The crucial role of L-type Ca2+ channels in the initiation of cardiac and smooth muscle contraction has made them major therapeutic targets for the treatment of cardiovascular disease. L-type channels share a common pharmacological profile, including high-affinity voltage- and frequency-dependent block by the phenylalkylamines, the benz(othi)azepines, and the dihydropyridines. These drugs are t...

The Hantzsch reaction was adapted to allow the rapid radiosynthesis of 13N-labelled 1,4-dihydropyridines, including [13N]nifedipine, for preclinical PET imaging.

The electronic nature of substituents attached to the 4-aryl moiety of 1,4-dihydropyridines strongly affects the photophysical and photochemical behavior of these family of compounds. The presence of an electron donor substituent on the 4-aryl moiety (or the absence of electron-withdrawing ones) modifies the luminescence lifetimes (τ < 100 ps) and diminishes the photodecomposition quantum yield...

P-Glycoprotein, the plasma membrane protein responsible for the multidrug resistance of some tumour cells, is an active transporter of a number of structurally unrelated hydrophobic drugs. We have characterized the modulation of its ATPase activity by a multidrug-resistance-related cytotoxic drug, vinblastine, and different multidrug-resistance-reversing agents, verapamil and the dihydropyridin...

2-monobromomethyl 1,4-dihydropyridines is selectively synthesized by bromination of the parent compound by 1.1 equivalents of pyridinium bromide perbromide in dichloromethane/pyridine at -20 °c. the same reagent in dichloromethane at 0 °c produce the 2,6-bis(bromomethyl) 1,4-dihydropyridines.

objectives in order to provide a pharmacological profile for some newly synthesized dihydropyridines, we investigated their effects on the isolated rat colon segments and the isolated rat atrium contractility. the tested compounds include alkyl ester analogues of nifedipine, in which the ortho-nitrophenyl group at position 4 is replaced by 2-alkylthio-1-benzyl-5-imidazolyl substituent, and nife...

hantzsch 1, 4-dihydropyridines (1,4-dhps) can be oxidized to the corresponding pyridine derivatives by thallium triacetate in high yields.

objective(s): the structure- activity relationship of a series of 36 molecules, showing l-type calcium channel blocking was studied using a qsar (quantitative structure–activity relationship) method. materials and methods: structures were optimized by the semi-empirical am1 quantum-chemical method which was also used to find structure-calcium channel blocking activity trends. several types of d...

Calcium channels are known to exist in muscle, neuronal and secretory cells. The 1,4-dihydropyridines are potent blockers of L-type Ca channels, and have been used as specific probes in the study of dihydropyridine-sensitive Ca channels. The receptor for the 1,4-dihydropyridines has been purified from skeletal muscle in order to characterize the biochemistry and molecular biology of the dihydro...

The venom of the black mamba contains a 60-amino acid peptide called calciseptine. The peptide has been fully sequenced. It is a smooth muscle relaxant and an inhibitor of cardiac contractions. Its physiological action resembles that of drugs, such as the 1,4-dihydropyridines, which are important in the treatment of cardiovascular diseases. Calciseptine, like the 1,4-dihydropyridines, selective...