Bosentan

Bosentan
(IUPAC) ime
	4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(pyrimidin-2-yl)pyrimidin-4-yl]benzene-1-sulfonamide
Klinički podaci
Identifikatori
CAS broj	147536-97-8
ATC kod	C02KX01
PubChem	104865
DrugBank	APRD00829
ChemSpider	94651
UNII	XUL93R30K2
ChEMBL	CHEMBL957
Hemijski podaci
Formula	C27H29N5O6S
Mol. masa	551.614 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C27H29N5O6S/c1-27(2,3)18-10-12-19(13-11-18)39(34,35)32-23-22(38-21-9-6-5-8-20(21)36-4)26(37-17-16-33)31-25(30-23)24-28-14-7-15-29-24/h5-15,33H,16-17H2,1-4H3,(H,30,31,32) ; Key: GJPICJJJRGTNOD-UHFFFAOYSA-N
Farmakokinetički podaci
Bioraspoloživost	50%
Vezivanje za proteine plazme	>98%
Metabolizam	Hepatički
Poluvreme eliminacije	5 sati
Farmakoinformacioni podaci
Trudnoća	?
Pravni status	℞ Prescription only
Način primene	Oralno

Bosentan je dualni antagonist endotelinkog receptora koji se koristi za lečenje plućne hipertenzije.^[5] On je prodaji u SAD-u, Evropskoj Uniji i drugim zemljama pod imenom Tracleer od strane kompanije Actelion Farmaceutikal.

Mehanizam dejstva

Bosentan je kompetitivni antagonist endotelin-1 na endotelin-A (ET-A) i endotelin-B (ET-B) receptorima. Pod normalnim uslovima, vezivanje endotelina-1 za ET-A ili ET-B receptore izaziva pulmonarnu vazokonstrikciju. Blokiranjem te interakcije, bosentan umanjuje pulmonarni vaskularni otpor. Bosentan ima neznatno veći afinitet za ET-A nego ET-B.

Literatura

↑ 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
↑ Channick RN, Simonneau G, Sitbon O, Robbins IM, Frost A, Tapson VF, Badesch DB, Roux S, Rainisio M, Bodin F, Rubin LJ (2001). „Effects of the dual endothelin-receptor antagonist bosentan in patients with pulmonary hypertension: a randomised placebo-controlled study”. Lancet 358 (9288): 1119-23. PMID 11597664.

Povezano

Vanjske veze

	Portal Medicina
	Portal Hemija

PubPK - farmakokinetika bosentana Arhivirano 2011-07-27 na Wayback Machine-u
Tracleer zvanični sajt
- Tracleer informacije of propisivanju Arhivirano 2017-03-05 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] 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

[5] Channick RN, Simonneau G, Sitbon O, Robbins IM, Frost A, Tapson VF, Badesch DB, Roux S, Rainisio M, Bodin F, Rubin LJ (2001). „Effects of the dual endothelin-receptor antagonist bosentan in patients with pulmonary hypertension: a randomised placebo-controlled study”. Lancet 358 (9288): 1119-23. PMID 11597664.

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