The Metabolic Fate of 1-(4-Methoxy-6-methyl-2-pyrimidinyl)-3-methyl-5-methoxypyrazole (Mepirizole, DA-398) in Rats and Rabbits

スポンサーリンク

概要

• 論文の詳細を見る

• The metabolic fate of 1-(4-methoxy-6-methyl-2-pyrimidinyl)-3-methyl-5-methoxy-pyrazole (mepirizole, DA-398) was investigated in rat and rabbit. Four metabolites were isolated as crystals from the urine of medicated rats and identified as 1-(4-methoxy-5-hydroxy-6-methyl-2-pyrimidinyl)-3-methyl-5-methoxypyrazole (UNM-1), 1-(4-methoxy-6-methyl-2-pyrimidinyl)-3-hydroxymethyl-5-methoxypyrazole (UNM-2), 1-(4-methoxy-6-methyl-2-pyrimidinyl)-5-methoxypyrazole-3-carboxylic acid (UAM-1) and 1-(4-methoxy-6-methyl-2-pyrimidinyl)-3-methyl-4-hydroxy-5-methoxypyrazole sulfate (URM-1). From the rabbit urine, UAM, UNM-2,UNM-4 (1-(4-methoxy-6-hydroxymethyl-2-pyrimidinyl)-3-methyl-5-methoxypyrazole) were isolated and the excretion of UNM-1,UNM-3 (2-hydroxy-4-methoxy-6-methylpyrimidine) and UNM-5 (1-(4-methoxy-6-methyl-2-pyrimidinyl)-3-methyl-4-hydroxy-5-methoxypyrazole) were identified on thin-layer chromatogram. The major metabolite was UAM-1 both in rat and in rabbit.

• 公益社団法人日本薬学会の論文
• 1970-09-25

著者

• 田中 良明

  Research Institute, Daiichi Seiyaku Co., Ltd.

• 高畠 英伍

  Department of Toxicology, Faculty of Pharmaceutical Sciences, Setsunan University

• 高畠 英伍

  Department Of Toxicology Faculty Of Pharmaceutical Sciences Setsunan University

• 高畠 英伍

  Faculty of Pharmaceutical Sciences, Nagasaki University

• 立沢 晴男

  Drug Metabolism Research Center, Research Institute, Daiichi Seiyaku Co., Ltd.

• 田中 良明

  Research Institute Daiichi Seiyaku Co. Ltd.

• 児玉 龍平

  Kwassui Women's Junior College

• 内藤 武男

  Research Laboratories, Daiichi Seiyaku Co., Ltd.

• 立沢 晴男

  Drug Metabolism Research Center Research Institute Daiichi Seiyaku Co. Ltd.

• 内藤 武男

  Research Laboratories Daiichi Seiyaku Co. Ltd.

• 児玉 龍平

  Kwassui Women's Junior College

• 堂森 廉三

  Research Institute Daiichi Seiyaku Co. Ltd.

