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HP-505

维基百科,自由的百科全书
HP-505
识别信息
  • 3-phenyl-3H-spiro[isobenzofuran-1,4'-piperidine]
CAS号59142-94-8  checkY
PubChem CID
ChemSpider
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
化学信息
化学式C18H19NO
摩尔质量265.36 g·mol−1
3D模型(JSmol英语JSmol
  • C1(C2OC3(CCNCC3)C4=C2C=CC=C4)=CC=CC=C1
  • InChI=1S/C18H19NO/c1-2-6-14(7-3-1)17-15-8-4-5-9-16(15)18(20-17)10-12-19-13-11-18/h1-9,17,19H,10-13H2
  • Key:ZFJQWOMHWFYLPD-UHFFFAOYSA-N

HP-505是一种有机化合物,化学式为C18H19NO。它是由赫美罗制药公司英语Hoechst-Marion-Roussel研发的三重再摄取抑制剂[1]HP-505在小鼠试验中发现是丁苯那嗪英语tetrabenazine诱导的上睑下垂英语ptosis的有效抑制剂,这表明它可能具有抗抑郁活性。[2]

药理学

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HP-505 IC50 (µM)[1]
5-HT NE DA NE:5-HT DA:5-HT
0.19 ± 0.04 0.34 ± 0.1 0.66 ± 0.15 1.8 3.5

化学性质

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HP-505在碳酸氢钠存在下,可以和2-氯-4-硝基吡啶-1-氧化物反应,得到N-(1-氧化-4-硝基吡啶-2-基)-HP-505。[3]

参考文献

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  1. ^ 1.0 1.1 Meyerson, Laurence R; Ong, Helen H; Martin, Lawrence L; Ellis, Daniel B. Effect of antidepressant agents on β-adrenergic receptor and neurotransmitter regulatory systems. Pharmacology Biochemistry and Behavior. June 1980, 12 (6): 943–948. PMID 6105676. S2CID 45400599. doi:10.1016/0091-3057(80)90457-8. 
  2. ^ Klioze, SS; Bauer, VJ; Geyer HM, 3rd. Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 2. Compounds containing a heteroatom attached to nitrogen.. Journal of Medicinal Chemistry. April 1977, 20 (4): 610–2. PMID 850252. doi:10.1021/jm00214a039. 
  3. ^ Allerton, Charlotte Moira Norfor; Owen, Dafydd Rhys; Ryckmans, Thomas; Stammen, Blanda Luzia Christa. Spiropiperidine derivatives, processes for preparing them, pharmaceutical compositions containing them, and their use as delta opioid receptor agonists. 2007 WO 2007057775 A1.