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Inhibition of Benzodiazepine Receptor Binding by Urinary Extracts: Effect of Ethanol
Author(s) -
Volicer L,
Ullman M. D.
Publication year - 1985
Publication title -
alcoholism: clinical and experimental research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.267
H-Index - 153
eISSN - 1530-0277
pISSN - 0145-6008
DOI - 10.1111/j.1530-0277.1985.tb05572.x
Subject(s) - chemistry , benzodiazepine , excretion , ethanol , thin layer chromatography , urine , receptor , chloroform , silicic acid , chromatography , medicine , endocrinology , pharmacology , biochemistry , biology , organic chemistry
Two fractions which inhibit benzodiazepine receptor binding were isolated from both rat and human urine. The method used involved alkaline methanorysis followed by chloroform extraction and silicic acid chromatography. This method precludes artrfactual formation of esters of β‐carboline carboxylic acid (BCC) during the extraction procedure. One of the fractions (fraction E) behaved similarly to methyl ester of BCC on thin‐layer chromatography and also had a similar fluorescent spectra. Administration of ethanol to male Sprague‐Dawley rats decreased the concentration and the total excretion of both inhibitory fractions in a dose‐dependent manner. In a clinical study on males with different family histories of alcoholism, ethanol decreased excretion of fraction E. The excretion was not affected by placebo, and it was similar in family history‐positive and family history‐negative subjects. These results suggest that ethanol affects the ‐γ‐aminobutyric acid‐benzodiazepine receptor complex by changing release, metabolism, and/or excretion of an endogenous benzodiazepine ligand.