Vilazodon

Iz Wikipedije, slobodne enciklopedije
Vilazodon
(IUPAC) ime
5-(4-[4-(5-cijano-1H-indol-3-il)butil]piperazin-1-il)benzofuran-2-karboksamid
Klinički podaci
Robne marke Viibryd
AHFS/Drugs.com Potrošačka informacije o leku
MedlinePlus a611020
Identifikatori
CAS broj 163521-12-8
ATC kod N06AX24
PubChem[1][2] 6918313
ChemSpider[3] 5293518
UNII S239O2OOV3 YesY
KEGG[4] D09698 YesY
ChEMBL[5] CHEMBL439849 YesY
Hemijski podaci
Formula C26H27N5O2 
Mol. masa 441,524 g/mol
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Poluvreme eliminacije 20-24 sata
Farmakoinformacioni podaci
Licenca

US FDA:link

Trudnoća C(US)
Pravni status -only (SAD)
Način primene Oralno

Vilazodon (Viibryd) je serotinergički antidepresiv koji je razvijen za tretman kliničke depresije.[6] FDA je odobrila upotrebu vilazodona 2011.[7][8][9]

Farmakologija[uredi - уреди | uredi izvor]

Vilazodon deluje kao inhibitor preuzimanja serotonina (IC50 = 0.5 nM) i parcijalni agonist 5-HT1A receptora (IC50 = 0.2 nM; IA = ~60-70%).[10][11] On ima neznatan afinitet za druge serotoninske receptore kao što je 5-HT1D, 5-HT2A, i 5-HT2C.[10][11]

References[uredi - уреди | uredi izvor]

  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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  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. PMID 20331846. doi:10.1186/1758-2946-2-3.  edit
  4. Joanne Wixon, Douglas Kell (2000). "Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG". Yeast 17 (1): 48–55. doi:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H. 
  5. 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. PMID 21948594. doi:10.1093/nar/gkr777.  edit
  6. de Paulis T (March 2007). "Drug evaluation: Vilazodone--a combined SSRI and 5-HT1A partial agonist for the treatment of depression". IDrugs : the Investigational Drugs Journal 10 (3): 193–201. PMID 17351874. 
  7. "FDA approves Clinical Data Inc's antidepressant". Reuters. 22. 1. 2011. 
  8. "FDA approves Clinical Data Inc's antidepressant". Reuters. 22. 1. 2011. 
  9. "Clinical Data, Inc. - Clinical Data, Inc. Submits New Drug Application for Vilazodone for the Treatment of Major Depressive Disorder". http://investor.clda.com/releasedetail.cfm?ReleaseID=453924. 
  10. 10,0 10,1 Page ME, Cryan JF, Sullivan A et al. (September 2002). "Behavioral and neurochemical effects of 5-(4-[4-(5-Cyano-3-indolyl)-butyl)-butyl]-1-piperazinyl)-benzofuran-2-carboxamide (EMD 68843): a combined selective inhibitor of serotonin reuptake and 5-hydroxytryptamine(1A) receptor partial agonist". The Journal of Pharmacology and Experimental Therapeutics 302 (3): 1220–7. PMID 12183683. doi:10.1124/jpet.102.034280. 
  11. 11,0 11,1 Hughes ZA, Starr KR, Langmead CJ et al. (March 2005). "Neurochemical evaluation of the novel 5-HT1A receptor partial agonist/serotonin reuptake inhibitor, vilazodone". European Journal of Pharmacology 510 (1–2): 49–57. PMID 15740724. doi:10.1016/j.ejphar.2005.01.018. 

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