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PMID: 7838664 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't

Non-specific effects of calcium entry antagonists in mast cells.

Pflugers Archiv : European journal of physiology ·Vol. 428 ·No. 5-6 ·1994-10-00 ·Pages 433-8

Franzius D, Hoth M, Penner R

Abstract

Calcium entry in non-excitable cells occurs through calcium-selective currents activated secondarily to store depletion and/or through non-selective cation channels (e.g., receptor- or second-messenger-activated channels). The driving force for calcium influx can be modified by chloride or potassium channels, which set the membrane potential of cells. Together, these conductances determine the extent of calcium entry. Mast cells are an excellent model system for studying calcium influx, because calcium-release-activated calcium currents (ICRAC), second-messenger-activated non-selective currents and chloride currents are present in these cells. Whole-cell patch-clamp recordings were used to test the effects of the commonly used calcium entry blockers econazole and SK&F 96365, as well as the antiallergic and anti-inflammatory drugs tenidap, ketotifen and cromolyn on these channels. All tested drugs blocked the three different channel types with a similar order of magnitude (IC50 values ranging from micromolar to millimolar). Hence, these drugs cannot be used to discriminate between different calcium entry mechanisms.

MeSH Terms
Animals Calcium/metabolism Calcium Channel Blockers/pharmacology Calcium Channels/drug effects,pharmacology Cromolyn Sodium/pharmacology Econazole/pharmacology Imidazoles/pharmacology Indoles/pharmacology Ketotifen/pharmacology Mast Cells/metabolism Oxindoles Rats
Chemicals
Calcium Channel Blockers Calcium Channels Imidazoles Indoles Oxindoles Econazole tenidap 1-(2-(3-(4-methoxyphenyl)propoxy)-4-methoxyphenylethyl)-1H-imidazole Cromolyn Sodium Calcium Ketotifen
Authors & Affiliations
3 authors, click to expand affiliations / ORCID
Franzius D
Department of Membrane Biophysics, Max-Planck-Institute for Biophysical Chemistry, Göttingen, Germany.
Hoth M
Penner R
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Article Info
Journal
Pflugers Archiv : European journal of physiology
Abbr.
Pflugers Arch
ISSN
0031-6768
DOI
10.1007/BF00374562
Published
1994-10-00
Pages
433-8
Language
English
Region
Germany
NLM ID
0154720
Subset
IM
External Links
PubMed source DOI: 10.1007/BF00374562 View journal details
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