H. Kimura

发表

Macrophage Migration Inhibitory Factor as an Emerging Drug Target to Regulate Antioxidant Response Element System

M. Takizawa, H. Yukitake, H. Kimura, 2017, Oxidative medicine and cellular longevity.

BTZO-1, a cardioprotective agent, reveals that macrophage migration inhibitory factor regulates ARE-mediated gene expression.

H. Oki, M. Takizawa, S. Tanida, 2010, Chemistry & biology.

TAK-063, a phosphodiesterase 10A inhibitor, modulates neuronal activity in various brain regions in phMRI and EEG studies with and without ketamine challenge

Steven C. R. Williams, D. Cash, C. Simmons, 2016, Neuroscience.

TAK‐063, a novel PDE10A inhibitor with balanced activation of direct and indirect pathways, provides a unique opportunity for the treatment of schizophrenia

H. Kimura, Kazunori Suzuki, 2018, CNS neuroscience & therapeutics.

A strategy to improve the success rate of CNS drug development: TAK-063, a novel PDE10A inhibitor, as a case study.

H. Kimura, 2017, Nihon yakurigaku zasshi. Folia pharmacologica Japonica.

Therapeutic potential of TAK-071, a muscarinic M1 receptor positive allosteric modulator with low cooperativity, for the treatment of cognitive deficits and negative symptoms associated with schizophrenia

Ryuji Yamada, H. Kimura, Emi Kurimoto, 2021, Neuroscience Letters.

Investigating the Therapeutic Potential of LSD1 Enzyme Activity-Specific Inhibition by TAK-418 for Social and Memory Deficits in Rodent Disease Models.

H. Kimura, Yukiko Yamamoto, Rina Baba, 2022, ACS chemical neuroscience.

Design, synthesis, and structure-activity relationship of TAK-418 and its derivatives as a novel series of LSD1 inhibitors with lowered risk of hematological side effects.

H. Oki, S. Iwasaki, S. Morimoto, 2022, European journal of medicinal chemistry.

BTZO-15, an ARE-Activator, Ameliorates DSS- and TNBS-Induced Colitis in Rats

M. Takizawa, Yoshimi Sato, T. Imaeda, 2011, PloS one.

TAK-925, an orexin 2 receptor-selective agonist, shows robust wake-promoting effects in mice

Y. Shimizu, Mitsuhiro Ito, H. Yukitake, 2019, Pharmacology Biochemistry and Behavior.

Translational Development Strategies for TAK-063, a Phosphodiesterase 10A Inhibitor

H. Kimura, K. Asin, Kazunori Suzuki, 2020, International Journal of Neuropsychopharmacology.

Development of two fluorine-18 labeled PET radioligands targeting PDE10A and in vivo PET evaluation in nonhuman primates.

Tomoaki Hasui, T. Taniguchi, C. Halldin, 2018, Nuclear medicine and biology.

Danavorexton, a selective orexin 2 receptor agonist, provides a symptomatic improvement in a narcolepsy mouse model

H. Kimura, Ayumi Kawano, T. Ishikawa, 2022, Pharmacology Biochemistry and Behavior.

Orexin 2 receptor–selective agonist danavorexton improves narcolepsy phenotype in a mouse model and in human patients

C. Davies, E. Mignot, Y. Dauvilliers, 2022, Proceedings of the National Academy of Sciences of the United States of America.

Orexin 2 receptor (OX2R) protein distribution measured by autoradiography using radiolabeled OX2R-selective antagonist EMPA in rodent brain and peripheral tissues

H. Kimura, K. Mitsukawa, 2021, Scientific Reports.

Balanced Activation of Striatal Output Pathways by Faster Off-Rate PDE10A Inhibitors Elicits Not Only Antipsychotic-Like Effects But Also Procognitive Effects in Rodents

Nidhi Kaushal, H. Kimura, Kazunori Suzuki, 2019, The international journal of neuropsychopharmacology.

TAK-137, an AMPA receptor potentiator with little agonistic effect, produces antidepressant-like effect without causing psychotomimetic effects in rats

K. Murakami, H. Kimura, Yasukazu Tajima, 2019, Pharmacology Biochemistry and Behavior.

Role of the AMPA receptor in antidepressant effects of ketamine and potential of AMPA receptor potentiators as a novel antidepressant

H. Kimura, A. Suzuki, Hiroe Hara, 2022, Neuropharmacology.

Design, Synthesis, and Evaluation of [18F]T-914 as a Novel Positron-Emission Tomography Tracer for Lysine-Specific Demethylase 1.

