Uptake of bepridil into isolated ventricular myocytes. Retention by actin

Isolated rat ventricular myocytes accumulate large amounts of bepridil intracellularly. The mode of transport is uncertain but uptake is of such a magnitude as to mask possible sarcolemmal binding sites. Bepridil is tightly bound within myocytes, there being only a minimal efflux into bepridil-free...

Full description

Saved in:
Bibliographic Details
Published inBiochemical pharmacology Vol. 32; no. 2; p. 227
Main Authors Cramb, G, Dow, J W
Format Journal Article
LanguageEnglish
Published England 15.01.1983
Subjects
Actins - metabolism
Animals
Anti-Arrhythmia Agents - metabolism
Bepridil
Binding Sites
In Vitro Techniques
Kinetics
Membranes - metabolism
Myocardium - metabolism
Protein Binding
Pyrrolidines - metabolism
Rats
Rats, Inbred Strains
Sarcolemma - metabolism
Temperature
Online AccessGet more information

Cover

More Information
Summary:Isolated rat ventricular myocytes accumulate large amounts of bepridil intracellularly. The mode of transport is uncertain but uptake is of such a magnitude as to mask possible sarcolemmal binding sites. Bepridil is tightly bound within myocytes, there being only a minimal efflux into bepridil-free medium. Purified F-actin binds bepridil in excess of 2 moles/mole actin, sufficient to account for the uptake of bepridil by myocytes incubated in 10 microM drug. At higher bepridil concentrations the amount transported into myocytes suggests that the drug may be distributed between actin-bound and cytoplasmic pools. Bepridil may alter cardiac contractility by a direct influence on the contractile filaments.
ISSN:0006-2952
DOI:10.1016/0006-2952(83)90548-8