Binding of imipramine and cocaine to a model lipid membrane View Full Text


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

1984-07

AUTHORS

Maarten E. A. Reith, Henry Sershen, Abel Lajtha

ABSTRACT

[3H]Imipramine and [3H]cocaine were concentrated at membranes of liposomes prepared from phosphatidylcholine, cholesterol, and dicetylphosphate. This "binding" has an apparent dissociation constant in the micromolar range and a density close to 2 pmol/micrograms of phosphatidylcholine. The potencies of various drugs in inhibiting the binding to liposomes correlated only weakly with those in inhibiting the high-affinity binding of [3H]imipramine and [3H]cocaine to brain membranes. However, there was a highly significant correlation between the potencies of drugs in inhibiting binding to liposomes and their lipophilic character, indicating the involvement of hydrophobic bonding. Although the amounts of phosphatidylcholine and cholesterol in brain preparations in assays for high-affinity binding to brain membranes were in the same range as those used in our assays with liposomes, the inhibition of the high-affinity binding to brain membranes was only weakly dependent upon the lipophilicity of the inhibiting drug. These results indicate that lipophilicity is but one of the factors in the complex binding interactions between lipophilic substances and integral brain membranes. In addition, the results are in agreement with the suggestion that phosphatidylcholine and cholesterol are not the primary sites of high-affinity binding [3H]imipramine and [3H]cocaine to brain membranes, although it cannot be ruled out that these lipids have different properties in natural biological membranes and in artificial liposome membranes. More... »

PAGES

965-977

References to SciGraph publications

Identifiers

URI

http://scigraph.springernature.com/pub.10.1007/bf00964527

DOI

http://dx.doi.org/10.1007/bf00964527

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1039843001

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/6504231


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