Chemical Reactivity of Morphine and Morphine-6-conjugates and Their Binding to Rat Brain
スポンサーリンク
概要
- 論文の詳細を見る
By substitution reaction with nucleophilic reagents such as lithium chloride and piperidine, morphine-6-conjugates were found to be convertible easily to 6-chloro-6-deoxy-morphine and 8-piperidino-6-deoxy-Δ^6-morphine, respectively. The reaction rates of these conjugates were roughly parallel with the analgesic activity, decreasing in the order sulfate>glucuronide≒acetate>phosphate>morphine. Furthermore, in the hope that the similar binding of morphine and its 6-conjugates to nucleophilic sites of the brain macromolecule which is closely related to the analgesic receptor might occur, the binding experiment to rat brain homogenates was conducted using morphine and morphine-6-glucuronide which is known to possess stronger analgesic activity than morphine. As the result, the 6-glucuronide showed greater affinity to rat brain but lesser extent of binding to rat liver and bovine serum albumin than morphine.
- 公益社団法人日本薬学会の論文
- 1976-05-25
著者
-
小栗 一太
九州大学薬学部衛生化学裁判化学教室
-
夏木 令子
Faculty of Pharmaceutical Sciences, Nagasaki University 1-14 Bunkyo-machi, Nagasaki
-
小栗 一太
Faculty of Pharmaceutical Sciences, Kyushu University
-
吉村 英敏
中村学園大・食物栄養
-
吉村 英敏
Faculty Of Pharmaceutical Sciences Kyushu University
-
飯田 成宇
Faculty of Pharmaceutical Sciences, Kyushu University
-
Yoshimura Hidetoshi
Department Of Food And Nutrition Nakamura Gakuen University
-
飯田 成宇
Faculty Of Pharmaceutical Sciences Kyushu University:(present Address)central Research Laboratory Mi
-
夏木 令子
Faculty Of Pharmaceutical Sciences Nagasaki University
関連論文
- 第23回学術年会を終えて
- 新規抗悪性腫瘍薬 S-1 の各配合成分の体内動態 (第3報) : ラットにおける S-1 反復投与時の各配合成分の吸収, 排泄および肝薬物代謝酵素系に与える影響
- β遮断薬 Bunitrolol の代謝反応における立体選択性と体内動態との関連性
- Reduced Nicotinamide Adenine Dinucleotide-dependent O-Deethylation of p-Nitrophenetole with Rabbit Liver Microsomes. II. Involvement of Cytochrome b_5
- Studies on Quinolizine Derivatives. XII. Synthesis of Diazacycl [3,3,3] azine Derivatives.
- Studies on Quinolizine Derivatives. XI. Synthesis of Azacycl [3,3,3] azine Derivatives. (4)
- Studies on Quinolizine Derivatives. IX. Synthesis of Azacycl [3,3,3] azine Derivatives
- Reactions of 1,1-Bismethylthio-2-nitroethylene. IV. Syntheses and Reactions of 4-Methylthio-2-buten-4-olide Derivatives
- Studies on Indole Derivatives. XXIII. Diels-Alder Reaction of 3-Indoledithiocarboxylic Acid Derivatives and Dimethyl Acetylenedicarboxylate and Reactions of Their Products
- Reaction of 1-Nitro-2,2-bis(methylthio)ethylene. II. Synthesis of 2-Hydroxyimino-3-methylthio-5-oxopyrroline Derivatives
- Studies on Indole Derivatives. XVI. Synthesis of Indoxyl Derivatives. (2). Reactions of 1-Acetyl-3-indolinone with Ketenethioacetal Derivatives
- Studies on Indole Derivatives. XV. Synthesis of Indoxyl Derivatives. (1). Crystal and Molecular Structure of Anhydro-2-benzyl-1-mercapto-3-methyl-9-oxo-(9H)-imidazo[1,5-α]indolium Hydroxide
- Effect of Morphine and Its Conjugates on the Isolated Ileal Preparation of Guinea-pig
- NADH-dependent O-Demethylation of p-Nitroanisole with Rabbit Liver Microsomes
- Metabolism of Drugs. LI. The Metabolic Fate of Alkylaryl Ethers in Rabbits
