Výsledky vyhledávání - "Taketoshi Okubo"

Synthesis of Diphenylmethyl Analogues and Their Affinity for the Melanocortin-4 Receptor and the Serotonin Transporter

Autor: Dai Nozawa, Shigeru Okuyama, Shigeyuki Chaki, Taketoshi Okubo, Atsuro Nakazato, Takaaki Ishii

Publikováno v: Chemical and Pharmaceutical Bulletin. 55:1044-1050

While examining antagonists of the melanocortin-4 receptor (MC4 receptor), we found that compound 12b, containing a diphenylmethyl moiety, had a relatively high affinity for the MC4 receptor. When diphenylmethyl analogues were further examined, compo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::73541f624af909bf057b5251fe701e4e
https://doi.org/10.1248/cpb.55.1044

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Identification of Arginine Analogues as Antagonists and Agonists for the Melanocortin-4 Receptor

Autor: Atsuro Nakazato, Dai Nozawa, Shigeru Okuyama, Taketoshi Okubo, Shigeyuki Chaki

Publikováno v: Chemical and Pharmaceutical Bulletin. 55:1232-1239

In the present study, conducted to explore potent and small molecular melanocortin-4 (MC4) receptor ligands, we found that tripeptide 3a, containing a D-Phe-Arg-2-Nal (Nal; naphthylalanine) sequence, exhibited a moderate affinity for the MC4 receptor

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3b7f0cf69ce56cc123240a05a19b9a20
https://doi.org/10.1248/cpb.55.1232

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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 factor 1 receptor antagonists

Autor: Hideo Tanaka, Toshihito Kumagai, Kazuyuki Tomisawa, Atsuro Nakazato, Shigeyuki Chaki, Shigeru Okuyama, Taketoshi Okubo

Publikováno v: Bioorganic & Medicinal Chemistry. 8:1183-1193

Recently, various non-peptide corticotropin-releasing factor1 (CRF1) receptor antagonists have been reported. Structure-affinity relationships (SARs) of non-peptide CRF antagonists suggest that such antagonists can be constructed of three units: a hy

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bc41c3b5ac785cf7e6857ff73227a5b0
https://doi.org/10.1016/s0968-0896(00)00045-6

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Binding characteristics of DAA1106, a novel and selective ligand for peripheral benzodiazepine receptors

Autor: Masashi Nagamine, Shigeru Okuyama, Takeo Funakoshi, Shigeyuki Chaki, Ryoko Yoshikawa, Taketoshi Okubo, Kazuyuki Tomisawa, Atsuro Nakazato

Publikováno v: European Journal of Pharmacology. 371:197-204

Here, we investigated the binding characteristics of [ 3 H ]N-(2,5-dimethoxybenzyl)-N-(5-fluoro-2-phenoxyphenyl)acetamide ([ 3 H ]DAA1106), a potent and selective ligand for peripheral benzodiazepine receptors, in mitochondrial fractions of the rat b

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::caea6acdbb0489c9b852f18dba6271ca
https://doi.org/10.1016/s0014-2999(99)00118-1

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In vitro pharmacological profile of nonpeptide CRF1 receptor antagonists, CRA1000 and CRA1001

Autor: Kazuyuki Tomisawa, Yuichi Oshida, Shigeyuki Chaki, Toshihito Kumagai, Yuko Hamajima, Atsuro Nakazato, Taketoshi Okubo, Yoko Ikeda, Shigeru Okuyama

Publikováno v: European Journal of Pharmacology. 371:205-211

We investigated pharmacological properties of CRA1000 (2-(N-(2-methylthio-4-isopropylphenyl)-N-ethylamino-4-(4-(3-fluorophenyl)-1,2,3,6-tetrahydropyridin-1-yl)-6-methylpyrimidine) and CRA1001 (2-(N-(2-bromo-4-isopropylphenyl)-N-ethylamino-4-(4-(3-flu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fdc27393334b05eb5daf60210fd992e7
https://doi.org/10.1016/s0014-2999(99)00120-x

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Neuropharmacological profile of peripheral benzodiazepine receptor agonists, DAA1097 and DAA1106

Autor: Taketoshi Okubo, Shigeru Okuyama, Shigeyuki Chaki, Kazuyuki Tomisawa, Ryoko Yoshikawa, Masasi Nagamine, Atsuro Nakazato, Yoshiko Suzuki, Shin-ichi Ogawa

Publikováno v: Life Sciences. 64:1455-1464

Receptor binding and behavioral profiles of N-(4-chloro-2-phenoxyphenyl)-N-(2-isopropoxybenzyl)acetamide (DAA1097) and N-(2,5-dimethoxybenzyl)-N-(5-fluoro-2-phenoxyphenyl)acetamide (DAA1106), novel, selective agonists for the peripheral benzocliazepi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0619678037ca6f4b87c859330705d05c
https://doi.org/10.1016/s0024-3205(99)00079-x

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Novel piperazines: potent melanocortin-4 receptor antagonists with anxiolytic-like activity

Autor: Dai Nozawa, Shigeru Okuyama, Taketoshi Okubo, Kazuaki Takamori, Atsuro Nakazato, Takaaki Ishii, Shigeyuki Chaki

Publikováno v: Bioorganicmedicinal chemistry. 15(6)

In the present study, we found that a novel piperazine compound, 11a, showed a moderate affinity (IC50 = 333 nM) for the MC4 receptor. We developed the new type of piperazine compounds and found that mono-piperazine 11b exhibited a high-affinity (IC5

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7b78b30ae47b03b05bed9acb087d9167
https://pubmed.ncbi.nlm.nih.gov/17267226

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Structure-activity relationships of novel piperazines as antagonists for the melanocortin-4 receptor

Autor: Hiroyuki Kakinuma, Dai Nozawa, Taketoshi Okubo, Shigeru Okuyama, Atsuro Nakazato, Shigeyuki Chaki, Takaaki Ishii

Publikováno v: Bioorganicmedicinal chemistry. 15(5)

During the investigation of antagonists for the MC4 receptor, we found that 10ab having a naphthyl group showed almost the same binding affinity for the MC4 receptor as that of the lead compound 1 with a benzoyl group. We also developed a new type of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d50c5e6182210bdeef35b4d0a08d27c5
https://pubmed.ncbi.nlm.nih.gov/17234422

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