Toshiki Kurosawa
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View article: Brain distribution and muscarinic receptor occupancy of an active metabolite of fesoterodine in rats
Brain distribution and muscarinic receptor occupancy of an active metabolite of fesoterodine in rats Open
Several large-scale clinical trials have shown that long-term use of antimuscarinic agents for overactive bladder treatment increases the risk of dementia and that this risk varies between agents. Fesoterodine, an overactive bladder antimu…
View article: Involvement of Proton-Coupled Organic Cation Antiporter in Human Blood–Brain Barrier Transport of Mesoridazine and Metoclopramide
Involvement of Proton-Coupled Organic Cation Antiporter in Human Blood–Brain Barrier Transport of Mesoridazine and Metoclopramide Open
Mesoridazine and metoclopramide are cationic drugs that are distributed in the human brain despite being substrates of multidrug resistance protein 1 (MDR1), an efflux transporter expressed at the blood-brain barrier (BBB). We investigated…
View article: Development and Functional Evaluation of MDR1-expressing Microvascular Endothelial-like Cells Derived from Human iPS Cells as an In vitro Blood-brain Barrier Model
Development and Functional Evaluation of MDR1-expressing Microvascular Endothelial-like Cells Derived from Human iPS Cells as an In vitro Blood-brain Barrier Model Open
In order to establish an in vitro model of the human blood-brain barrier (BBB), MDR1-overexpressing human induced pluripotent stem cells (hiPSCs) were generated, and they were differentiated to MDR1-expressing brain microvascular endotheli…
View article: Construction of human iPS cells-derived blood-brain barrier model and evaluation of transporter function
Construction of human iPS cells-derived blood-brain barrier model and evaluation of transporter function Open
血液脳関門（Blood-Brain Barrier：BBB）は、脳毛細血管内皮細胞同士が密着結合を形成することで、脳と血液間における物質輸送を厳密に制御している。脳内へのドラッグデリバリー技術、そして有効な中枢疾患治療薬の開発にとって、ヒト脳への移行性を評価できるin vitroモデルの構築が重要であるが、既存の動物および細胞評価系は種差や密着結合形成能の問題が指摘されている。近年、ヒトiPS細胞から脳毛細血管内皮細胞へ分化誘導する技術が開発され、強力な密着結合性を有するヒ…
View article: Naltrexone Transport by a Proton-Coupled Organic Cation Antiporter in hCMEC/D3 Cells, an <i>in Vitro</i> Human Blood–Brain Barrier Model
Naltrexone Transport by a Proton-Coupled Organic Cation Antiporter in hCMEC/D3 Cells, an <i>in Vitro</i> Human Blood–Brain Barrier Model Open
Naltrexone is a mu-opioid receptor antagonist used in the treatment of opioid and alcohol dependence. The blood-brain barrier (BBB) transport characteristics of naltrexone was investigated by means of hCMEC/D3 cells, a human immortalized b…
View article: Proteomics-Based Transporter Identification by the PICK Method: Involvement of TM7SF3 and LHFPL6 in Proton-Coupled Organic Cation Antiport at the Blood–Brain Barrier
Proteomics-Based Transporter Identification by the PICK Method: Involvement of TM7SF3 and LHFPL6 in Proton-Coupled Organic Cation Antiport at the Blood–Brain Barrier Open
A proton-coupled organic cation (H+/OC) antiporter working at the blood–brain barrier (BBB) in humans and rodents is thought to be a promising candidate for the efficient delivery of cationic drugs to the brain. Therefore, it is important …
View article: Correction to: Construction and Functional Evaluation of a Three-Dimensional Blood–Brain Barrier Model Equipped With Human Induced Pluripotent Stem Cell-Derived Brain Microvascular Endothelial Cells
Correction to: Construction and Functional Evaluation of a Three-Dimensional Blood–Brain Barrier Model Equipped With Human Induced Pluripotent Stem Cell-Derived Brain Microvascular Endothelial Cells Open
View article: Construction and Functional Evaluation of a Three-Dimensional Blood–Brain Barrier Model Equipped With Human Induced Pluripotent Stem Cell-Derived Brain Microvascular Endothelial Cells
Construction and Functional Evaluation of a Three-Dimensional Blood–Brain Barrier Model Equipped With Human Induced Pluripotent Stem Cell-Derived Brain Microvascular Endothelial Cells Open
View article: Transport Characteristics of 6-Mercaptopurine in Brain Microvascular Endothelial Cells Derived From Human Induced Pluripotent Stem Cells
Transport Characteristics of 6-Mercaptopurine in Brain Microvascular Endothelial Cells Derived From Human Induced Pluripotent Stem Cells Open
View article: Functional Investigation of Solute Carrier Family 35, Member F2, in Three Cellular Models of the Primate Blood-Brain Barrier
Functional Investigation of Solute Carrier Family 35, Member F2, in Three Cellular Models of the Primate Blood-Brain Barrier Open
View article: Transport of Pregabalin Via L-Type Amino Acid Transporter 1 (SLC7A5) in Human Brain Capillary Endothelial Cell Line
Transport of Pregabalin Via L-Type Amino Acid Transporter 1 (SLC7A5) in Human Brain Capillary Endothelial Cell Line Open
Our results indicate that LAT1, but not LAT2, recognizes pregabalin as a substrate. It is suggested that LAT1 mediates pregabalin transport at the BBB.
View article: Design, Synthesis, and Blood–Brain Barrier Transport Study of Pyrilamine Derivatives as Histone Deacetylase Inhibitors
Design, Synthesis, and Blood–Brain Barrier Transport Study of Pyrilamine Derivatives as Histone Deacetylase Inhibitors Open
We designed and synthesized a pyrilamine derivative 1 as a selective class I HDAC inhibitor that targets pyrilamine-sensitive proton-coupled organic cation antiporter (PYSOCA) at the blood-brain barrier (BBB). Introduction of pyrila…