[3H]Nitrendipine-labeled calcium channels discriminate inorganic calcium agonists and antagonists

R. J. Gould, K. M M Murphy, Solomon H Snyder

Research output: Contribution to journalArticle

Abstract

[3H]Nitrendipine binds with high affinity to brain membranes with a drug specificity indicating association with sites mediating the pharmacologic actions of dihydropyridine slow-calcium-channel antagonist drugs. In brain membranes, [3H]nitrendipine binding is absolutely dependent on the presence of calcium ions. Interactions of cations with [3H]nitrendipine binding sites correlate with their physiologic actions at voltage-dependent calcium channels. Ions such as strontium and barium, which mimic calcium physiologically, share the action of calcium in enhancing [3H]nitrendipine binding. Ions such as lanthanum and cobalt, which block the effects of calcium, can inhibit [3H]nitrendipine binding and block the stimulating actions of calcium. The ability to monitor the influence of ions on an agonist-antagonist continuum at [3H]nitrendipine binding sites provides a molecular probe to explore the regulation of cellular function by calcium and other cations.

Original languageEnglish (US)
Pages (from-to)3656-3660
Number of pages5
JournalProceedings of the National Academy of Sciences of the United States of America
Volume79
Issue number11 I
StatePublished - 1982

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Nitrendipine
Calcium Channels
Calcium
Ions
Cations
Binding Sites
Pharmacologic Actions
Molecular Probes
Lanthanum
Strontium
Membranes
Brain
Calcium Channel Blockers
Barium
Cobalt
Pharmaceutical Preparations

ASJC Scopus subject areas

  • General
  • Genetics

Cite this

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abstract = "[3H]Nitrendipine binds with high affinity to brain membranes with a drug specificity indicating association with sites mediating the pharmacologic actions of dihydropyridine slow-calcium-channel antagonist drugs. In brain membranes, [3H]nitrendipine binding is absolutely dependent on the presence of calcium ions. Interactions of cations with [3H]nitrendipine binding sites correlate with their physiologic actions at voltage-dependent calcium channels. Ions such as strontium and barium, which mimic calcium physiologically, share the action of calcium in enhancing [3H]nitrendipine binding. Ions such as lanthanum and cobalt, which block the effects of calcium, can inhibit [3H]nitrendipine binding and block the stimulating actions of calcium. The ability to monitor the influence of ions on an agonist-antagonist continuum at [3H]nitrendipine binding sites provides a molecular probe to explore the regulation of cellular function by calcium and other cations.",
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T1 - [3H]Nitrendipine-labeled calcium channels discriminate inorganic calcium agonists and antagonists

AU - Gould, R. J.

AU - Murphy, K. M M

AU - Snyder, Solomon H

PY - 1982

Y1 - 1982

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AB - [3H]Nitrendipine binds with high affinity to brain membranes with a drug specificity indicating association with sites mediating the pharmacologic actions of dihydropyridine slow-calcium-channel antagonist drugs. In brain membranes, [3H]nitrendipine binding is absolutely dependent on the presence of calcium ions. Interactions of cations with [3H]nitrendipine binding sites correlate with their physiologic actions at voltage-dependent calcium channels. Ions such as strontium and barium, which mimic calcium physiologically, share the action of calcium in enhancing [3H]nitrendipine binding. Ions such as lanthanum and cobalt, which block the effects of calcium, can inhibit [3H]nitrendipine binding and block the stimulating actions of calcium. The ability to monitor the influence of ions on an agonist-antagonist continuum at [3H]nitrendipine binding sites provides a molecular probe to explore the regulation of cellular function by calcium and other cations.

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