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• W2080329119 startingPage "847" @default.
• W2080329119 abstract "The pharmacological actions of methylxanthines such as theophylline and caffeine may be due to blockade of adenosine receptors and/or inhibition of phosphodiesterase (PDE) activities. In the last years, potent xanthines have been developed that display some selectivity for A1 and A2 adenosine receptors. Little is known about the PDE inhibitory potency of these xanthines. The aim of the present study was to determine the potencies of A1 and A2 receptor selective xanthines as inhibitors of several PDE isozymes, the PDE I-V subtypes. The ic50 values of 8-phenyl- and 8-cycloalkyl-1, 3-dialkylxanthines for inhibiton of PDE isozymes from different sources are up to 10,000-fold higher than their antagonistic potencies at adenosine receptors. However, the A1 receptor selective antagonists 1, 3-diethyl-8-phenyl-xanthine and 1,3-dipropyl-8-cyclopentylxanthine are comparatively potent inhibitors of PDE IV activity with ic50 values in the 10 μM range and are, therefore, nearly as potent as the PDE IV selective inhibitor, rolipram. The A2 receptor selective 1,3-dipropyl-7-methylxanthine is about 10–300-fold more potent as an adenosine receptor antagonist than as a PDE inhibitor. The results indicate that some of these novel xanthines can be used as selective adenosine receptor antagonists without interference due to inhibitory effects on PDEs." @default.
• W2080329119 created "2016-06-24" @default.
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• W2080329119 date "1993-02-01" @default.
• W2080329119 modified "2023-10-04" @default.
• W2080329119 title "Adenosine receptor-blocking xanthines as inhibitors of phosphodiesterase isozymes" @default.
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• W2080329119 doi "https://doi.org/10.1016/0006-2952(93)90168-v" @default.
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