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Page 1
Mechanism based neurotoxicity of mGlu5 positive allosteric modulators--development challenges for a promising novel antipsychotic target.
Parmentier-Batteur S, Hutson PH, Menzel K, Uslaner JM, Mattson BA, O'Brien JA, Magliaro BC, Forest T, Stump CA, Tynebor RM, Anthony NJ, Tucker TJ, Zhang XF, Gomez R, Huszar SL, Lambeng N, Fauré H, Le Poul E, Poli S, Rosahl TW, Rocher JP, Hargreaves R, Williams TM. Parmentier-Batteur S, et al. Among authors: magliaro bc. Neuropharmacology. 2014 Jul;82:161-73. doi: 10.1016/j.neuropharm.2012.12.003. Epub 2013 Jan 2. Neuropharmacology. 2014. PMID: 23291536
Discovery, Optimization, and Biological Characterization of 2,3,6-Trisubstituted Pyridine-Containing M4 Positive Allosteric Modulators.
Schubert JW, Harrison ST, Mulhearn J, Gomez R, Tynebor R, Jones K, Bunda J, Hanney B, Wai JM, Cox C, McCauley JA, Sanders JM, Magliaro B, O'Brien J, Pajkovic N, Huszar Agrapides SL, Taylor A, Gotter A, Smith SM, Uslaner J, Browne S, Risso S, Egbertson M. Schubert JW, et al. ChemMedChem. 2019 May 6;14(9):943-951. doi: 10.1002/cmdc.201900088. Epub 2019 Mar 28. ChemMedChem. 2019. PMID: 30920765
The selective phosphodiesterase 9 (PDE9) inhibitor PF-04447943 (6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one) enhances synaptic plasticity and cognitive function in rodents.
Hutson PH, Finger EN, Magliaro BC, Smith SM, Converso A, Sanderson PE, Mullins D, Hyde LA, Eschle BK, Turnbull Z, Sloan H, Guzzi M, Zhang X, Wang A, Rindgen D, Mazzola R, Vivian JA, Eddins D, Uslaner JM, Bednar R, Gambone C, Le-Mair W, Marino MJ, Sachs N, Xu G, Parmentier-Batteur S. Hutson PH, et al. Among authors: magliaro bc. Neuropharmacology. 2011 Sep;61(4):665-76. doi: 10.1016/j.neuropharm.2011.05.009. Epub 2011 May 19. Neuropharmacology. 2011. PMID: 21619887
3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts.
Brnardic EJ, Fraley ME, Garbaccio RM, Layton ME, Sanders JM, Culberson C, Jacobson MA, Magliaro BC, Hutson PH, O'Brien JA, Huszar SL, Uslaner JM, Fillgrove KL, Tang C, Kuo Y, Sur SM, Hartman GD. Brnardic EJ, et al. Among authors: magliaro bc. Bioorg Med Chem Lett. 2010 May 15;20(10):3129-33. doi: 10.1016/j.bmcl.2010.03.089. Epub 2010 Mar 31. Bioorg Med Chem Lett. 2010. PMID: 20409708
Discovery of 5-aryl-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis.
Layton ME, Reif AJ, Hartingh TJ, Rodzinak K, Dudkin V, Wang C, Arrington K, Kelly MJ 3rd, Garbaccio RM, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Tang C, Kuo Y, Jacobson MA. Layton ME, et al. Among authors: magliaro bc. Bioorg Med Chem Lett. 2016 Feb 15;26(4):1260-4. doi: 10.1016/j.bmcl.2016.01.021. Epub 2016 Jan 11. Bioorg Med Chem Lett. 2016. PMID: 26810316
Optimization of Novel Aza-benzimidazolone mGluR2 PAMs with Respect to LLE and PK Properties and Mitigation of CYP TDI.
Pero JE, Rossi MA, Kelly MJ 3rd, Lehman HD, Layton ME, Garbaccio RM, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Tang C, Kuo Y, Joyce LA, Sherer EC, Jacobson MA. Pero JE, et al. Among authors: magliaro bc. ACS Med Chem Lett. 2016 Jan 10;7(3):312-7. doi: 10.1021/acsmedchemlett.5b00459. eCollection 2016 Mar 10. ACS Med Chem Lett. 2016. PMID: 26985321 Free PMC article.
Discovery of 4-arylquinoline-2-carboxamides, highly potent and selective class of mGluR2 negative allosteric modulators: From HTS to activity in animal models.
Shu Y, Diamond TL, Hershey JC, Huang S, Magliaro BC, O'Brien JA, Schlegel KS, Puri V, Uebele VN, Uslaner JM, Wang C, Converso A. Shu Y, et al. Among authors: magliaro bc. Bioorg Med Chem Lett. 2020 May 1;30(9):127066. doi: 10.1016/j.bmcl.2020.127066. Epub 2020 Feb 28. Bioorg Med Chem Lett. 2020. PMID: 32173198
Discovery of Oxazolobenzimidazoles as Positive Allosteric Modulators for the mGluR2 Receptor.
Garbaccio RM, Brnardic EJ, Fraley ME, Hartman GD, Hutson PH, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Small JH, Tang C, Kuo Y, Jacobson MA. Garbaccio RM, et al. Among authors: magliaro bc. ACS Med Chem Lett. 2010 Jul 12;1(8):406-10. doi: 10.1021/ml100115a. eCollection 2010 Nov 11. ACS Med Chem Lett. 2010. PMID: 24900224 Free PMC article.
Discovery of [11C]MK-6884: A Positron Emission Tomography (PET) Imaging Agent for the Study of M4Muscarinic Receptor Positive Allosteric Modulators (PAMs) in Neurodegenerative Diseases.
Tong L, Li W, Lo MM, Gao X, Wai JM, Rudd M, Tellers D, Joshi A, Zeng Z, Miller P, Salinas C, Riffel K, Haley H, Purcell M, Holahan M, Gantert L, Schubert JW, Jones K, Mulhearn J, Egbertson M, Meng Z, Hanney B, Gomez R, Harrison ST, McQuade P, Bueters T, Uslaner J, Morrow J, Thomson F, Kong J, Liao J, Selyutin O, Bao J, Hastings NB, Agrawal S, Magliaro BC, Monsma FJ Jr, Smith MD, Risso S, Hesk D, Hostetler E, Mazzola R. Tong L, et al. Among authors: magliaro bc. J Med Chem. 2020 Mar 12;63(5):2411-2425. doi: 10.1021/acs.jmedchem.9b01406. Epub 2020 Mar 3. J Med Chem. 2020. PMID: 32101422 Free article.
Iterative Focused Screening with Biological Fingerprints Identifies Selective Asc-1 Inhibitors Distinct from Traditional High Throughput Screening.
Kutchukian PS, Warren L, Magliaro BC, Amoss A, Cassaday JA, O'Donnell G, Squadroni B, Zuck P, Pascarella D, Culberson JC, Cooke AJ, Hurzy D, Schlegel KS, Thomson F, Johnson EN, Uebele VN, Hermes JD, Parmentier-Batteur S, Finley M. Kutchukian PS, et al. Among authors: magliaro bc. ACS Chem Biol. 2017 Feb 17;12(2):519-527. doi: 10.1021/acschembio.6b00913. Epub 2017 Jan 6. ACS Chem Biol. 2017. PMID: 28032990 Free article.
13 results