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Molecular Pharmacology, Vol 6, 597-603, Copyright © 1970 by the American Society for Pharmacology and Experimental Therapeutics
1 Departments of Medicine and Physiology, Vanderbilt University School of Medicine,
Nashville, Tennessee 37203
The lipolytic potencies of 64 compounds, mostly xanthine derivatives, were determined in epididymal fat cells. Nine of the compounds of widely varying lipolytic potency were examined as inhibitors of cyclic AMP phosphodiesterase activity. Substantial lipolytic effects were seen at concentrations producing less than 20% inhibition of phosphodiesterase activity. The most active compound, 1-methyl-3-isobutylxanthine, was about 15 times more potent than theophylline in both systems. Over a 20-fold range of concentrations, there was close agreement between the lipolytic activities of the compounds and their activities as inhibitors of phosphodiesterase. The close correlation between these two activities strongly indicates that the lipolytic activity of the xanthine derivatives is a result of inhibition of cyclic AMP phosphodiesterase.
Note:
ACKNOWLEDGMENTS
We are indebted to Dr. Donald E. Pearson,
Professor of Chemistry, Vanderbilt University,
for his helpful discussions. We also thank Drs.
I. C. Winter, K. J. Rorig, and others of G. D.
Searle and Company for the synthesis, purification, and gift of many of the test compounds.
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