More than 40 years after their introduction in therapy, 1,4-dihydropyridines (DHPs) are still amongst the most prescribed drugs in the world. Though they all share a similar mechanism of action blocking L-type voltage-gated Ca(2+) channels, DHPs differ in crucial pharmacological properties like tissue selectivity and cardiodepressant activity. This review examines how changes in the DHP structu...

The synthesis of various substituted Biginelli 3,4-dihydropyrimidinone/thione and Hantzsch 1,4dihydropyridine derivatives has been achieved using a modified procedure in the presence of potassium ter-butoxide (tBuOK) as a catalyst under solvent-free conditions, in good to excellent yields.

In the title compound, C(18)H(17)N(3), the dihedral angle between the dihydropyridine and phenyl rings is 72.57 (5)° and that between the dihydropyridine ring and malononitrile plane is 5.19 (20)°. The C-C bond lengths in the pyridine ring are considerably shorter than those of normal single bonds, indicating that electrons on the dihydropyridine ring, including the non-bonding electrons of the...

MC3T3-E1 osteogenic cells in a growing state were voltage-clamped by the whole-cell patch-clamp method. The MC3T3-E1 cells exhibited a transient, fast-inactivating Ca inward current upon depolarizing pulses from a holding potential of -80 mV. This current had a threshold of activation of about -50 mV and was insensitive to the dihydropyridine, nifedipine. These results show that MC3T3-E1 cells ...

The spontaneous firing patterns of striatal cholinergic interneurons are sculpted by potassium currents that give rise to prominent afterhyperpolarizations (AHPs). Large-conductance calcium-activated potassium (BK) channel currents contribute to action potential (AP) repolarization; small-conductance calcium-activated potassium channel currents generate an apamin-sensitive medium AHP (mAHP) aft...

A simple and mild one-pot three-component reaction for the preparation 1,4-dihydropyridines has been developed from various aldehyde substrates, 1,3-dicarbonyl compounds (dimedone) and ammonium acetate (Hantzsch method) in the presence of a catalytic amount of phospho sulfonic acid (PSA) as an efficient and heterogeneous solid acid in EtOH at room temperature. Preparation of PSA is straightforw...