新β-遮断薬Carteolol Hydrochloride[5-(3-tert-butylamion-2-hydroxypropoxy)-3,4-dihydrocarbostyril Hydrochloride, OPC-1085]の生体内運命(第5報)ラット, イヌおよびヒトにおける代謝産物の同定

スポンサーリンク

概要

• 論文の詳細を見る

• The metabolism of carteolol hydrochloride was investigated in rats and dogs after oral administration of ^<14>C-carteolol hydrochloride. The metabolites were identified by gas chromatography-mass spectrometry. In the rat, summation of radioactivity excreted in urine and feces during 48 hr was about 35% and 62%, respectively. The major radioactive metabolites including glucuronides were carteolol (35%) and 8-hydroxycarteolol (47%) from urine, and carteolol (35%), 8-hydroxycarteolol (20%), and dihydroxycarteolol (33%) from feces. On the other hand, in the dog, the summation of radioactivity excreted in urine and feces during 48 hr was about 62 % and 27 %, respectively. The major radioactive metabolites including glucuronides were carteolol (35%), 8-hydroxycarteolol (45%), and dihydroxycarteolol (9%) from urine, and carteolol (23%) and 8-hydroxycarteolol (61%) from feces. Carteolol and 8-hydroxycarteolol were also identified from human urine. The minor metabolites were identified as 5-hydroxy-3,4-dihydrocarbostyril and 5,8-dihydroxy-3,4-dihydrocarbostyril from the rat and the dog, and as 5-carboxymethoxy-3,4-dihydrocarbostyril from dog urine. Antagonism of 8-hydroxycarteolol, the main metabolite, against the positive chronotropic and hypotensive actions of isoproterenol was examined in anesthetized dogs.

• 社団法人日本薬学会の論文
• 1977-04-25

著者

• 宇野 敏行

  大塚製薬株式会社徳島工場第三研究所

• 森 英雄

  Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd.,

• 木戸 勝

  Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd.,

• 木戸 勝

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• 中川 量之

  2nd Tokushima Institute Of New Drugs Research Otsuka Pharmaceutical Co. Ltd.

• 中川 量之

  大塚製薬株式会社有機化学研究所

• 中川 量之

  大塚製薬株式会社徳島研究所

• 森 英雄

  大塚製薬株式会社徳島工場第一研究所

• 木戸 勝

  大塚製薬株式会社徳島工場第一研究所

• 村上 七美

  大塚製薬株式会社徳島工場第一研究所

• 森田 誠治

  大塚製薬株式会社徳島工場第一研究所

• 郡 英明

  大塚製薬株式会社徳島工場第一研究所

• 石原 高文

  大塚製薬株式会社徳島工場第三研究所

• 郡 英明

  大塚製薬株式会社徳島工場第三研究所

• 森田 誠治

  Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd.

