Accession Number:

ADA237159

Title:

Development and Testing of an In Vitro Assay for Screening of Potential Therapeutic Agents Active against Na Channel Neurotoxins

Descriptive Note:

Final rept. 1 Jan 86-30 Jun 89,

Corporate Author:

ALABAMA UNIV IN BIRMINGHAM SCHOOL OF MEDICINE

Personal Author(s):

Report Date:

1991-04-12

Pagination or Media Count:

61.0

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 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.

Subject Categories:

  • Medicine and Medical Research

Distribution Statement:

APPROVED FOR PUBLIC RELEASE