Ligand occupation and the functional states of the nicotinic-cholinergic receptor

Palmer Taylor, Steven M. Sine

Research output: Contribution to journalArticlepeer-review

3 Scopus citations

Abstract

Simultaneous measurements of receptor occupation and the change in ion permeability elicited by the ligands enable one to define the linkage between agonist association and activation of the ion channel. The nicotinic receptor behaves effectively as a co-operative dimer. Two agonist molecules are required for activation while a single bound antagonist is sufficient to block the response of the receptor oligomer. The two agonist binding sites on the oligomer do not show precise functional equivalence as might be anticipated from the arrangement of subunits of this protein in the membrane.

Original languageEnglish (US)
Pages (from-to)197-200
Number of pages4
JournalTrends in Pharmacological Sciences
Volume3
Issue numberC
DOIs
StatePublished - 1982

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology

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