Avanafil, a potent and highly selective phosphodiesterase-5 inhibitor for erectile dysfunction

…, K Fujishige, T Sasaki, T Kobayashi, K Kojima… - The Journal of …, 2012 - auajournals.org
Purpose : We investigated the in vitro inhibitory effects of avanafil, a novel, potent inhibitor of
phosphodiesterase-5, on 11 phosphodiesterases. We also studied its potentiation of penile …

Exclusion of assembled M re B by anionic phospholipids at cell poles confers cell polarity for bidirectional growth

T Kawazura, K Matsumoto, K Kojima… - Molecular …, 2017 - Wiley Online Library
Cell polarity determines the direction of cell growth in bacteria. MreB actin spatially regulates
peptidoglycan synthesis to enable cells to elongate bidirectionally. MreB densely localizes …

[HTML][HTML] Discovery of evocalcet, a next-generation calcium-sensing receptor agonist for the treatment of hyperparathyroidism

…, T Kawata, R Ohashi, H Fukuda, K Kojima… - Bioorganic & Medicinal …, 2018 - Elsevier
The calcium-sensing receptor (CaSR) plays an important role in sensing extracellular calcium
ions and regulating parathyroid hormone secretion by parathyroid gland cells, and the …

Broad but distinct role of pregnane x receptor on the expression of individual cytochrome p450s in human hepatocytes

K Kojima, K Nagata, T Matsubara… - Drug metabolism and …, 2007 - Elsevier
In the present study, we have utilized a target selective human pregnane X receptor-siRNA (hPXR-siRNA)-adenovirus
expression system to examine the contribution of hPXR on the …

Prediction of human distribution volumes of compounds in various elimination phases using physiologically based pharmacokinetic modeling and experimental …

H Shimizu, K Yoshida, T Nakada, K Kojima… - Drug Metabolism and …, 2019 - ASPET
Predicting the pharmacokinetics of compounds in humans is an important part of the drug
development process. In this study, the plasma concentration profiles of 10 marketed …

Discovery of a pyrazolo [1, 5-a] pyrimidine derivative (MT-3014) as a highly selective PDE10A inhibitor via core structure transformation from the stilbene moiety

…, Y Watanabe, M Takakuwa, K Kojima… - Bioorganic & Medicinal …, 2019 - Elsevier
We have developed a new class of PDE10A inhibitor, a pyrazolo[1,5-a]pyrimidine derivative
MT-3014 (1). A previous compound introduced was deprioritized due to concerns for E/Z-…

An LC/ESI-SRM/MS method to screen chemically modified hemoglobin: simultaneous analysis for oxidized, nitrated, lipidated, and glycated sites

K Kojima, SH Lee, T Oe - Analytical and bioanalytical chemistry, 2016 - Springer
Proteins are continuously exposed to various reactive chemical species (reactive oxygen/nitrogen
species, endogenous/exogenous aldehydes/epoxides, etc.) due to physiological and …

Antipsychotic-like effects of a novel phosphodiesterase 10A inhibitor MT-3014 in rats

…, J Anabuki, T Tezuka, S Sato, K Kojima… - Pharmacology …, 2020 - Elsevier
Phosphodiesterase (PDE) 10A is an attractive therapeutic target for schizophrenia. Here,
we investigated the antipsychotic-like effects of a novel PDE10A inhibitor, 1-({2-(7-fluoro-3-…

Discovery of 2-[(E)-2-(7-Fluoro-3-methylquinoxalin-2-yl) vinyl]-6-pyrrolidin-1-yl-N-(tetrahydro-2H-pyran-4-yl) pyrimidin-4-amine Hydrochloride as a Highly Selective …

…, H Taniguchi, Y Watanabe, K Kojima… - Chemical and …, 2018 - jstage.jst.go.jp
Phosphodiesterase (PDE) 10A is a dual hydrolase of cAMP and cGMP and highly expressed
in striatal medium spiny neurons. Inhibition of PDE10A modulates the activity of medium …

Study on high frequency current interruption characteristics of vacuum circuit breaker

K Kojima, R Oshiro, E Kaneko - 2016 27th International …, 2016 - ieeexplore.ieee.org
It is well known that vacuum circuit breakers (VCB) have such superior characteristics as
small size, light weight, small noise, frequent interruption, easy maintenance, and no …