Short-term treatment of the endothelium with dihydropyridine calcium antagonists resulted in an increased release in NO that is not due to a modulation of L-type calcium channels, because macrovascular endothelial cells do not express this channel. We investigated whether long-term (48 hours) treatment of porcine endothelial cell cultures with the dihydropyridine calcium antagonist nifedipine r...

BACKGROUND The effects of the 3 classes of L-type calcium-channel blockers (CCBs) on vascular endothelial function have not been clarified in patients with coronary vasospasm. METHODS AND RESULTS Twenty-five normotensive patients (age 64.0+/-1.4 years) with coronary vasospasm were randomly treated for 3 months with benidipine, diltiazem, and verapamil, which belong to the dihydropyridine, ben...

RATIONALE Dihydropyridines are widely used for the treatment of several cardiac diseases due to their blocking activity on L-type Ca(2+) channels and their renowned antioxidant properties. METHODS We synthesized six novel dihydropyridine molecules and performed docking studies on the binding site of the L-type Ca(2+) channel. We used biochemical techniques on isolated adult rat cardiomyocytes...

Reaction of methoxyvinylmethylketone with different amines and aldehydes under Lewis-acid catalysed conditions results in a novel, formal, step-wise [1+2+1+2]-cycloaddition to give dihydropyridine products.

1,4 Dihydropyridines are very versatile compounds and have important role as therapeutic agents. The 1, 4 (1,4 DHPs) well known calcium channel blocker their use in treatment of cardiovascular diseases is common. These also to antimicrobial activities. N-heterocyclic represent framework for agricultural pharmaceutical industries. antibacterial antifungal Hence, the substituted 4- Dihydropyridin...

Molecular interactions of 4-diphenylmethoxy-1-methylpiperidine derivatives with the calcium channel CaV1.1 (pdb:6JP5) are described. All compounds tested, previously shown to inhibit adrenergic vascular contractions, display similar binding energetics and trans-membrane domain 6JP5 on opposite side relative pore, where nifedipine, a known dihydropyridine Ca2+ blocker binds. Additionally, tested...

A series of dihydropyridines were identified that have an effect on the accumulation of tau, an important target in Alzheimer's disease. The dihydropyridine collection was expanded using the Hantzsch multicomponent reaction to develop preliminary structure-activity relationships.

We have investigated the modulation of L-type calcium channel currents in isolated ventricular cells by the dihydropyridine derivative amlodipine, a weak base with a pKa of 8.6. Under conditions that favor neutral drug molecules, amlodipine block resembles other, previously described, neutral dihydropyridine derivatives: block is more pronounced at depolarized voltages, repetitive pulsing is no...

The purpose of this study was to determine if there are alterations in the dihydropyridine and/or ryanodine receptors that might explain the excitation-contraction uncoupling associated with eccentric contraction-induced skeletal muscle injury. The left anterior crural muscles (i.e., tibialis anterior, extensor digitorum longus, and extensor hallucis longus) of mice were injured in vivo by 150 ...

The dihydropyridine calcium channel blocker, nitrendipine, was studied for its effects on the sodium current of single cultured ventricular cells from neonatal rats. The patch-clamp method of recording whole cell currents was used, and sodium currents were isolated by suppressing potassium and calcium currents. Potassium currents were blocked by replacing potassium with cesium in the internal a...