- The Occurrence of (ω-1)-Hydroxylation as the Major Metabolism of Alkylaryl Ethers in Rabbits
- 薬物動態研究事始め(4)
- 学術貢献賞受賞 山本郁男氏の業績
- 医薬品の生体内変化に関する研究(第85報)1-p-Chlorophenyl-2,3-dimethyl-4-dimethylaminobutan-2-ol Hydrochlorideの代謝に関する研究
- Cytochrome P450 と mEH および UGTとの蛋白質相互作用
- Properties of Nitrofuran Reductases from Escherichia coli B/r
- モルモット肝UDP-グルクロン酸転移酵素 UGT2B21 および UGT2B22のcDNA クローニングとCOS-1 cell における発現 - ヘテロオリゴマー形成によるモルヒネ活性代謝物生成について -
- モルヒネの活性代謝物生成に関するモルモット肝 UDP-グルクロン酸転移酵素の cDNA クローニングについて
- モルヒネ活性代謝物生成に関与するモルモット肝UDP-グルクロン酸転移酵素について
- Identification of in Vitro Metabolites of 2,4,6,2', 4', 6'-Hexachlorobiphenyl from Phenobarbital-Treated Dog Liver Microsomes
- Analysis of Nitrogen Containing Compounds, p-Coumaroyltyramine and Feruloyltyramine, for Discrimination of Cannabis Seeds by HPLC
- Metabolic Studies on Polychlorinated Biphenyls. III. Complete Structure and Acute Toxicity of the Metabolites of 2,4,3', 4'-Tetrachlorobiphenyl
- Metabolic Studies on Polychlorinated Biphenyls. II. Metabolic Fate of 2,4,3', 4'-Tetrachlorobiphenyl in Rats
- Metabolic Studies on Polychlorinated Biphenyls. I. Metabolic Fate of 3,4,3', 4'-Tetrachlorobiphenyl in Rats
- BrucineによるCYP2B subfamily P450の誘導:種差による検討
- フェノバルビタール型PCBのウサギ肝における代謝
- Effect of Cytochrome P450 Inducers on Liver Microsomal Metabolism of Tetrachlorobiphenyls in Rats, Guinea Pigs and Hamsters
- Metabolic Formation of Dimethylamine and Methylamine from Basic Drugs Containing N-Methyl Group : A Newly Established Chromatographic Assay and Its Application to the Determination of Deaminase Activity
- Purification and Characterization of a Morphine UDP-Glucuronyltransferase Isoform from Untreated Rat Liver
- A New Metabolite of 2,4,3', 4'-Tetrachlorobiphenyl in Rat Feces
- Synthesis and Pharmacological Activity of Sulfate Conjugates at 6-Position of N-Substituted Normorphine Derivatives
- Rat Liver DT-Diaphorase as a Nitroso-Reductase
- 覚せい剤及び関連化合物の代謝 : その生化学的側面
- Synthesis and Analgesic Effect of Normorphine-3- and -6-glucuronides
- 乱用薬物の代謝
- 駆け出しの頃(私はあの時、こう閃いた!-研究の壁を突破し、大きく飛躍するため-)
- モルヒネとヘロインの法中毒学
- Reconstitution of Apo-DT-diaphorase with Flavin-Adenine Dinucleotide
- CIS-TRANS ISOMERIZATION OF A NITROFURAN AF-2 BY RAT LIVER MICROSOMAL PREPARATIONS
- 共通一次入試と学生気質(入試制度と薬学教育)
- 薬物代謝からみた中毒 (プライマリ・ケアのための急性中毒の救急初期治療)
- REDUCTION OF METHYL 5-NITRO-2-FUROATE BY XANTHINE OXIDASE : AN EVIDENCE FOR HYDROXYLAMINOFURAN FORMATION
- Metabolism of Drugs. LXXIII. The Metabolic Fate of Nitrofuran Derivatives. (1) Studies on the Absorption and Excretion
- Metabolism of Drugs. LXX. Further Study on Antipyrine Metabolism
- Metabolism of Drugs. LXIX. Studies on the Urinary Metabolites of Morphine in Several Mammalian Species
- 医薬品の生体内変化に関する研究(第66報) : Pantethineの生体内変化について
- On the Structure of Morphine-6-glucuronide in a Solid State
- Metabolism of Drugs. LXIV. Species Differences of Metabolism of Phenacetylurea
- Metabolism of Drugs. LX. The Synthesis of Codeine and Morphine Glucuronides
- メチルオレンジ法によるモルヒネ定量の変法
- Forensic Chemical Study on Marihuana. I. A Detection Method of the Principal Constituents by Thin-layer and Gas Chromatographies
- Morphine Phosphate Estersの合成ならびに薬理作用について
