Agomelatin
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.
(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 | ||
KEGG[4] | D02578 | ||
ChEMBL[5] | CHEMBL10878 | ||
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 | |||
Trudnoća | ? | ||
Pravni status | ℞ Prescription only | ||
Način primene | Oralno |
Mehanizam dejstva
urediAgomelatin 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- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ Pdr Staff (2009). PDR: Physicians Desk Reference 2010 (Physicians' Desk Reference (Pdr)). Rozelle, N.S.W: Thomson Reuters. ISBN 1-56363-748-0.
- ↑ „Summary of Product Characteristics” (PDF). European Medicine Agency. 2003. Arhivirano iz originala na datum 2014-10-29. Pristupljeno 22. 9. 2010.
Spoljašnje veze
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- Official product site Arhivirano 2019-07-29 na Wayback Machine-u
- Manufacturer web site
- Agomelatine Psychonauts Google Group[mrtav link]
- Novartis pipeline Arhivirano 2011-02-16 na Wayback Machine-u
- Antidepressant-like activity of S 20098 (agomelatine) in the forced swimming test in rodents: involvement of melatonin and serotonin receptors
- The Novel Melatonin Agonist Agomelatine (S20098) Is an Antagonist at 5-Hydroxytryptamine2C Receptors, Blockade of Which Enhances the Activity of Frontocortical Dopaminergic and Adrenergic Pathways
- Agomelatine treatment has promising results in transgenic murine model