PRX-08066 is a drug discovered and developed by Predix (later Epix) Pharmaceuticals [Dale S. Dhanoa et al. Patent US 7,030,240 B2], which acts as a potent and selective antagonist at the serotonin5-HT2Breceptor, with a 5-HT2Bbinding affinity (Ki) of 3.4nM, and high selectivity over the closely related 5-HT2A and 5-HT2C receptors and other receptor targets. PRX-08066 and other selective 5-HT2B antagonists are being researched for the treatment of pulmonary arterial hypertension, following the discovery that the potent 5-HT2B agonist norfenfluramine produces pulmonary arterial hypertension and subsequent heart valve damage. In animal studies, PRX-08066 has been found to reduce several key indicators of pulmonary arterial hypertension and improved cardiac output, with similar efficacy to established drugs for this condition such as bosentan, sildenafil, beraprost and iloprost. [1] It is also being researched for potential anti-cancer applications, due to its ability to inhibit fibroblast activation.[2]
^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. doi:10.1124/jpet.109.165001. PMID 20430844.
^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. doi:10.1002/cncr.25049. PMID 20564397.
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08066, drug, discovered, developed, predix, later, epix, pharmaceuticals, dale, dhanoa, patent, which, acts, potent, selective, antagonist, serotonin, ht2b, receptor, with, ht2b, binding, affinity, high, selectivity, over, closely, related, ht2a, ht2c, recepto. PRX 08066 is a drug discovered and developed by Predix later Epix Pharmaceuticals Dale S Dhanoa et al Patent US 7 030 240 B2 which acts as a potent and selective antagonist at the serotonin 5 HT2B receptor with a 5 HT2B binding affinity Ki of 3 4nM and high selectivity over the closely related 5 HT2A and 5 HT2C receptors and other receptor targets PRX 08066 and other selective 5 HT2B antagonists are being researched for the treatment of pulmonary arterial hypertension following the discovery that the potent 5 HT2B agonist norfenfluramine produces pulmonary arterial hypertension and subsequent heart valve damage In animal studies PRX 08066 has been found to reduce several key indicators of pulmonary arterial hypertension and improved cardiac output with similar efficacy to established drugs for this condition such as bosentan sildenafil beraprost and iloprost 1 It is also being researched for potential anti cancer applications due to its ability to inhibit fibroblast activation 2 PRX 08066IdentifiersIUPAC name 5 4 6 chlorothieno 2 3 d pyrimidin 4 ylamino piperidin 1 yl methyl 2 fluorobenzonitrileCAS Number866206 54 4 YPubChem CID11502243ChemSpider9677045UNII82SK298EBUCompTox Dashboard EPA DTXSID60235710Chemical and physical dataFormulaC 19H 17Cl F N 5SMolar mass401 89 g mol 13D model JSmol Interactive imageSMILES s3c2ncnc c2cc3Cl NC4CCN CC4 Cc ccc1F cc1C NReferences 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 doi 10 1124 jpet 109 165001 PMID 20430844 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 doi 10 1002 cncr 25049 PMID 20564397 This drug article relating to the nervous system is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title PRX 08066 amp oldid 1170068636, wikipedia, wiki, book, books, library,
