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Quinacrine and Ethidium Bromide Bind the Same Locus on the Nicotinic Acetylcholine Receptor from Torpedo californica

Lurtz, Monica M. and Hareland, Michele L. and Pedersen, Steen E. (1997) Quinacrine and Ethidium Bromide Bind the Same Locus on the Nicotinic Acetylcholine Receptor from Torpedo californica. Biochemistry, 36 (8). pp. 2068-2075. ISSN 0006-2960. https://resolver.caltech.edu/CaltechAUTHORS:20180213-071127392

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Abstract

Quinacrine is a noncompetitive antagonist of the nicotinic acetylcholine receptor (AChR) which displays severalfold fluorescent enhancement upon binding to AChR-rich membranes from Torpedo californica electric organ. It is demonstrated that the fluorescence enhancement comprises two components:  specific interaction at a high-affinity binding site on the AChR, and interaction with the lipid bilayer. The interaction with the lipid bilayer can be attenuated by other noncompetitive antagonists, but at concentrations substantially higher than those required for binding to the AChR. It is further shown that quinacrine can inhibit the binding of [3H]phencyclidine and [3H]ethidium in a manner fully consistent with simple competitive inhibition. The data support a model for high-affinity quinacrine binding to the same, single locus of the acetylcholine receptor as phencyclidine and ethidium. This site is likely within the lumen of the ion channel.


Item Type:Article
Related URLs:
URLURL TypeDescription
http://dx.doi.org/10.1021/bi962547pDOIArticle
https://pubs.acs.org/doi/full/10.1021/bi962547pPublisherArticle
Additional Information:© 1997 American Chemical Society. Received 10 October 1996. Published online 25 February 1997. This work was supported by U.S. Public Health Service Grants NS28879 and NS35212. S.E.P. was supported by Research Career Development Award NS01618, M.M.L. was supported by Public Health Training Grant HL07676, and M.L.H. was supported by NSF Grant BIR-9322251. Arlene Samano is thanked for superb technical assistance in binding experiments.
Funders:
Funding AgencyGrant Number
NIHNS28879
NIHNS35212
NIHNS01618
NIH Predoctoral FellowshipHL07676
NSFBIR-9322251
Issue or Number:8
Record Number:CaltechAUTHORS:20180213-071127392
Persistent URL:https://resolver.caltech.edu/CaltechAUTHORS:20180213-071127392
Official Citation:Quinacrine and Ethidium Bromide Bind the Same Locus on the Nicotinic Acetylcholine Receptor from Torpedo californica Monica M. Lurtz, Michele L. Hareland, and Steen E. Pedersen Biochemistry 1997 36 (8), 2068-2075 DOI: 10.1021/bi962547p
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:84799
Collection:CaltechAUTHORS
Deposited By: Ruth Sustaita
Deposited On:13 Feb 2018 21:03
Last Modified:03 Oct 2019 19:22

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