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Discovery of a potent, orally bioavailable beta(3) adrenergic receptor agonist, (R)-N-[4-[2-[[2-hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4 -[4-(trifluoromethyl)phenyl]thiazol-2-yl]benzenesulfonamide.
Mathvink RJ, Tolman JS, Chitty D, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Tota L, Wyvratt MJ, Fisher MH, Weber AE. Mathvink RJ, et al. J Med Chem. 2000 Oct 19;43(21):3832-6. doi: 10.1021/jm000286i. J Med Chem. 2000. PMID: 11052788
The pharmacokinetics of a thiazole benzenesulfonamide beta 3-adrenergic receptor agonist and its analogs in rats, dogs, and monkeys: improving oral bioavailability.
Stearns RA, Miller RR, Tang W, Kwei GY, Tang FS, Mathvink RJ, Naylor EM, Chitty D, Colandrea VJ, Weber AE, Colletti AE, Strauss JR, Keohane CA, Feeney WP, Iliff SA, Chiu SH. Stearns RA, et al. Among authors: mathvink rj. Drug Metab Dispos. 2002 Jul;30(7):771-7. doi: 10.1124/dmd.30.7.771. Drug Metab Dispos. 2002. PMID: 12065435
Metabolism of a thiazole benzenesulfonamide derivative, a potent and elective agonist of the human beta3-adrenergic receptor, in rats: identification of a novel isethionic acid conjugate.
Tang W, Stearns RA, Miller RR, Ngui JS, Mathvink RJ, Weber AE, Kwei GY, Strauss JR, Keohane CA, Doss GA, Chiu SH, Baillie TA. Tang W, et al. Among authors: mathvink rj. Drug Metab Dispos. 2002 Jul;30(7):778-87. doi: 10.1124/dmd.30.7.778. Drug Metab Dispos. 2002. PMID: 12065436
A selective human beta3 adrenergic receptor agonist increases metabolic rate in rhesus monkeys.
Fisher MH, Amend AM, Bach TJ, Barker JM, Brady EJ, Candelore MR, Carroll D, Cascieri MA, Chiu SH, Deng L, Forrest MJ, Hegarty-Friscino B, Guan XM, Hom GJ, Hutchins JE, Kelly LJ, Mathvink RJ, Metzger JM, Miller RR, Ok HO, Parmee ER, Saperstein R, Strader CD, Stearns RA, MacIntyre DE, et al. Fisher MH, et al. Among authors: mathvink rj. J Clin Invest. 1998 Jun 1;101(11):2387-93. doi: 10.1172/JCI2496. J Clin Invest. 1998. PMID: 9616210 Free PMC article.
3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties.
Weber AE, Ok HO, Alvaro RF, Candelore MR, Cascieri MA, Chiu SH, Deng L, Forrest MJ, Hom GJ, Hutchins JE, Kao J, MacIntyre DE, Mathvink RJ, McLoughlin D, Miller RR, Newbold RC, Olah TV, Parmee ER, Perkins L, Stearns RA, Strader CD, Szumiloski J, Tang YS, Tota L, Fisher MH, et al. Weber AE, et al. Among authors: mathvink rj. Bioorg Med Chem Lett. 1998 Aug 18;8(16):2111-6. doi: 10.1016/s0960-894x(98)00381-3. Bioorg Med Chem Lett. 1998. PMID: 9873496
15 results