The effect of the calcium channel agonist, Bay K-8644 on human vascular smooth muscle

Venkat Gopalakrishnan, Laura E. Park, Christopher Triggle

Research output: Contribution to journalArticle

29 Citations (Scopus)

Abstract

Bay K-8644, a calcium channel activator, caused a dose-dependent (ED50 = 12.8 nM) elevation of tone in the human umbilical artery. The response to Bay K-8644 was dependent upon extracellular calcium (Ca2+), competitively antagonized by the channel antagonist, nifedipine, and, in addition, the sensitivity to Bay K-8644 was increased by, but not dependent upon, elevating extracellular potassium. Bay K-8644 competitively displaced, IC50 = 1.8 nM, specific [3H]nitrendipine binding to a microsome fraction derived from the umbilical artery, suggesting that the Ca2+ channel activator and the structurally related dihydropyridine antagonists bind to a single site to affect Ca2+ channel function in human vascular smooth muscle.

Original languageEnglish
Pages (from-to)447-451
Number of pages5
JournalEuropean Journal of Pharmacology
Volume113
Issue number3
DOIs
Publication statusPublished - 31 Jul 1985
Externally publishedYes

    Fingerprint

Keywords

  • Bay K-8644
  • Calcium channel activator
  • Human umbilical artery
  • Nifedipine

ASJC Scopus subject areas

  • Pharmacology

Cite this