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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
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.
Metabolism, pharmacokinetics, and anticonvulsant activity of a deuterated analog of the α2/3-selective GABAkine KRM-II-81.
Golani LK, Divović B, Sharmin D, Pandey KP, Mian MY, Cerne R, Zahn NM, Meyer MJ, Tiruveedhula VVNPB, Smith JL, Ping X, Jin X, Lippa A, Schkeryantz JM, Arnold LA, Cook JM, Savić MM, Witkin JM. Golani LK, et al. Among authors: cerne r. Biopharm Drug Dispos. 2022 Apr;43(2):66-75. doi: 10.1002/bdd.2313. Epub 2022 Mar 10. Biopharm Drug Dispos. 2022. PMID: 35194800
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