• 森田 誠治

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• 郡 英明

  大塚製薬株式会社徳島工場第3研究所

• 森田 誠治

  大塚製薬株式会社徳島工場第3研究所

関連論文

• 90(P28) Tripterygium属植物に含まれる免疫抑制活性、抗HIV活性物質の探索(ポスター発表の部)
• Anti-plasmin Inhibitor. VI. : Structure of Phlorofucofuroeckol A, a Novel Phlorotannin with Both Dibenzo-1,4-dioxin and Dibenzofuran Elements, from Ecklonia kurome OKAMURA
• Anti-plasmin Inhibitor. V. : Structures of Novel Dimeric Eckols Isolated from the Brown Alga Ecklonia kurome OKAMURA
• Structure of an Anti-plasmin Inhibitor, Eckol, Isolated from the Brown Alga Ecklonia kurome OKAMURA and Inhibitory Activities of Its Derivatives on Plasma Plasmin Inhibitors
• 17 クロメのplasmin inhibitors阻害物質ポリヒドロキシジベンゾ-p-ジオキシン
• Studies on Antibacterial Agents. II. : Synthesis and Antibacterial Activities of Substituted 1,2-Dihydro-6-oxo-6H-pyrrolo[3,2,1-ij]quinoline-5-carboxylic Acids
• Studies on Antibacterial Agents. I. : Synthesis of Substituted 6,7-Dihydro-1-oxo-1H, 5H, -benzo{i, j]-quinolizine-2-carboxylic Acids
• Studies on Antibacterial Agents. III. : Synthesis and Antibacterial Activities of Substituted 1,4-Dihydro-8-methyl-4-oxoquinoline-3-carboxylic Acids
• Studies on 2(1H)-Quinolinone Derivatives as Neuroleptic Agents. I. : Synthesis and Biological Activities of (4-Phenyl-1-piperazinyl)-propoxy-2(1H)-quinolinone Derivatives
• Studies on Positive Inotropic Agents. VI. : Synthesis of 1-Aromatic Ring Substituted 4-(3,4-Dimethoxybenzoyl)-piperazine Derivatives
• Studies on Positive Inotropic Agents. V. : Synthesis of 1-Heteroaroylpiperazine Derivatives
• 陽性変力作用薬の研究(第3報)6-(Substituted 1-oxoalkyl)-2(1H)quinolinone誘導体の合成
• Studies on Positive Inotropic Agents. II. : Synthesis of(4-Substituted 1-piperazinylcarbonyl)-2-(1H)-quinolinone Derivatives
• Studies on Positive Inotropic Agents. I. Synthesis of 3,4-Dihydro-6-[4-(3,4-dimethoxybenzoyl)-1-piperazinyl]-2 (1H)-quinolinone and Related Compounds
• The Crystal Structures of 5-Hydroxy-3,4-dihydro-2-quinolone and 5-Hydroxy-1-methyl-3,4-dihydro-2-quinolone
• The Crystal Structures of 2-Quinolone and 8-Acetoxy-2-quinolone
• The Molecular Structure of Procaterol Hydrochloride Hemihydrate [5-(1-Hydroxy-2-isopropylaminobutyl)-8-hydroxy-2-quinolone Hydrochloride Hemihydrate, OPC-2009]
• Syntheses and β-Adrenergic Blocking Activities of Carbostyril Derivatives
• Synthesis of 5,8-Dihydroxy-3,4-dihydrocarbostyril
• The Crystal Structure of Carteolol Hydrochloride : 5-(3-tert-Butylamino-2-hydroxy) propoxy-3,4-dihydro-2-quinolone, OPC-1085
• 新β-遮断薬Carteolol Hydrochloride[5-(3-tert-butylamion-2-hydroxypropoxy)-3,4-dihydrocarbostyril Hydrochloride, OPC-1085]の生体内運命(第5報)ラット, イヌおよびヒトにおける代謝産物の同定
• 5-(3-tert-Butylamino-2-hydroxypropoxy)-3,4-dihydrocarbostyril Hydrochloride(OPC-1085)のけい光定量とけい光体の構造について
• 5-(3-tert-Butylamino-2-hydroxypropoxy)-8-hydroxy-3,4-dihydrocarbostyril Hydrochlorideの合成とそのβ-遮断作用について
• 光学活性5-(3-tert-Butylamino-2-hydroxypropoxy)-3,4-dihydrocarbostyril Hydrochlorideの合成とそのβ-遮断作用について
