{"@context":{"@vocab":"https://cir.nii.ac.jp/schema/1.0/","rdfs":"http://www.w3.org/2000/01/rdf-schema#","dc":"http://purl.org/dc/elements/1.1/","dcterms":"http://purl.org/dc/terms/","foaf":"http://xmlns.com/foaf/0.1/","prism":"http://prismstandard.org/namespaces/basic/2.0/","cinii":"http://ci.nii.ac.jp/ns/1.0/","datacite":"https://schema.datacite.org/meta/kernel-4/","ndl":"http://ndl.go.jp/dcndl/terms/","jpcoar":"https://github.com/JPCOAR/schema/blob/master/2.0/"},"@id":"https://cir.nii.ac.jp/crid/1390282679247148672.json","@type":"Article","productIdentifier":[{"identifier":{"@type":"DOI","@value":"10.1254/fpj.84.109"}},{"identifier":{"@type":"COI","@value":"1:CAS:528:DyaL2cXks1Gru7c%3D"}},{"identifier":{"@type":"PMID","@value":"6149174"}},{"identifier":{"@type":"NDL_BIB_ID","@value":"3000624"}},{"identifier":{"@type":"URI","@value":"http://id.ndl.go.jp/bib/3000624"}},{"identifier":{"@type":"URI","@value":"https://ndlsearch.ndl.go.jp/books/R000000004-I3000624"}},{"identifier":{"@type":"NAID","@value":"130000761055"}},{"identifier":{"@type":"URI","@value":"https://search.jamas.or.jp/link/ui/1985059222"}}],"resourceType":"学術雑誌論文(journal article)","dc:title":[{"@value":"新しい睡眠導入剤１Ｈ‐１，２，４‐Ｔｒｉａｚｏｌｙｌ　ｂｅｎｚｏｐｈｅｎｏｎｅ誘導体４５０１９１‐Ｓの薬理　Ｉ　　行動薬理学的研究"},{"@language":"en","@value":"Pharmacological studies of a new sleep-inducer, 1H-1, 2, 4-triazolyl benzophenone derivatives (450191-S) (I). Behavioral analysis"},{"@language":"ja-Kana","@value":"アタラシイ スイミン ドウニュウザイ 1H-1,2,4 Triazolyl b"}],"dc:language":"ja","description":[{"type":"abstract","notation":[{"@language":"en","@value":"The behavioral effects of 450191-S and its metabolites were investigated in mice, rats, cats and rhesus monkeys, and they were compared with those of related benzodiazepines (BDZ) such as diazepam and nitrazepam. Oral administration of 450191-S consistently caused sedation without excitability in mice and rats, and it was only 1/2 to 1/266 as potent as the BDZ in producing motor incoordination as assessed by traction, rotarod performance and inclined screen tests in mice, induced much less ataxia in cats and monkeys, and inhibited respiration in anesthetized cats. The locomotor activities of mice and rats measured by Animex and the open field test were not affected by 450191-S, but rearing and preening decreased with 450191-S as with the BDZ. 450191-S was equipotent with nitrazepam and 2 to 6 times more potent than diazepam and estazolam in potentiating chlorprothixene-induced hypnosis and thiopental-Na-induced anesthesia. These effects were not different with successive 14-day administration of 450191-S. Anti-pentylenetetrazol, picrotoxin and bicuculline convulsions of 450191-S had the same potency as nitrazepam, but caused much less anti-electroshock convulsion than the BDZ. 450191-S had potent antianxiety activity as observed by anti-aggressive and anti-conflict activities and