Agomelatin

Agomelatin
(IUPAC) ime
	N-[2-(7-metoksinaftalen-1-il)etil]acetamid
Klinički podaci
AHFS/Drugs	Internacionalno ime leka
Identifikatori
CAS broj	138112-76-2
ATC kod	N06AX22
PubChem	82148
ChemSpider	74141
UNII	137R1N49AD
KEGG	D02578
ChEMBL	CHEMBL10878
Hemijski podaci
Formula	C15H17NO2
Mol. masa	243,301
SMILES	eMolekuli&PubHem
InChI
	InChI=1S/C15H17NO2/c1-11(17)16-9-8-13-5-3-4-12-6-7-14(18-2)10-15(12)13/h3-7,10H,8-9H2,1-2H3,(H,16,17); Key: YJYPHIXNFHFHND-UHFFFAOYSA-N
Farmakokinetičkipodaci
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) jeantidepresiv.On je u prodaji za tretmankliničke depresije.^[6]^[7]Poznato je da ima manje izražene seksualne nuspojave, kao i slabije diskontinuacione efekte u poređenju sa drugim antidepresivima.

Mehanizam dejstva

Agomelatin je melatonergički agonist (MT1(K_i=0.10nM±0.01nM) iMT2receptori (K_i=0.12nM±0.02nM)) i5-HT_2C antagonist(IC₅₀=270nM; pK_i=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

↑Li Q, Cheng T, Wang Y, Bryant SH (2010).„PubChem as a public resource for drug discovery.”.Drug Discov Today15(23-24): 1052-7.DOI:10.1016/j.drudis.2010.10.003.PMID 20970519.edit
↑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 Chemistry4:217-241.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 Cheminform2(1): 3.DOI:10.1186/1758-2946-2-3.PMID 20331846.edit
↑Joanne Wixon, Douglas Kell (2000).„Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”.Yeast17(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 Res40(Database issue): D1100-7.DOI:10.1093/nar/gkr777.PMID 21948594.edit
↑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 izoriginalana datum 2014-10-29.Pristupljeno 22. 9. 2010.

Spoljašnje veze

	Portal Medicina
	Portal Hemija

{{refbegin|2}{

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010).„PubChem as a public resource for drug discovery.”.Drug Discov Today15(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 Chemistry4:217-241.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 Cheminform2(1): 3.DOI:10.1186/1758-2946-2-3.PMID 20331846.edit

[4] Joanne Wixon, Douglas Kell (2000).„Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”.Yeast17(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 Res40(Database issue): D1100-7.DOI:10.1093/nar/gkr777.PMID 21948594.edit

[Goodman_Gilman-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.

[PDR-7] Pdr Staff (2009).PDR: Physicians Desk Reference 2010 (Physicians' Desk Reference (Pdr)).Rozelle, N.S.W: Thomson Reuters.ISBN 1-56363-748-0.

[emea-8] „Summary of Product Characteristics”(PDF). European Medicine Agency. 2003. Arhivirano izoriginalana datum 2014-10-29.Pristupljeno 22. 9. 2010.

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