Loksapin

Loksapin
(IUPAC) ime
	2-hloro-11-(4-metilpiperazin-1-il)dibenzo[b,f][1,4]oksazepin
Klinički podaci
AHFS/Drugs.com	Monografija
MedlinePlus	a682311
Identifikatori
CAS broj	1977-10-2
ATC kod	N05AH01
PubChem	3964
DrugBank	DB00408
ChemSpider	3827
UNII	LER583670J
KEGG	D02340
ChEBI	CHEBI:50841
ChEMBL	CHEMBL831
Hemijski podaci
Formula	C18H18ClN3O
Mol. masa	327,808 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C18H18ClN3O/c1-21-8-10-22(11-9-21)18-14-12-13(19)6-7-16(14)23-17-5-3-2-4-15(17)20-18/h2-7,12H,8-11H2,1H3 ; Key: XJGVXQDUIWGIRW-UHFFFAOYSA-N
Fizički podaci
Tačka topljenja	109–110 °C (228–230 °F)
Farmakokinetički podaci
Metabolizam	Gastrointestinalni, pik koncentracije se javlja između 1-2 sata
Poluvreme eliminacije	Oralno 4 h
Izlučivanje	Najveći deo se izlučuje u toku 24 sata
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

Loksapin (Loksapak, Loksitan) je tipični antipsihotik koji se prvenstveno koristi za lečenje šizofrenije. On je član (benzodiazepinske) dibenzoksazepinske klase, te je strukturno srodan sa klozapinom.^[6]

Loksapin može da bude metabolisan N-demetilacijom do amoksapina, tetracikličnog antidepresiva.^[7]

Hemija

Jedan od mogućih sintetičkih pristupa je:^[8]

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.
↑ 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
↑ Glazer WM (1999). „Does loxapine have "atypical" properties? Clinical evidence”. The Journal of Clinical Psychiatry 60 (Suppl 10): 42–6. PMID 10340686.
↑ Cheung SW, Tang SW, Remington G (March 1991). „Simultaneous quantitation of loxapine, amoxapine and their 7- and 8-hydroxy metabolites in plasma by high-performance liquid chromatography”. Journal of Chromatography 564 (1): 213–21. DOI:10.1016/0378-4347(91)80083-O. PMID 1860915.
↑ Schmutz, J.; Kunzle, F.; Hunziker, F.; Gauch, R.; Helv. Chim. Acta 1967, 50, 245.

Spoljašnjve veze

Product monograph from Medscape (free registration required).

[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.

[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 Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit

[pmid10340686-6] Glazer WM (1999). „Does loxapine have "atypical" properties? Clinical evidence”. The Journal of Clinical Psychiatry 60 (Suppl 10): 42–6. PMID 10340686.

[pmid1860915-7] Cheung SW, Tang SW, Remington G (March 1991). „Simultaneous quantitation of loxapine, amoxapine and their 7- and 8-hydroxy metabolites in plasma by high-performance liquid chromatography”. Journal of Chromatography 564 (1): 213–21. DOI:10.1016/0378-4347(91)80083-O. PMID 1860915.

[8] Schmutz, J.; Kunzle, F.; Hunziker, F.; Gauch, R.; Helv. Chim. Acta 1967, 50, 245.

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