Výsledky vyhledávání - "Tomoaki Hasui"

Discovery of Pyrazolo[1,5-a]pyrazin-4-ones as Potent and Brain Penetrant GluN2A-Selective Positive Allosteric Modulators Reducing AMPA Receptor Binding Activity

Autor: Fumie Sakurai, Takafumi Yukawa, Asato Kina, Masataka Murakami, Kazuaki Takami, Sachie Morimoto, Masaki Seto, Makoto Kamata, Tohru Yamashita, Kosuke Nakashima, Naohiro Narita, Ezio Bettini, Annarosa Ugolini, Mauro Corsi, Tomoaki Hasui

Publikováno v: Bioorganicmedicinal chemistry. 56

N-Methyl-d-aspartate receptors (NMDARs) are members of the ionotropic glutamate receptor family and play a crucial role in learning and memory by regulating synaptic plasticity. Activation of NMDARs containing GluN2A, one of the NMDAR subunits, has r

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0577fbe36ce276db8c9af5aad210f2b0
https://pubmed.ncbi.nlm.nih.gov/35051811

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Discovery of Potent, Selective, and Brain-Penetrant 1H-Pyrazol-5-yl-1H-pyrrolo[2,3-b]pyridines as Anaplastic Lymphoma Kinase (ALK) Inhibitors

Autor: Imamura Keisuke, Tomoaki Hasui, Y. Hiura, Kumar Singh Saikatendu, Ikuo Fujimori, Morio Murakami, Takeshi Wakabayashi, Tsuyoshi Ishii, Hua Zou, J.D. Lawson, S.W. Lane, Y. Kikko, Masaomi Miyamoto, Hiroshi Imoto, A. Nakatani, M. Kasahara, Youichi Kawakita, Takeshi Kato, Makoto Fushimi

Publikováno v: Journal of Medicinal Chemistry. 62:4915-4935

Anaplastic lymphoma kinase (ALK), a member of the receptor tyrosine kinase family, is predominantly expressed in the brain and implicated in neuronal development and cognition. However, the detailed function of ALK in the central nervous system (CNS)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::105d8ebf76c6528756c5e37999ecf92f
https://doi.org/10.1021/acs.jmedchem.8b01630

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

Autor: Tomoaki Hasui, Nahid Amini, Takanobu Kuroita, Christer Halldin, Ryuji Nakao, Vladimir Stepanov, Akihiro Takano, Shotaro Miura, Kosuke Nakashima, Takahiko Taniguchi, Haruhide Kimura

Publikováno v: Journal of Labelled Compounds and Radiopharmaceuticals. 58:202-208

Phosphodiesterase 10A (PDE10A) is a member of the PDE family of enzymes that degrades cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). Our aim was to label a series of structurally related PDE10A inhibitors with carbon

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e4b1df92eabaa047d2f524dd4e84c506
https://doi.org/10.1002/jlcr.3284

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

Autor: Akina Harada, Kazunori Suzuki, Naomi Kamiguchi, Haruhide Kimura, Christer Halldin, Tomoaki Hasui, Shotaro Miura, Akihiro Takano, Takahiko Taniguchi, Vladimir Stepanov, Tsuyoshi Ishii, Takanobu Kuroita

Publikováno v: Nuclear Medicine and Biology. 42:146-154

Introduction Phosphodiesterase 10A (PDE10A) is a dual-substrate PDE that hydrolyzes both cAMP and cGMP and is selectively expressed in striatal medium spiny neurons. Recent studies have suggested that PDE10A inhibition is a novel approach for the tre

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::16da50c5b394f3f3f37ed12757332689
https://doi.org/10.1016/j.nucmedbio.2014.09.005

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

Autor: Tomoaki Hasui, Christer Halldin, Nahid Amini, Ryuji Nakao, Takahiko Taniguchi, Akihiro Takano, Vladimir Stepanov, Shotaro Miura, Haruhide Kimura

Publikováno v: Nuclear medicine and biology. 57

Introduction Phosphodiesterase 10A (PDE10A) is a member of the PDE enzyme family that degrades cyclic adenosine and guanosine monophosphates (cAMP and cGMP). Based on the successful development of [ 11 C]T-773 as PDE10A positron emission tomography (

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::70696e7dc5d7b53341b9bf513d2d37d0
https://pubmed.ncbi.nlm.nih.gov/29223715

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Design, synthesis, and structure–activity relationships of dihydrofuran-2-one and dihydropyrrol-2-one derivatives as novel benzoxazin-3-one-based mineralocorticoid receptor antagonists

Autor: Lisa A. De Meese, Hideki Matsui, Tomoaki Hasui, Norio Ohyabu, Noriyuki Habuka, Cassandra Gauthier, Boyd Steven Armen, Taiichi Ohra, Satoshi Endo, Shoji Fukumoto, Satoshi Sogabe, Atsushi Mizukami, Kouhei Asano, Tony Pisal Tang, Christopher Stephen Siedem

Publikováno v: Bioorganic & Medicinal Chemistry. 21:5983-5994

Dihydrofuran-2-one and dihydropyrrol-2-one derivatives were identified as novel, potent and selective mineralocorticoid receptor (MR) antagonists by the structure-based drug design approach utilizing the crystal structure of MR/compound complex. Intr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5767cc8f9cdb303d93ba5db42e16aca3
https://doi.org/10.1016/j.bmc.2013.07.043

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Design and synthesis of potent and selective pyridazin-4(1H)-one-based PDE10A inhibitors interacting with Tyr683 in the PDE10A selectivity pocket

Autor: Hideyuki Oki, Takahiko Taniguchi, Tomoaki Hasui, Makoto Fushimi, Masato Yoshikawa, Hironori Kokubo, Jun Kunitomo, Takenori Hitaka, Kosuke Nakashima

Publikováno v: Bioorganicmedicinal chemistry. 24(16)

Utilizing structure-based drug design techniques, we designed and synthesized phosphodiesterase 10A (PDE10A) inhibitors based on pyridazin-4(1H)-one. These compounds can interact with Tyr683 in the PDE10A selectivity pocket. Pyridazin-4(1H)-one deriv

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b445ab10c6d97d93e23106fd2cc873d4
https://pubmed.ncbi.nlm.nih.gov/27301679

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B(OMe)3as a Nonacidic Iminium Ion Generator in Mannich- and Ugi-Type Reactions

Autor: Michinori Suginome, Kousuke Hidaka, Tomoaki Hasui, Yusuke Tanaka

Publikováno v: European Journal of Organic Chemistry. 2009:1148-1151

Mannich-type reactions of aldehydes with secondary amines and a ketene silyl acetal were promoted by trimethoxyborane in DMSO to afford the corresponding β-amino esters in good yields. B(OMe)3 also promoted Ugi-type reactions ofaldehydes with second

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::29eaad4966d5a7c398ee806b34f98387
https://doi.org/10.1002/ejoc.200801190

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