Effects of Monatepil Maleate, a New Ca^<2+> Channel Antagonist With α_1 : Adrenoceptor Antagonistic Activity, on Cholesterol Absorption and Catabolism in High Cholesterol Diet : Fed Rabbits
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概要
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The mechanism of the prophylactic effect against hyperlipidemia by monatepil maleate was investigated in animal models. Monatepil maleate is an antihypertensive agent with Ca2+-channel antagonistic, α1-adrenergic receptor-blocking, and lipid peroxidation inhibitory activity. In high cholesterol diet-fed rabbits, monatepil maleate (30 mg/kg, p.o., once daily for 9 weeks) showed a prophylactic effect against increases in total cholesterol and β-lipoprotein. Monatepil maleate significantly accelerated the clearance of radioactivity from the blood after intravenous injection of low-density lipoprotein (LDL) labeled with [1α, 2α (n)-3H]cholesterol, increasing biliary excretion of [3H]-bile acids without modifying bile acid composition. Furthermore, monatepil maleate tended to inhibit the absorption of orally administered [1α, 2α (n)-3H]cholesterol from the gastrointestinal tract in these rabbits. In Watanabe heritable hyperlipidemic (WHHL) rabbits, an animal model of hepatic LDL receptor deficiency, monatepil maleate (30 mg/kg, p.o., once daily for 6 months) did not suppress the increase in plasma lipids. These results suggest that the plasma lipid lowering effect of monatepil maleate requires the presence of hepatic LDL receptors. It is also suggested that monatepil maleate improves plasma lipid metabolism through two mechanisms: enhancement of clearance of plasma LDL, which may be mediated by up-regulation of hepatic LDL receptors, and acceleration of conversion of free cholesterol to bile acids in the liver.
- 社団法人 日本薬理学会の論文
- 1998-11-01
著者
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SUMIYA Toshiki
Department of Epidemiology, Research Institute, National Cardiovascular Center
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YASUDA MASASHI
Department of Computers and Systems Engineering, Tokyo Denki University
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Kurono Masuo
Department Of Physicochemical A Nalysis Disco Very Research Laboratories
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Hosoki Kanoo
Department Of Pharmacology I Discovery Research Laboratories
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Sumiya Toshiki
Department Of Pharmacology I Discovery Research Laboratories
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MASUDA YOSHINOBU
Department of Pharmacology, Research Laboratories, Dainippon Pharmaceutical Co., Ltd.
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Fujitani B
Department Of Pharmacology I Discovery Research Laboratories
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Ikeno Akihisa
Department Of Pharmacology I Discovery Research Laboratories
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MINATO Hisao
Department of Pharmacology I, Discovery Research Laboratories
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FUJITANI Buichi
Department of Pharmacology I, Discovery Research Laboratories
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Masuda Y
Division Of Toxicology Niigata College Of Pharmacy
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Masuda Yoshinobu
Department Of Pharmacology Research Laboratories Dainippon Pharmaceutical Co. Ltd.
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Yasuda Masashi
Department Of Computers And Systems Engineering Tokyo Denki University
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Minato Hisao
Department Of Pharmacology I Discovery Research Laboratories
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Sumiya Toshiki
Department Of Cardiovascular Medicine Institute Of Health Biosciences The University Of Tokushima Gr
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