Development and Testing of an In Vitro Assay for Screening of Potential Therapeutic Agents Active against Na Channel Neurotoxins
Abstract
Based upon experimental observations of extensive conformational allosterism associated with ligand binding at the voltage-sensitive sodium channel, a rapid screening procedure has been developed to probe the interaction of new ligands/agents with a spectrum of binding domains on this vital mediator of electrical signalling in nerve and muscle. Under screening assay conditions, allosteric up-or down-modulation of specific batrachotoxinin-A benzoate binding is exploited as a sensitive indicator of the interaction of test substances with any of at least five different sodium channel domains. Interaction with the sodium channel protecin or with sodium channel neurotoxins is a mechanistic prerequisite for any compound if it is to provide effective pharmacologic antagonism of sodium channel poisoning.
Document Details
- Document Type
- Technical Report
- Publication Date
- Apr 12, 1991
- Accession Number
- ADA237159
Entities
People
- George B. Brown
Organizations
- University of Alabama at Birmingham