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Page 1
Discovery, Structure-Activity Relationship, and Biological Characterization of a Novel Series of 6-((1 H-Pyrazolo[4,3- b]pyridin-3-yl)amino)-benzo[ d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mGlu4).
Bollinger SR, Engers DW, Panarese JD, West M, Engers JL, Loch MT, Rodriguez AL, Blobaum AL, Jones CK, Thompson Gray A, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Bollinger SR, et al. Among authors: loch mt. J Med Chem. 2019 Jan 10;62(1):342-358. doi: 10.1021/acs.jmedchem.8b00994. Epub 2018 Oct 10. J Med Chem. 2019. PMID: 30247901
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: loch mt. 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.
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: loch mt. 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.
Development and Antiparkinsonian Activity of VU0418506, a Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor 4 Homomers without Activity at mGlu2/4 Heteromers.
Niswender CM, Jones CK, Lin X, Bubser M, Thompson Gray A, Blobaum AL, Engers DW, Rodriguez AL, Loch MT, Daniels JS, Lindsley CW, Hopkins CR, Javitch JA, Conn PJ. Niswender CM, et al. Among authors: loch mt. ACS Chem Neurosci. 2016 Sep 21;7(9):1201-11. doi: 10.1021/acschemneuro.6b00036. Epub 2016 Aug 5. ACS Chem Neurosci. 2016. PMID: 27441572 Free PMC article.
Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines.
Abe M, Seto M, Gogliotti RG, Loch MT, Bollinger KA, Chang S, Engelberg EM, Luscombe VB, Harp JM, Bubser M, Engers DW, Jones CK, Rodriguez AL, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW. Abe M, et al. Among authors: loch mt. ACS Med Chem Lett. 2017 Sep 1;8(10):1110-1115. doi: 10.1021/acsmedchemlett.7b00317. eCollection 2017 Oct 12. ACS Med Chem Lett. 2017. PMID: 29057060 Free PMC article.
VU6010608, a Novel mGlu7 NAM from a Series of N-(2-(1H-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides.
Reed CW, McGowan KM, Spearing PK, Stansley BJ, Roenfanz HF, Engers DW, Rodriguez AL, Engelberg EM, Luscombe VB, Loch MT, Remke DH, Rook JM, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW. Reed CW, et al. Among authors: loch mt. ACS Med Chem Lett. 2017 Nov 8;8(12):1326-1330. doi: 10.1021/acsmedchemlett.7b00429. eCollection 2017 Dec 14. ACS Med Chem Lett. 2017. PMID: 29259756 Free PMC article.
Discovery of VU2957 (Valiglurax): An mGlu4 Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease.
Panarese JD, Engers DW, Wu YJ, Bronson JJ, Macor JE, Chun A, Rodriguez AL, Felts AS, Engers JL, Loch MT, Emmitte KA, Castelhano AL, Kates MJ, Nader MA, Jones CK, Blobaum AL, Conn PJ, Niswender CM, Hopkins CR, Lindsley CW. Panarese JD, et al. Among authors: loch mt. ACS Med Chem Lett. 2018 Oct 16;10(3):255-260. doi: 10.1021/acsmedchemlett.8b00426. eCollection 2019 Mar 14. ACS Med Chem Lett. 2018. PMID: 30891122 Free PMC article.
Synthesis and pharmacological evaluation of bivalent tethered ligands to target the mGlu2/4 heterodimeric receptor results in a compound with mGlu2/2 homodimer selectivity.
Fulton MG, Loch MT, Rodriguez AL, Lin X, Javitch JA, Conn PJ, Niswender CM, Lindsley CW. Fulton MG, et al. Among authors: loch mt. Bioorg Med Chem Lett. 2020 Jul 1;30(13):127212. doi: 10.1016/j.bmcl.2020.127212. Epub 2020 Apr 25. Bioorg Med Chem Lett. 2020. PMID: 32371100 Free PMC article.
Discovery and optimization of a novel CNS penetrant series of mGlu4 PAMs based on a 1,4-thiazepane core with in vivo efficacy in a preclinical Parkinsonian model.
Kent CN, Fulton MG, Stillwell KJ, Dickerson JW, Loch MT, Rodriguez AL, Blobaum AL, Boutaud O, Rook JL, Niswender CM, Conn PJ, Lindsley CW. Kent CN, et al. Among authors: loch mt. Bioorg Med Chem Lett. 2021 Apr 1;37:127838. doi: 10.1016/j.bmcl.2021.127838. Epub 2021 Feb 5. Bioorg Med Chem Lett. 2021. PMID: 33556572
Positive allosteric modulators (PAMs) of the group II metabotropic glutamate receptors: Design, synthesis, and evaluation as ex-vivo tool compounds.
Yamada Y, Gilliland K, Xiang Z, Haymer D, Crocker KE, Loch MT, Schulte ML, Rodriguez AL, Niswender CM, Jeffrey Conn P, Lindsley CW, Melancon BJ. Yamada Y, et al. Among authors: loch mt. Bioorg Med Chem Lett. 2021 Oct 15;50:128342. doi: 10.1016/j.bmcl.2021.128342. Epub 2021 Aug 27. Bioorg Med Chem Lett. 2021. PMID: 34461178
13 results