Agomelatin

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Agomelatin
(IUPAC) ime
N-[2-(7-metoksinaftalen-1-il)etil]acetamid
Klinički podaci
AHFS/Drugs.com Internacionalno ime leka
Identifikatori
CAS broj 138112-76-2
ATC kod N06AX22
PubChem[1][2] 82148
ChemSpider[3] 74141
UNII 137R1N49AD YesY
KEGG[4] D02578 YesY
ChEMBL[5] CHEMBL10878 YesY
Hemijski podaci
Formula C15H17NO2 
Mol. masa 243,301
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Bioraspoloživost <5%
Metabolizam hepatički (90% CYP1A2; 10% CYP2C9)
Poluvreme eliminacije < 2 h
Farmakoinformacioni podaci
Licenca

EU EMEA:link

Trudnoća  ?
Pravni status Prescription only
Način primene Oralno

Agomelatin (Valdoksan, Melitor, Timanaks) je antidepresiv. On je u prodaji za tretman kliničke depresije.[6][7] Poznato je da ima manje izražene seksualne nuspojave, kao i slabije diskontinuacione efekte u poređenju sa drugim antidepresivima.

Mehanizam dejstva[uredi - уреди | uredi izvor]

Agomelatin je melatonergički agonist (MT1 (Ki=0.10nM±0.01nM) i MT2 receptori (Ki=0.12nM±0.02nM)) i 5-HT2C antagonist (IC50=270nM; pKi=6.15±0.04). Iz studija vezivanja proizilazi da on nema uticaja na unos monoamina i da nema afiniteta za adrenergičke, histaminergičke, holinergičke, dopaminergičke i benzodiazepinske receptore, niti druge serotonergičke receptore.[8]

Reference[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. Hardman JG, Limbird LE, Gilman AG. (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10 izd.). New York: McGraw-Hill. DOI:10.1036/0071422803. ISBN 0-07-135469-7. http://books.mcgraw-hill.com/medical/goodmanandgilman/. 
  7. Pdr Staff (2009). PDR: Physicians Desk Reference 2010 (Physicians' Desk Reference (Pdr)). Rozelle, N.S.W: Thomson Reuters. ISBN 1-56363-748-0. http://www.pdr.net/Default.aspx. 
  8. "Summary of Product Characteristics" (PDF). European Medicine Agency. 2003. http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000915/WC500046227.pdf. pristupljeno 22. 9. 2010.. 

Spoljašnje veze[uredi - уреди | uredi izvor]

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