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151 results

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Page 1
Development of novel azabenzofuran TRPA1 antagonists as in vivo tools.
Copeland KW, Boezio AA, Cheung E, Lee J, Olivieri P, Schenkel LB, Wan Q, Wang W, Wells MC, Youngblood B, Gavva NR, Lehto SG, Geuns-Meyer S. Copeland KW, et al. Among authors: youngblood b. Bioorg Med Chem Lett. 2014 Aug 1;24(15):3464-8. doi: 10.1016/j.bmcl.2014.05.069. Epub 2014 Jun 6. Bioorg Med Chem Lett. 2014. PMID: 24953819
Optimization of potency and pharmacokinetic properties of tetrahydroisoquinoline transient receptor potential melastatin 8 (TRPM8) antagonists.
Horne DB, Tamayo NA, Bartberger MD, Bo Y, Clarine J, Davis CD, Gore VK, Kaller MR, Lehto SG, Ma VV, Nishimura N, Nguyen TT, Tang P, Wang W, Youngblood BD, Zhang M, Gavva NR, Monenschein H, Norman MH. Horne DB, et al. Among authors: youngblood bd. J Med Chem. 2014 Apr 10;57(7):2989-3004. doi: 10.1021/jm401955h. Epub 2014 Mar 19. J Med Chem. 2014. PMID: 24597733
AMG2850, a potent and selective TRPM8 antagonist, is not effective in rat models of inflammatory mechanical hypersensitivity and neuropathic tactile allodynia.
Lehto SG, Weyer AD, Zhang M, Youngblood BD, Wang J, Wang W, Kerstein PC, Davis C, Wild KD, Stucky CL, Gavva NR. Lehto SG, et al. Naunyn Schmiedebergs Arch Pharmacol. 2015 Apr;388(4):465-76. doi: 10.1007/s00210-015-1090-9. Epub 2015 Feb 10. Naunyn Schmiedebergs Arch Pharmacol. 2015. PMID: 25662185 Free PMC article.
Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity.
Schenkel LB, Olivieri PR, Boezio AA, Deak HL, Emkey R, Graceffa RF, Gunaydin H, Guzman-Perez A, Lee JH, Teffera Y, Wang W, Youngblood BD, Yu VL, Zhang M, Gavva NR, Lehto SG, Geuns-Meyer S. Schenkel LB, et al. Among authors: youngblood bd. J Med Chem. 2016 Mar 24;59(6):2794-809. doi: 10.1021/acs.jmedchem.6b00039. Epub 2016 Mar 4. J Med Chem. 2016. PMID: 26942860
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement.
Marx IE, Dineen TA, Able J, Bode C, Bregman H, Chu-Moyer M, DiMauro EF, Du B, Foti RS, Fremeau RT Jr, Gao H, Gunaydin H, Hall BE, Huang L, Kornecook T, Kreiman CR, La DS, Ligutti J, Lin MJ, Liu D, McDermott JS, Moyer BD, Peterson EA, Roberts JT, Rose P, Wang J, Youngblood BD, Yu V, Weiss MM. Marx IE, et al. Among authors: youngblood bd. ACS Med Chem Lett. 2016 Sep 21;7(12):1062-1067. doi: 10.1021/acsmedchemlett.6b00243. eCollection 2016 Dec 8. ACS Med Chem Lett. 2016. PMID: 27994738 Free PMC article.
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities.
Weiss MM, Dineen TA, Marx IE, Altmann S, Boezio A, Bregman H, Chu-Moyer M, DiMauro EF, Feric Bojic E, Foti RS, Gao H, Graceffa R, Gunaydin H, Guzman-Perez A, Huang H, Huang L, Jarosh M, Kornecook T, Kreiman CR, Ligutti J, La DS, Lin MJ, Liu D, Moyer BD, Nguyen HN, Peterson EA, Rose PE, Taborn K, Youngblood BD, Yu V, Fremeau RT Jr. Weiss MM, et al. J Med Chem. 2017 Jul 27;60(14):5969-5989. doi: 10.1021/acs.jmedchem.6b01851. Epub 2017 Apr 20. J Med Chem. 2017. PMID: 28287723
Discovery of TRPM8 Antagonist ( S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine.
Horne DB, Biswas K, Brown J, Bartberger MD, Clarine J, Davis CD, Gore VK, Harried S, Horner M, Kaller MR, Lehto SG, Liu Q, Ma VV, Monenschein H, Nguyen TT, Yuan CC, Youngblood BD, Zhang M, Zhong W, Allen JR, Chen JJ, Gavva NR. Horne DB, et al. Among authors: youngblood bd. J Med Chem. 2018 Sep 27;61(18):8186-8201. doi: 10.1021/acs.jmedchem.8b00518. Epub 2018 Sep 10. J Med Chem. 2018. PMID: 30148953
Rat NaV1.7 loss-of-function genetic model: Deficient nociceptive and neuropathic pain behavior with retained olfactory function and intra-epidermal nerve fibers.
Grubinska B, Chen L, Alsaloum M, Rampal N, Matson DJ, Yang C, Taborn K, Zhang M, Youngblood B, Liu D, Galbreath E, Allred S, Lepherd M, Ferrando R, Kornecook TJ, Lehto SG, Waxman SG, Moyer BD, Dib-Hajj S, Gingras J. Grubinska B, et al. Among authors: youngblood b. Mol Pain. 2019 Jan-Dec;15:1744806919881846. doi: 10.1177/1744806919881846. Mol Pain. 2019. PMID: 31550995 Free PMC article.
151 results