Mode of action and functional significance of estrogen-inducing dendritic growth, spinogenesis, and synaptogenesis in the developing Purkinje cell

K Sasahara, H Shikimi, S Haraguchi… - Journal of …, 2007 - Soc Neuroscience
Neurosteroids are synthesized de novo from cholesterol in the brain. To understand neurosteroid
action in the brain, data on the regio- and temporal-specific synthesis of neurosteroids …

Pharmacokinetics and metabolism of delamanid, a novel anti-tuberculosis drug, in animals and humans: importance of albumin metabolism in vivo

K Sasahara, Y Shimokawa, Y Hirao, N Koyama… - Drug Metabolism and …, 2015 - ASPET
Delamanid, a new anti-tuberculosis drug, is metabolized to M1, a unique metabolite formed
by cleavage of the 6-nitro-2,3-dihydroimidazo[2,1-b] oxazole moiety, in plasma albumin in …

Estradiol promotes purkinje dendritic growth, spinogenesis, and synaptogenesis during neonatal life by inducing the expression of BDNF

S Haraguchi, K Sasahara, H Shikimi, S Honda… - The Cerebellum, 2012 - Springer
Neurosteroids are synthesized de novo from cholesterol in the brain. In rodents, the Purkinje
cell actively produces several kinds of neurosteroids including estradiol during neonatal life…

Metabolic mechanism of delamanid, a new anti-tuberculosis drug, in human plasma

Y Shimokawa, K Sasahara, N Koyama, K Kitano… - Drug Metabolism and …, 2015 - ASPET
The metabolism of delamanid (OPC-67683, Deltyba), a novel treatment of multidrug-resistant
tuberculosis, was investigated in vitro using plasma and purified protein preparations from …

Delamanid does not inhibit or induce cytochrome p450 enzymes in vitro

Y Shimokawa, K Sasahara, N Yoda… - Biological and …, 2014 - jstage.jst.go.jp
Delamanid is a new drug for the treatment of multidrug-resistant tuberculosis. Individuals who
are co-infected with human immunodeficiency virus and Mycobacterium tuberculosis may …

Feature importance of machine learning prediction models shows structurally active part and important physicochemical features in drug design

K Sasahara, M Shibata, H Sasabe, T Suzuki… - Drug Metabolism and …, 2021 - Elsevier
The objective of this study was to obtain the indicators of physicochemical parameters and
structurally active sites to design new chemical entities with desirable pharmacokinetic …

Absorption, distribution and excretion of the anti‐tuberculosis drug delamanid in rats: Extensive tissue distribution suggests potential therapeutic value for …

M Shibata, Y Shimokawa, K Sasahara… - … & Drug Disposition, 2017 - Wiley Online Library
Delamanid (OPC‐67683, Deltyba™, nitro‐dihydro‐imidazooxazoles derivative) is approved
for the treatment of adult pulmonary multidrug‐resistant tuberculosis. The absorption, …

In vitro evaluations for pharmacokinetic drug-drug interactions of a novel serotonin-dopamine activity modulator, brexpiprazole

…, T Koga, M Furukawa, M Matsunaga, K Sasahara… - Xenobiotica, 2021 - Taylor & Francis
Brexpiprazole, a serotonin-dopamine activity modulator, is indicated for the treatment of
schizophrenia and also adjunctive therapy to antidepressants for the treatment of Major …

Predicting drug metabolism and pharmacokinetics features of in-house compounds by a hybrid machine-learning model

K Sasahara, M Shibata, H Sasabe, T Suzuki… - Drug Metabolism and …, 2021 - Elsevier
We constructed machine learning-based pharmacokinetic prediction models with very high
performance. The models were trained on 26138 and 16613 compounds involved in …

Molecular dynamics and density functional studies on the metabolic selectivity of antipsychotic thioridazine by cytochrome P450 2D6: Connection with crystallographic …

K Sasahara, A Mashima, T Yoshida… - Bioorganic & Medicinal …, 2015 - Elsevier
CYP2D6, a cytochrome P450 isoform, significantly contributes to the metabolism of many
clinically important drugs. Thioridazine (THD) is one of the phenothiazine-type antipsychotics, …