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Tenidap: a novel inhibitor of calcium influx in a mast cell line
P L Cleveland1, P J Millard, H J Showell
1Department of Pharmacology, Cornell University, Ithaca, New York.
Abstract:
The anti-inflammatory agent tenidap has previously been shown to inhibit antigen-induced secretion in tumor mast cells. We have investigated the possibility that this effect is due to modulation of the Ca2+ response in mast cells and in particular that tenidap might be an inhibitor of the Ca2+ influx pathway or channel in these and other non-excitable cells. Tenidap inhibited the antigen-induced increase in intracellular Ca2+ measured both in cell suspensions and at the single cell level using digital imaging of Fura-2 fluorescence. Tenidap also inhibited both antigen- and thapsigargin-induced 45Ca influx across the plasma membrane at concentrations similar to those required for the inhibition of secretion. Somewhat unexpectedly, the compound itself caused some release of calcium from intracellular stores; however, this effect did not appear to be related to the inhibition of calcium influx or secretion. In mouse pituitary tumour (AtT-20) cells, tenidap inhibited depolarization-induced increases in intracellular Ca2+ suggesting that this compound also inhibits Ca2+ influx through voltage-sensitive calcium channels. We conclude that tenidap has a number of interesting effects on calcium handling which makes it a potentially valuable tool for the study of calcium movements particularly in non-excitable cells.
Insights
The anti-inflammatory drug tenidap inhibits calcium (Ca2+) influx in mast cells and other non-excitable cells. This action suggests tenidap is a valuable tool for studying calcium signaling pathways.
Area of Science:
- Immunology
- Cell Biology
- Pharmacology
Background:
- Tenidap, an anti-inflammatory agent, is known to inhibit antigen-induced secretion in tumor mast cells.
- The mechanism underlying tenidap's effect on mast cell secretion is not fully understood.
- Investigating tenidap's impact on calcium (Ca2+) response is crucial for understanding its anti-inflammatory properties.
Purpose of the Study:
- To determine if tenidap modulates the Ca2+ response in mast cells.
- To investigate tenidap's potential as an inhibitor of Ca2+ influx pathways or channels.
- To explore tenidap's effects on Ca2+ handling in non-excitable cells.
Main Methods:
- Measurement of intracellular Ca2+ in cell suspensions and single cells using Fura-2 fluorescence.
- Quantification of 45Ca influx across the plasma membrane.
- Assessment of tenidap's effect on depolarization-induced Ca2+ increases in AtT-20 cells.
Main Results:
- Tenidap inhibited antigen-induced increases in intracellular Ca2+ in mast cells.
- Tenidap suppressed both antigen- and thapsigargin-induced 45Ca influx.
- Tenidap inhibited depolarization-induced Ca2+ influx in mouse pituitary tumor cells.
- Tenidap also induced some release of calcium from intracellular stores, independent of influx inhibition.
Conclusions:
- Tenidap inhibits Ca2+ influx in mast cells and other non-excitable cells.
- Tenidap acts on voltage-sensitive calcium channels.
- Tenidap is a valuable pharmacological tool for studying calcium movements in non-excitable cells.
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