Development and Testing of an In Vitro Assay for Screening of Potential Therapeutic Agents Active against Na Channel Neurotoxins
Final rept. 1 Jan 86-30 Jun 89,
ALABAMA UNIV IN BIRMINGHAM SCHOOL OF MEDICINE
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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 ligandsagents 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.
- Medicine and Medical Research