ArticlePflugers Archiv : European journal of physiology1993
The benzazepine/benzothiazepine binding domain of the cardiac L-type Ca2+ channel is accessible only from the extracellular side.
Article in Pflugers Archiv : European journal of physiology, 1993. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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8 citing papers in PubMed, 22 citations in OpenAlex.
- Phenylalkylamines in calcium channels: computational analysis of experimental structures.Journal of computer-aided molecular design · 2020Article
- Structural model for phenylalkylamine binding to L-type calcium channels.The Journal of biological chemistry · 2009Article
- Roscovitine, a cyclin-dependent kinase inhibitor, affects several gating mechanisms to inhibit cardiac L-type (Ca(V)1.2) calcium channels.British journal of pharmacology · 2007Article
- Molecular pharmacology of high voltage-activated calcium channels.Journal of bioenergetics and biomembranes · 2003Review
- Molecular mechanism of use-dependent calcium channel block by phenylalkylamines: role of inactivation.Proceedings of the National Academy of Sciences of the United States of America · 1997Article
- Action of tertiary phenylalkylamines on cardiac transient outward current from outside the cell membrane.Naunyn-Schmiedeberg's archives of pharmacology · 1996Article
- Extra- and intracellular action of quaternary devapamil on muscle L-type Ca(2+)-channels.British journal of pharmacology · 1996Article
- Extracellular site of action of phenylalkylamines on L-type calcium current in rat ventricular myocytes.Naunyn-Schmiedeberg's archives of pharmacology · 1995Article
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Authors and funding
4 authors at 2 institutions in 3 countries.
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No grant is acknowledged in the PubMed record.
Abstract
The whole-cell tight seal recording technique was used to investigate location of benzothiazepine binding site of the cardiac L-type Ca2+ channel. For this we utilized a permanently charged compound, SQ 32.428, out of a series of benzazepine drugs which have been characterized as competitive inhibitors of diltiazem binding. The non-permanently charged derivative SQ 32.910 was initially tested to electrophysiologically establish Ca2+ antagonistic properties of benzazepines. Upon extracellular application, either compound was able to completely block Ca2+ currents. At a stimulating frequency of 0.2 Hz IC50 concentrations of SQ 32.910 and SQ 32.428 were determined as 35 nM and 15 microM, respectively. Intracellular application of SQ 32.428 was then compared to control experiments in the absence of drug. Initially, adequate drug dialysis was confirmed with 100 microM D890, which produced a progressive inhibition of Ca2+ currents within 10 min after whole-cell access. In contrast, internal application of 100 microM SQ 32.428 did not change time-course of Ca2+ currents compared to control run-down. These results show that the benzazepine/benzothiazepine binding domain of the cardiac L-type Ca2+ channel is accessible only from the extracellular side and therefore suggest an extracellular location on the alpha 1-subunit of the Ca2+ channel protein.
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