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64 results

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Page 1
Discovery and development of a potent and highly selective small molecule muscarinic acetylcholine receptor subtype I (mAChR 1 or M1) antagonist in vitro and in vivo probe.
Weaver CD, Sheffler DJ, Lewis LM, Bridges TM, Williams R, Nalywajko NT, Kennedy JP, Mulder MM, Jadhav S, Aldrich LA, Jones CK, Marlo JE, Niswender CM, Mock MM, Zheng F, Conn PJ, Lindsley CW. Weaver CD, et al. Among authors: sheffler dj. Curr Top Med Chem. 2009;9(13):1217-26. doi: 10.2174/156802609789753635. Curr Top Med Chem. 2009. PMID: 19807667 Free PMC article. Review.
A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning.
Sheffler DJ, Williams R, Bridges TM, Xiang Z, Kane AS, Byun NE, Jadhav S, Mock MM, Zheng F, Lewis LM, Jones CK, Niswender CM, Weaver CD, Lindsley CW, Conn PJ. Sheffler DJ, et al. Mol Pharmacol. 2009 Aug;76(2):356-68. doi: 10.1124/mol.109.056531. Epub 2009 Apr 30. Mol Pharmacol. 2009. PMID: 19407080 Free PMC article.
Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe.
Reid PR, Bridges TM, Sheffler DJ, Cho HP, Lewis LM, Days E, Daniels JS, Jones CK, Niswender CM, Weaver CD, Conn PJ, Lindsley CW, Wood MR. Reid PR, et al. Among authors: sheffler dj. Bioorg Med Chem Lett. 2011 May 1;21(9):2697-701. doi: 10.1016/j.bmcl.2010.12.015. Epub 2010 Dec 9. Bioorg Med Chem Lett. 2011. PMID: 21194936 Free PMC article.
Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.
Lebois EP, Digby GJ, Sheffler DJ, Melancon BJ, Tarr JC, Cho HP, Miller NR, Morrison R, Bridges TM, Xiang Z, Daniels JS, Wood MR, Conn PJ, Lindsley CW. Lebois EP, et al. Among authors: sheffler dj. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6451-5. doi: 10.1016/j.bmcl.2011.08.084. Epub 2011 Aug 24. Bioorg Med Chem Lett. 2011. PMID: 21930376 Free PMC article.
Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012.
Melancon BJ, Lamers AP, Bridges TM, Sulikowski GA, Utley TJ, Sheffler DJ, Noetzel MJ, Morrison RD, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Wood MR. Melancon BJ, et al. Among authors: sheffler dj. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1044-8. doi: 10.1016/j.bmcl.2011.11.110. Epub 2011 Dec 6. Bioorg Med Chem Lett. 2012. PMID: 22197142 Free PMC article.
Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor.
Melancon BJ, Gogliotti RD, Tarr JC, Saleh SA, Chauder BA, Lebois EP, Cho HP, Utley TJ, Sheffler DJ, Bridges TM, Morrison RD, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Wood MR. Melancon BJ, et al. Among authors: sheffler dj. Bioorg Med Chem Lett. 2012 May 15;22(10):3467-72. doi: 10.1016/j.bmcl.2012.03.088. Epub 2012 Mar 29. Bioorg Med Chem Lett. 2012. PMID: 22507963 Free PMC article.
Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.
Sheffler DJ, Wenthur CJ, Bruner JA, Carrington SJ, Vinson PN, Gogi KK, Blobaum AL, Morrison RD, Vamos M, Cosford ND, Stauffer SR, Daniels JS, Niswender CM, Conn PJ, Lindsley CW. Sheffler DJ, et al. Bioorg Med Chem Lett. 2012 Jun 15;22(12):3921-5. doi: 10.1016/j.bmcl.2012.04.112. Epub 2012 Apr 30. Bioorg Med Chem Lett. 2012. PMID: 22607673 Free PMC article.
Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor.
Salovich JM, Vinson PN, Sheffler DJ, Lamsal A, Utley TJ, Blobaum AL, Bridges TM, Le U, Jones CK, Wood MR, Daniels JS, Conn PJ, Niswender CM, Lindsley CW, Hopkins CR. Salovich JM, et al. Among authors: sheffler dj. Bioorg Med Chem Lett. 2012 Aug 1;22(15):5084-8. doi: 10.1016/j.bmcl.2012.05.109. Epub 2012 Jun 6. Bioorg Med Chem Lett. 2012. PMID: 22738637 Free PMC article.
Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012.
Melancon BJ, Utley TJ, Sevel C, Mattmann ME, Cheung YY, Bridges TM, Morrison RD, Sheffler DJ, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Wood MR. Melancon BJ, et al. Among authors: sheffler dj. Bioorg Med Chem Lett. 2012 Aug 1;22(15):5035-40. doi: 10.1016/j.bmcl.2012.06.018. Epub 2012 Jun 15. Bioorg Med Chem Lett. 2012. PMID: 22749871 Free PMC article.
Synthesis and biological characterization of a series of novel diaryl amide M₁ antagonists.
Poslusney MS, Sevel C, Utley TJ, Bridges TM, Morrison RD, Kett NR, Sheffler DJ, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Wood MR. Poslusney MS, et al. Among authors: sheffler dj. Bioorg Med Chem Lett. 2012 Nov 15;22(22):6923-8. doi: 10.1016/j.bmcl.2012.09.011. Epub 2012 Sep 23. Bioorg Med Chem Lett. 2012. PMID: 23062550 Free PMC article.
64 results