Search Results - "Kumagai, Toshihito"

Receptor binding, behavioral, and electrophysiological profiles of nonpeptide corticotropin-releasing factor subtype 1 receptor antagonists CRA1000 and CRA1001 by Okuyama, S, Chaki, S, Kawashima, N, Suzuki, Y, Ogawa, S, Nakazato, A, Kumagai, T, Okubo, T, Tomisawa, K

“…Receptor binding, behavioral, and electrophysiological profiles of 2-[N-(2-methylthio-4-isopropylphenyl)-N-ethylamino]-4-[4-(3-flu orophe…”
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Synthesis, SARs, and Pharmacological Characterization of 2-Amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Derivatives as Potent, Selective, and Orally Active Group II Metabotropic Glutamate Receptor Agonists by Nakazato, Atsuro, Kumagai, Toshihito, Sakagami, Kazunari, Yoshikawa, Ryoko, Suzuki, Yoshiko, Chaki, Shigeyuki, Ito, Hisanaka, Taguchi, Takeo, Nakanishi, Shigetada, Okuyama, Shigeru

“…(+)-2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (4, LY354740), a highly selective and orally active group II metabotropic glutamate receptor (mGluR)…”
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Scalable Synthesis of (+)-2-Amino-3-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic Acid as a Potent and Selective Group II Metabotropic Glutamate Receptor Agonist by Sakagami, Kazunari, Kumagai, Toshihito, Taguchi, Takeo, Nakazato, Atsuro

“…We successfully synthesized the potent and selective group II mGluR agonist (+)-1 (MGS0008) via a process incorporating the key step of efficient fluorination…”
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In vitro pharmacological profile of nonpeptide CRF1 receptor antagonists, CRA1000 and CRA1001 by CHAKI, S, OKUYAMA, S, NAKAZATO, A, KUMAGAI, T, OKUBO, T, IKEDA, Y, OSHIDA, Y, HAMAJIMA, Y, TOMISAWA, K

“…We investigated pharmacological properties of CRA1000 (2-(N-(2-methylthio-4-isopropylphenyl)-N-ethylamino-4-(4-(3-fluoro…”
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A selective dopamine D4 receptor antagonist, NRA0160: a preclinical neuropharmacological profile by Okuyama, S, Kawashima, N, Chaki, S, Yoshikawa, R, Funakoshi, T, Ogawa, S I, Suzuki, Y, Ikeda, Y, Kumagai, T, Nakazato, A, Nagamine, M, Tomisawa, K

“…NRA0160, 5 - [2- ( 4- ( 3 - fluorobenzylidene) piperidin-1-yl) ethyl] - 4 -(4-fluorophenyl) thiazole-2-carboxamide, has a high affinity for human cloned…”
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Total Syntheses of PI-201 and Related Compounds by Murata, Takeshi, Kumagai, Toshihito, Ishikawa, Makoto, Tadano, Kin-ichi, Ogawa, Seiichiro

“…The thermal intramolecular Diels–Alder cycloaddition of a 2 : 1 mixture of ethyl (2E,8E and Z, 10E,13R)-13-(t-butyldimethylsilyl)…”
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The atypical antipsychotic profile of NRA0045, a novel dopamine D4 and 5‐hydroxytryptamine2A receptor antagonist, in rats by Okuyama, Shigeru, Chaki, Shigeyuki, Kawashima, Naoya, Suzuki, Yoshiko, Ogawa, Shin‐ichi, Kumagai, Toshihito, Nakazato, Atsuro, Nagamine, Masashi, Yamaguchi, Kazumasa, Tomisawa, Kazuyuki

