PRX-08066

PRX-08066
(IUPAC) ime
	5-((4-(6-hlorotieno[2,3-d]pirimidin-4-ilamino)piperidin-1-il)metil)-2-fluorobenzonitril
Klinički podaci
Identifikatori
ATC kod	nije dodeljen
PubChem	11502243
ChemSpider	9677045
Hemijski podaci
Formula	C19H17ClFN5S
Mol. masa	401,887 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C19H17ClFN5S/c20-17-8-15-18(23-11-24-19(15)27-17)25-14-3-5-26(6-4-14)10-12-1-2-16(21)13(7-12)9-22/h1-2,7-8,11,14H,3-6,10H2,(H,23,24,25) ; Key: IENZFHBNCRQMNP-UHFFFAOYSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

PRX-08066 je lek koji deluje kao potentan i selektivan antagonist na serotoninskom 5-HT_2B receptoru, sa afinitetom vezivanja (K_i) na 5-HT_2B od 3,4 nM, i visokom selektivnošću u odnosu na blisko srodne 5-HT_2A i 5-HT_2C receptore. PRX-08066 i drugi selektivni 5-HT_2B antagonisti se koriste za tretman plučne arterijske hipertenzije, nakon otkrića da potentni 5-HT_2B agonist norfenfluramin proizvodi plućnu arterijsku hipertenziju i naknadno oštećenje srčanih zalizaka. U životinjskim studijama, utvrđeno je da PRX-08066 redukuje nekoliko ključnih indikatora plućne arterijske hipertenzije i poboljšava srčani izlaz, sa sličnom efikasnošću u odnosu na ustaljene lekova za ta oboljenja, kao što su bosentan, sildenafil, beraprost o iloprost. ^[4] On se takođe istražuje za potencijalnu antikancernu primenu, usled njegove sposobnosti da inhibira aktivaciju fibroblasta.^[5]

Reference[uredi - уреди | uredi izvor]

↑ 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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003. 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. PMID 20331846. doi:10.1186/1758-2946-2-3. edit
↑ Porvasnik SL, Germain S, Embury J, Gannon KS, Jacques V, Murray J, Byrne BJ, Shacham S, Al-Mousily F (August 2010). "PRX-08066, a novel 5-hydroxytryptamine receptor 2B antagonist, reduces monocrotaline-induced pulmonary arterial hypertension and right ventricular hypertrophy in rats". The Journal of Pharmacology and Experimental Therapeutics 334 (2): 364–72. PMID 20430844. doi:10.1124/jpet.109.165001.
↑ Svejda B, Kidd M, Giovinazzo F, Eltawil K, Gustafsson BI, Pfragner R, Modlin IM (June 2010). "The 5-HT(2B) receptor plays a key regulatory role in both neuroendocrine tumor cell proliferation and the modulation of the fibroblast component of the neoplastic microenvironment". Cancer 116 (12): 2902–12. PMID 20564397. doi:10.1002/cncr.25049.

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	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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003. 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. PMID 20331846. doi:10.1186/1758-2946-2-3. edit

[pmid20430844-4] Porvasnik SL, Germain S, Embury J, Gannon KS, Jacques V, Murray J, Byrne BJ, Shacham S, Al-Mousily F (August 2010). "PRX-08066, a novel 5-hydroxytryptamine receptor 2B antagonist, reduces monocrotaline-induced pulmonary arterial hypertension and right ventricular hypertrophy in rats". The Journal of Pharmacology and Experimental Therapeutics 334 (2): 364–72. PMID 20430844. doi:10.1124/jpet.109.165001.

[pmid20564397-5] Svejda B, Kidd M, Giovinazzo F, Eltawil K, Gustafsson BI, Pfragner R, Modlin IM (June 2010). "The 5-HT(2B) receptor plays a key regulatory role in both neuroendocrine tumor cell proliferation and the modulation of the fibroblast component of the neoplastic microenvironment". Cancer 116 (12): 2902–12. PMID 20564397. doi:10.1002/cncr.25049.

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PRX-08066

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