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Monatepil maleate (AJ-2615) is a potent and orally active Ca2+-channel antagonist and a noncompetitive ACAT inhibitor. Monatepil maleate decreases blood pressure and improves plasma lipid metabolism. Monatepil maleate has the potential for the research of hyperlipidemia[1][2]. | [Definition]
ChEBI: Monatepil maleate is a dibenzothiepine. | [in vivo]
Monatepil maleate (30 mg/kg; p.o.; once daily for 9 weeks) improves plasma lipid metabolism[1].
Monatepil maleate (30 mg/kg; p.o.; once daily for 6 weeks) inhibits ACAT activity and esterifies cholesterol content in high cholesterol diet monkeys[2]. | Animal Model: | 8 weeks, Male japanese white rabbits (high cholesterol diet-fed)[1] | | Dosage: | 30 mg/kg | | Administration: | P.o.; once daily for 9 weeks | | Result: | Improved plasma lipid metabolism and reduced atherosclerotic lesions, decreased blood pressure. |
| Animal Model: | 4-7 kg, 4-7 years monkeys (high cholesterol diet for 6 months)[2] | | Dosage: | 30 mg/kg | | Administration: | P.o.; once daily for 6 weeks | | Result: | Inhibited the increases of ACAT activity and esterified cholesterol content. |
| [References]
[1] Ikeno A, et al. Effects of monatepil maleate, a new Ca2+ channel antagonist with alpha1-adrenoceptor antagonistic activity, on cholesterol absorption and catabolism in high cholesterol diet-fed rabbits. Jpn J Pharmacol. 1998 Nov;78(3):303-12. DOI:10.1254/jjp.78.303
[2] Sumiya T, et al. Inhibitory effect of monatepil maleate on acyl-CoA:cholesterol acyltransferase activity in the liver of cholesterol-fed Japanese monkeys. Am J Hypertens. 1997 Jul;10(7 Pt 1):779-85. DOI:10.1016/s0895-7061(97)00066-6 |
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