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Characterization of binding of the Ca++ channel antagonist, [3H]nitrendipine, to guinea-pig ileal smooth muscle.
The data suggest that [3H]nitrendipine binding in smooth muscle is to a site which mediates the pharmacologic response, which is consistent with previous reports. Expand
Calcium channel ligands.
Investigators are examining the efficacy of Ca2+ blockers in a number of additional disorders both within and without the cardiovascular system, in­ cluding achalasia, asthma, atherosclerosis, dysmenorrhea, intestinal spasm, labyrinthine disorders, migraine, peripheral vascular disorders, premature labor, and urinary incontinence. Expand
High affinity binding of a calcium channel antagonist to smooth and cardiac muscle.
High affinity binding of the Ca 2+ -channel antagonist nitrendipine has been measured in microsomal membrane fractions from guinea pig ileal longitudinal smooth muscle and was sensitive to displacement by a series of 1,4-dihydropyridine analogs of nifedipine. Expand
New developments in Ca2+ channel antagonists.
  • R. Janis, D. Triggle
  • Computer Science, Medicine
  • Journal of medicinal chemistry
  • 21 February 1984
The recent radioligand binding assay supports the conclusion, drawn earlier from the chemical and pharmacological heterogeneity of these agents, that there exists multiple sites and mechanisms of action for the Ca2+ channel antagonists. Expand
Ca2+ channel ligands: Structure‐function relationships of the 1,4‐dihydropyridines
Review of Ca 2+ channel: mecanism of action, structure, pharmacology, regulation. Structure activity relationships of the 1,4-dihydropyridines
Sites of action of Ca2+ channel inhibitors.
Inhibition of [3H]nitrendipine binding and blockade of K+ responses in guinea pig ileum by 1,4-dihydropyridines are well correlated, supporting the view that the observed binding is to Ca2+ channel. Expand
Aortic reactivity of rats with genetic and experimental renal hypertension.
The isometric tensions produced by low concentrations of norepinephrine (1 × 10−10 and 3 × 10−10M) or potassium (10 mM) were greater in aortic rings from mature rats with hypertension produced byExpand
1,4‐Dihydropyridine Ca2+ channel antagonists and activators: A comparison of binding characteristics with pharmacology
This comparison of the binding characteristics and pharmacology of 1,4‐dihydropyridines indicates that the high‐affinity binding sites studied in cardiac and smooth muscle cells represent a majorExpand
Characteristics of the binding of [3H]nitrendipine to rabbit ventricular membranes: modification by other Ca++ channel antagonists and by the Ca++ channel agonist Bay K 8644.
The results suggest that organic antagonists do not act by physically blocking the Ca++ channel and support the hypothesis that the high affinity binding sites for [3H]nitrendipine in isolated cardiac membranes are associated with Ca++ channels that are inactivated or are otherwise unavailable for opening. Expand