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Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 4: SAR reveals positive cooperativity across multiple mGlu receptor subtypes leading to subtype unselective PAMs.
Davis DC, Bungard JD, Chang S, Rodriguez AL, Blobaum AL, Boutaud O, Melancon BJ, Niswender CM, Jeffrey Conn P, Lindsley CW. Davis DC, et al. Among authors: niswender cm. Bioorg Med Chem Lett. 2021 Jan 15;32:127724. doi: 10.1016/j.bmcl.2020.127724. Epub 2020 Nov 27. Bioorg Med Chem Lett. 2021. PMID: 33253881
An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission.
Shirey JK, Xiang Z, Orton D, Brady AE, Johnson KA, Williams R, Ayala JE, Rodriguez AL, Wess J, Weaver D, Niswender CM, Conn PJ. Shirey JK, et al. Among authors: niswender cm. Nat Chem Biol. 2008 Jan;4(1):42-50. doi: 10.1038/nchembio.2007.55. Epub 2007 Dec 2. Nat Chem Biol. 2008. PMID: 18059262
Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4.
Niswender CM, Johnson KA, Weaver CD, Jones CK, Xiang Z, Luo Q, Rodriguez AL, Marlo JE, de Paulis T, Thompson AD, Days EL, Nalywajko T, Austin CA, Williams MB, Ayala JE, Williams R, Lindsley CW, Conn PJ. Niswender CM, et al. Mol Pharmacol. 2008 Nov;74(5):1345-58. doi: 10.1124/mol.108.049551. Epub 2008 Jul 29. Mol Pharmacol. 2008. PMID: 18664603 Free PMC article.
Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity.
Marlo JE, Niswender CM, Days EL, Bridges TM, Xiang Y, Rodriguez AL, Shirey JK, Brady AE, Nalywajko T, Luo Q, Austin CA, Williams MB, Kim K, Williams R, Orton D, Brown HA, Lindsley CW, Weaver CD, Conn PJ. Marlo JE, et al. Among authors: niswender cm. Mol Pharmacol. 2009 Mar;75(3):577-88. doi: 10.1124/mol.108.052886. Epub 2008 Dec 1. Mol Pharmacol. 2009. PMID: 19047481 Free PMC article.
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. Among authors: niswender cm. 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 of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins.
Bridges TM, Marlo JE, Niswender CM, Jones CK, Jadhav SB, Gentry PR, Plumley HC, Weaver CD, Conn PJ, Lindsley CW. Bridges TM, et al. Among authors: niswender cm. J Med Chem. 2009 Jun 11;52(11):3445-8. doi: 10.1021/jm900286j. J Med Chem. 2009. PMID: 19438238 Free PMC article.
258 results