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
Farmakokinetički podaci
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) je atipični antipsihotik koji je razvijen za tretman šizofrenije i akutne manije vezane za bipolar poremećaj. Lek je ušao u fazu III kliničkih ispitivanja dok je Organon još bio deo Akzo Nobela.^[5] Preliminarni podaci indiciraju da asenapin proizvodi minimalne antiholinergičke i kardiovaskularne nuspojave, kao i minimalno uvećanje telesne težine. Preko 3000 pacijenata je učestvovalo u kliničkim ispitivanjima, i FDA je odobrila lek 2009.^[6]^[7]

Sinteza

Jedan od mogućih sintetičkih puteva je^[8]

U reducionom koraku se koristi natrijum u tečnom amonijaku.

References

↑ 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
↑ 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. 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. Retrieved 2008-12-28.^{[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 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] 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. 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. Retrieved 2008-12-28.^{[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.

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