Discovery of novel pyrazolylpyridine derivatives for 20-hydroxyeicosatetraenoic acid synthase inhibitors with selective CYP4A11/4F2 inhibition

…, E Gunji, T Fukunaga, S Inatani… - Journal of Medicinal …, 2022 - ACS Publications
20-Hydroxyeicosatetraenoic acid (20-HETE) is one of the major oxidized arachidonic acid (AA)
metabolites produced by cytochrome P450 (CYP) 4A11 and CYP4F2 isozymes in the …

Preclinical metabolism and disposition of TP0473292, a novel oral prodrug of the potent metabotropic glutamate 2/3 receptor antagonist TP0178894 for the treatment …

S Inatani, M Ochi, K Kinoshita, J Yamaguchi… - Drug Metabolism and …, 2023 - ASPET
TP0473292 is an adamantane carboxylic acid (ACA) ester prodrug for enhancing the oral
bioavailability of the hydrophilic glutamate analog TP0178894, a novel metabotropic …

Introduction of a carboxylic acid group into pyrazolylpyridine derivatives increased selectivity for inhibition of the 20-HETE synthase CYP4A11/4F2

…, N Kojima, T Fukunaga, M Hirate, S Inatani… - Bioorganic & Medicinal …, 2023 - Elsevier
20-Hydroxyeicosatetraenoic acid (20-HETE) is a lipid mediator and one of the major
arachidonic acid metabolites whose formation is mainly catalyzed by the enzymes cytochrome …

Renoprotective Effect of TP0472993, a Novel and Selective 20-Hydroxyeicosatetraenoic Acid Synthesis Inhibitor, in Mouse Models of Renal Fibrosis

…, N Kojima, H Koretsune, Y Hasegawa, S Inatani… - … of Pharmacology and …, 2023 - ASPET
Kidney fibrosis is considered the essential pathophysiological process for the progression
of chronic kidney disease (CKD) toward renal failure. 20-Hydroxyeicosatetraenoic acid (20-…

Prediction of a clinically effective dose of THY1773, a novel V1B receptor antagonist, based on preclinical data

S Inatani, A Mizuno‐Yasuhira, M Kamiya… - … & Drug Disposition, 2021 - Wiley Online Library
THY1773 is a novel arginine vasopressin 1B (V 1B ) receptor antagonist that is under
development as an oral drug for the treatment of major depressive disorder (MDD). Here we report …

Pharmacological characterization of TP0591816, a novel macrocyclic respiratory syncytial virus fusion inhibitor with antiviral activity against F protein mutants

I Yoshida, K Arikawa, Y Honma, S Inatani… - Antimicrobial Agents …, 2020 - Am Soc Microbiol
Human respiratory syncytial virus (RSV) is a major cause of lower respiratory tract infections
in early childhood. However, no vaccines have yet been approved for prevention of RSV …

Bottom-up physiologically based pharmacokinetic modelling for predicting the human pharmacokinetic profiles of the ester prodrug MGS0274 and its active metabolite …

M Ochi, K Kinoshita, J Yamaguchi, H Endo - Xenobiotica, 2022 - Taylor & Francis
For ester prodrugs that are used to improve the gastrointestinal absorption of highly
hydrophilic, pharmacologically active substances, it is challenging to predict the human …

Accelerated Neural Differentiation of Human Induced Pluripotent Stem Cells Using Chlorate Treatment

S Nishihara - Stem Cells and Cancer Stem Cells, Volume 7 …, 2012 - Springer
The development of rapid, efficient and safe methods for neural induction from human induced
pluripotent stem (iPS) cells is a necessary part of the development of cell replacement …

Three-dimensional magnetohydrodynamic analysis of a magnetic sail using a deployable modular structure

S Arita, Y Yamagiwa - Journal of Spacecraft and Rockets, 2023 - arc.aiaa.org
To obtain significant drag from a magnetic sail, it is necessary to generate a large magnetic
moment. However, even with superconducting coils, a coil radius of several kilometers is …

Relationship between Magnetic Field Interference and Electromagnetic Drag in Multicoil Magnetic Sails

S Arita, Y Yamagiwa - International Journal of Aeronautical and Space …, 2023 - Springer
In contrast to single-coil magnetic sails, multicoil magnetic sails do not require active attitude
control and can retain a large drag force without increasing their power consumption by …