Laporte AM, et al. Interactions of lesopitron (E-4424) with central 5-HT1A receptors: in vitro and in vivo studies in the rat. European Journal of Pharmacology. April 1994, 255 (1–3): 185–96. PMID 8026543. doi:10.1016/0014-2999(94)90097-3. 
  2. ^ 2.0 2.1 Micheli F. Lesopitron (Esteve). IDrugs: The Investigational Drugs Journal. February 2001, 4 (2): 218–24. PMID 16032484. 
  3. ^ 3.0 3.1 Fresquet A, Sust M, Lloret A, et al. Efficacy and safety of lesopitron in outpatients with generalized anxiety disorder. The Annals of Pharmacotherapy. February 2000, 34 (2): 147–53. PMID 10676820. doi:10.1345/aph.19041. 

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