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Page 1
Discovery of 4-(5-Membered)Heteroarylether-6-methylpicolinamide Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5.
Childress ES, Capstick RA, Crocker KE, Ledyard ML, Bender AM, Maurer MA, Billard NB, Cho HP, Rodriguez AL, Niswender CM, Peng W, Rook JM, Chang S, Blobaum AL, Boutaud O, Thompson Gray A, Jones CK, Conn PJ, Felts AS, Lindsley CW, Temple KJ. Childress ES, et al. Among authors: rodriguez al. ACS Med Chem Lett. 2024 Nov 18;15(12):2210-2219. doi: 10.1021/acsmedchemlett.4c00481. eCollection 2024 Dec 12. ACS Med Chem Lett. 2024. PMID: 39691522 Free PMC article.
Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines.
Sharma S, Kedrowski J, Rook JM, Smith RL, Jones CK, Rodriguez AL, Conn PJ, Lindsley CW. Sharma S, et al. Among authors: rodriguez al. J Med Chem. 2009 Jul 23;52(14):4103-6. doi: 10.1021/jm900654c. J Med Chem. 2009. PMID: 19537763 Free PMC article.
Substituted 1-Phenyl-3-(pyridin-2-yl)urea negative allosteric modulators of mGlu5: discovery of a new tool compound VU0463841 with activity in rat models of cocaine addiction.
Amato RJ, Felts AS, Rodriguez AL, Venable DF, Morrison RD, Byers FW, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Jones CK, Emmitte KA. Amato RJ, et al. Among authors: rodriguez al. ACS Chem Neurosci. 2013 Aug 21;4(8):1217-28. doi: 10.1021/cn400070k. Epub 2013 May 29. ACS Chem Neurosci. 2013. PMID: 23682684 Free PMC article.
N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats.
Lovell KM, Felts AS, Rodriguez AL, Venable DF, Cho HP, Morrison RD, Byers FW, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Emmitte KA. Lovell KM, et al. Among authors: rodriguez al. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3713-8. doi: 10.1016/j.bmcl.2013.05.020. Epub 2013 May 17. Bioorg Med Chem Lett. 2013. PMID: 23727046 Free PMC article.
Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1.
Manka JT, Rodriguez AL, Morrison RD, Venable DF, Cho HP, Blobaum AL, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Emmitte KA. Manka JT, et al. Among authors: rodriguez al. Bioorg Med Chem Lett. 2013 Sep 15;23(18):5091-6. doi: 10.1016/j.bmcl.2013.07.029. Epub 2013 Jul 23. Bioorg Med Chem Lett. 2013. PMID: 23932792 Free PMC article.
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
Felts AS, Rodriguez AL, Morrison RD, Venable DF, Manka JT, Bates BS, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. Felts AS, et al. Among authors: rodriguez al. Bioorg Med Chem Lett. 2013 Nov 1;23(21):5779-85. doi: 10.1016/j.bmcl.2013.09.001. Epub 2013 Sep 10. Bioorg Med Chem Lett. 2013. PMID: 24074843 Free PMC article.
A novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptors.
Cho HP, Engers DW, Venable DF, Niswender CM, Lindsley CW, Conn PJ, Emmitte KA, Rodriguez AL. Cho HP, et al. Among authors: rodriguez al. ACS Chem Neurosci. 2014 Jul 16;5(7):597-610. doi: 10.1021/cn5000343. Epub 2014 May 15. ACS Chem Neurosci. 2014. PMID: 24798819 Free PMC article.
Discovery of VU0431316: a negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
Bates BS, Rodriguez AL, Felts AS, Morrison RD, Venable DF, Blobaum AL, Byers FW, Lawson KP, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. Bates BS, et al. Among authors: rodriguez al. Bioorg Med Chem Lett. 2014 Aug 1;24(15):3307-14. doi: 10.1016/j.bmcl.2014.06.003. Epub 2014 Jun 11. Bioorg Med Chem Lett. 2014. PMID: 24969015 Free PMC article.
Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents.
Engers JL, Rodriguez AL, Konkol LC, Morrison RD, Thompson AD, Byers FW, Blobaum AL, Chang S, Venable DF, Loch MT, Niswender CM, Daniels JS, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. Engers JL, et al. Among authors: rodriguez al. J Med Chem. 2015 Sep 24;58(18):7485-500. doi: 10.1021/acs.jmedchem.5b01005. Epub 2015 Sep 10. J Med Chem. 2015. PMID: 26335039 Free PMC article.
Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2.
Felts AS, Rodriguez AL, Smith KA, Engers JL, Morrison RD, Byers FW, Blobaum AL, Locuson CW, Chang S, Venable DF, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Emmitte KA. Felts AS, et al. Among authors: rodriguez al. J Med Chem. 2015 Nov 25;58(22):9027-40. doi: 10.1021/acs.jmedchem.5b01371. Epub 2015 Nov 11. J Med Chem. 2015. PMID: 26524606 Free PMC article.
219 results