Accession Number:

ADA222751

Title:

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

Descriptive Note:

Annual rept. 15 Sep 1985-14 Sep 1986,

Corporate Author:

CALIFORNIA UNIV RIVERSIDE

Personal Author(s):

Report Date:

1986-10-15

Pagination or Media Count:

50.0

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 agonistantagonist and NCI sites on the AChR, ethidium was originally thought only to interact with the agonistantagonist 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 agonistantagonist and NCI site. JES

Subject Categories:

  • Biochemistry

Distribution Statement:

APPROVED FOR PUBLIC RELEASE