• Takabatake E

  Department Of Toxicology Faculty Of Pharmaceutical Sciences Setsunan University

関連論文

• Investigations on Steroids. VI. Pharmacological Studies. (2). Endocrinological Properties and Acute Toxicity of 17β-Hydroxy-17α-methyl-5α-androstano[2,3-c]furazan (Androfurazanol)
• 17α-Methyl-17β-hydroxy-5α-androstano[2,3-c]furazan (Androfurazanol), A New Active Anabolic Steroid
• Synthesis of Antimicrobial Agents. VII. Synthesis and Antibacterial Activities of Furo [2,3-g] quinoline Derivatives
• Synthesis of Antimicrobial Agents. VI. Studies on the Synthesis of Furo [3,2-b] [1,8] naphthyridine Derivatives
• Partial Purification and Substrate Specificity of Flavin-Containing Monooxygenase from Rat Brain Microsomes
• Determination of Flavin-Containing Monooxygenase Activity in Rat Brain Microsomes with Benzydamine N-Oxidation
• 環境中ベリリウムの動態に関する研究大気中ベリリウム及びストロンチウムの挙動について
• TRIMETHADIONE TOLERANCE TEST FOR EVALUATION OF FUNCTIONAL RESERVE OF THE LIVER IN PATIENTS WITH LIVER CIRRHOSIS AND ESOPHAGEAL VARICES
• THE EFFECT OF INDOMETHACIN ON HEPATIC DRUG-OXIDIZING CAPACITY IN THE RAT : TRIMETHADIONE AND ANTIPYRINE METABOLISM AS AN INDICATOR
• Purification and Characterization of Hamster Hepatic Microsomal N, O-Acetyltransferase
• Effect of Ring Substituent on the Stability of the Epoxide Derived from Phenyl Vinyl Ether
• An Unstable Epoxy Intermediate Formed by the Microsomal Oxidation of 4-Nitrophenyl Vinyl Ether
• The Role of Epoxides in the Metabolic Activation of Styrene to Mutagens (Regular Presentations) (Proceedings of the 8th Symposium on Environmental Pollutants and Toxicology)
• The Reaction of S-Acylthiamine and 2-Mercaptoethanol
• 薬学教育における薬剤師教育
• 薬物の経皮吸収におけるレシチンの効果(第2報)ゲル軟膏からのインドメタシンの経皮吸収に対するレシチンの促進効果の機構
• 薬物の経皮吸収におけるレシチンの効果(第1報)インドメタシンゲル軟膏のラット背部経皮吸収と排泄
• Protein Binding of Timiperone, 4'-Fluoro-4-[4-(2-thioxo-1-benzimi-dazolinyl) piperidino] butyrophenone, a Neuroleptic
• 新規Butyrophenone系抗精神病薬, Timiperoneの全身オートラジオグラフィーによるラット, サル体内分布に関する研究
• 含フッ素ピリミジン系スルファニルアミド誘導体の合成と抗菌性
• ピリミジン系スルファニルアミド誘導体の合成と抗菌性
• Studies on Pyrimidinylpyrazoles. III. Tautomerism of 1-and 2-Pyrimidinylpyrazolines
• Studies on Pyrimidinylpyrazoles. II. Ring Closures of N^2-Pyrimidinyl-3-oxobutyrohydrazides
• Studies on Nucleosides and Nucleotides. VIII. Nucleophilic Substitution of Secondary Sulfonyloxy Groups of Pyrimidine Nucleosides. (1)
• The Nucleophilic Substitution of Secondary Sulfonyloxy Groups of Pyrimidine Nucleosides
• ABSORPTION AND EXCRETION OF INDOMETHACIN GEL OINTMENT CONTAINING EGG LECITHIN
• Modification of Drug-Metabolizing Enzyme Activity of Rats in Carrageenin-Inflammation
• The Effect of AF2 [2-(2-Furyl)-3-(5-nitro-2-furyl) acrylamide] on Hepatic Microsomal Mixed Function Oxidase System in Rats
• Metabolism of Benzydamine Hydrochloride
• Comparative N-Demethylation of Antihistaminic Agents possessing Dimethylaminoalkyl Group by Liver Preparations from Four Animal Species
• The Inductive Effect of Mepirizole on the Drug Metabolizing Enzymes of Rat Liver
• The Metabolic Fate of 1-(4-Methoxy-6-methyl-2-pyrimidinyl)-3-methyl-5-methoxypyrazole (Mepirizole, DA-398) in Rats and Rabbits
• Medicinal Chemical Studies on Antiplasmin Drugs. II. Separation of Stereoisomers of 4-Aminomethylcyclohexanecarboxylic Acid and Assignment of Their Configuration
• Medicinal Chemical Studies on Antiplasmin Drugs. I. Establishment of the Screening Assay Method for Antiplasmin Drugs and the Superiority of trans-4-Aminomethylcyclohexanecarboxylic Acid (Tranexamic Acid) to cis-Form
• trans-4-Aminomethylcyclohexanecarboxylic Acid as a Potent Antiplasmin Agent
• 化学療法薬の合成(第2報)1,8-Naphthyridine誘導体の合成と抗トリコモナス活性
• Investigations on Steroids. XII. Metabolites of Furazabol (17β-Hydroxy-17α-methyl-5α-androstano [2,3-c] furazan) administered to Rats
• Analytical Studies on Mepirizole and Its Metabolites. III. Gas Chromatographic Determination of Mepirizole and Its Metabolites in Biological Fluids
• Pantethineの生物学的研究 : (III)実験小動物胎仔にたいするPantethineの影響
• Studies on Nucleosides and Nucleotides. XII. Syntheses of 3'-Amino-3'-deoxypentofuranosylcytosines
• 高速液体クロマトグラフィーによるヒト血清中 Ticlopidine 定量法
