Zobrazeno 1 - 10
of 55
pro vyhledávání: '"Akito Yasuhara"'
Autor:
Hirohiko Hikichi, Tetsuaki Hiyoshi, Toshiyuki Marumo, Yasumitsu Tomishima, Ayaka Kaku, Izumi Iida, Hiroki Urabe, Tomoko Tamita, Akito Yasuhara, Jun-ichi Karasawa, Shigeyuki Chaki
Publikováno v:
Journal of Pharmacological Sciences, Vol 127, Iss 3, Pp 352-361 (2015)
Glutamatergic dysfunction has been implicated in psychiatric disorders such as schizophrenia. The stimulation of metabotropic glutamate (mGlu) 2 receptor has been shown to be effective in a number of animal models of schizophrenia. In this study, we
Externí odkaz:
https://doaj.org/article/b56722cac0fc4fd59c23db537c537189
Autor:
Akito Yasuhara, Daiji Kambe, Shuji Yamamoto, Kumi Abe, Yasunori Kawakita, Minoru Moriya, Hiroshi Ohta, Naohiro Tsukiyama
Publikováno v:
CHEMICAL & PHARMACEUTICAL BULLETIN. 64:1630-1640
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 orally available glycine transporter 1 (GlyT1) inhibitor. In this artic
Autor:
Shuji, Yamamoto, Hiroshi, Ohta, Kumi, Abe, Daiji, Kambe, Naohiro, Tsukiyama, Yasunori, Kawakita, Minoru, Moriya, Akito, Yasuhara
Publikováno v:
Chemicalpharmaceutical bulletin. 64(11)
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 orally available glycine transporter 1 (GlyT1) inhibitor. In this artic
Autor:
Akito Yasuhara, Shigeyuki Chaki
Publikováno v:
The Open Medicinal Chemistry Journal
Metabotropic glutamate receptors (mGlu receptors) have emerged as new therapeutic targets for psychiatric disorders, such as schizophrenia, depression and anxiety with their regulatory roles in glutamatergic transmissions. To date, several ligands se
Autor:
Izumi Iida, Yasumitsu Tomishima, Hiroki Urabe, Ayaka Kaku, Toshiyuki Marumo, Akito Yasuhara, Hirohiko Hikichi, Jun-ichi Karasawa, Tomoko Tamita, Shigeyuki Chaki, Tetsuaki Hiyoshi
Publikováno v:
Journal of Pharmacological Sciences, Vol 127, Iss 3, Pp 352-361 (2015)
Glutamatergic dysfunction has been implicated in psychiatric disorders such as schizophrenia. The stimulation of metabotropic glutamate (mGlu) 2 receptor has been shown to be effective in a number of animal models of schizophrenia. In this study, we
Autor:
Atsuro Nakazato, Akito Yasuhara, Koji Yoshida, Yasunori Kawakita, Kazunari Sakagami, Yoshiki Fukasawa, Masato Nakamura
Publikováno v:
Drug Metabolism and Disposition. 34:369-374
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 receptors. However, the oral bioavailability of MGS0039 is 10.9% in ra
Publikováno v:
Tetrahedron Letters. 43:6579-6582
The cyclization reaction of ethynylanilines having phenyl, alkyl, methoxy, cyano, chloro, and ethoxycarbonyl groups with (polystyrylmethyl)trimethylammonium fluoride in dry MeCN under an argon atmosphere at 100°C proceeded in good yields to give the
Autor:
Yasumitsu Tomishima, Izumi Iida, Tetsuaki Hiyoshi, Hirohiko Hikichi, Akito Yasuhara, Toshiyuki Marumo, Shigeyuki Chaki, Tomoko Tamita, Hiroki Urabe, Jun-ichi Karasawa
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 351(3)
Excess glutamatergic neurotransmission has been implicated in the pathophysiology of schizophrenia, and the activation of metabotropic glutamate 2 (mGlu2) receptor may exert antipsychotic effects by normalizing glutamate transmission. In the present
Publikováno v:
Tetrahedron. 57:9697-9710
The regioselectivity of the cyclization reaction of 2-ethynylbenzyl alcohol and 2-ethynylbenzylamine derivatives promoted by TBAF was investigated. Six-membered ring derivatives were obtained from the compounds, which have a butyl group on the triple
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:2511-2514
6-alpha-methylpenicillin N was synthesised via known routes from 6-aminopenicillanic acid, and tested as a substrate for recombinant DAOCS and DAOC/DACS. Incubation with DAOCS resulted in conversion of 2-oxoglutarate without oxidation of the penicill