103379-03-9
Chemical Structure
Monatepil maleate
Synonym(s): AJ-2615
- CAS No.: 103379-03-9
- Formula:C32H34FN3O5S
- Molecular Weight:591.69
IUPAC Name: N-(6,11-dihydrodibenzo[b,e]thiepin-11-yl)-4-(4-(4-fluorophenyl)piperazin-1-yl)butanamide maleate
InChIKey: ZDZXCYHMVFLGMT-BTJKTKAUSA-N
SMILES: OC(/C=C\C(O)=O)=O.FC(C=C1)=CC=C1N(CC2)CCN2CCCC(NC3C4=CC=CC=C4CSC5=CC=CC=C53)=O
Biological Activity: Monatepil (AJ-2615 free base) maleate is a calcium antagonist with potent α1-adrenoceptor blocking activity. Monatepil maleate inhibits vasopressin- or methacholine-induced ischemic electrocardiographic changes in a rat model of vasospastic angina and reduces the mean arterial pressure in anesthetized rats. Monatepil maleate also enhances low-density lipoprotein (LDL) receptor activity in human skin fibroblasts. Monatepil maleate can be used in research related to hypertension, atherosclerosis, hyperlipidemia and vasospastic angina[1][2][3].
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Monatepil maleate | Monatepil (AJ-2615 free base) maleate is a calcium antagonist with potent α1-adrenoceptor blocking activity. Monatepil maleate inhibits vasopressin- or methacholine-induced ischemic electrocardiographic changes in a rat model of vasospastic angina and reduces the mean arterial pressure in anesthetized rats. Monatepil maleate also enhances low-density lipoprotein (LDL) receptor activity in human skin fibroblasts. Monatepil maleate can be used in research related to hypertension, atherosclerosis, hyperlipidemia and vasospastic angina. | |||||||||||||||||||||
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References
- [1]. Miyazaki M, et al. Antihypertensive, antiatherosclerotic, and plasma lipid-lowering effects of monatepil, a novel calcium antagonist with alpha 1-adrenoceptor-blocking activity in experimental animals. American journal of hypertension. 1994 Oct;7(10 Pt 2):131S-40S.
- [2]. Yamamoto T, et al. Preventive effect of a new calcium antagonist, monatepil, on drug-induced ischaemic electrocardiographic changes in rats. Clinical and experimental pharmacology & physiology. 1993 Nov;20(11):673-8.
- [3]. Sasaki J, et al. Comparative effects of monatepil, a novel calcium antagonist with alpha 1-adrenergic-blocking activity, and nitrendipine on lipoprotein and carbohydrate metabolism in patients with hypertension. American journal of hypertension. 1994 Oct;7(10 Pt 2):161S-166S.