• 薬物併用時の代謝に関する研究(第2報)Chlormezanoneのマウス体内動態およびAspirinとの相互作用
• 薬物併用時の代謝に関する研究(第1報)Aspirinのマウス体内動態におよぼすChlormezanoneの影響
• AspirinとChlormezanoneの鎮痛抗炎症作用, 急性毒性と代謝における薬物相互作用
• STUDIES ON METABOLISM AND TOXICITY OF STYRENE. II. MUTAGENESIS IN SALMONELLA TYPHIMURIUM BY METABOLIC ACTIVATION OF STYRENE WITH 3-METHYLCHOLANTHRENE PRETREATED RAT LIVER
• STUDIES ON METABOLISM AND TOXICITY OF STYRENE. I. BIOTRANSFORMATION OF STYRENE TO STYRENE GLYCOL VIA STYRENE OXIDE BY RAT LIVER MICROSOMES
• Synthesis of Antimicrobial Agents. IV. Synthesis and Antimicrobial Activities of Imidazo [4,5-b] [1,8] naphthyridine Derivatives
• Synthesis of Antimicrobial Agents. III. Synthesis and Antimicrobial Activities of Thiazolo [5,4-b] naphthyridine Derivatives
• Synthesis of Antimicrobial Agents. I. Synthesis and Antimicrobial Activities of Thiazoloquinoline Derivatives
• ナリジクス酸関連化合物研究の現況 (新しい医薬品の開発)
• Synthetic Chemotherapeutic Agents. IV. Synthesis of 3-Substituted Thiazolo [5,4-f] quinoline Derivatives. (2)
• Synthetic Chemotherapeutic Agents. III. Synthesis of 3-Substituted Thiazolo [5,4-f] quinoline Derivatives. (1)
• Synthetic Chemotherapeutic Agents. II. Synthesis of 2-Substituted Thiazolo [5,4-f] quinoline Derivatives. (2)
• Synthetic Chemotherapeutic Agents. I. Synthesis of 2-Substituted Thiazolo [5,4-f] quinoline Derivatives. (1)
• Syntheses of the Urinary Metabolites of 1-(4-Methoxy-6-methyl-2-pyrimidinyl)-3-methyl-5-methoxypyrazole (Mepirizole, DA-398)
• Synthesis of 1-Substituted 1,4-Dihydro-7-[2-(5-nitro-2-furyl) vinyl]-4-oxo-1,8-naphthyridine Derivatives. II
• Synthesis of 1-Substituted 1,4-Dihydro-7-[2-(5-nitro-2-furyl) vinyl]-4-oxo-1,8-naphthyridine Derivatives. I
• Rearrangement of Sulfonamide Derivatives. V. Syntheses of Methyl α-Phenyl-2- and 4-piperidineacetate.
• スルフォンアミド誘導体の転位反応(第4報)ピリジン及びキノリン1-オキシドのスルフォンアミド誘導体の転位反応
• スルフォンアミド誘導体の転位反応(第3報)反応機構に就いての考察
• Synthesis and Antibacterial Activities of Substituted 7-Oxo-2,3-dihydro-7H-pyrido [1,2,3-de] [1,4] benzoxazine-6-carboxylic Acids
• Analytical Studies on Mepirizole and Its Metabolites. IV. Quantitative Determination of Mepirizole in Human Serum by Mass Fragmentography, and Isotope Effect on Drug Metabolism
• Analytical Studies on Mepirizole and Its Metabolites. II. Identification of the Human Urinary Metabolites of Mepirizole with Stable Isotope Labeling
• Analytical Studies on Mepirizole and Its Metabolites. : I. Mass Spectra of Mepirizole and Its Some Metabolites
• Studies on Nucleosides and Nucleotides. VII. Synthesis of 2-Amino-6-substituted-9-β-D-ribofuranosylpurines
• The Metabolism and Excretion of Trimethadione in Patients with Percutaneous Transhepatic Biliary Drainage and Renal Dysfunction
• Sex-Related Differences in Hepatic Drug-Oxidizing Capacity of Streptozotocin-Induced Diabetic Rats
• TRIMETHADIONE METABOLISM IN PATIENTS WITH NORMAL LIVER AND IN PATIENTS WITH CHRONIC LIVER DISEASE
• HEPATIC TRIMETHADIONE-OXIDIZING CAPACITY REMAINS NORMAL IN PATIENTS WITH EXTRAHEPATIC CHOLELITHIASIS
• Effect of Tolbutamide on the Metabolism of Parathion
• Effects of Mushroom Toxins on Glycogenolysis : Comparison of Toxicity of Phalloidin, α-Amanitin and DL-Propargylglycine in Isolated Rat Hepatocytes
• EFFECTS OF CIMETIDINE AND DIETHYLAMINOETHYL 2,2-DIPHENYLVALERATE HCL (SKF 525-A) ON TRIMETHADIONE METABOLISM IN THE RAT
• Synthesis of 3-Pyridinols. I. Reaction of 5-Unsubstituted Oxazoles with Acrylonitrile
• Studies on Pyrimidinylpyrazoles. I. Syntheses of 1-and 2-Pyrimidinyl-3-methylpyrazolin-5-one Derivatives
• Reaction of Oxazoles with Dienophiles
• Synthesis of 3-Pyridinols. III. Synthesis of Pyridoxine Skeletons from 4-Methyloxazole
• Synthesis of 3-Pyridinols. II. Reaction of 4-Methyloxzaole with Dienophiles
• Metabolism of Benzydamine Hydrochloride : Species Differences and the Identification of Unconjugated Metabolites in Rabbit Urine
• A New Synthetic Method for Pyrimidine Nucleoside
• Effect of Diphenylhydantoin on the Drug Metabolism and the Fatty Acid Composition of Phospholipids in Hepatic Microsomes
• Effects of Phenobarbital, Ethanol and Ethionine on the Content and Fatty Acid Composition of Hepatic Microsomal Phospholipids

もっと見る 閉じる

スポンサーリンク