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

Calcium Channel Agonists
3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester
Vascular Smooth Muscle
Umbilical Arteries
Nitrendipine
Nifedipine
Microsomes
Inhibitory Concentration 50
Potassium
Calcium

Keywords

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

ASJC Scopus subject areas

  • Pharmacology

Cite this

The effect of the calcium channel agonist, Bay K-8644 on human vascular smooth muscle. / Gopalakrishnan, Venkat; Park, Laura E.; Triggle, Christopher.

In: European Journal of Pharmacology, Vol. 113, No. 3, 31.07.1985, p. 447-451.

Research output: Contribution to journalArticle

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