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Related Experiment Videos

Voltage-dependent decrease in the availability of single calcium channels by nitrendipine in guinea-pig ventricular

Y Kawashima1, R Ochi

  • 1Department of Physiology, School of Medicine, Juntendo University, Tokyo, Japan.

The Journal of Physiology
|August 1, 1988
PubMed
Summary

Nitrendipine blocks calcium channels by prolonging unavailable states. This drug binding mechanism affects channel availability and alters state transition rates in guinea-pig ventricular cells.

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Area of Science:

  • Cardiovascular Pharmacology
  • Ion Channel Physiology

Background:

  • Calcium (Ca2+) channels are crucial for cardiac function.
  • Nitrendipine is a known calcium channel blocker.

Purpose of the Study:

  • To elucidate the mechanism of calcium channel block by nitrendipine.
  • To investigate the effects of nitrendipine on channel gating kinetics.

Main Methods:

  • Single-channel patch-clamp recordings from guinea-pig ventricular cells.
  • Utilized barium (Ba2+) as the charge carrier.
  • Applied voltage-clamp protocols with depolarization pulses.

Main Results:

  • Nitrendipine shifted the availability-voltage relationship hyperpolarizing.
  • The drug shortened the mean duration of the available channel state.

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  • Nitrendipine prolonged the slow component of the unavailable state duration.

    • Conclusions:

    • The mechanism of nitrendipine-induced calcium channel block involves prolonged unavailable states.
    • Drug binding during depolarization and maintained during holding potentials underlies the blockade.
    • Rate constants for state transitions were quantified.