Metabolism of 4-Ethoxy-2-methyl-5-morpholino-3 (2H)-pyridazinone (M73101), a New Anti-inflammatory Agent. II. Species Differences of Metabolism and Excretion
スポンサーリンク
概要
- 論文の詳細を見る
The species differences of metabolism of 4-ethoxy-2-methyl-5-morpholino-3 (2H)-pyridazinone (M73101) were studied. The urinary and fecal metabolites in six animals (dog, mouse, rabbit, rat, monkey, and guinea pig) were analyzed qualitatively and quantitatively by thin-layer chromatography and gas-liquid chromatography in addition to gas chromatography-mass spectrum determination. From the results of qualitative analysis, seven to ten metabolites in urine were identified in each animal. From the results of quantitative analysis, total excretion percentage of unchanged M73101 and its metabolites in urine were 50.0,48.4,73.8,56.1,52.7,and 21.1% of the dose administered in dogs, mice, rabbits, rats, monkeys, and guinea pigs, respectively. The main metabolite excreted in urine was 5-[2-(carboxymethyloxy) ethylamino]-4-ethoxy-2-methyl-3 (2H)-pyridazinone (M-9) in dogs, mice, rabbits, and rats and 5-(N-carboxymethyl-N-2-hydroxy-ethylamino)-4-ethoxy-2-methyl-3 (2H)-pyridazinone (M-8) in monkeys and guinea pigs. For the fecal excretion, 59.4,19.5,17.7,and 15.3% of the dose administered were excreted in guinea pigs, mice, dogs, and rats, respectively, and rabbits and monkeys hardly excreted any metabolites. From the results of urinary and fecal excretion, the main excretion route was through liver and bile duct into feces in guinea pigs and was into urine in other five animals. For the effects of the dose administered on metabolism, dose-dependent variations of metabolism characteristic of guinea pigs were observed in biliary excretion, that is, main metabolite was M-8 in low dose (20mg/kg) while M-9 in high dose (500mg/kg) but such phenomenon was not found in rats.
- 社団法人日本薬学会の論文
- 1979-02-25
著者
-
大木 正彦
Research Laboratories, Morishita Pharmaceutical Co., Ltd.
-
林 敏廣
Research Laboratories Morishita Pharmaceutical Co. Ltd.
-
青山 みちよ
Research Laboratories, Morishita Pharmaceutical Co., Ltd.
-
福田 實
Research Laboratories, Morishita Pharmaceutical Co., Ltd.
-
岸川 虎比古
Research Laboratories, Morishita Pharmaceutical Co., Ltd.
-
福田 實
Research Laboratories Morishita Pharmaceutical Co. Ltd.
-
大木 正彦
Research Laboratories Morishita Pharmaceutical Co. Ltd.
-
岸川 虎比古
Research Laboratories Morishita Pharmaceutical Co. Ltd.
-
青山 みちよ
Research Laboratories Morishita Pharmaceutical Co. Ltd.
関連論文
- Studies on Hypolipidemic Agents. IV. Influence of a New Hypolipidemic Agent, 5-Tridecylpyrazole-3-carboxylic Acid, on Cholesterol Metabolism in Rats
- Studies on Hypolipidemic Agents. III. Comparison of the Hypolipidemic Properties of 5-Tridecylpyrazole-3-carboxylic Acid and Clofibrate
- Studies on Hypolipidemic Agents. II. Synthesis and Pharmacological Properties of Alkylpyrazole Derivatives
- Studies on Hypolipidemic Agents. I. Synthesis and Pharmacological Properties of Nicotinic Acid-Ethanolamine Derivatives
- Metabolism of 4-Ethoxy-2-methyl-5-morpholino-3 (2H)-pyridazinone (Emorfazone). V. Effect of Inducer Pretreatment on Oxygenation of the Morpholino Moiety in Guinea Pigs
- Metabolism of 4-Ethoxy-2-methyl-5-morpholino-3 (2H)-pyridazinone (M73101), a New Anti-inflammatory Agent. II. Species Differences of Metabolism and Excretion
- Metabolism of 4-Ethoxy-2-methyl-5-morpholino-3 (2H)-pyridazinone (M73101), a New Anti-inflammatory Agent. I. : Identification of the Metabolites in Rabbit and Their Pharmacological Studies
- Studies on Glucuronosides of Heterocyclic Compounds. I. Studies on the Synthesis and Properties of 2-Pyridyl β-D-Glucopyranosiduronic Acid and Its O→N Rearrangement
- Studies on Antiviral Agents. V. Synthesis and Antiviral Activity of N-Chloro Compounds.
- Studies on New Antiulcer Agents. I. Synthesis and Antisecretory Activity of Pyridazine Derivatives
- Synthesis of Purine and Pyrimidine Derivatives of Arsonic Acid.
- Studies on Chemotherapeutic Agents.III. A Synthesis of 3-Phenylpurine Derivatives
- Studies on Chemotherapeutic Agents.II. A Synthesis of Purine Nucleosides of _D-Glucuronic Acid
- Studies on Chemotherapeutic Agents.I. A Synthesis of Pyrimidine Nucleosides of D-glucuronic Acid and Its Derivatives
- A Synthesis of Uracil and Cytosine Nucleosides containing D-Glucuronic Acid and its Derivatives as the Sugar Component
- Studies on Chemotherapeutic Agents. V. A Synthesis of Benzimidazole Nucleosides of D-Glucopyranuronamide