- Characteristics of the Gastrointestinal Absorption of Morphine in Rats
- ノスカピンの生体内運命に関する研究(第1報)家兎尿中代謝物の検索
- 油症研究-この10年間の推移
- ポリ塩素化ビフェニル(PCB)と関連化合物 (環境汚染物質と毒性--有機物質編)
- Metabolism of Drugs. LXXXI. Further Studies on Metabolism of Prolintane in Rabbits
- Metabolism of Drugs. LXXVI. The Metabolic Fate of Prolintane in Rabbits
- Inhibition of Hepatic Microsomal Cytochrome P450 by Cannabidiol in Adult Male Rats
- THE PHARMACOLOGICAL ACTIVITY OF CANNABINOL AND ITS MAJOR METABOLITE, 11-HYDROXYCANNABINOL(Communication to the Editor)
- HUMAN LIVER MICROSOMAL OXIDATION OF Δ^8-TETRAHYDROCANNABINOL
- Binding of Nitrofuran Derivatives to Nucleic Acids and Protein
- モルモット肝臓のモルヒネ活性代謝物生成に関与する主要なUDP-グルクロン酸転移酵素について
- Suppression of Liver Microsomal Drug-Metabolizing Enzyme Activities in Adult Female Rats Pretreated with Cannabidiol
- Metabolism of Drugs. LXXXVI. The Metabolic Fate of Nitrofuran Derivatives. (4). The Portal Absorption of Nitrofuran Derivatives and the Absorption Rate as a Function of Age in Rats
- 医薬品の生体内変化に関する研究(第74報)メタプロテレノールの代謝について2
- 3-Methylcholanthrenceおよびantioxiantによるセレン結合性タンパク質の誘導の用量依存性について
- フェノバルビタールにより誘導される2種のモルヒネUDP-グルクロン酸転移酵素分子種
- Metabolism of Drugs. LXXV. The Enzymatic Degradation of Isoprophenamine
- Cytochrome P4502Bサブファミリーの誘導機構 : 研究進展と問題点の現状
- 乱用薬物の代謝とその機構
- 光アフィニティーリガンドによるフェノバルビタール結合性蛋白質の探索
- Phenobarbital 誘導性のモルモット肝 P450 : 分子種と遺伝子構造
- Metabolism of Drugs. LXXII. Synthesis of Nalorphine-3- and -6-glucuronide and Identification of Urinary Metabolites of Nalorphine in Rabbits
- Metabolism of Drugs. LXXX. The Metabolic Fate of Nitrofuran Derivatives. (3). Studies on Enzymes in Small Intestinal Mucosa of Rat Catalyzing Degradation of Nitrofuran Derivatives
- Metabolism of Drugs. LXXIX. The Metabolic Fate of Nitrofuran Derivatives. (2). Degradation by Small Intestinal Mucosa and Absorption from Gastrointestinal Tract
- Susceptibility of Aromatic Nitro Compounds to Xanthine Oxidase-catalyzed Reduction
- トキシコロジーと薬物代謝学(薬学におけるトキシコロジーの発展)
- オクテット
- Chemical Reactivity of Morphine and Morphine-6-conjugates and Their Binding to Rat Brain
- 医薬品の生体内変化に関する研究(第84報)Morphine Glucuronidesのウサギ, モルモットおよびマウスにおける代謝
- 医薬品の生体内変化に関する研究(第83報)Morphine Glucuronidesのラットにおける代謝
- 医薬品の生体内変化に関する研究(第77報)アンチピリンのin Vitro代謝
- 第12回薬物代謝と薬効・毒性シンポジウム
- In Vivo Metabolism of 11-Hydroxy-Δ^8-tetrahydrocannabinol to Two Carboxylic Acids and the Effects of SKF 525-A, Cobaltous Chloride and Phenobarbital on Their Formation in Rats
- Spectral Interaction of 11-Hydroxy-Δ^8-tetrahydrocannabinol with Rabbit and Rat Liver Microsomal Cytochrome P-450
- 「座長のあり方」の前に(年会一般講演の座長のあり方)
- Morphineおよび関連化合物の抱合型代謝物とその薬効
- Synthesis of Δ^8-Tetrahydrocannabinol Glucuronide and Sulfate, and Their Metabolic Disposition in Rats
- Detection of Morphine in Urine. II. An Improved Method by Thin-Layer Chromatography Utilizing Potassium Platinum Iodide as the Reagent for Both Coloration and Fluorescence
- ヨウ化白金酸カリウムによるモルヒネの瑩光反応ならびにその検出法への応用
- Detection of Morphine in Urine
- Specificity and Mechanism of the Color Reaction of Cocaine with Cobaltous Thiocyanate
- Pharmaco kinetics and analgesic actions of locally retentive morphine suppository.
- 中毒原因物質の分析法 : 現状と進歩(化学物質による急性中毒 : 最近の話題, 救急救命と中毒物質の分離・同定)