Theoretical characterization of ion channel blockade. Competitive binding to periodically accessible receptors.

Journal Article (Journal Article)

Competitive ligand binding to periodically activated or accessible receptors is influenced by the interaction between ligand binding kinetics and the interval of time the binding site is accessible. This interaction produces a paradoxical reduction in bound receptors under certain conditions. A mathematical description of multi-ligand binding to a single binding site is presented for both the continuously and transiently accessible cases. The theoretical results predict paradoxical "agonism" and are consistent with the results of studies of lidocaine and bupivacaine binding to cardiac sodium channels.

Full Text

Duke Authors

Cited Authors

  • Starmer, CF

Published Date

  • September 1987

Published In

Volume / Issue

  • 52 / 3

Start / End Page

  • 405 - 412

PubMed ID

  • 2443192

Pubmed Central ID

  • PMC1330005

Electronic International Standard Serial Number (EISSN)

  • 1542-0086

International Standard Serial Number (ISSN)

  • 0006-3495

Digital Object Identifier (DOI)

  • 10.1016/s0006-3495(87)83229-0


  • eng