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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: cerne r. 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.
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: cerne r. 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.
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: cerne r. 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.
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: cerne r. 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.
The α2,3-selective potentiators of GABAA receptors, KRM-II-81 and MP-III-80, produce anxiolytic-like effects and block chemotherapy-induced hyperalgesia in mice without tolerance development.
Biggerstaff A, Kivell B, Smith JL, Mian MY, Golani LK, Rashid F, Sharmin D, Knutson DE, Cerne R, Cook JM, Witkin JM. Biggerstaff A, et al. Among authors: cerne r. Pharmacol Biochem Behav. 2020 Sep;196:172996. doi: 10.1016/j.pbb.2020.172996. Epub 2020 Jul 12. Pharmacol Biochem Behav. 2020. PMID: 32668266
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: cerne r. 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.
53 results