Antithrombotic and ulcerogenic effects of fenflumizole, a new anti-inflammatory imidazole derivative, in rats.
スポンサーリンク
概要
- 論文の詳細を見る
Fenflumizole (2-(2, 4-difluorophenyl)-4, 5-bis(4-methoxyphenyl) imidazole) was given to rats in a single oral dose of 30 mg/kg. The plasma concentration of fenflumizole reached a peak 2-3 hr after the dosing in non-fasted as well as fasted rats. Two metabolites (demethylation products) of fenflumizole were also detected in the plasma, but only in traces. Fenflumizole (30 and 100 mg/kg) and aspirin (100 mg/kg), given orally 2 hr prior to i.v. arachidonate (80 mg/kg), were effective in protecting the rats from death. Fenflumizole in single oral doses of 100 to 800 mg/kg dose-dependently developed erosions in the rat gastric mucosa, but was much less ulcerogenic than aspirin (3.12-200 mg/kg). Thus, fenflumizole seems to possess a potent antithrombotic activity and a relatively low gastro-ulcerogenicity in rats.
- 公益社団法人 日本薬理学会の論文
著者
-
NABATA Hiroyuki
Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, University of Tokyo
-
SAKAI Kazushige
Departinent of Pharmacology, Research Laboratories, Chugai Pharmaceutical Co.
-
YAMAZAKI Tamotsu
Department of Pharmacology, Research Laboratories, Chugai Pharmaceutical Co., Ltd.
-
UCHINO Masako
Drug Metabolism, Research Laboratories, Chugai Pharmaceutical Co., Ltd.
-
OKAZAKI Akira
Drug Metabolism, Research Laboratories, Chugai Pharmaceutical Co., Ltd.
関連論文
- EFFECTS OF A NEW CORONARY VASODILATOR, N-(2-HYDROXYETHYL)NICOTINAMIDE NITRATE (SG-75) AND NITROGLYCERIN ON CARDIOVASCULAR HEMODYNAMICS IN YOUNG AND AGED BEAGLE DOGS
- PHARMACOLOGICAL STUDIES OF PANAX GINSENG ROOT: ESTIMATION OF PHARMACOLOGICAL ACTIONS OF PANAX GINSENG ROOT
- A POSSIBLE PURINERGIC MECHANISM FOR REACTIVE ISCHEMIA IN ISOLATED, CROSS-CIRCULATED RAT KIDNEY
- TRYPTAMINERGIC VASOCONSTRICTION INDUCED BY ADENOSINE IN THE FEMORAL VASCULAR BED OF THE RAT
- EFFECTS OF N-(2-HYDROXYETHYL)NICOTINAMIDE NITRATE (SG-75) ON METHACHOLINE-INDUCED ECG CHANGES IN INTACT ANESTHETIZED RATS
- FEMORAL VASCULAR RESPONSES TO PURINE AND PYRIMIDINE DERIVATIVES: RELEASE OF 5-HYDROXYTRYPTAMINE BY PURINE DERIVATIVES IN ISOLATED, CROSS-CIRCULATED RAT HINDLIMB
- DEVELOPMENT OF TOLERANCE AND A NEW CORONARY VASODILATOR, N-(2-HYDROXYETHYL)NICOTINAMIDE NITRATE (SG-75): A COMPARISON WITH NITROGLYCERIN
- DEVELOPMENT OF CORONARY COLLATERAL CIRCULATION IN MINIATURE SWINE AND EFFECTS OF SEVERAL DRUGS
- THE HYPOTENSIVE MECHANISMS OF THE NEW ANTI-ANGINAL DRUG, N-(2-HYDROXYETHYL)NICOTINAMIDE NITRATE (SG-75) IN BEAGLE DOGS
- PHARMACODYNAMIC AND METABOLISM STUDIES ON A NEW CORONARY VASODILATOR, N-(2-HYDROXYETHYL) NICOTINAMIDE NITRATE (SG-75)
- VASCULARLY PERFUSED RAT SMALL INTESTINE: A RESEARCH MODEL FOR DRUG ABSORPTION
- POSITIVE AND NEGATIVE CHRONOTROPIC RESPONSE OF THE S-A NODE TO OXYFEDRINE
- PHARMACOLOGICAL STUDIES OF NEUTRAL SAPONINS (GNS) OF PANAX GINSENG ROOT
- PHARMACOLOGICAL FEATURES OF PERIPHERAL VASCULAR BEDS OF BEAGLES
- Protective Effects of the Antianginal Agent Nicorandil on Arachidonate-Induced Sudden Death in Rats: Comparison with Several Antianginal Agents and Cyclooxygenase Inhibitors
- Investigations into the mechanism of the antihypertensive effect of SGB-1534, a novel .ALPHA.1-adrenoceptor antagonist, in rats.
- Antithrombotic and ulcerogenic effects of fenflumizole, a new anti-inflammatory imidazole derivative, in rats.
- Antiplatelet effects of fenflumizole, a new anti-inflammatory drug, in dogs.
- Comparison of cardiovascular effects of SGB-1534 and prazosin, selective .ALPHA.1-adrenoceptor antagonists, in anesthetized dogs.
- Comparative effects of nicorandil and nitroglycerin on tracheal and vascular smooth muscle in the dog, in vivo and in vitro.
- Comparison of development of tolerance between nicorandil and nitroglycerin in anesthetized, open-chest dogs.
- Effects of a new anti-inflammatory imidazole derivative, fenflumizole, on platelet aggregation in the rabbit.