had almost the same effect as diazepam on operant behavior. The metabolites M-1, M-2, M-A and M-3 showed approximately the same potency as 450191-S in inducing anesthetic potentiation and antianxiety activity, but they were much more potent in causing disturbance of the somatic functions. These results indicate that 450191-S possesses inhibitory effects on the central nervous system, including a potent sleep-inducing effect, and is characterized by markedly weak muscle relaxant activity and motor incoordination."},{"@value":"マウス，ラット，ネコおよびアカゲザルを用いてlH-1，2，4-triazolyl benzophenone誘導体450191-Sおよびその代謝物の作用を行動薬理学的に解析し，diazepam，nitrazepam，cstazolam，triazolamその他のbenzodiazepines(BDZ)と比較を行った。マウス，ラットの行動は450191-Sの経口投与後鎮静的で発揚症状は現われず，マウスのAnimexおよびラットのオープンフィールド試験における自発運動にも著変を来たさなかったが，rearing，preeningを対照薬と同様に抑制した．450191-Sのchlorprothixene睡眠およびthiopental-Na 麻酔増強作用はnitrazepamと同程度，diazepam，estazolamより2～6倍強かった．450191-Sのpentylenetetrazol，picrotoxin，bicucullineけいれん抑制作用はnitrazepamと同程度であったが，抗電撃けいれん作用はいずれの対照薬よりも弱かった．450191-Sのネコ，サルの威嚇行動抑制作用は対照薬と同程度，マウスの抗闘争作用はtriazolam以外の対照薬より強く，嗅球摘出ラットのmuricideおよび情動過多反応の抑制はdiazepamとほぼ同程度であった．450191-Sの抗confiict作用はestazolam以外の対照薬とほぼ同じで，Sidman回避反応，低率分化餌強化，脳内自己刺激などのオペラント行動に対してはdiazepamと同程度の作用を示した．450191-Sは2週間の連続投与によっても麻酔増強作用ないし抗pcntylenetetrazolけいれん作用に耐性を発現しなかった．450191-Sの筋弛緩を含む体性機能の異常はどの対照薬よりも著しく弱かった．マウスの懸垂，回転棒，傾斜板試験による450191-Sの協調運動抑制作用は対照薬の1/2～1/266で著しく弱く，ネコとサルの歩行失調および麻酔ネコの呼吸運動抑制作用も対照薬より明らかに弱かった。450191-Sの血漿中代謝物M-1，M-2，M-A，M-3は母化合物450191-Sとほぼ同程度の麻酔増強作用と抗不安作用を示したが，筋弛緩や運動障害作用は母化合物より著しく強かった．以上，450191-Sは催眠作用を含む中枢神経抑制作用を有する反面，筋弛緩作用および運動失調などの副作用はきわめて弱いので安全性の高い化合物と推定された．"}],"abstractLicenseFlag":"disallow"}],"creator":[{"@id":"https://cir.nii.ac.jp/crid/1410001204270434177","@type":"Researcher","personIdentifier":[{"@type":"NRID","@value":"9000021401800"}],"foaf:name":[{"@language":"en","@value":"YAMAMOTO Ken-ichi"},{"@language":"ja","@value":"山本 研一"}],"jpcoar:affiliationName":[{"@language":"en","@value":"Division of Neuropharmacology, Shionogi Research Laboratories, Shionogi and Co., Ltd."},{"@language":"ja","@value":"塩野義製薬(株)研究所神経薬理学部門"}]},{"@id":"https://cir.nii.ac.jp/crid/1410282679247148673","@type":"Researcher","personIdentifier":[{"@type":"NRID","@value":"9000021222013"}],"foaf:name":[{"@language":"en","@value":"HIROSE Katsumi"},{"@language":"ja","@value":"広瀬 勝巳"}],"jpcoar:affiliationName":[{"@language":"en","@value":"Division of Neuropharmacology, Shionogi Research Laboratories, Shionogi and Co., Ltd."},{"@language":"ja","@value":"塩野義製薬(株)研究所神経薬理学部門"}]},{"@id":"https://cir.nii.ac.jp/crid/1410282679247148675","@type":"Researcher","personIdentifier":[{"@type":"NRID","@value":"9000021222017"}],"foaf:name":[{"@language":"en","@value":"MATSUSHITA Akira"},{"@language":"ja","@value":"松下 享"}],"jpcoar:affiliationName":[{"@language":"en","@value":"Division of Neuropharmacology, Shionogi 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