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Page 1
Bioisosteres of ethyl 8-ethynyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo [1,5-a][1,4]diazepine-3-carboxylate (HZ-166) as novel alpha 2,3 selective potentiators of GABAA receptors: Improved bioavailability enhances anticonvulsant efficacy.
Witkin JM, Smith JL, Ping X, Gleason SD, Poe MM, Li G, Jin X, Hobbs J, Schkeryantz JM, McDermott JS, Alatorre AI, Siemian JN, Cramer JW, Airey DC, Methuku KR, Tiruveedhula VVNPB, Jones TM, Crawford J, Krambis MJ, Fisher JL, Cook JM, Cerne R. Witkin JM, et al. Among authors: gleason sd. Neuropharmacology. 2018 Jul 15;137:332-343. doi: 10.1016/j.neuropharm.2018.05.006. Epub 2018 May 3. Neuropharmacology. 2018. PMID: 29778948 Free article.
Further evaluation of the potential anxiolytic activity of imidazo[1,5-a][1,4]diazepin agents selective for α2/3-containing GABAA receptors.
Witkin JM, Cerne R, Wakulchik M, S J, Gleason SD, Jones TM, Li G, Arnold LA, Li JX, Schkeryantz JM, Methuku KR, Cook JM, Poe MM. Witkin JM, et al. Among authors: gleason sd. Pharmacol Biochem Behav. 2017 Jun;157:35-40. doi: 10.1016/j.pbb.2017.04.009. Epub 2017 Apr 22. Pharmacol Biochem Behav. 2017. PMID: 28442369 Free PMC article.
The α2,3-selective potentiator of GABAA receptors, KRM-II-81, reduces nociceptive-associated behaviors induced by formalin and spinal nerve ligation in rats.
Witkin JM, Cerne R, Davis PG, Freeman KB, do Carmo JM, Rowlett JK, Methuku KR, Okun A, Gleason SD, Li X, Krambis MJ, Poe M, Li G, Schkeryantz JM, Jahan R, Yang L, Guo W, Golani LK, Anderson WH, Catlow JT, Jones TM, Porreca F, Smith JL, Knopp KL, Cook JM. Witkin JM, et al. Among authors: gleason sd. Pharmacol Biochem Behav. 2019 May;180:22-31. doi: 10.1016/j.pbb.2019.02.013. Epub 2019 Feb 27. Pharmacol Biochem Behav. 2019. PMID: 30825491 Free PMC article.
Anxiolytic-like effects through a GLUK5 kainate receptor mechanism.
Alt A, Weiss B, Ornstein PL, Gleason SD, Bleakman D, Stratford RE Jr, Witkin JM. Alt A, et al. Among authors: gleason sd. Neuropharmacology. 2007 Jun;52(7):1482-7. doi: 10.1016/j.neuropharm.2007.02.005. Epub 2007 Mar 2. Neuropharmacology. 2007. PMID: 17418283
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: gleason sd. CNS Neurol Disord Drug Targets. 2017;16(10):1099-1110. doi: 10.2174/1871527316666171101132047. CNS Neurol Disord Drug Targets. 2017. PMID: 29090671
Negative allosteric modulation of alpha 5-containing GABAA receptors engenders antidepressant-like effects and selectively prevents age-associated hyperactivity in tau-depositing mice.
Xu NZ, Ernst M, Treven M, Cerne R, Wakulchik M, Li X, Jones TM, Gleason SD, Morrow D, Schkeryantz JM, Rahman MT, Li G, Poe MM, Cook JM, Witkin JM. Xu NZ, et al. Among authors: gleason sd. Psychopharmacology (Berl). 2018 Apr;235(4):1151-1161. doi: 10.1007/s00213-018-4832-9. Epub 2018 Jan 26. Psychopharmacology (Berl). 2018. PMID: 29374303
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. Among authors: gleason sd. 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
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: gleason sd. Neuropharmacology. 2017 Nov;126:257-270. doi: 10.1016/j.neuropharm.2017.07.028. Epub 2017 Jul 28. Neuropharmacology. 2017. PMID: 28757050
39 results