“…The atypical antipsychotic profile of (R)‐(+)‐2‐amino‐4‐(4‐fluorophenyl)‐5‐[1‐[4‐(4‐fluorophenyl)‐4‐oxobutyl] pyrrolidin‐3‐yl] thiazole (NRA0045), a potent…”
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The atypical antipsychotic profile of NRA0045, a novel dopamine D 4 and 5‐hydroxytryptamine 2A receptor antagonist, in rats by Okuyama, Shigeru, Chaki, Shigeyuki, Kawashima, Naoya, Suzuki, Yoshiko, Ogawa, Shin‐ichi, Kumagai, Toshihito, Nakazato, Atsuro, Nagamine, Masashi, Yamaguchi, Kazumasa, Tomisawa, Kazuyuki

“…The atypical antipsychotic profile of ( R )‐(+)‐2‐amino‐4‐(4‐fluorophenyl)‐5‐[1‐[4‐(4‐fluorophenyl)‐4‐oxobutyl] pyrrolidin‐3‐yl] thiazole (NRA0045), a potent…”
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Chemical modification of aryl-1,2,3,6-tetrahydropyridinopyrimidine derivative to discover corticotropin-releasing factor1 receptor antagonists Aryl-1,2,3,6-tetrahydropyridino-purine, -3H-1,2,3-triazolo[4,5-d]pyrimidine, -purin-8-one, and -7H-pyrrolo[2,3-d]pyrimidine derivatives by Kumagai, T

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Synthesis and structure–affinity relationships of 4-(5-Aryl-1,2,3,6-tetrahydropyridino)pyrimidine derivatives as corticotropin-releasing factor1 receptor antagonists by Kumagai, T

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In vitro and in vivo receptor binding profile of NRA0161 and NRA0562, novel atypical antipsychotics by Funakoshi, Takeo, Chaki, Shigeyuki, Yoshikakwa, Ryoko, Okuyama, Shigeru, Nakazato, Atsuro, Kumagai, Toshihito, Nagamine, Masashi, Tomisawa, Kazuyuki

“…Both NRA0161 and NRA0562 showed high affinities for dopamine D_4.2 , D_3 and 5-HT_2A receptors with K_i ：values of 1.00, 3.12 and 2.52 nM (NRA0161), and 1.44,…”
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Behavioral and electrophysiological characterization of NRA0160 and NRA0215 in mice and rats by Suzuki, Yoshiko, Kawashima, Naoya, Chaki, Shigeyuki, Okuyama, Shigeru, Ikeda, Yoko, Kumagai, Toshihito, Nakazato, Atsuro, Nagamine, Masashi, Yoshida, Masanori, Tomisawa, Kazuyuki

“…NRA0160 has a selective and high affinity for dopamine D_4 receptor and NRA0215 has a high affinity for dopamine D_4 receptor, serotonin (5-HT)_2A receptor and…”
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In vivo receptor occupancy of an atypical antipsychotic, NRA0045, in rats by Chaki, Shigeyuki, Funakoshi, Takeo, Yoshikawa, Ryoko, Okuyama, Shigeru, Ikeda, Yoko, Kumagai, Toshihito, Nakazato, Atsuro, Nagamine, Masashi, Yoshida, Masanori, Tomisawa, Kazuyuki

“…In vivo receptor occupancy of NRA0045 was assessed by in vivo receptor binding using [^^3 H]spiperone, [^^3 H] MDL100,907 and [^^3 H]YM-09151-2 as…”
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In vitro and in vivo pharmacological profile of 5-{2-[4-(6-fluoro-1H-indole-3-yl)piperidin-1-yl]ethyl}-4-(4-fluorophenyl)thiazole-2-carboxylic acid amide (NRA0562), a novel and putative atypical antipsychotic by Funakoshi, Takeo, Chaki, Shigeyuki, Kawashima, Naoya, Suzuki, Yoshiko, Yoshikawa, Ryoko, Kumagai, Toshihito, Nakazato, Atsuro, Kameo, Kazuya, Goto, Makoto, Okuyama, Shigeru

