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Models of drug interaction with the sodium channel.

Publication ,  Journal Article
Grant, AO
Published in: Clin Invest Med
October 1991

The local anesthetic-class of anti-arrhythmic drugs block the inward sodium current in nerve and cardiac muscle. A number of models for the interaction of these drugs with the neuronal sodium channel have been extended to cardiac muscle. The models assume a single binding site for the entire class of agents. The kinetics of drug interaction with this site depend on the Na channel conformation, open and inactivated channels having greater affinity than resting channels. An alternative formulation considers drug-receptor affinity as fixed, but access to the binding site is controlled by channel gating. Several clinically relevant predictions, such as competitive displacement of multiple agents, can be made from these models.

Duke Scholars

Published In

Clin Invest Med

ISSN

0147-958X

Publication Date

October 1991

Volume

14

Issue

5

Start / End Page

447 / 457

Location

Canada

Related Subject Headings

  • Sodium Channels
  • Receptors, Cell Surface
  • Models, Biological
  • Humans
  • Heart
  • General Clinical Medicine
  • Anti-Arrhythmia Agents
  • Animals
  • 32 Biomedical and clinical sciences
  • 11 Medical and Health Sciences
 

Citation

APA
Chicago
ICMJE
MLA
NLM
Grant, A. O. (1991). Models of drug interaction with the sodium channel. Clin Invest Med, 14(5), 447–457.
Grant, A. O. “Models of drug interaction with the sodium channel.Clin Invest Med 14, no. 5 (October 1991): 447–57.
Grant AO. Models of drug interaction with the sodium channel. Clin Invest Med. 1991 Oct;14(5):447–57.
Grant, A. O. “Models of drug interaction with the sodium channel.Clin Invest Med, vol. 14, no. 5, Oct. 1991, pp. 447–57.
Grant AO. Models of drug interaction with the sodium channel. Clin Invest Med. 1991 Oct;14(5):447–457.

Published In

Clin Invest Med

ISSN

0147-958X

Publication Date

October 1991

Volume

14

Issue

5

Start / End Page

447 / 457

Location

Canada

Related Subject Headings

  • Sodium Channels
  • Receptors, Cell Surface
  • Models, Biological
  • Humans
  • Heart
  • General Clinical Medicine
  • Anti-Arrhythmia Agents
  • Animals
  • 32 Biomedical and clinical sciences
  • 11 Medical and Health Sciences