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Adatanserin

С Википедије, слободне енциклопедије
Adatanserin
IUPAC ime
N-[2-(4-pirimidin-2-ilpiperazin-1-il)etil]adamantan-1-karboksamid
Identifikatori
CAS broj127266-56-2 ДаY
ATC kodnone
PubChemCID 130918
ChemSpider115774 ДаY
UNIIW5U6WQM26H ДаY
Hemijski podaci
FormulaC21H31N5O
Molarna masa369,50 g/mol
  • 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) ДаY
  • Key:HPFLVTSWRFCPCV-UHFFFAOYSA-N ДаY

Adatanserin (WY-50,324, SEB-324) je mešoviti 5-HT1A receptor parcijalni agonist i antagonist 5-HT2A i 5-HT2C receptora.[1][2][3] On je razvijan kao kao antidepresiv ali je razboj zaustavljen.[3][4]

Adantaserin poseduje neuroprotektivna svojstva protiv ishemijom indukovane glutamatergičke ekscitotoksičnosti. Taj efekat je posredovan blokadom 5-HT2A receptora.[5]

  1. ^ Singh A, Lucki I (1993). „Antidepressant-like activity of compounds with varying efficacy at 5-HT1A receptors”. Neuropharmacology. 32 (4): 331—40. PMID 8497336. doi:10.1016/0028-3908(93)90153-T. 
  2. ^ Kleven MS, Koek W (1996). „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. 276 (2): 388—97. PMID 8632301. 
  3. ^ а б Abou-Gharbia MA; Childers WE; Fletcher H (1999). „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. 42 (25): 5077—94. PMID 10602693. doi:10.1021/jm9806704. 
  4. ^ Stahl, S. M. (2000). Essential psychopharmacology: neuroscientific basis and practical application. Cambridge, UK: Cambridge University Press. ISBN 978-0-521-64615-4. 
  5. ^ Dawson LA, Galandak J, Djali S (2002). „Attenuation of ischemic efflux of endogenous amino acids by the novel 5-HT(1A)/5-HT(2) receptor ligand adatanserin”. Neurochemistry International. 40 (3): 203—9. PMID 11741003. doi:10.1016/S0197-0186(01)00082-1.