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

Abstract

A rapid screening assay based upon the ability of (3H)BTX-B binding to rat brain synaptoneurosomes to report sensitively on ligand-receptor interactions at any of at least five distinct sodium channel binding domains in a single assay has been refined and reduced to practice. Data are presented to demonstrate the expected response from a series of sodium channel-active agents, including tetrodotoxin (TTX), saxitoxin, alpha-scorpion toxin, local anesthetics, and pyrethroid insecticides. Further radioligand binding assays and electrophysiological testing of HM-197, a simple hexahydropyrimidine analog of TTX, shows that its relatively potent effect to inhibit the binding of (3H)BTX-B is not mediated through an interaction at sodium channel binding sites for TTX, local anesthetics or batrachotoxin.

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Document Details

Document Type
Technical Report
Publication Date
Feb 08, 1988
Accession Number
ADA193097

Entities

People

  • George B. Brown

Organizations

  • University of Alabama at Birmingham

Tags

DTIC Thesaurus Topics

  • Amino Acids
  • Benzimidazoles
  • Brain
  • Cells
  • Chemistry
  • Flow Rate
  • Heterocyclic Compounds
  • Insecticides
  • Liquid Chromatography
  • Local Anesthetics
  • Materials
  • Mixtures
  • New York
  • Peripheral Nervous System
  • Pharmacology
  • Phrenic Nerves
  • Scorpions

Fields of Study

  • Biology
  • Chemistry

Readers

  • Environmental Engineering.
  • Molecular and Cellular Biochemistry