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Discovery and Optimization of Potent and CNS Penetrant M5-Preferring Positive Allosteric Modulators Derived from a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold.
Bender AM, Cho HP, Nance KD, Lingenfelter KS, Luscombe VB, Gentry PR, Voigtritter K, Berizzi AE, Sexton PM, Langmead CJ, Christopoulos A, Locuson CW, Bridges TM, Chang S, O'Neill JC, Zhan X, Niswender CM, Jones CK, Conn PJ, Lindsley CW. Bender AM, et al. Among authors: zhan x. ACS Chem Neurosci. 2018 Jul 18;9(7):1572-1581. doi: 10.1021/acschemneuro.8b00126. Epub 2018 Apr 26. ACS Chem Neurosci. 2018. PMID: 29678111 Free PMC article.
Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazines as novel, CNS penetrant pan-muscarinic antagonists.
Bender AM, Weiner RL, Luscombe VB, Ajmera S, Cho HP, Chang S, Zhan X, Rodriguez AL, Niswender CM, Engers DW, Bridges TM, Conn PJ, Lindsley CW. Bender AM, et al. Among authors: zhan x. Bioorg Med Chem Lett. 2017 Aug 1;27(15):3576-3581. doi: 10.1016/j.bmcl.2017.05.042. Epub 2017 May 15. Bioorg Med Chem Lett. 2017. PMID: 28633897 Free PMC article.
Discovery of a novel, CNS penetrant M4 PAM chemotype based on a 6-fluoro-4-(piperidin-1-yl)quinoline-3-carbonitrile core.
Bewley BR, Spearing PK, Weiner RL, Luscombe VB, Zhan X, Chang S, Cho HP, Rodriguez AL, Niswender CM, Conn PJ, Bridges TM, Engers DW, Lindsley CW. Bewley BR, et al. Among authors: zhan x. Bioorg Med Chem Lett. 2017 Sep 15;27(18):4274-4279. doi: 10.1016/j.bmcl.2017.08.043. Epub 2017 Aug 20. Bioorg Med Chem Lett. 2017. PMID: 28866269 Free PMC article.
Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping.
Long MF, Engers JL, Chang S, Zhan X, Weiner RL, Luscombe VB, Rodriguez AL, Cho HP, Niswender CM, Bridges TM, Conn PJ, Engers DW, Lindsley CW. Long MF, et al. Among authors: zhan x. Bioorg Med Chem Lett. 2017 Nov 15;27(22):4999-5001. doi: 10.1016/j.bmcl.2017.10.016. Epub 2017 Oct 9. Bioorg Med Chem Lett. 2017. PMID: 29037946 Free PMC article.
Partial mGlu₅ Negative Allosteric Modulators Attenuate Cocaine-Mediated Behaviors and Lack Psychotomimetic-Like Effects.
Gould RW, Amato RJ, Bubser M, Joffe ME, Nedelcovych MT, Thompson AD, Nickols HH, Yuh JP, Zhan X, Felts AS, Rodriguez AL, Morrison RD, Byers FW, Rook JM, Daniels JS, Niswender CM, Conn PJ, Emmitte KA, Lindsley CW, Jones CK. Gould RW, et al. Among authors: zhan x. Neuropsychopharmacology. 2016 Mar;41(4):1166-78. doi: 10.1038/npp.2015.265. Epub 2015 Aug 28. Neuropsychopharmacology. 2016. PMID: 26315507 Free PMC article.
3,797 results