(1S)-1,5-Anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-d-glucitol (TS-071) is a Potent, Selective Sodium-Dependent Glucose Cotransporter 2 …
…, M Arai, Y Kawakita… - Journal of medicinal …, 2010 - ACS Publications
Derivatives of a novel scaffold, C-phenyl 1-thio-d-glucitol, were prepared and evaluated for
sodium-dependent glucose cotransporter (SGLT) 2 and SGLT1 inhibition activities. …
sodium-dependent glucose cotransporter (SGLT) 2 and SGLT1 inhibition activities. …
Increase of intracellular glutathione by low-dose γ-ray irradiation is mediated by transcription factor AP-1 in RAW 264.7 cells
Y Kawakita, M Ikekita, R Kurozumi… - Biological and …, 2003 - jstage.jst.go.jp
The mechanism of the elevation of intracellular glutathione induced by low-dose g-rays was
examined in RAW 264.7 cells. The expression of mRNA for g-glutamylcysteine synthetase (g…
examined in RAW 264.7 cells. The expression of mRNA for g-glutamylcysteine synthetase (g…
Efficacy of a glycine transporter 1 inhibitor TASP0315003 in animal models of cognitive dysfunction and negative symptoms of schizophrenia
…, M Iijima, D Kambe, S Yamamoto, Y Kawakita… - …, 2015 - Springer
Rationale Since the hypofunction of the N-methyl-D-aspartate (NMDA) receptor is known to
be involved in the pathophysiology of schizophrenia, the enhancement of NMDA receptor …
be involved in the pathophysiology of schizophrenia, the enhancement of NMDA receptor …
In vitro and in vivo evaluation of the metabolism and bioavailability of ester prodrugs of mgs0039 (3-(3, 4-dichlorobenzyloxy)-2-amino-6-fluorobicyclo [3.1. 0] hexane-2 …
M Nakamura, Y Kawakita, A Yasuhara… - Drug metabolism and …, 2006 - ASPET
MGS0039 (3-(3,4-dichlorobenzyloxy)-2-amino-6-fluorobicyclo-[3.1.0]hexane-2,6-dicarboxylic
acid) has been identified as a potent and selective antagonist for metabotropic glutamate …
acid) has been identified as a potent and selective antagonist for metabotropic glutamate …
Synthesis, in vitro pharmacology, and pharmacokinetic profiles of 2-[1-amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-1-fluorocyclopropanecarboxylic acid and its 6 …
…, A Yasuhara, S Chaki, R Yoshikawa, Y Kawakita… - Bioorganic & medicinal …, 2008 - Elsevier
In this paper, we describe the synthesis of (+)-(1R ∗ ,2R ∗ )-2-[(1S ∗ )-1-amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-1-fluorocyclopropanecarboxylic
acid (+)-16a, a compound, that is, …
acid (+)-16a, a compound, that is, …
[HTML][HTML] Novel compound induces erythropoietin secretion through liver effects in chronic kidney disease patients and healthy volunteers
…, F Sato, H Watase, T Numazaki, Y Kawakita… - American Journal of …, 2018 - karger.com
Background: TP0463518 is a novel hypoxia-inducible factor prolyl hydroxylase inhibitor
developed to aid in the treatment of anemia associated with chronic kidney disease (CKD) and …
developed to aid in the treatment of anemia associated with chronic kidney disease (CKD) and …
Discovery of 3-Chloro-N-{(S)-[3-(1-ethyl-1H-pyrazol-4-yl) phenyl][(2S)-piperidine-2-yl] methyl}-4-(trifluoromethyl) pyridine-2-carboxamide as a Potent Glycine …
…, K Abe, K Oda, T Aoki, Y Kawakita… - Chemical and …, 2016 - jstage.jst.go.jp
A novel glycine transporter 1 (GlyT1) inhibitor was designed by the superposition of different
chemotypes to enhance its inhibitory activity. Starting from 2-chloro-N-{(S)-phenyl [(2S)-…
chemotypes to enhance its inhibitory activity. Starting from 2-chloro-N-{(S)-phenyl [(2S)-…
Identification of 1-Methyl-N-(propan-2-yl)-N-({2-[4-(trifluoromethoxy) phenyl] pyridin-4-yl} methyl)-1H-imidazole-4-carboxamide as a Potent and Orally Available …
…, K Abe, D Kambe, N Tsukiyama, Y Kawakita… - Chemical and …, 2016 - jstage.jst.go.jp
We previously identified 3-chloro-N-{(S)-[3-(1-ethyl-1H-pyrazol-4-yl) phenyl][(2S)-piperidine-2-yl]
methyl}-4-(trifluoromethyl) pyridine-2-carboxamide (5, TP0439150) as a potent and …
methyl}-4-(trifluoromethyl) pyridine-2-carboxamide (5, TP0439150) as a potent and …
Improvement of labeling efficiency of glycoprotein-liposome conjugates with iodine-125 by using Bolton-Hunter Reagent and their distribution in mice
Y Kawakita, S Kojima, N Yamazaki - Radioisotopes (Tokyo), 2000 - osti.gov
We have developed a new type of glycoprotein-liposome conjugates and examined their
potential utilities as drug-targeting carriers which exploit cellular functions of carbohydrate-…
potential utilities as drug-targeting carriers which exploit cellular functions of carbohydrate-…
[PDF][PDF] IN VITRO AND IN VIVO EVALUATION OF THE METABOLISM AND BIOAVAILABILITY OF ESTER PRODRUGS OF MSG0039, A POTENT MGLUR …
M Nakamura, Y Kawakita, A Yasuhara… - Drug Metabolism and …, 2005 - Citeseer
MGS0039 has been identified as a potent and selective antagonist for metabotropic glutamate
receptors (mGluRs). However, the oral bioavailability of MGS0039 is 10.9% in rats, due to …
receptors (mGluRs). However, the oral bioavailability of MGS0039 is 10.9% in rats, due to …