Befiradol

Из Википедије, слободне енциклопедије
Befiradol
(IUPAC) ime
3-​hloro-​4-​fluorofenil-​[4-​fluoro-​4-​([(5-​metilpiridin-​2-il)metilamino]metil)piperidin-​1-​il]metanon
Klinički podaci
Identifikatori
CAS broj 208110-64-9
ATC kod nije dodeljen
PubChem[1][2] 9865384
ChemSpider[3] 8041076
UNII RAT9OHA1YH YesY
ChEMBL[4] CHEMBL45305 YesY
Hemijski podaci
Formula C20H22ClF2N3O 
Mol. masa 393.857 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status Nije kontrolisan

Befiradol (F-13,640) je veoma potentan i visoko selektivan pun agonist 5-HT1A receptora. On ima veoma moćno analgetsko i antialodinsko dejstvo koje je uporedivo sa visokim dozama opioidnih lekova protiv bolova, ali sa malobrojnijim i manje izraženim nuspojavama, kao i zanemarljivim razvojem tolerancije pri dužoj upotrebi.[5][6][7][8][9][10] Jedna SAR studija je pokazala da zamena dihalofenil grupe sa 3-benzotiofenilom povećava maksimalnu efikasnost od 84% na 124% (Ki=2.7 nM)[11]

Reference[уреди]

  1. ^ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.“. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. ^ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities“. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. ^ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining“. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. ^ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery“. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.  edit
  5. ^ Bardin L, Tarayre JP, Malfetes N, Koek W, Colpaert FC (April 2003). „Profound, non-opioid analgesia produced by the high-efficacy 5-HT(1A) agonist F 13640 in the formalin model of tonic nociceptive pain“. Pharmacology 67 (4): 182–94. DOI:10.1159/000068404. PMID 12595749. 
  6. ^ Bruins Slot LA, Koek W, Tarayre JP, Colpaert FC (April 2003). „Tolerance and inverse tolerance to the hyperalgesic and analgesic actions, respectively, of the novel analgesic, F 13640“. European Journal of Pharmacology 466 (3): 271–9. DOI:10.1016/S0014-2999(03)01566-8. PMID 12694810. 
  7. ^ -{Bardin L, Assié MB, Pélissou M, Royer-Urios I, Newman-Tancredi A, Ribet JP, Sautel F, Koek W, Colpaert FC (March 2005). „Dual, hyperalgesic, and analgesic effects of the high-efficacy 5-hydroxytryptamine 1A (5-HT1A) agonist F 13640 [(3-chloro-4-fluoro-phenyl)-[4-fluoro-4[(5-methyl-pyridin-2-ylmethyl)-amino]-methyl}piperidin-1-yl]methanone, fumaric acid salt]: relationship with 5-HT1A receptor occupancy and kinetic parameters“. The Journal of Pharmacology and Experimental Therapeutics 312 (3): 1034–42. DOI:10.1124/jpet.104.077669. PMID 15528450. 
  8. ^ Colpaert FC, Deseure K, Stinus L, Adriaensen H (February 2006). „High-efficacy 5-hydroxytryptamine 1A receptor activation counteracts opioid hyperallodynia and affective conditioning“. The Journal of Pharmacology and Experimental Therapeutics 316 (2): 892–9. DOI:10.1124/jpet.105.095109. PMID 16254131. 
  9. ^ Deseure K, Bréand S, Colpaert FC (July 2007). „Curative-like analgesia in a neuropathic pain model: parametric analysis of the dose and the duration of treatment with a high-efficacy 5-HT(1A) receptor agonist“. European Journal of Pharmacology 568 (1–3): 134–41. DOI:10.1016/j.ejphar.2007.04.022. PMID 17512927. 
  10. ^ Bernard Vacher, Bernard Bonnaud, Wouter Koek. Pyridin-2-yl-methylamine derivatives, method of preparing and application as medicine. US Patent 6020345, May 21, 1999.
  11. ^ Bollinger S, Hübner H, Heinemann FW, Meyer K, Gmeiner P (October 2010). „Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists“. J. Med. Chem. 53 (19): 7167–79. DOI:10.1021/jm100835q. PMID 20860381. 


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