Spatial Relationships between Drug Binding Sites on the Surface of the Acetylcholine Receptor

Abstract

This report is divided into three sections dealing with the development of fluorescent probes of the nicotinic acetylcholine receptor (AChR) . Section I summarizes our characterization of the interaction of ethidium with the noncompetitive inhibitory (NCI) site identified by phencycliding (PCP) binding. Due to an incomplete understanding of the interrelation ship between the agonist/antagonist and NCI sites on the AChR, ethidium was originally thought only to interact with the agonist/antagonist sites. However, we show that ethidium, indeed, binds selectively to the NCI site when the AChR is in the desensitized state. Section II deals with our efforts to convert the a-toxin- bound AChR to the desensitized state with butanol. Our hope was that, if the a- toxin bound could be converted to the desensitized state, ethidium could be utilized in conjunction with specifically labelled a-toxins to measure the distances between agonist/antagonist and NCI site. (JES)

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Document Details

Document Type
Technical Report
Publication Date
Oct 15, 1986
Accession Number
ADA222751

Entities

People

  • David A. Johnson

Organizations

  • University of California, Riverside

Tags

Communities of Interest

  • Biomedical
  • Weapons Technologies

DTIC Thesaurus Topics

  • California
  • Chromatography
  • Classification
  • Drug Abuse
  • Emission Spectra
  • Energy Transfer
  • High Pressure
  • Laser Dyes
  • Liquid Chromatography
  • Local Anesthetics
  • Measurement
  • Protein Sequence Analysis
  • Quantum Yields
  • Scattering
  • Security
  • Spectra
  • Spectroscopy

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