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A novel series of [3.2.1] azabicyclic biaryl ethers as alpha3beta4 and alpha6/4beta4 nicotinic receptor agonists.
Lowe JA 3rd, DeNinno SL, Coe JW, Zhang L, Mente S, Hurst RS, Mather RJ, Ward KM, Shrikhande A, Rollema H, Johnson DE, Horner W, Gorczyca R, Tingley FD 3rd, Kozak R, Majchrzak MJ, Tritto T, Sadlier J, Shaffer CL, Ellerbrock B, Osgood SM, MacDougall MC, McDowell LL. Lowe JA 3rd, et al. Among authors: horner w. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4749-52. doi: 10.1016/j.bmcl.2010.06.142. Bioorg Med Chem Lett. 2010. PMID: 20663668
The 5-hydroxytryptamine4 receptor agonists prucalopride and PRX-03140 increase acetylcholine and histamine levels in the rat prefrontal cortex and the power of stimulated hippocampal θ oscillations.
Johnson DE, Drummond E, Grimwood S, Sawant-Basak A, Miller E, Tseng E, McDowell LL, Vanase-Frawley MA, Fisher KE, Rubitski DM, Stutzman-Engwall KJ, Nelson RT, Horner WE, Gorczyca RR, Hajos M, Siok CJ. Johnson DE, et al. J Pharmacol Exp Ther. 2012 Jun;341(3):681-91. doi: 10.1124/jpet.112.192351. Epub 2012 Mar 9. J Pharmacol Exp Ther. 2012. PMID: 22408061
Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia.
Dounay AB, Anderson M, Bechle BM, Campbell BM, Claffey MM, Evdokimov A, Evrard E, Fonseca KR, Gan X, Ghosh S, Hayward MM, Horner W, Kim JY, McAllister LA, Pandit J, Paradis V, Parikh VD, Reese MR, Rong S, Salafia MA, Schuyten K, Strick CA, Tuttle JB, Valentine J, Wang H, Zawadzke LE, Verhoest PR. Dounay AB, et al. Among authors: horner w. ACS Med Chem Lett. 2012 Jan 25;3(3):187-92. doi: 10.1021/ml200204m. eCollection 2012 Mar 8. ACS Med Chem Lett. 2012. PMID: 24900455 Free PMC article.
Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions.
Tuttle JB, Anderson M, Bechle BM, Campbell BM, Chang C, Dounay AB, Evrard E, Fonseca KR, Gan X, Ghosh S, Horner W, James LC, Kim JY, McAllister LA, Pandit J, Parikh VD, Rago BJ, Salafia MA, Strick CA, Zawadzke LE, Verhoest PR. Tuttle JB, et al. Among authors: horner w. ACS Med Chem Lett. 2012 Oct 24;4(1):37-40. doi: 10.1021/ml300237v. eCollection 2013 Jan 10. ACS Med Chem Lett. 2012. PMID: 24900560 Free PMC article.
Reduction of brain kynurenic acid improves cognitive function.
Kozak R, Campbell BM, Strick CA, Horner W, Hoffmann WE, Kiss T, Chapin DS, McGinnis D, Abbott AL, Roberts BM, Fonseca K, Guanowsky V, Young DA, Seymour PA, Dounay A, Hajos M, Williams GV, Castner SA. Kozak R, et al. Among authors: horner w. J Neurosci. 2014 Aug 6;34(32):10592-602. doi: 10.1523/JNEUROSCI.1107-14.2014. J Neurosci. 2014. PMID: 25100593 Free PMC article.
Quantitative Translational Analysis of Brain Kynurenic Acid Modulation via Irreversible Kynurenine Aminotransferase II Inhibition.
Chang C, Fonseca KR, Li C, Horner W, Zawadzke LE, Salafia MA, Welch KA, Strick CA, Campbell BM, Gernhardt SS, Rong H, Sawant-Basak A, Liras J, Dounay A, Tuttle JB, Verhoest P, Maurer TS. Chang C, et al. Among authors: horner w. Mol Pharmacol. 2018 Aug;94(2):823-833. doi: 10.1124/mol.118.111625. Epub 2018 May 31. Mol Pharmacol. 2018. PMID: 29853495
116 results