Abstract
Stable cell lines are potentially excellent tools for large-scale screening of new compounds. Two carboxyterminal-deleted constructs of the two splice variants a and b of the calcium channel class C αl subunit were expressed stably in HEK 293 cells. Each cell line produced regular L-type calcium currents. The opening and closing of the calcium channel elicited by potassium depolarization was followed by Fura-2 transients. These transients were blocked by the calcium channel blocker mibefradil with a concentration for 50% inhibition of 1.7 μM. The cell lines expressing the truncated cardiac α1C−a or smooth muscle α1C−b calcium channel were both blocked by nisoldipine under patch clamp conditions. Nisoldipme interacted with higher affinity with the α1C−b channel than with the α1C−a channel. These results indicate that the two cell lines retain the differential dihydropyridine sensitivity of smooth muscle and cardiac calcium channels and may be potential tools for the screening of L-type calcium channel blockers.
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Seisenberger, C., Welling, A., Schuster, A. et al. Two stable cell lines for screening of calcium channel blockers. Naunyn-Schmiedeberg's Arch Pharmacol 352, 662–669 (1995). https://doi.org/10.1007/BF00171326
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DOI: https://doi.org/10.1007/BF00171326