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Interaction of Calcium Channel Blockers with Non-Neuronal Benzodiazepine Binding Sites

The ability of calcium channel blockers to displace the binding of benzodiazepine ligands was investigated in rat heart, kidney, and brain. The dihydropyridine calcium channel blockers nifedipine and nitrendipine displaced the binding of the non-neuronal-site ligand [3H]Ro5-4864, but not that of the...

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Published in:	Proceedings of the National Academy of Sciences - PNAS 1984-03, Vol.81 (5), p.1549-1552
Main Authors:	Cantor, E. H., Kenessey, A., Semenuk, G., Spector, S.
Format:	Article
Language:	English
Subjects:	Animals Benzodiazepines Benzodiazepines - metabolism Binding sites Brain - metabolism Calcium Calcium channel blockers Calcium Channel Blockers - pharmacology Dihydropyridines Drug interactions Kidney - metabolism Kidneys Kinetics Ligands Male Myocardium - metabolism Nifedipine - analogs & derivatives Nifedipine - pharmacology Nitrendipine Pharmacology Protein Binding Rats Rats, Inbred Strains Receptors Receptors, Cell Surface - drug effects Receptors, Cell Surface - metabolism Receptors, GABA-A Structure-Activity Relationship
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cited_by	cdi_FETCH-LOGICAL-c451t-3a4ec112a2182950bf51f33a0bc64ab1db645164167873810313517689c1f3d3
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container_issue	5
container_start_page	1549
container_title	Proceedings of the National Academy of Sciences - PNAS
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creator	Cantor, E. H. Kenessey, A. Semenuk, G. Spector, S.
description	The ability of calcium channel blockers to displace the binding of benzodiazepine ligands was investigated in rat heart, kidney, and brain. The dihydropyridine calcium channel blockers nifedipine and nitrendipine displaced the binding of the non-neuronal-site ligand [3H]Ro5-4864, but not that of the neuronal-site ligands [3H]flurazepam or [3H]clonazepam. The inhibition was competitive, with Kivalues in the micromolar range. Other calcium channel blockers--i.e., verapamil and diltiazem--were inactive at both sites. Thus, nonneuronal benzodiazepines bind to a class of sites that also binds dihydropyridines. This implies a role for benzodiazepines in the mediation of calcium-dependent phenomena.
doi_str_mv	10.1073/pnas.81.5.1549
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H.</creatorcontrib><creatorcontrib>Kenessey, A.</creatorcontrib><creatorcontrib>Semenuk, G.</creatorcontrib><creatorcontrib>Spector, S.</creatorcontrib><title>Interaction of Calcium Channel Blockers with Non-Neuronal Benzodiazepine Binding Sites</title><title>Proceedings of the National Academy of Sciences - PNAS</title><addtitle>Proc Natl Acad Sci U S A</addtitle><description>The ability of calcium channel blockers to displace the binding of benzodiazepine ligands was investigated in rat heart, kidney, and brain. The dihydropyridine calcium channel blockers nifedipine and nitrendipine displaced the binding of the non-neuronal-site ligand [3H]Ro5-4864, but not that of the neuronal-site ligands [3H]flurazepam or [3H]clonazepam. The inhibition was competitive, with Kivalues in the micromolar range. Other calcium channel blockers--i.e., verapamil and diltiazem--were inactive at both sites. Thus, nonneuronal benzodiazepines bind to a class of sites that also binds dihydropyridines. 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subjects	Animals Benzodiazepines Benzodiazepines - metabolism Binding sites Brain - metabolism Calcium Calcium channel blockers Calcium Channel Blockers - pharmacology Dihydropyridines Drug interactions Kidney - metabolism Kidneys Kinetics Ligands Male Myocardium - metabolism Nifedipine - analogs & derivatives Nifedipine - pharmacology Nitrendipine Pharmacology Protein Binding Rats Rats, Inbred Strains Receptors Receptors, Cell Surface - drug effects Receptors, Cell Surface - metabolism Receptors, GABA-A Structure-Activity Relationship
title	Interaction of Calcium Channel Blockers with Non-Neuronal Benzodiazepine Binding Sites
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