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The Positive Allosteric Modulator of α2/3-Containing GABAA Receptors, KRM-II-81, Is Active in Pharmaco-Resistant Models of Epilepsy and Reduces Hyperexcitability after Traumatic Brain Injury.
Witkin JM, Li G, Golani LK, Xiong W, Smith JL, Ping X, Rashid F, Jahan R, Cerne R, Cook JM, Jin X. Witkin JM, et al. Among authors: li g. J Pharmacol Exp Ther. 2020 Jan;372(1):83-94. doi: 10.1124/jpet.119.260968. Epub 2019 Nov 6. J Pharmacol Exp Ther. 2020. PMID: 31694876 Free PMC article.
Synthesis and Characterization of a Novel γ-Aminobutyric Acid Type A (GABAA) Receptor Ligand That Combines Outstanding Metabolic Stability, Pharmacokinetics, and Anxiolytic Efficacy.
Poe MM, Methuku KR, Li G, Verma AR, Teske KA, Stafford DC, Arnold LA, Cramer JW, Jones TM, Cerne R, Krambis MJ, Witkin JM, Jambrina E, Rehman S, Ernst M, Cook JM, Schkeryantz JM. Poe MM, et al. Among authors: li g. J Med Chem. 2016 Dec 8;59(23):10800-10806. doi: 10.1021/acs.jmedchem.6b01332. Epub 2016 Nov 28. J Med Chem. 2016. PMID: 27933953 Free PMC article.
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: li g, li x. Psychopharmacology (Berl). 2018 Apr;235(4):1151-1161. doi: 10.1007/s00213-018-4832-9. Epub 2018 Jan 26. Psychopharmacology (Berl). 2018. PMID: 29374303
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: li g, li x. 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.
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: li g. 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.
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