Calcium-channel antagonist binding to isolated vascular smooth muscle membranes

C. R. Triggle, Devendra K. Agrawal, G. T. Bolger, E. E. Daniel, C. Y. Kwan, E. M. Luchowski, D. J. Triggle

Research output: Contribution to journalArticle

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Abstract

The binding characteristics of the calcium-channel antagonist nitrendipine an analog of nifedipine, have been measured in plasma membrane enriched microsomal fractions from the canine thoracic aorta, canine mesenteric artery, and rat mesenteric artery. The dissociation constants, K(D) for the high-affinity binding sites were, respectively, 0.308, 0.254, and 0.101 nM and B(max) values for binding capacity were 20.3, 25.0, and 18.0 fmol/mg of microsomal protein. Studies with isolated tissues, in which the sensitivity of the high potassium mechanical response to nitrendipine was determined, indicate that the appearance K(D) for nitrendipine in the canine mesenteric artery, as reflected by the IC 50 (mean inhibition constant) value, is 4.5-5.3 nM and for the rat mesenteric artery 2.5-6.6 nM.

Original languageEnglish
Pages (from-to)1738-1741
Number of pages4
JournalCanadian Journal of Physiology and Pharmacology
Volume60
Issue number12
StatePublished - 1982
Externally publishedYes

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Mesenteric Arteries
Calcium Channel Blockers
Nitrendipine
Vascular Smooth Muscle
Canidae
Membranes
Nifedipine
Thoracic Aorta
Potassium
Binding Sites
Cell Membrane
Proteins

All Science Journal Classification (ASJC) codes

  • Physiology
  • Pharmacology

Cite this

Triggle, C. R., Agrawal, D. K., Bolger, G. T., Daniel, E. E., Kwan, C. Y., Luchowski, E. M., & Triggle, D. J. (1982). Calcium-channel antagonist binding to isolated vascular smooth muscle membranes. Canadian Journal of Physiology and Pharmacology, 60(12), 1738-1741.

Calcium-channel antagonist binding to isolated vascular smooth muscle membranes. / Triggle, C. R.; Agrawal, Devendra K.; Bolger, G. T.; Daniel, E. E.; Kwan, C. Y.; Luchowski, E. M.; Triggle, D. J.

In: Canadian Journal of Physiology and Pharmacology, Vol. 60, No. 12, 1982, p. 1738-1741.

Research output: Contribution to journalArticle

Triggle, CR, Agrawal, DK, Bolger, GT, Daniel, EE, Kwan, CY, Luchowski, EM & Triggle, DJ 1982, 'Calcium-channel antagonist binding to isolated vascular smooth muscle membranes', Canadian Journal of Physiology and Pharmacology, vol. 60, no. 12, pp. 1738-1741.
Triggle, C. R. ; Agrawal, Devendra K. ; Bolger, G. T. ; Daniel, E. E. ; Kwan, C. Y. ; Luchowski, E. M. ; Triggle, D. J. / Calcium-channel antagonist binding to isolated vascular smooth muscle membranes. In: Canadian Journal of Physiology and Pharmacology. 1982 ; Vol. 60, No. 12. pp. 1738-1741.
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