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Page 1
Solubilized phenyl-pyrazole ureas as potent, selective 5-HT(2A) inverse-agonists and their application as antiplatelet agents.
Dosa PI, Strah-Pleynet S, Jayakumar H, Casper M, Decaire M, Xiong Y, Lehmann J, Choi K, Elwell K, Wong A, Webb RR, Adams JW, Ramirez J, Richman JG, Thomsen W, Semple G, Teegarden BR. Dosa PI, et al. Among authors: teegarden br. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5486-9. doi: 10.1016/j.bmcl.2009.07.073. Epub 2009 Jul 18. Bioorg Med Chem Lett. 2009. PMID: 19665894
Discovery of 1-[3-(4-bromo-2-methyl-2h-pyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea (nelotanserin) and related 5-hydroxytryptamine2A inverse agonists for the treatment of insomnia.
Teegarden BR, Li H, Jayakumar H, Strah-Pleynet S, Dosa PI, Selaya SD, Kato N, Elwell KH, Davidson J, Cheng K, Saldana H, Frazer JM, Whelan K, Foster J, Espitia S, Webb RR, Beeley NR, Thomsen W, Morairty SR, Kilduff TS, Al-Shamma HA. Teegarden BR, et al. J Med Chem. 2010 Mar 11;53(5):1923-36. doi: 10.1021/jm9007328. J Med Chem. 2010. PMID: 20143782
Discovery and structure-activity relationship of 3-methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): a highly selective 5-hydroxytryptamine2A receptor inverse agonist for the treatment of arterial thrombosis.
Xiong Y, Teegarden BR, Choi JS, Strah-Pleynet S, Decaire M, Jayakumar H, Dosa PI, Casper MD, Pham L, Feichtinger K, Ullman B, Adams J, Yuskin D, Frazer J, Morgan M, Sadeque A, Chen W, Webb RR, Connolly DT, Semple G, Al-Shamma H. Xiong Y, et al. Among authors: teegarden br. J Med Chem. 2010 Jun 10;53(11):4412-21. doi: 10.1021/jm100044a. J Med Chem. 2010. PMID: 20455563
Synthesis and in vivo evaluation of phenethylpiperazine amides: selective 5-hydroxytryptamine(2A) receptor antagonists for the treatment of insomnia.
Xiong Y, Ullman B, Choi JS, Cherrier M, Strah-Pleynet S, Decaire M, Dosa PI, Feichtinger K, Teegarden BR, Frazer JM, Yoon WH, Shan Y, Whelan K, Hauser EK, Grottick AJ, Semple G, Al-Shamma H. Xiong Y, et al. Among authors: teegarden br. J Med Chem. 2010 Aug 12;53(15):5696-706. doi: 10.1021/jm100479q. J Med Chem. 2010. PMID: 20684606
APD791, 3-methoxy-n-(3-(1-methyl-1h-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide, a novel 5-hydroxytryptamine 2A receptor antagonist: pharmacological profile, pharmacokinetics, platelet activity and vascular biology.
Adams JW, Ramirez J, Shi Y, Thomsen W, Frazer J, Morgan M, Edwards JE, Chen W, Teegarden BR, Xiong Y, Al-Shamma H, Behan DP, Connolly DT. Adams JW, et al. Among authors: teegarden br. J Pharmacol Exp Ther. 2009 Oct;331(1):96-103. doi: 10.1124/jpet.109.153189. Epub 2009 Jul 23. J Pharmacol Exp Ther. 2009. PMID: 19628629
Anti-thrombotic and vascular effects of AR246686, a novel 5-HT2A receptor antagonist.
Adams JW, Ramirez J, Ortuno D, Shi Y, Thomsen W, Richman JG, Morgan M, Dosa P, Teegarden BR, Al-Shamma H, Behan DP, Connolly DT. Adams JW, et al. Among authors: teegarden br. Eur J Pharmacol. 2008 May 31;586(1-3):234-43. doi: 10.1016/j.ejphar.2007.11.056. Epub 2007 Dec 3. Eur J Pharmacol. 2008. PMID: 18358471
Synthesis and SAR of N-benzoyl-L-biphenylalanine derivatives: discovery of TR-14035, a dual alpha(4)beta(7)/alpha(4)beta(1) integrin antagonist.
Sircar I, Gudmundsson KS, Martin R, Liang J, Nomura S, Jayakumar H, Teegarden BR, Nowlin DM, Cardarelli PM, Mah JR, Connell S, Griffith RC, Lazarides E. Sircar I, et al. Among authors: teegarden br. Bioorg Med Chem. 2002 Jun;10(6):2051-66. doi: 10.1016/s0968-0896(02)00021-4. Bioorg Med Chem. 2002. PMID: 11937364