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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
Aminoalkoxybenzyl pyrrolidines as novel human urotensin-II receptor antagonists.
Jin J, Dhanak D, Knight SD, Widdowson K, Aiyar N, Naselsky D, Sarau HM, Foley JJ, Schmidt DB, Bennett CD, Wang B, Warren GL, Moore ML, Keenan RM, Rivero RA, Douglas SA. Jin J, et al. Bioorg Med Chem Lett. 2005 Jul 1;15(13):3229-32. doi: 10.1016/j.bmcl.2005.04.074. Bioorg Med Chem Lett. 2005. PMID: 15936190
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
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.
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