RT Journal Article
SR Electronic
T1 The Use of a Cholinergic Fluorescent Probe for the Study of the Receptor Proteolipid
JF Molecular Pharmacology
JO Mol Pharmacol
FD American Society for Pharmacology and Experimental Therapeutics
SP 530
OP 537
VO 7
IS 5
A1 G. WEBER
A1 D. P. BORRIS
A1 E. DE ROBERTIS
A1 F. J. BARRANTES
A1 J. L. LA TORRE
A1 MARÍA C. LLORENTE DE CARLIN
YR 1971
UL http://molpharm.aspetjournals.org/content/7/5/530.abstract
AB 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. ACKNOWLEDGMENT The authors are indebted to Dr. Telma Caputi for her collaboration in the computation of the data.