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Intracellular localization of the calcium- and calmodulin antagonist fendiline
R Weyhenmeyer1, M Gross, B Maurer-Schultze
1Abteilung Pharmakokinetik der Thiemann Arzneimittel GmbH, Waltrop Fed. Rep. of Germany.
Abstract:
Microautoradiograpic studies of mouse heart sections were performed to evaluate intracellular localization of the antianginal drug fendiline (Sensit). 15 microCi 3H-fendiline/g b. w. (0.5 mg/kg b.w.) were injected intravenously. 10 min p.a. the heart was removed and either frozen in acetone/dry ice or, after perfusion in situ with dextran 40 and formaldehyde, fixed in formaldehyde. Frozen, paraffin-embedded, and semithin epoxy resin sections were prepared and coated with Ilford K2 emulsion. After 7 to 30 days exposure and development in amidol silver grains were counted above cells, nuclei and extracellular space. The results show that fendiline is able to enter myocardial cells.
Insights
The antianginal drug fendiline readily enters mouse heart cells, as shown by microautoradiography. This study confirms fendiline
Area of Science:
- Pharmacology
- Cardiovascular Research
- Cell Biology
Background:
- The antianginal drug fendiline is used to treat heart conditions.
- Understanding drug distribution within heart tissue is crucial for efficacy.
Purpose of the Study:
- To investigate the intracellular localization of fendiline in mouse myocardial cells.
- To determine if fendiline penetrates heart cells.
Main Methods:
- Microautoradiography was used on mouse heart sections.
- Mice were injected with radiolabeled 3H-fendiline.
- Heart tissue was prepared using various sectioning and fixation techniques.
- Silver grains were counted to quantify fendiline localization.
Main Results:
- Fendiline was detected within myocardial cells.
- Significant silver grain counts were observed above cellular and nuclear compartments.
- Fendiline demonstrated the ability to cross the cell membrane into cardiomyocytes.
Conclusions:
- Fendiline is capable of intracellular localization within the heart.
- These findings support the cellular uptake mechanism of fendiline in the myocardium.