Endothelin is a potent endothelium-derived vasoconstrictor peptide recently characterized from porcine and human vascular endothelial cells. Here we provide evidence that endothelin activates the dihydropyridine-sensitive, voltage-dependent Ca2+ channel in porcine coronary artery smooth muscle. The vasoconstrictor action of endothelin is efficiently antagonized by low doses of the dihydropyridi...

To compare the antianginal eŠects of 1,4-dihydropyridine-type calcium-channel blockers, we evaluated the eŠects of benidipine, amlodipine, nifedipine, and efonidipine on vasopressin-induced myocardial ischemia in rats, an experimental model of angina. Intravenous administration of benidipine (3 mg/kg), amlodipine (1000 mg/kg), and nifedipine (100 mg/kg) suppressed the vasopressin-induced S-wave...

hronic stable angina (CSA) represents the largest cardiovascular disorder in the United States and is the initial clinical presentation of ischemic heart disease in 50% of patients. CSA is the result of the progression of coronary atherosclerosis and becomes symptomatic once the luminal diameter of the vessel is occluded by >50%. Current medical therapy is targeted at reducing the frequency of ...

An efficient and expeditious catalyst-free procedure was developed for the one- pot synthesis of 1, 4-dihydropyridine derivatives via the three-component reaction of various aldehydes, ethyl acetoacetate, and ammonium acetate in PEG-400. The reaction was carried out at 110°С and the products were obtained in good to high yields.

β-site amyloid precursor protein cleaving enzyme (BACE-1) is a validated target for Alzheimer therapy due to its distinctive role in pathogenesis of AD. In the present contribution, a series of new 3,5-bis-N-(aryl/heteroaryl) carbamoyl-4-aryl-1,4-dihydropyridine structures were synthesized as BACE-1 inhibitors (6a-6n). In vitro BACE-1 inhibitory activities were determined by enzymatic fluoresce...

Current researches have showed that N3, N5-diaryl-2, 6-dimethyl -1, 4-dihydropyrine-3, 5- dicarboxamide analogues demonstrate notable anti-tubercular activity. In this study, Hantzsch condensation was used to design and synthesize new analogues of dihydropyridine (DHP). Different diary carboxamides were inserted at positions 3 and 5 of the DHP ring. 4(5)-chloro-2-ethyl-5(4)-imidazolyl moiety wa...

The effect of temperature and air humidity on the stability of 7 derivatives of 1,4-dihydropyridine (nifedipine, nisoldipine, nitrendipine, nimodipine, nicardipine, felodipine and amlodipine) in solid state has been studied by accelerated testing. Quantitative analysis of the compounds studied was made by UV spectrophotometry, identification of the thermodegradation products and reference to th...