Zobrazeno 1 - 10
of 25
pro vyhledávání: '"Shuzo Takehara"'
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:1245-1250
(R)-N-(1-Benzyl-2-pyrrolidinylmethyl)-6-methylthio-3,4-dihydro-2H-1,4-benzoxazine-8-carboxamide exhibited high affinities for all of D2, 5-HT1 A, and 5-HT2 receptors (Ki=0.0042 μM, Ki=0.017 μM, and Ki=0.027 μM, respectively).
Autor:
K. Inaba, Masamitsu Sakamori, Mitsuyoshi Yasumoto, Takanobu Kuroita, Takeshi Kawakita, Shuzo Takehara
Publikováno v:
Chemical and Pharmaceutical Bulletin. 42:95-100
A series of N-(azabicyclo-3-yl)-2,3-dihydrobenzofuran-7-carboxamide derivatives were synthesized and evaluated for serotonin-3 (5-HT3) receptor antagonistic activities assessed by 5-HT3 receptor binding (in vitro) and by the ability to antagonize the
Publikováno v:
Folia Pharmacologica Japonica. 100:137-142
The binding of Y-25130 on serotonin 3 (5-HT3) receptors was evaluated by examining its effect on 3H-BRL 43694 (3H-granisetron) binding to rat cerebral cortex membranes in comparison with those of granisetron, ondansetron and metoclopramide. Y-25130,
Autor:
Yasuto Morimoto, Tohru Nakao, Minoru Obata, Takashi Yakushiji, Tetsuya Tahara, Kenji Morita, Hiroshi Tanaka, Shuzo Takehara, Minoru Kawakami
Publikováno v:
Chemical and Pharmaceutical Bulletin. 39:2556-2563
A series of 2-aryl-5,6-dihydro-(1)benzothiepino[5,4-c]pyridazin-3(2H)- ones and related compounds were synthesized and evaluated for their ability to displace 3H-diazepam from rat brain membranes in vitro, and to prevent bicuculline induced convulsio
Publikováno v:
YAKUGAKU ZASSHI. 110:922-931
A series of 6H-(1)benzothiopyrano[3,4-e][1,2,4]triazolo[4,3- b]pyridazines and 6,7-dihydro-(1)benzothiepino[4,5- e][1,2,4]triazolo [4,3-b]pyridazines were prepared and tested for their ability to displace [3H] diazepam from rat brain membranes. An ap
Autor:
Shuzo Takehara, Hiroshi Yasumatsu, Toshihiko Morimoto, Masatake Fujimura, Kenji Hashimoto, Koreichi Kimura, Makoto Kuriyama, Keiji Yamagami, Hiroshi Tanaka
Publikováno v:
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 26(4)
The neuropharmacological profile of Y-931, 8-fluoro-12- (4-methylpiperazin-1-yl)- 6H-[1]benzothieno [2,3-b][1,5]benzodiazepine maleate, was investigated in comparison with those of typical and claimed atypical antipsychotic drugs. Similar to clozapin
N-((1-long alkyl-2-pyrrolidinyl) methyl) benzamides with potent serotonin 5-HT1A receptor affinities
Publikováno v:
Chemical and Pharmaceutical Bulletin. 39:3370-3372
A series of N-(2-pyrrolidinylmethyl)-2-methoxy-5-sulfamoylbenzamide derivatives bearing a long alkyl chain at the 1-position of the pyrrolidine ring was synthesized and found to possess high affinities for serotonin 5-HT1A receptors.
Autor:
Yasuto Morimoto, Michihide Setoguchi, Hiroshi Yasumatsu, Shuzo Takehara, Yoshinobu Yamamoto, Tohru Nakao, Takemi Fukuda
Publikováno v:
British journal of pharmacology. 111(4)
1. The pharmacological properties of a benzodiazepine receptor (BZR) partial agonist, Y-23684 were investigated in comparison with those of diazepam, a conventional BZR full agonist. 2. Y-23684 and diazepam showed high and selective affinity for the
Autor:
Futoshi Takao, Minoru Maeda, Watanabe K, Toshimitsu Fukumura, Shigeki Sasaki, Shuzo Takehara, Norihiro Obana
Publikováno v:
Chemicalpharmaceutical bulletin. 41(2)
New fluorinated ligands with N-[(1-ethyl-2-pyrrolidinyl)methyl]-2, 3-dihydrobenzofuran-7-carboxamide skeleton, which are useful as a prototype to develop 18F labelled in vivo radiotracer for positron emission tomography (PET), were synthesized, and t
Publikováno v:
Japanese journal of pharmacology. 59(4)
This paper describes the 5-hydroxytryptamine3 (5-HT3) receptor antagonism of Y-25130 ((+-)-N-(1-azabicyclo[2.2.2]oct-3-yl)-6-chloro-4-methyl-3-oxo-3,4-dih yd ro- 2H-1,4-benzoxazine-8-carboxamide monohydrochloride) in the rat cerebral cortex, isolated