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Molecular Pharmacology, Vol 7, 530-537, Copyright © 1971 by the American Society for Pharmacology and Experimental Therapeutics

The Use of a Cholinergic Fluorescent Probe for the Study of the Receptor Proteolipid

G. WEBER 1, D. P. BORRIS 1, E. DE ROBERTIS 2, F. J. BARRANTES 2, J. L. LA TORRE 2, and MARÍA C. LLORENTE DE CARLIN 2

1 Department of Chemistry, University of Illinois, Urbana, Illinois 61801
2 Instituto de Anatomía General y Embriología, Facultad de Medicina, Universidad de Buenos Aires, Argentina

A trimethylammonium derivative, 1-dimethylaminonaphthalene-5-sulfonamidoethyl-trimethylammonium perchlorate, was synthesized and used as a fluorescent probe for the study of the receptor proteolipid extracted from the electric organ of Electrophorus electricus.

A special technique based on the preferred partition coefficient of the proteolipid for organic solvents and of the trimethylammonium derivative for water was developed. Such a method permits time accurate and rapid titration of the proteolipid with the cholinergic fluorescent probe and also the study of the action of other drugs competing for the binding sites.

A cooperative type of interaction between the fluorescent trimethylammonium derivative and the receptor proteolipid was observed, and the competition of acetylcholine, dimethyl-d-tubocurarine, and decamethonium for the binding sites of the fluorescent probe was demonstrated.

Note:
ACKNOWLEDGMENT The authors are indebted to Dr. Telma Caputi for her collaboration in the computation of the data.

Submitted on February 3, 1971




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