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Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.
van Niel MB, Collins I, Beer MS, Broughton HB, Cheng SK, Goodacre SC, Heald A, Locker KL, MacLeod AM, Morrison D, Moyes CR, O'Connor D, Pike A, Rowley M, Russell MG, Sohal B, Stanton JA, Thomas S, Verrier H, Watt AP, Castro JL. van Niel MB, et al. Among authors: thomas s. J Med Chem. 1999 Jun 17;42(12):2087-104. doi: 10.1021/jm981133m. J Med Chem. 1999. PMID: 10377215
Identification of metabolites of a substance P (neurokinin 1 receptor) antagonist in rat hepatocytes and rat plasma.
Hop CE, Wang Y, Kumar S, Elipe MV, Raab CE, Dean DC, Poon GK, Keohane CA, Strauss J, Chiu SH, Curtis N, Elliott J, Gerhard U, Locker K, Morrison D, Mortishire-Smith R, Thomas S, Watt AP, Evans DC. Hop CE, et al. Among authors: thomas s. Drug Metab Dispos. 2002 Aug;30(8):937-43. doi: 10.1124/dmd.30.8.937. Drug Metab Dispos. 2002. PMID: 12124313
Accelerated metabolite identification by "extraction-NMR".
Gerhard U, Thomas S, Mortishire-Smith R. Gerhard U, et al. Among authors: thomas s. J Pharm Biomed Anal. 2003 Jul 14;32(3):531-8. doi: 10.1016/s0731-7085(03)00218-8. J Pharm Biomed Anal. 2003. PMID: 14565558
Metabolite identification in drug discovery.
Watt AP, Mortishire-Smith RJ, Gerhard U, Thomas SR. Watt AP, et al. Curr Opin Drug Discov Devel. 2003 Jan;6(1):57-65. Curr Opin Drug Discov Devel. 2003. PMID: 12613277 Review.
A new pyridazine series of GABAA alpha5 ligands.
van Niel MB, Wilson K, Adkins CH, Atack JR, Castro JL, Clarke DE, Fletcher S, Gerhard U, Mackey MM, Malpas S, Maubach K, Newman R, O'Connor D, Pillai GV, Simpson PB, Thomas SR, MacLeod AM. van Niel MB, et al. Among authors: thomas sr. J Med Chem. 2005 Sep 22;48(19):6004-11. doi: 10.1021/jm050249x. J Med Chem. 2005. PMID: 16162003
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