G. Tamagnan, O. Barret, C. Sandiego, 2021, Journal of medicinal chemistry.

The chondroprotective agent ITZ-1 inhibits interleukin-1beta-induced matrix metalloproteinase-13 production and suppresses nitric oxide-induced chondrocyte death.

Kiyofumi Yamada, M. Takizawa, H. Yukitake, 2009, Journal of pharmacological sciences.

The phosphodiesterase 10A selective inhibitor, TAK-063, induces c-Fos expression in both direct and indirect pathway medium spiny neurons and sub-regions of the medial prefrontal cortex in rats

H. Kimura, Sayuri Nakamura, A. Nakatani, 2017, Neuroscience Research.

Characterization of the binding properties of T-773 as a PET radioligand for phosphodiesterase 10A.

Christer Halldin, Vladimir Stepanov, Akihiro Takano, 2015, Nuclear medicine and biology.

Molecular Imaging of PDE10A Knockout Mice with a Novel PET Radiotracer: [11C]T-773

B. Gulyás, T. Taniguchi, C. Halldin, 2015, Molecular Imaging and Biology.

A homozygous loss‐of‐function mutation in PDE2A associated to early‐onset hereditary chorea

C. Davies, S. Efthymiou, H. Houlden, 2018, Movement disorders : official journal of the Movement Disorder Society.

An Approach to Discovering Novel Muscarinic M1 Receptor Positive Allosteric Modulators with Potent Cognitive Improvement and Minimized Gastrointestinal Dysfunction

Y. Shimizu, H. Kimura, Takahiro Sugimoto, 2018, The Journal of Pharmacology and Experimental Therapeutics.

Discovery of 1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one (TAK-063), a highly potent, selective, and orally active phosphodiesterase 10A (PDE10A) inhibitor.

Hironori Kokubo, Makoto Fushimi, Kosuke Nakashima, 2014, Journal of medicinal chemistry.

A novel Na+‐Independent alanine‐serine‐cysteine transporter 1 inhibitor inhibits both influx and efflux of D‐Serine

M. Yoshikawa, H. Kimura, K. Sakimura, 2016, Journal of neuroscience research.

ITZ-1, a client-selective Hsp90 inhibitor, efficiently induces heat shock factor 1 activation.

Takashi Ito, M. Takizawa, Y. Yoneda, 2010, Chemistry & biology.

Preferential enhancement of GluN2B-containing native NMDA receptors by the endogenous modulator 24S-hydroxycholesterol in hippocampal neurons

I. Módy, H. Kimura, Toshiya Nishi, 2019, Neuropharmacology.

BTZO-2, an antioxidant response element-activator, provides protection against lethal endotoxic shock in mice.

M. Takizawa, S. Tanida, Yoshimi Sato, 2013, European journal of pharmacology.

Strategies for Utilizing Neuroimaging Biomarkers in CNS Drug Discovery and Development: CINP/JSNP Working Group Report

Hiroshi Ito, Yasumasa Okamoto, Shigeto Yamawaki, 2016, The international journal of neuropsychopharmacology.

De Novo Mutations in PDE10A Cause Childhood-Onset Chorea with Bilateral Striatal Lesions

L. Vissers, J. Hardy, C. Davies, 2016, American journal of human genetics.

The Phosphodiesterase 10A Selective Inhibitor TAK-063 Improves Cognitive Functions Associated with Schizophrenia in Rodent Models

H. Kimura, N. Suzuki, Kazunori Suzuki, 2016, The Journal of Pharmacology and Experimental Therapeutics.

In Vivo Pharmacological Characterization of TAK-063, a Potent and Selective Phosphodiesterase 10A Inhibitor with Antipsychotic-Like Activity in Rodents

Haruhide Kimura, Akina Harada, Kazunori Suzuki, 2015, The Journal of Pharmacology and Experimental Therapeutics.

