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Xanthine derivatives as adenosine receptor antagonists

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Abstract

The potency of a series of xanthine derivatives as adenosine antagonists was studied in fat cells (A1-receptors) and hippocampal slices (A2-receptors) and on L-[3H]phenylisopropyladenosine (PIA) binding in membranes from rat cortex. The order of potency in all three tests systems was:diethyl-8-phenyl-theophylline 8-phenyltheophylline 8-p-sulfophenyltheophylline verrophylline isobutlmethylxanthine theophylline caffeine theobromine. Enprofylline was about 20 times more potent in the hippocampus system than in the other two systems.

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