Kvetijapin

Kvetijapin
(IUPAC) ime
	2-(2-(4-dibenzo[b,f][1,4]tiazepin- 11-il- 1-piperazinil)etoksi)etanol
Klinički podaci
Robne marke	Serokvel
AHFS/Drugs.com	Monografija
MedlinePlus	a698019
Identifikatori
CAS broj	111974-69-7
ATC kod	N05AH04
PubChem	5002
DrugBank	DB01224
ChemSpider	4827
UNII	BGL0JSY5SI
KEGG	D08456
ChEBI	CHEBI:8707
ChEMBL	CHEMBL716
Hemijski podaci
Formula	C21H25N3O2S
Mol. masa	383,5099 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C21H25N3O2S/c25-14-16-26-15-13-23-9-11-24(12-10-23)21-17-5-1-3-7-19(17)27-20-8-4-2-6-18(20)22-21/h1-8,25H,9-16H2 ; Key: URKOMYMAXPYINW-UHFFFAOYSA-N
Farmakokinetički podaci
Bioraspoloživost	9%
Metabolizam	Hepatički
Poluvreme eliminacije	6 sata
Izlučivanje	Renalno
Farmakoinformacioni podaci
Trudnoća	C(US)
Pravni status	℞-only (SAD)
Način primene	Oralnot

Kvetijapin (Serokvel, Ketipinor) je atipični antipsihotik koji je odorobren za lečenje šizofrenije, bipolarnog poremećaja i kao dodatni tretman za depresiju.

Godišnja prodaja ovog leka je vredna oko USD $5,7 milijardi globalno, do čega je $2.9 milijardi u SAD-u.^[6] Američki patent,^[7] je trebalo da istekne 2011, ali je njegov vek produžen radi pedijatrijske ekskluzivnosti do marta 2012.^[8]^[9]^[10]

Farmakologija

Poređenje afiniteta (Ki, nM)^[11]
Receptor	Kvetijapin	Norkvetijapin
D₁	428	99.8
D₂	626	489
5-HT_1A	1040	191
5-HT_2A	38	2.9
α_1B	14.6	46.4
α₂	617	1290
H₁	4.41	1.15
M₁	1086	38.3
NET	>10000	34.8

Kvetijapin poseduje sledeća farmakološka dejstva:^[12]^[13]^[14]^[15]

D₁ (IC₅₀ = 1268nM), D₂ (IC₅₀ = 329nM), D₃, i D₄ receptor antagonist
5-HT_1A (IC₅₀ = 717nM), 5-HT_2A (IC₅₀ = 148nM), 5-HT_2C, and 5-HT₇ receptor antagonist
α₁-adrenergički (IC₅₀ = 94nM) i α₂-adrenergički receptor (IC₅₀ = 271nM) antagonist
H₁ receptor (IC₅₀ = 30nM) antagonist
mACh receptor (IC₅₀ = >5000nM) antagonist

Sinteza

Jedan od mogućih sintetičkih puteva je:^[16]

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
↑ Details for Seroquel
↑ „Patent Document, U.S. Patent and Trademark Office”. Arhivirano iz originala na datum 2017-01-06. Pristupljeno 2014-04-05.
↑ Blockbuster Drugs That Will Go Generic Soon
↑ Seroquel patent expiration
↑ „Quepin Full Prescribing Information in Drug Reference Encyclopedia”. Pristupljeno 3. 4. 2010.
↑ AstraZeneca Pharmaceuticals LP (March 2011). „SEROQUEL (quetiapine fumarate) tablet, extended release”. DailyMed. National Library of Medicine. Section 12.2: Pharmacodynamics. Pristupljeno 26. 4. 2011.
↑ AstraZeneca (PDF). Seroquel (quietapine fumarate) tablets. 276521. Arhivirano iz originala na datum 2008-04-14. Pristupljeno 2014-04-05.
↑ Richelson E, Souder T (November 2000). „Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds”. Life Sciences 68 (1): 29–39. DOI:10.1016/S0024-3205(00)00911-5. PMID 11132243.
↑ Davis, Kenneth L; Neuropsychopharmacology, American College of (2002). Neuropsychopharmacology: the fifth ... - Google Books. ISBN 9780781728379.
↑ Seroquel Official FDA information, side effects and uses
↑ Warawa, E. J.; Migler, B. M.; 1988, U.S. Patent 4.879.288.

Literatura

Davis, Kenneth L; Neuropsychopharmacology, American College of (2002). Neuropsychopharmacology: the fifth ... - Google Books. ISBN 9780781728379.

Vanjske veze

	Portal Medicina
	Portal Hemija

„Quetiapine”. MedlinePlus. The American Society of Health-System Pharmacists, Inc.. 1. 9. 2008..
NAMI pregled Arhivirano 2003-09-25 na Wayback Machine-u

[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

[6] Details for Seroquel

[7] „Patent Document, U.S. Patent and Trademark Office”. Arhivirano iz originala na datum 2017-01-06. Pristupljeno 2014-04-05.

[8] Blockbuster Drugs That Will Go Generic Soon

[9] Seroquel patent expiration

[10] „Quepin Full Prescribing Information in Drug Reference Encyclopedia”. Pristupljeno 3. 4. 2010.

[dailymed_PI-11] AstraZeneca Pharmaceuticals LP (March 2011). „SEROQUEL (quetiapine fumarate) tablet, extended release”. DailyMed. National Library of Medicine. Section 12.2: Pharmacodynamics. Pristupljeno 26. 4. 2011.

[Seroquel-12] AstraZeneca (PDF). Seroquel (quietapine fumarate) tablets. 276521. Arhivirano iz originala na datum 2008-04-14. Pristupljeno 2014-04-05.

[pmid11132243-13] Richelson E, Souder T (November 2000). „Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds”. Life Sciences 68 (1): 29–39. DOI:10.1016/S0024-3205(00)00911-5. PMID 11132243.

[urlNeuropsychopharmacology:_the_fifth_..._-_Google_Books-14] Davis, Kenneth L; Neuropsychopharmacology, American College of (2002). Neuropsychopharmacology: the fifth ... - Google Books. ISBN 9780781728379.

[15] Seroquel Official FDA information, side effects and uses

[16] Warawa, E. J.; Migler, B. M.; 1988, U.S. Patent 4.879.288.

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