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The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease.
Jones CK, Bubser M, Thompson AD, Dickerson JW, Turle-Lorenzo N, Amalric M, Blobaum AL, Bridges TM, Morrison RD, Jadhav S, Engers DW, Italiano K, Bode J, Daniels JS, Lindsley CW, Hopkins CR, Conn PJ, Niswender CM. Jones CK, et al. Among authors: blobaum al. J Pharmacol Exp Ther. 2012 Feb;340(2):404-21. doi: 10.1124/jpet.111.187443. Epub 2011 Nov 16. J Pharmacol Exp Ther. 2012. PMID: 22088953 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: blobaum 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.
Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in Schizophrenics.
Garcia-Barrantes PM, Cho HP, Niswender CM, Byers FW, Locuson CW, Blobaum AL, Xiang Z, Rook JM, Conn PJ, Lindsley CW. Garcia-Barrantes PM, et al. Among authors: blobaum al. J Med Chem. 2015 Oct 22;58(20):7959-71. doi: 10.1021/acs.jmedchem.5b00727. Epub 2015 Oct 8. J Med Chem. 2015. PMID: 26426481 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: blobaum 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.
N-Alkylpyrido[1',2':1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents.
Felts AS, Rodriguez AL, Morrison RD, Venable DF, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. Felts AS, et al. Among authors: blobaum al. Bioorg Med Chem Lett. 2016 Apr 15;26(8):1894-900. doi: 10.1016/j.bmcl.2016.03.026. Epub 2016 Mar 9. Bioorg Med Chem Lett. 2016. PMID: 26988308 Free PMC article.
Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy.
Gogliotti RD, Engers DW, Garcia-Barrantes PM, Panarese JD, Gentry PR, Blobaum AL, Morrison RD, Daniels JS, Thompson AD, Jones CK, Conn PJ, Niswender CM, Lindsley CW, Hopkins CR. Gogliotti RD, et al. Among authors: blobaum al. Bioorg Med Chem Lett. 2016 Jun 15;26(12):2915-2919. doi: 10.1016/j.bmcl.2016.04.041. Epub 2016 Apr 19. Bioorg Med Chem Lett. 2016. PMID: 27131990 Free PMC article.
Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4).
Gogliotti RD, Blobaum AL, Morrison RM, Daniels JS, Salovich JM, Cheung YY, Rodriguez AL, Loch MT, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Gogliotti RD, et al. Among authors: blobaum al. Bioorg Med Chem Lett. 2016 Jul 1;26(13):2984-2987. doi: 10.1016/j.bmcl.2016.05.029. Epub 2016 May 11. Bioorg Med Chem Lett. 2016. PMID: 27234146 Free PMC article.
mGlu7 potentiation rescues cognitive, social, and respiratory phenotypes in a mouse model of Rett syndrome.
Gogliotti RG, Senter RK, Fisher NM, Adams J, Zamorano R, Walker AG, Blobaum AL, Engers DW, Hopkins CR, Daniels JS, Jones CK, Lindsley CW, Xiang Z, Conn PJ, Niswender CM. Gogliotti RG, et al. Among authors: blobaum al. Sci Transl Med. 2017 Aug 16;9(403):eaai7459. doi: 10.1126/scitranslmed.aai7459. Sci Transl Med. 2017. PMID: 28814546 Free PMC article.
Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.
Felts AS, Rodriguez AL, Morrison RD, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Emmitte KA. Felts AS, et al. Among authors: blobaum al. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1679-1685. doi: 10.1016/j.bmcl.2018.04.053. Epub 2018 Apr 22. Bioorg Med Chem Lett. 2018. PMID: 29705142 Free PMC article.
Activation of the mGlu1 metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M4 muscarinic receptor allosteric modulators.
Yohn SE, Foster DJ, Covey DP, Moehle MS, Galbraith J, Garcia-Barrantes PM, Cho HP, Bubser M, Blobaum AL, Joffe ME, Cheer JF, Jones CK, Lindsley CW, Conn PJ. Yohn SE, et al. Among authors: blobaum al. Mol Psychiatry. 2020 Nov;25(11):2786-2799. doi: 10.1038/s41380-018-0206-2. Epub 2018 Aug 16. Mol Psychiatry. 2020. PMID: 30116027 Free PMC article.
103 results