Nonmodal gating of cardiac calcium channels as revealed by dihydropyridines.

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Nonmodal gating of cardiac calcium channels as revealed by dihydropyridines

The hypothesis that dihydropyridine (DHP)-sensitive calcium channels have three distinct modes of gating has been examined. The major prediction is that the relative frequencies among modes depend on DHP concentration while the kinetics within a mode do not. We tested this by studying whole-cell and single-channel calcium currents in neonatal rat and adult guinea pig cardiac myocytes in differe...

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Isoform-specific inhibition of L-type calcium channels by dihydropyridines is independent of isoform-specific gating properties.

Dihydropyridines (DHPs) block L-type Ca2+ channels more potently at depolarized membrane potentials, consistent with high affinity binding to the inactivated state. Nisoldipine (a DHP antagonist) blocks the smooth muscle channel more potently than the cardiac one, a phenomenon observed not only in native channels but also in expressed channels. We examined whether this tissue specificity was at...

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Coupled gating between cardiac calcium release channels (ryanodine receptors).

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Coupled gating between individual cardiac ryanodine calcium release channels.

In order to study interactions between ryanodine receptor calcium release (RyR2) channels during excitation-contraction coupling in cardiac muscle, we used bilayer lipid membrane (BLM) and improved the method of cardiac sarcoplasmic vesicle fusion into BLM. We increased fusion gradient for the vesicles, used chloride ions for fusion up to concentration of 1.2 mol/l and fused the vesicles by add...

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Block of L-type calcium channels by charged dihydropyridines. Sensitivity to side of application and calcium

We have studied block of L-type calcium channels by intracellular and extracellular application of the ionized dihydropyridine derivatives amlodipine and SDZ 207-180. We find that extracellular application of either drug causes voltage-dependent block of calcium channels. However, neither drug is effective when applied intracellularly. The insensitivity of calcium channels to intracellular drug...

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ژورنال

عنوان ژورنال: Journal of General Physiology

سال: 1989

ISSN: 0022-1295,1540-7748

DOI: 10.1085/jgp.93.6.1243