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Page 1
Forebrain-selective AMPA-receptor antagonism guided by TARP γ-8 as an antiepileptic mechanism.
Kato AS, Burris KD, Gardinier KM, Gernert DL, Porter WJ, Reel J, Ding C, Tu Y, Schober DA, Lee MR, Heinz BA, Fitch TE, Gleason SD, Catlow JT, Yu H, Fitzjohn SM, Pasqui F, Wang H, Qian Y, Sher E, Zwart R, Wafford KA, Rasmussen K, Ornstein PL, Isaac JT, Nisenbaum ES, Bredt DS, Witkin JM. Kato AS, et al. Among authors: gardinier km. Nat Med. 2016 Dec;22(12):1496-1501. doi: 10.1038/nm.4221. Epub 2016 Nov 7. Nat Med. 2016. PMID: 27820603
Modulation of TARP γ8-Containing AMPA Receptors as a Novel Therapeutic Approach for Chronic Pain.
Knopp KL, Simmons RMA, Guo W, Adams BL, Gardinier KM, Gernert DL, Ornstein PL, Porter W, Reel J, Ding C, Wang H, Qian Y, Burris KD, Need A, Barth V, Swanson S, Catlow J, Witkin JM, Zwart R, Sher E, Choong KC, Wall TM, Schober D, Felder CC, Kato AS, Bredt DS, Nisenbaum ES. Knopp KL, et al. Among authors: gardinier km. J Pharmacol Exp Ther. 2019 Jun;369(3):345-363. doi: 10.1124/jpet.118.250126. Epub 2019 Mar 25. J Pharmacol Exp Ther. 2019. PMID: 30910921
Perampanel, an antagonist of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors, for the treatment of epilepsy: studies in human epileptic brain and nonepileptic brain and in rodent models.
Zwart R, Sher E, Ping X, Jin X, Sims JR Jr, Chappell AS, Gleason SD, Hahn PJ, Gardinier K, Gernert DL, Hobbs J, Smith JL, Valli SN, Witkin JM. Zwart R, et al. J Pharmacol Exp Ther. 2014 Oct;351(1):124-33. doi: 10.1124/jpet.114.212779. Epub 2014 Jul 15. J Pharmacol Exp Ther. 2014. PMID: 25027316
Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8.
Gardinier KM, Gernert DL, Porter WJ, Reel JK, Ornstein PL, Spinazze P, Stevens FC, Hahn P, Hollinshead SP, Mayhugh D, Schkeryantz J, Khilevich A, De Frutos O, Gleason SD, Kato AS, Luffer-Atlas D, Desai PV, Swanson S, Burris KD, Ding C, Heinz BA, Need AB, Barth VN, Stephenson GA, Diseroad BA, Woods TA, Yu H, Bredt D, Witkin JM. Gardinier KM, et al. J Med Chem. 2016 May 26;59(10):4753-68. doi: 10.1021/acs.jmedchem.6b00125. Epub 2016 Apr 29. J Med Chem. 2016. PMID: 27067148
Electroencephalographic, cognitive, and neurochemical effects of LY3130481 (CERC-611), a selective antagonist of TARP-γ8-associated AMPA receptors.
Witkin JM, Li J, Gilmour G, Mitchell SN, Carter G, Gleason SD, Seidel WF, Eastwood BJ, McCarthy A, Porter WJ, Reel J, Gardinier KM, Kato AS, Wafford KA. Witkin JM, et al. Among authors: gardinier km. Neuropharmacology. 2017 Nov;126:257-270. doi: 10.1016/j.neuropharm.2017.07.028. Epub 2017 Jul 28. Neuropharmacology. 2017. PMID: 28757050
Targeted Blockade of TARP-γ8-Associated AMPA Receptors: Anticonvulsant Activity with the Selective Antagonist LY3130481 (CERC-611).
Witkin JM, Schober DA, Gleason SD, Catlow JT, Porter WJ, Reel J, Jin X, Hobbs J, Gehlert D, Gernert DL, Gardinier KM, Kato AS, Ping X, Smith JL. Witkin JM, et al. Among authors: gardinier km. CNS Neurol Disord Drug Targets. 2017;16(10):1099-1110. doi: 10.2174/1871527316666171101132047. CNS Neurol Disord Drug Targets. 2017. PMID: 29090671
Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1S,3R)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Positive Allosteric Modulator of the Human Dopamine D1 Receptor.
Hao J, Beck JP, Schaus JM, Krushinski JH, Chen Q, Beadle CD, Vidal P, Reinhard MR, Dressman BA, Massey SM, Boulet SL, Cohen MP, Watson BM, Tupper D, Gardinier KM, Myers J, Johansson AM, Richardson J, Richards DS, Hembre EJ, Remick DM, Coates DA, Bhardwaj RM, Diseroad BA, Bender D, Stephenson G, Wolfangel CD, Diaz N, Getman BG, Wang XS, Heinz BA, Cramer JW, Zhou X, Maren DL, Falcone JF, Wright RA, Mitchell SN, Carter G, Yang CR, Bruns RF, Svensson KA. Hao J, et al. Among authors: gardinier km. J Med Chem. 2019 Oct 10;62(19):8711-8732. doi: 10.1021/acs.jmedchem.9b01234. Epub 2019 Sep 30. J Med Chem. 2019. PMID: 31532644
Structural Determinants of the γ-8 TARP Dependent AMPA Receptor Antagonist.
Lee MR, Gardinier KM, Gernert DL, Schober DA, Wright RA, Wang H, Qian Y, Witkin JM, Nisenbaum ES, Kato AS. Lee MR, et al. Among authors: gardinier km. ACS Chem Neurosci. 2017 Dec 20;8(12):2631-2647. doi: 10.1021/acschemneuro.7b00186. Epub 2017 Sep 5. ACS Chem Neurosci. 2017. PMID: 28825787
15 results