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Discovery of DS-1971a, a Potent, Selective NaV1.7 Inhibitor.
Shinozuka T, Kobayashi H, Suzuki S, Tanaka K, Karanjule N, Hayashi N, Tsuda T, Tokumaru E, Inoue M, Ueda K, Kimoto H, Domon Y, Takahashi S, Kubota K, Yokoyama T, Shimizugawa A, Koishi R, Fujiwara C, Asano D, Sakakura T, Takasuna K, Abe Y, Watanabe T, Kitano Y. Shinozuka T, et al. Among authors: asano d. J Med Chem. 2020 Sep 24;63(18):10204-10220. doi: 10.1021/acs.jmedchem.0c00259. Epub 2020 May 26. J Med Chem. 2020. PMID: 32392056
CYP2C8-Mediated Formation of a Human Disproportionate Metabolite of the Selective NaV1.7 Inhibitor DS-1971a, a Mixed Cytochrome P450 and Aldehyde Oxidase Substrate.
Asano D, Hamaue S, Zahir H, Shiozawa H, Nishiya Y, Kimura T, Kazui M, Yamamura N, Ikeguchi M, Shibayama T, Inoue SI, Shinozuka T, Watanabe T, Yahara C, Watanabe N, Yoshinari K. Asano D, et al. Drug Metab Dispos. 2022 Mar;50(3):235-242. doi: 10.1124/dmd.121.000665. Epub 2021 Dec 20. Drug Metab Dispos. 2022. PMID: 34930785
Physiologically Based Pharmacokinetic Modeling for Quantitative Prediction of Exposure to a Human Disproportionate Metabolite of the Selective NaV1.7 Inhibitor DS-1971a, a Mixed Substrate of Cytochrome P450 and Aldehyde Oxidase, Using Chimeric Mice With Humanized Liver.
Asano D, Nakamura K, Nishiya Y, Shiozawa H, Takakusa H, Shibayama T, Inoue SI, Shinozuka T, Hamada T, Yahara C, Watanabe N, Yoshinari K. Asano D, et al. Drug Metab Dispos. 2023 Jan;51(1):67-80. doi: 10.1124/dmd.122.001000. Epub 2022 Oct 23. Drug Metab Dispos. 2023. PMID: 36273823
N-Aryl Indoles as a Novel Class of Potent NaV1.7 Inhibitors.
Karanjule N, Hayashi N, Suzuki S, Tsuda T, Tokumaru E, Tanaka K, Kimoto H, Domon Y, Takahashi S, Kubota K, Kitano Y, Yokoyama T, Koishi R, Fujiwara C, Inaba S, Asano D, Sakakura T, Takasuna K, Shinozuka T. Karanjule N, et al. Among authors: asano d. ACS Med Chem Lett. 2023 May 24;14(6):788-793. doi: 10.1021/acsmedchemlett.3c00079. eCollection 2023 Jun 8. ACS Med Chem Lett. 2023. PMID: 37312847
Discovery of 1-[2-(1-methyl-1H-pyrazol-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-6-yl]-3-(pyridin-4-ylmethyl)urea as a potent NAMPT (nicotinamide phosphoribosyltransferase) activator with attenuated CYP inhibition.
Akiu M, Tsuji T, Sogawa Y, Terayama K, Yokoyama M, Tanaka J, Asano D, Sakurai K, Sergienko E, Sessions EH, Gardell SJ, Pinkerton AB, Nakamura T. Akiu M, et al. Among authors: asano d. Bioorg Med Chem Lett. 2021 Jul 1;43:128048. doi: 10.1016/j.bmcl.2021.128048. Epub 2021 Apr 19. Bioorg Med Chem Lett. 2021. PMID: 33887438
64 results