• (3-Amino-2-hydroxy)propoxy-3,4-dihydrocarbostyril誘導体の麻酔犬におけるβ-受容体遮断作用
• 22 発芽誘因物質ソルゴラクトンの合成研究(口頭発表の部)
• 92 カサガイの一種Collisella limatulaの生産するトリテルペン防御物質である(±)-及びmeso-リマツロンの合成(ポスター発表の部)
• Studies on Gastric Antiulcer Active Agents. III. : Synthesis of 1-Substituted 4-(5-Tetrazolyl)thio-1-butanones and Related Compounds
• Studies on Gastric Antiulcer Active Agents. II. : Synthesis of Tetrazole Alkanamides and Related Compounds
• Studies on 2(1H)-Quinolinone Derivatives as Gastric Antiulcer Active Agents. Synthesis and Antiulcer Activities of Optically Active α-Amino Acid Derivatives of 2(1H)-Quinolinone and Oxindole(Medicinal Chemistry,Chemical)
• Studies on 2(1H)-Quinolinone Derivatives as Gastric Antiulcer Active Agents. Synthesis and Antiulcer Activity of the Metabolites of 2-(4-Chlorobenzoylamino)-3-[2(1H)-quinolinon-4-yl]propionic Acid
• 3-芳香環置換2-(4-Chlorobenzoylamino)propionic Acid誘導体の合成と抗潰瘍作用について
• Studies on 2 (1H)-Quinolinone Derivatives as Gastric Antiulcer Active Agents. 2-(4-Chlorobenzoylamino)-3-[2 (1H)-quinolinon-4-yl] propionic Acid and Related Compounds
• Synthesis and Antiulcer Activity of 4-Substituted 8-[(2-Benzimidazolyl)sulfinylmethyl]-1,2,3,4-tetra-hydroquinolines and Related Compounds
• Studies on Proton Pump Inhibitors. III. : Synthesis of 8-[(2-Benzimidazolyl)sulfinylmethyl]-1,2-dihydroquinolines and Related Compounds
• Studies on Proton Pump Inhibitors. II. : Synthesis and Antiulcer Activity of 8-[(2-Benzimidazolyl)-sulfinylmethyl]-1,2,3,4-tetrahydroquinolines and Related Compounds
• Studies on Proton Pump Inhibitors. I. : Synthesis of 8-[(2-Benzimidazoly)sulfinyl]-5,6,7,8-tetrahydroquinolines and Related Compounds
• NaBN_4-NiCl_2による除草剤Diquatの還元 : 二種の立体異性体Perhydro-8a, 10a-diazaphenanthreneの構造について
• 61 海藻の抗微生物活性成分
• Studies on 2-Oxoquinoline Derivatives as Blood Platelet Aggregation Inhibitors. I. Alkyl 4-(2-Oxo-1,2,3,4-tetrahydro-6-quinolyloxy) butyrates and Related Compounds
• Studies on 2-Oxoquinoline Derivatives as Blood Platelet Aggregation Inhibitors. IV. Synthesis and Biological Activity of the Metabolites of 6-[4-(1-Cyclohexyl-1H-5-tetrazolyl) butoxy]-2-oxo-1,2,3,4-tetrahydroquinoline (OPC-13013)
• 5-(3-Aryloxypropyl)-1-cyclohexyltetrazole類の合成と血小板凝集抑制作用について
• Studies on 2-Oxoquinoline Derivatives as Blood Platelet Aggregation Inhibitors. II. 6-[3-(1-Cyclohexyl-5-tetrazolyl) propoxy]-1,2-dihydro-2-oxoquinoline and Related Compounds
• Studies on 2-Oxoquinoline Derivatives as Blood Platelet Aggregation Inhibitors. III. N-Cyclohexyl-N-(2-hydroxyethyl)-4-(1,2-dihydro-2-oxo-6-quinolyloxy)-butyramide and Related Compounds
• β-受容体遮断作用を有する8-アシルアミノ-3,4-ジヒドロカルボスチリル誘導体の合成
• 抗血小板剤シロスタゾールの研究開発
• 生体試料の前処理法として水系ゲルろ過カラムを接続したクロマトグラフィー
• 新β-遮断薬Carteolol hydrochloride（OPC-1085）の生体内動態（第6報）―ラット，家兎，イヌおよびヒトにおける薬動力学―
• 新β-遮断薬Carteolol hydrochloride (OPC-1085) の生体内動態 (第3報) 全身オートラジオグラフィーによるマウス生体内分布

もっと見る 閉じる

スポンサーリンク