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New Imidazodiazepine Analogue, 5-(8-Bromo-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,5-a][1,4]diazepin-3-yl)oxazole, Provides a Simplified Synthetic Scheme, High Oral Plasma and Brain Exposures, and Produces Antiseizure Efficacy in Mice, and Antiepileptogenic Activity in Neural Networks in Brain Slices from a Patient with Mesial Temporal Lobe Epilepsy.
Sharmin D, Divović B, Ping X, Cerne R, Smith JL, Rezvanian S, Mondal P, Meyer MJ, Kiley ME, Arnold LA, Mian MY, Pandey KP, Jin X, Mitrović JR, Djorović D, Lippa A, Cook JM, Golani LK, Scholze P, Savić MM, Witkin JM. Sharmin D, et al. Among authors: arnold la. ACS Chem Neurosci. 2024 Feb 7;15(3):517-526. doi: 10.1021/acschemneuro.3c00555. Epub 2024 Jan 4. ACS Chem Neurosci. 2024. PMID: 38175916
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: arnold la. Biopharm Drug Dispos. 2022 Apr;43(2):66-75. doi: 10.1002/bdd.2313. Epub 2022 Mar 10. Biopharm Drug Dispos. 2022. PMID: 35194800
Structural Analogs of the GABAkine KRM-II-81 Are Orally Bioavailable Anticonvulsants without Sedation.
Pandey KP, Divović B, Rashid F, Golani LK, Cerne R, Zahn NM, Meyer MJ, Arnold LA, Sharmin D, Mian MY, Smith JL, Ping X, Jin X, Lippa A, Tiruveedhula VVNPB, Cook JM, Savić MM, Witkin JM. Pandey KP, et al. Among authors: arnold la. J Pharmacol Exp Ther. 2023 Apr;385(1):50-61. doi: 10.1124/jpet.122.001362. Epub 2023 Feb 6. J Pharmacol Exp Ther. 2023. PMID: 36746611 Free PMC article.
Comparative anticonvulsant activity of the GABAkine KRM-II-81 and a deuterated analog.
Ping X, Meyer MJ, Zahn NM, Golani LK, Sharmin D, Pandey KP, Revanian S, Mondal P, Jin X, Arnold LA, Cerne R, Cook JM, Divović B, Savić MM, Lippa A, Smith JL, Witkin JM. Ping X, et al. Among authors: arnold la. Drug Dev Res. 2023 May;84(3):527-531. doi: 10.1002/ddr.22042. Epub 2023 Feb 7. Drug Dev Res. 2023. PMID: 36748904
Targeting Nitric Oxide Production in Microglia with Novel Imidazodiazepines for Nonsedative Pain Treatment.
Nieman AN, Li G, Zahn NM, Mian MY, Mikulsky BN, Hoffman DA, Wilcox TM, Kehoe AS, Luecke IW, Poe MM, Alvarez-Carbonell D, Cook JM, Stafford DC, Arnold LA. Nieman AN, et al. Among authors: arnold la. ACS Chem Neurosci. 2020 Jul 1;11(13):2019-2030. doi: 10.1021/acschemneuro.0c00324. Epub 2020 Jun 18. ACS Chem Neurosci. 2020. PMID: 32511908 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: arnold la. 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.
Design and Synthesis of Novel Deuterated Ligands Functionally Selective for the γ-Aminobutyric Acid Type A Receptor (GABAAR) α6 Subtype with Improved Metabolic Stability and Enhanced Bioavailability.
Knutson DE, Kodali R, Divović B, Treven M, Stephen MR, Zahn NM, Dobričić V, Huber AT, Meirelles MA, Verma RS, Wimmer L, Witzigmann C, Arnold LA, Chiou LC, Ernst M, Mihovilovic MD, Savić MM, Sieghart W, Cook JM. Knutson DE, et al. Among authors: arnold la. J Med Chem. 2018 Mar 22;61(6):2422-2446. doi: 10.1021/acs.jmedchem.7b01664. Epub 2018 Mar 6. J Med Chem. 2018. PMID: 29481759 Free PMC article.
113 results