Dihydropyridine and peripheral type benzodiazepine binding sites: subcellular distribution and molecular size determination.

European journal of pharmacology ·Vol. 119 ·No. 3 ·1985-12-17 ·Pages 153-67

Doble A, Benavides J, Ferris O, Bertrand P, Menager J, Vaucher N, Burgevin MC, Uzan A, Gueremy C, Le Fur G

Abstract

Electrophysiological and pharmacological studies have shown that peripheral-type benzodiazepine receptors modulate voltage-sensitive calcium channels in the heart. We have compared these binding sites with binding sites for [3H]dihydropyridines, which are believed to label such channels. Although no direct or allosteric interaction could be demonstrated between the two sites, their subcellular distribution--sarcolemma and ryanodine-sensitive sarcoplasmic reticulum--was parallel. Size determination of the two sites suggests that the receptors for these two classes of compounds are separate molecules packaged in the same membrane compartment.

MeSH Terms

Animals Benzodiazepinones/metabolism,pharmacology Binding Sites Calcium/metabolism Calcium Channel Blockers/metabolism Calcium Channels Cell Fractionation Dogs Ion Channels Isoquinolines/metabolism,pharmacology Isradipine Male Molecular Weight Myocardium/metabolism,ultrastructure Nifedipine/analogs & derivatives,metabolism,pharmacology Nitrendipine Oxadiazoles/metabolism Rats Rats, Inbred Strains Receptors, GABA-A/metabolism Receptors, Nicotinic/metabolism Sarcolemma/metabolism Sarcoplasmic Reticulum/metabolism Verapamil/metabolism,pharmacology

Chemicals

Benzodiazepinones Calcium Channel Blockers Calcium Channels Ion Channels Isoquinolines Oxadiazoles Receptors, GABA-A Receptors, Nicotinic 4'-chlorodiazepam Nitrendipine Verapamil Nifedipine Calcium PK 11195 Isradipine

Authors & Affiliations

10 authors, click to expand affiliations / ORCID

Doble A

Benavides J

Ferris O

Bertrand P

Menager J

Vaucher N

Burgevin M C

Uzan A

Gueremy C

Le Fur G

Article Info

Journal

European journal of pharmacology

Abbr.

Eur J Pharmacol

ISSN

0014-2999

DOI

10.1016/0014-2999(85)90291-2

Published

1985-12-17

Pages

153-67

Language

English

Region

Netherlands

NLM ID

1254354

Subset

External Links

PubMed source DOI: 10.1016/0014-2999(85)90291-2 View journal details

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Dihydropyridine and peripheral type benzodiazepine binding sites: subcellular distribution and molecular size determination.

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