Almoreksant

Almoreksant
(IUPAC) ime
	(2R)-2-[(1S)- 6,7-dimethoxy- 12-[4-(trifluoromethyl)phenyl]ethyl 3,4-dihydroisoquinolin-2(1H)-yl]- N-methyl- 2-phenylacetamide
Klinički podaci
Identifikatori
CAS broj	871224-64-5
ATC kod	nije dodeljen
PubChem	23727689
ChemSpider	21377865
Hemijski podaci
Formula	C29H32ClF3N2O3
Mol. masa	512,6 g/mol (slobodna baza)
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C29H31F3N2O3/c1-33-28(35)27(20-7-5-4-6-8-20)34-16-15-21-17-25(36-2)26(37-3)18-23(21)24(34)14-11-19-9-12-22(13-10-19)29(30,31)32/h4-10,12-13,17-18,24,27H,11,14-16H2,1-3H3,(H,33,35)/t24-,27+/m0/s1 ; Key: DKMACHNQISHMDN-RPLLCQBOSA-N
Farmakokinetički podaci
Metabolizam	Hepatčki
Farmakoinformacioni podaci
Trudnoća	?
Pravni status
Način primene	Oralno

Almoreksant (INN), kode ACT-078573, je kompetitivni antagonist OX₁ i OX₂ oreksinskih receptor. Ovaj lek je razvila farmaceutska kompanija Actelion za lečenje primarne insomnije. Njegova klinička ispitivanja faze III su završen su novembra 2009.^[4]

Januara 2011 Actelion i GSK su objavili prestanak daljih kliničkih ispitivanja zbog nuspojava.^[5]

Mehanizam akcije[uredi | uredi kod]

Almoreksant je kompetitivni, dualni antagonist receptora OX₁ i OX₂. On selektivno inhibira aktivaciju OX₁ i OX₂ receptora.

Almoreksant je bio u razvoju za lečenje nesanice.

↑ 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
↑ „Almorexant in Adult Subjects With Chronic Primary Insomnia (RESTORA 1), ClinicalTrials.gov”. Pristupljeno 3. 02. 2010.
↑ „Actelion and GSK Discontinue Clinical Development of Almorexant”. .

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