Asenapin

Asenapin
(IUPAC) ime
	(3aRS,12bRS)-rel-5-hloro-2,3,3a,12b-tetrahidro-; 2-metil-1H-dibenz[2,3:6,7]oksepino[4,5-c]pirol
Klinički podaci
AHFS/Drugs.com	Monografija
MedlinePlus	a610015
Identifikatori
CAS broj	65576-45-6
ATC kod	N05AH05
PubChem	163091
ChemSpider	2300725
UNII	JKZ19V908O
ChEMBL	CHEMBL1201756
Hemijski podaci
Formula	C17H16ClNO
Mol. masa	285,77 g/mol
SMILES	eMolekuli&PubHem
InChI
	InChI=1S/C17H16ClNO/c1-19-9-14-12-4-2-3-5-16(12)20-17-7-6-11(18)8-13(17)15(14)10-19/h2-8,14-15H,9-10H2,1H3/t14-,15-/m0/s1; Key: VSWBSWWIRNCQIJ-GJZGRUSLSA-N
Farmakokinetičkipodaci
Bioraspoloživost	35% sablingualno
Vezivanje za proteine plazme	95%
Metabolizam	hepatički
Poluvreme eliminacije	24 sata
Izlučivanje	50% urin, 40% izmet
Farmakoinformacioni podaci
Trudnoća	C(US)
Pravni status	Rx only
Način primene	sablingualno

Asenapin(Safris,Sikrest) jeatipični antipsihotikkoji je razvijen za tretmanšizofrenijei akutne manije vezane zabipolar poremećaj.Lek je ušao ufazu IIIkliničkih ispitivanja dok je Organon još bio deoAkzo Nobela.^[5]Preliminarni podaci indiciraju da asenapin proizvodi minimalne antiholinergičke i kardiovaskularne nuspojave, kao i minimalno uvećanje telesne težine. Preko 3000 pacijenata je učestvovalo ukliničkim ispitivanjima,iFDAje odobrila lek2009.^[6]^[7]

Sinteza

Jedan od mogućih sintetičkih puteva je^[8]

U reducionom koraku se koristinatrijumu tečnomamonijaku.

References

↑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
↑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
↑„Bipolar Disorder”.Clinical Trials Update(Genetic Engineering & Biotechnology News): str. 52,55. 15. 06. 2007..
↑"Schering-Plough Announces Asenapine NDA Accepted for Filing by the U.S. FDA"(Press release). Schering-Plough. 2007-11-26.Retrieved2008-12-28.^{[mrtav link]}
↑„FDA Drug Safety Communication: Serious allergic reactions reported with the use of Saphris (asenapine maleate)”.
↑J. van der Burg,U.S. Patent 4,145,434.

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 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] 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

[GEN200706-5] „Bipolar Disorder”.Clinical Trials Update(Genetic Engineering & Biotechnology News): str. 52,55. 15. 06. 2007..

[6] "Schering-Plough Announces Asenapine NDA Accepted for Filing by the U.S. FDA"(Press release). Schering-Plough. 2007-11-26.Retrieved2008-12-28.^{[mrtav link]}

[7] „FDA Drug Safety Communication: Serious allergic reactions reported with the use of Saphris (asenapine maleate)”.

[8] J. van der Burg,U.S. Patent 4,145,434.

[1]

[2]

[3]

[4]

[5]

[6]

[7]

[8]