“…In vitro and in vivo pharmacological properties of 5-{2-[4-(6-fluoro-1H-indole-3-yl)piperidin-1-yl]ethyl}-4-(4-fluorophenyl)thiazole-2-carboxylic acid amide…”
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Effects of (R)-(+)-2-amino-4-(4-nuorophenyl)-5-[1-[4-(4-fluorophenyl) - 4 - oxoburyl] Pyrrolidin - 3 yl] thiazole (NRA0045) on the neuronal activity of dopamine neurons in rats by Kawashima, Naoya, Okuyama, Shigeru, Chaki, Shigeyuki, Ikeda, Yoke, Kumagai, Toshihito, Nakazato, Atsuro, Nagamine, Masashi, Yoshida, Masanori, Tomisawa, Kazuyuki

“…NRA0045 is a potent dopamine D_4 and serotonin (5-HT)_2A receptor antagonist. The firing rate of the A9 or A10 dopamine neurons was inhibited by…”
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Synthesis and SAR of 1-Alkyl-2-phenylethylamine Derivatives Designed from N,N-Dipropyl-4-methoxy-3-(2-phenylethoxy)phenylethylamine To Discover σ1 Ligands by Nakazato, Atsuro, Kumagai, Toshihito, Ohta, Kohmei, Chaki, Shigeyuki, Okuyama, Shigeru, Tomisawa, Kazuyuki

“…The synthesis and structure−activity relationships (SAR) of 1-alkyl-2-phenylethylamine derivatives 5−8 designed from…”
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In vitro and in vivo pharmacological profile of 4-(4-fluorobenzylidene)-1-[2-[5-(4-fluorophenyl)-1H-pyrazol-4-yl] ethyl] piperidine (NRA0161) by Suzuki, Yoshiko, Funakoshi, Takeo, Chaki, Shigeyuki, Kawashima, Naoya, Ogawa, Shin, Kumagai, Toshihito, Nakazato, Atsurou, Komurasaki, Toshi, Okuyama, Shigeru

“…Atypical antipsychotic properties of 4-(4-fluorobenzylidene)-1-[2-[5-(4-fluorophenyl)-1H-pyrazol-4-yl]ethyl] piperidine (NRA0161) were investigated by in vitro…”
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Atypical antipsychotic profile of NRA0160 and NRA0215 in rats by Ogawa, Shin-ichi, Okuyama, Shigeru, Suzuki, Yoshiko, Chaki, Shigeyuki, Ikeda, Yoko, Kumagai, Toshihito, Nakazato, Atsuro, Nagamine, Masashi, Yoshida, Masanori, Tomisawa, Kazuyuki

“…NRA0160 has a selective and high affinity for dopamine D_4 receptor and NRA0215 has a high affinity for dopamine D_4 receptor and serotonin (5-HT)_2A receptor…”
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Design, synthesis and structure-affinity relationships of 4-methylidenepiperidine and 4-aryl-1,2,3,6-tetrahydropyridine derivatives as corticotropin-releasing factor1 receptor antagonists by Nakazato, A, Kumagai, T, Okubo, T, Tanaka, H, Chaki, S, Okuyama, S, Tomisawa, K

“…Recently, various non-peptide corticotropin-releasing factor1 (CRF1) receptor antagonists have been reported. Structure-affinity relationships (SARs) of…”
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In vitro and in vivo pharmacological profile of 5-[2-[4-(6-fluoro-1H-indole-3-yl)piperidin-1-yl]ethyl]-4-(4-fluorophenyl)thiazole-2-carboxylic acid amide (NRA0562), a novel and putative atypical antipsychotic by Funakoshi, Takeo, Chaki, Shigeyuki, Kawashima, Naoya, Suzuki, Yoshiko, Yoshikawa, Ryoko, Kumagai, Toshihito, Nakazato, Atsuro, Kameo, Kazuya, Goto, Makoto, Okuyama, Shigeru

“…In vitro and in vivo pharmacological properties of 5-[2-[4-(6-fluoro-1H-indole-3-yl)piperidin-1-yl]ethyl]-4-(4-fluorophenyl)thiazole-2-carboxylic acid amide…”
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