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GSK1562590, a slowly dissociating urotensin-II receptor antagonist, exhibits prolonged pharmacodynamic activity ex vivo.
Behm DJ, Aiyar NV, Olzinski AR, McAtee JJ, Hilfiker MA, Dodson JW, Dowdell SE, Wang GZ, Goodman KB, Sehon CA, Harpel MR, Willette RN, Neeb MJ, Leach CA, Douglas SA. Behm DJ, et al. Among authors: aiyar nv. Br J Pharmacol. 2010 Sep;161(1):207-28. doi: 10.1111/j.1476-5381.2010.00889.x. Br J Pharmacol. 2010. PMID: 20718751 Free PMC article.
Nonpeptidic urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375.
Douglas SA, Behm DJ, Aiyar NV, Naselsky D, Disa J, Brooks DP, Ohlstein EH, Gleason JG, Sarau HM, Foley JJ, Buckley PT, Schmidt DB, Wixted WE, Widdowson K, Riley G, Jin J, Gallagher TF, Schmidt SJ, Ridgers L, Christmann LT, Keenan RM, Knight SD, Dhanak D. Douglas SA, et al. Among authors: aiyar nv. Br J Pharmacol. 2005 Jul;145(5):620-35. doi: 10.1038/sj.bjp.0706229. Br J Pharmacol. 2005. PMID: 15852036 Free PMC article.
The peptidic urotensin-II receptor ligand GSK248451 possesses less intrinsic activity than the low-efficacy partial agonists SB-710411 and urantide in native mammalian tissues and recombinant cell systems.
Behm DJ, Stankus G, Doe CP, Willette RN, Sarau HM, Foley JJ, Schmidt DB, Nuthulaganti P, Fornwald JA, Ames RS, Lambert DG, Calo' G, Camarda V, Aiyar NV, Douglas SA. Behm DJ, et al. Among authors: aiyar nv. Br J Pharmacol. 2006 May;148(2):173-90. doi: 10.1038/sj.bjp.0706716. Br J Pharmacol. 2006. PMID: 16547525 Free PMC article.
Development of potent and selective small-molecule human Urotensin-II antagonists.
McAtee JJ, Dodson JW, Dowdell SE, Girard GR, Goodman KB, Hilfiker MA, Sehon CA, Sha D, Wang GZ, Wang N, Viet AQ, Zhang D, Aiyar NV, Behm DJ, Carballo LH, Evans CA, Fries HE, Nagilla R, Roethke TJ, Xu X, Yuan CC, Douglas SA, Neeb MJ. McAtee JJ, et al. Among authors: aiyar nv. Bioorg Med Chem Lett. 2008 Jun 15;18(12):3500-3. doi: 10.1016/j.bmcl.2008.05.027. Epub 2008 May 10. Bioorg Med Chem Lett. 2008. PMID: 18502123
Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.
McAtee JJ, Dodson JW, Dowdell SE, Erhard K, Girard GR, Goodman KB, Hilfiker MA, Jin J, Sehon CA, Sha D, Shi D, Wang F, Wang GZ, Wang N, Wang Y, Viet AQ, Yuan CC, Zhang D, Aiyar NV, Behm DJ, Carballo LH, Evans CA, Fries HE, Nagilla R, Roethke TJ, Xu X, Douglas SA, Neeb MJ. McAtee JJ, et al. Among authors: aiyar nv. Bioorg Med Chem Lett. 2008 Jul 1;18(13):3716-9. doi: 10.1016/j.bmcl.2008.05.058. Epub 2008 May 20. Bioorg Med Chem Lett. 2008. PMID: 18524591
Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues.
Behm DJ, McAtee JJ, Dodson JW, Neeb MJ, Fries HE, Evans CA, Hernandez RR, Hoffman KD, Harrison SM, Lai JM, Wu C, Aiyar NV, Ohlstein EH, Douglas SA. Behm DJ, et al. Among authors: aiyar nv. Br J Pharmacol. 2008 Oct;155(3):374-86. doi: 10.1038/bjp.2008.266. Epub 2008 Jun 30. Br J Pharmacol. 2008. PMID: 18587423 Free PMC article.
117 results