Prolonged inhibition of vascular contraction and calcium influx by the novel 1,4-dihydropyridine calcium antagonist cinaldipine (FRC-8653)

Jpn J Pharmacol. 1991 Jun;56(2):225-9. doi: 10.1254/jjp.56.225.

Abstract

We examined the effects of FRC-8653, a novel dihydropyridine calcium antagonist, on the contraction of an arterial preparation and the calcium influx into vascular smooth muscle cells to clarify the long-lasting hypotensive activity of this drug. Inhibition by FRC-8653 persisted for more than 7 hr after its removal, whereas nifedipine and nicardipine exhibited shorter durations of suppressive activity. These results suggest that prolonged inhibition of calcium influx through L-channels contributes to the long-lasting vasodilative and antihypertensive activity of FRC-8653.

MeSH terms

  • Animals
  • Antihypertensive Agents / pharmacology
  • Calcium / metabolism*
  • Calcium Channel Blockers / pharmacology*
  • Dihydropyridines / pharmacology*
  • In Vitro Techniques
  • Male
  • Mesenteric Arteries / drug effects
  • Muscle, Smooth, Vascular / drug effects*
  • Nicardipine / pharmacology
  • Nifedipine / pharmacology
  • Rats
  • Rats, Inbred Strains
  • Time Factors
  • Vasodilator Agents / pharmacology

Substances

  • Antihypertensive Agents
  • Calcium Channel Blockers
  • Dihydropyridines
  • Vasodilator Agents
  • cilnidipine
  • Nicardipine
  • Nifedipine
  • Calcium