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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Bibliographic Details
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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Summary: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.
ISSN:0027-8424
1091-6490
DOI:10.1073/pnas.81.5.1549