T-448, a specific inhibitor of LSD1 enzyme activity, improves learning function without causing thrombocytopenia in mice

H. Oki, R. Hara, S. Iwasaki, 2018, Neuropsychopharmacology.

Role of the AMPA receptor in antidepressant effects of ketamine and potential of AMPA receptor potentiators as a novel antidepressant

H. Kimura, Hiroe Hara, Atsushi Suzuki, 2022, Neuropharmacology.

Strictly regulated agonist-dependent activation of AMPA-R is the key characteristic of TAK-653 for robust synaptic responses and cognitive improvement

S. Sogabe, Y. Kosugi, T. Kaku, 2021, Scientific Reports.

Electrophysiological characterization of a novel AMPA receptor potentiator, TAK-137, in rat hippocampal neurons

H. Kimura, Yasukazu Tajima, A. Kunugi, 2019, Neuroscience Letters.

Preclinical characterization of AMPA receptor potentiator TAK‐137 as a therapeutic drug for schizophrenia

H. Kimura, N. Suzuki, Motohisa Suzuki, 2019, Pharmacology research & perspectives.

TAK-137, an AMPA-R potentiator with little agonistic effect, has a wide therapeutic window

S. Sogabe, Y. Kosugi, T. Kaku, 2018, Neuropsychopharmacology.

HBT1, a Novel AMPA Receptor Potentiator with Lower Agonistic Effect, Avoided Bell-Shaped Response in In Vitro BDNF Production

S. Sogabe, H. Kimura, Yasukazu Tajima, 2018, The Journal of Pharmacology and Experimental Therapeutics.

Novel AMPA Receptor Potentiators TAK-137 and TAK-653 as Potential Rapid-Acting Antidepressants

H. Kimura, 2021, Contemporary Clinical Neuroscience.

LSD1 enzyme inhibitor TAK-418 unlocks aberrant epigenetic machinery and improves autism symptoms in neurodevelopmental disorder models

H. Oki, S. Igaki, Ryuji Yamada, 2021, Science Advances.

TAK-653, an AMPA receptor potentiator with minimal agonistic activity, produces an antidepressant-like effect with a favorable safety profile in rats

Ryuji Yamada, H. Kimura, Yasukazu Tajima, 2021, Pharmacology Biochemistry and Behavior.

TAK-071, a muscarinic M1 receptor positive allosteric modulator, attenuates scopolamine-induced quantitative electroencephalogram power spectral changes in cynomolgus monkeys

H. Kimura, Motohisa Suzuki, Emi Kurimoto, 2018, bioRxiv.

Design and synthesis of a novel 2-oxindole scaffold as a highly potent and brain-penetrant phosphodiesterase 10A inhibitor.

M. Yoshikawa, J. Kunitomo, H. Kokubo, 2015, Bioorganic & medicinal chemistry.

Brain PET measurement of PDE10A occupancy by TAK‐063, a new PDE10A inhibitor, using [11C]T‐773 in nonhuman primates

Christer Halldin, Vladimir Stepanov, Ryuji Nakao, 2016, Synapse.

In Vivo Pharmacological Comparison of TAK-071, a Positive Allosteric Modulator of Muscarinic M1 Receptor, and Xanomeline, an Agonist of Muscarinic M1/M4 Receptor, in Rodents

H. Kimura, Motohisa Suzuki, Emi Kurimoto, 2019, Neuroscience.

Orexin 2 receptor‐selective agonist danavorexton (TAK‐925) promotes wakefulness in non‐human primates and healthy individuals

Yaming Hang, H. Faessel, H. Yukitake, 2023, Journal of sleep research.

Combined treatment with a selective PDE10A inhibitor TAK‐063 and either haloperidol or olanzapine at subeffective doses produces potent antipsychotic‐like effects without affecting plasma prolactin levels and cataleptic responses in rodents

M. Corsi, A. Ugolini, Clizia Capuani, 2017, Pharmacology research & perspectives.

TAK-063, a PDE10A Inhibitor with Balanced Activation of Direct and Indirect Pathways, Provides Potent Antipsychotic-Like Effects in Multiple Paradigms

M. Miyamoto, H. Kimura, Hirobumi Suzuki, 2016, Neuropsychopharmacology.

Phosphodiesterase 10A Inhibition Leads to Brain Region-Specific Recovery Based on Stroke Type

Morteza Dehghani, S. Carmichael, H. Kimura, 2020, Translational Stroke Research.

