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Gaku Sakaguchi

RIKEN Brain Science Institute

66

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Discovery of Atabecestat (JNJ-54861911): A Thiazine-Based β-Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor Advanced to the Phase 2b/3 EARLY Clinical Trial

2021 Journal of Medicinal Chemistry
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Post-stroke pain caused by peripheral sensory hypersensitization after transient focal cerebral ischemia in rats

2019 Brain Research
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Discovery of an Extremely Potent Thiazine-Based β-Secretase (BACE1) Inhibitor with Reduced Cardiovascular and Liver Toxicity at a Low Projected Human Dose

2019 Journal of Medicinal Chemistry
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Mice deficient in protein tyrosine phosphatase receptor type Z (PTPRZ) show reduced responsivity to methamphetamine despite an enhanced response to novelty

2019 PLOS ONE
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Ibudilast produces anti-allodynic effects at the persistent phase of peripheral or central neuropathic pain in rats: Different inhibitory mechanism on spinal microglia from minocycline and propentofylline

2018 European Journal of Pharmacology
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Structure of BACE1 in complex with N-(3-((4R,5R,6S)-2-amino-6-(1,1-difluoroethyl)-5-fluoro-4-methyl-5,6-dihydro-4H-1,3-oxazin-4-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide

2018
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Rational Design of Novel 1,3-Oxazine Based β-Secretase (BACE1) Inhibitors: Incorporation of a Double Bond To Reduce P-gp Efflux Leading to Robust Aβ Reduction in the Brain

2018 Journal of Medicinal Chemistry
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Suppression of the acute upregulation of phosphorylated-extracellular regulated kinase in ventral tegmental area by a μ-opioid receptor agonist is related to resistance to rewarding effects in a mouse model of bone cancer.

2017 Journal of Pharmacological Sciences
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PRECLINICAL MULTI-SPECIES PHARMACOKINETIC/PHARMACODYNAMIC ANALYSIS OF THE ORAL BACE INHIBITOR JNJ-54861911

2017 Alzheimers & Dementia
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Pharmacological evaluation of novel (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives as TRPV4 antagonists for the treatment of pain

2017 Bioorganic & Medicinal Chemistry
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