Eplivanserin

Eplivanserin
(IUPAC) ime
	(Z,E)-1-(2-fluorofenil)-3-(4-hidroksifnil)-2-propen-1-on O-[2-(dimetilamino)etil]oksim
Klinički podaci
Identifikatori
CAS broj	130579-75-8 ; 130580-02-8 (fumarat)
ATC kod	nije dodeljen
PubChem	5493160
ChemSpider	13267837
UNII	3CO94WO6DJ
KEGG	D10006
Hemijski podaci
Formula	C19H21FN2O2
Mol. masa	328,381 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C19H21FN2O2/c1-22(2)13-14-24-21-19(17-5-3-4-6-18(17)20)12-9-15-7-10-16(23)11-8-15/h3-12,23H,13-14H2,1-2H3/b12-9+,21-19- ; Key: VAIOZOCLKVMIMN-PRJWTAEASA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status
Način primene	Oralno

Eplivanserin (SR-46,349; Ciltiri) je bio eksperimentalni lek za tretman insomnije koj je razvijala kompanija Sanofi Aventis.^[5]

Sanofi Aventis je decembra 2009. povukla svoju svoju aplikaciju za odobrenje kod FDA i Evropske medicinske agencije.^[6]

Mehanizam dejstva

Eplivanserin je inverzni agonist serotoninskog receptora 5-HT_2A. U kontrastu sa drugim sedirajućim lekovima koji deluju na 5-HT_2A receptore (e.g., mirtazapin, klozapin, risperidon), eplivanserin praktično nema afiniteta za dopaminske, histaminske i adrenergičke receptore.^[7]

Rezultati ispitivanja

Placebo kontrolisana ispitivanja faze II sa 351 subjekata su pokazala da eplivanserin redukuje period pre početka sna za 39 minuta (u poređenju sa 26 minuta za placebo).^[7]

Reference

↑ 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
↑ 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. edit
↑ 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.
↑ „Future Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD -- Neurotransmitter.net”.
↑ Spencer, Mimosa; Berton, Elena (21. 12. 2009.). „Sanofi-Aventis Discontinues Eplivanserin For Insomnia”. Dow Jones & Co. Pristupljeno 27. 1. 2010.
↑ ^7,0 ^7,1 Teergarden, BR; Al Shamma, H, Xiong, Y (2008). „5-HT2A Inverse-Agonists for the Treatment of Insomnia”. Current Topics in Medicinal Chemistry 8 (11): 969–976. DOI:10.2174/156802608784936700. PMID 18673166.

Povezano

Spoljašnje veze

	Portal Medicina
	Portal Hemija

[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] 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.

[urlFuture_Treatments_for_Depression,_Anxiety,_Sleep_Disorders,_Psychosis,_and_ADHD_--_Neurotransmitter.net-5] „Future Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD -- Neurotransmitter.net”.

[6] Spencer, Mimosa; Berton, Elena (21. 12. 2009.). „Sanofi-Aventis Discontinues Eplivanserin For Insomnia”. Dow Jones & Co. Pristupljeno 27. 1. 2010.

[Teergarden-7] 7,0 ^7,1 Teergarden, BR; Al Shamma, H, Xiong, Y (2008). „5-HT2A Inverse-Agonists for the Treatment of Insomnia”. Current Topics in Medicinal Chemistry 8 (11): 969–976. DOI:10.2174/156802608784936700. PMID 18673166.

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