Ca 2+ channel sensitivity towards the blocker isradipine is affected by alternative splicing of the human α 1C subunit gene
Abstract
L-type Ca 2+ channels are important targets for drugs, such as dihydropyridines (DHPs), in the treatment of cardiovascular diseases. Channel expression is regulated by alternative splicing. It has been suggested that in the cardiovascular system tissue-specific expression of different L-type Ca 2+ channel splice variants may underlie the observed differences in sensitivities to channel block by DHPs. We investigated the sensitivity of Ca 2+ channel splice variants derived from the human α 1C gene to the DHP isradipine. Among seven α 1C channels we observed up to 10-fold differences in IC 50 values for isradipine, as well as changes in the voltage dependence of DHP action.
- Publication:
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FEBS Letters
- Pub Date:
- January 1998
- DOI:
- Bibcode:
- 1998FEBSL.427..220Z
- Keywords:
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- Ca 2+ channel;
- Splice variant;
- Channel blocker;
- Dihydropyridine;
- Xenopus oocyte