Effects of oxodipine and elgodipine on (+)-[3H]-isradipine binding to cardiac and vascular membranes: cardiovascular selectivity

Fundam Clin Pharmacol. 1994;8(6):546-52. doi: 10.1111/j.1472-8206.1994.tb00836.x.

Abstract

We studied the effects of six dihydropyridines on the specific binding of (+)-[3H]-isradipine to vascular (portal vein) and cardiac isolated membranes to achieve the relative cardiovascular selectivity of these compounds. Elgodipine, (+)-oxodipine and nifedipine had a significantly higher affinity for the vascular L-type calcium channel than for the cardiac calcium channel while nicardipine showed opposite properties. The other dihydropyridines (nitrendipine and (+)-isradipine) had similar affinities for the cardiac and vascular calcium channels. As the membrane potential of isolated membranes is about 0 mV, these results suggest that the differences in binding of these dihydropyridines to L-type calcium channels in vascular and cardiac cells may be attributed to differences in the molecular structure of these calcium channels.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Binding Sites
  • Calcium Channel Blockers / pharmacology*
  • Dihydropyridines / pharmacology*
  • Horses
  • In Vitro Techniques
  • Isradipine / metabolism*
  • Myocardium / metabolism*
  • Portal Vein / metabolism*
  • Rats

Substances

  • Calcium Channel Blockers
  • Dihydropyridines
  • elgodipine
  • oxodipine
  • Isradipine