T‐495, a novel low cooperative M1 receptor positive allosteric modulator, improves memory deficits associated with cholinergic dysfunction and is characterized by low gastrointestinal side effect risk

M. Fushimi, Y. Shimizu, M. Miyamoto, 2020, Pharmacology research & perspectives.

0141 A Novel, Orally Available Orexin 2 Receptor-Selective Agonist, TAK-994, Shows Wake-Promoting Effects Following Chronic Dosing in an Orexin-Deficient Narcolepsy Mouse Model

H. Kimura, Motohisa Suzuki, T. Ishikawa, 2020 .

Discovery of a novel, orally available Orexin 2 receptor-selective agonist, TAK-994, as a therapeutic drug for narcolepsy

M. Suzuki, H. Kimura, Y. Kajita, 2019 .

A novel, orally available orexin 2 receptor-selective agonist, tak-994, ameliorates narcolepsy-like symptoms in narcolepsy mouse models

M. Suzuki, H. Kimura, T. Ishikawa, 2019 .

0055 An Orexin 2 Receptor-selective Agonist, TAK-925, Ameliorates Narcolepsy-like Symptoms and Obesity in Orexin/ataxin-3 Transgenic Mice

H. Yukitake, H. Kimura, Motohisa Suzuki, 2019, Sleep.

HBT1, a novel AMPA receptor potentiator with lower agonistic effect, avoided bell-shaped response in in vitro BDNF production.

S. Sogabe, H. Kimura, Yasukazu Tajima, 2018 .

TAK-071, a novel M1 positive allosteric modulator with low cooperativity, improves cognitive function in rodents with few cholinergic side effects

Y. Shimizu, M. Yamada, H. Kimura, 2018, Neuropsychopharmacology.

Evaluation of a novel PDE10A PET radioligand, [11C]T‐773, in nonhuman primates: Brain and whole body PET and brain autoradiography

Christer Halldin, Vladimir Stepanov, Ryuji Nakao, 2015, Synapse.

Characterization of Binding and Inhibitory Properties of TAK-063, a Novel Phosphodiesterase 10A Inhibitor

Maki Miyamoto, Kosuke Nakashima, T. Taniguchi, 2015, PloS one.

Diurnal Fluctuations of Orexin-A and -B in Cynomolgus Monkey Cerebrospinal Fluid Determined by a Novel Analytical Method Using Antiadsorptive Additive Treatment Followed by Nanoflow Liquid Chromatography–High-Resolution Mass Spectrometry

Ryuji Yamada, H. Kimura, M. Kakehi, 2023, ACS chemical neuroscience.

Role of tissue plasminogen activator in the sensitization of methamphetamine‐induced dopamine release in the nucleus accumbens

T. Nabeshima, Hyoung‐Chun Kim, H. Mizoguchi, 2008, Journal of neurochemistry.

Inhibition of KDM1A activity restores adult neurogenesis and improves hippocampal memory in a mouse model of Kabuki syndrome

H. Bjornsson, E. Pich, J. Dunlop, 2020, bioRxiv.

Nucleus accumbens pathways control cell-specific gene expression in the medial prefrontal cortex

A. Sawa, T. Hikida, H. Toyoshiba, 2020, Scientific Reports.

TAK-994, a Novel Orally Available Brain-Penetrant Orexin 2 Receptor-Selective Agonist, Suppresses Fragmentation of Wakefulness and Cataplexy-Like Episodes in Mouse Models of Narcolepsy

K. Tohyama, H. Kimura, T. Koike, 2023, The Journal of Pharmacology and Experimental Therapeutics.

TAK-063, a Novel Phosphodiesterase 10A Inhibitor, Protects from Striatal Neurodegeneration and Ameliorates Behavioral Deficits in the R6/2 Mouse Model of Huntington’s Disease

H. Kimura, Kazunori Suzuki, A. Harada, 2017, The Journal of Pharmacology and Experimental Therapeutics.

Chronic cerebral hypoperfusion by permanent internal carotid ligation produces learning impairment without brain damage in rats

H. Nishikawa, M. Miyamoto, M. Miyamoto, 1997, Neuroscience.

Nucleus accumbens pathways control cell-specific gene expression in the medial prefrontal cortex

A. Sawa, T. Hikida, Tom Macpherson, 2020, Scientific Reports.

Development of a series of novel carbon-11 labeled PDE10A inhibitors.

Christer Halldin, Vladimir Stepanov, Ryuji Nakao, 2015, Journal of labelled compounds & radiopharmaceuticals.