Phosphodiesterase inhibitor

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A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase (PDE), therefore preventing the inactivation of the intracellular second messengers cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) by the respective PDE subtype(s).

Contents

History

The different forms or subtypes of phosphodiesterase were initially isolated from rat brains by Uzunov and Weiss in 1972[1] and were soon afterwards shown to be selectively inhibited in the brain and in other tissues by a variety of drugs.[2][3] The potential for selective phosphodiesterase inhibitors as therapeutic agents was predicted as early as 1977 by Weiss and Hait.[4] This prediction meanwhile has proved to be true in a variety of fields.

Classification

Nonselective phosphodiesterase inhibitors

Methylated xanthines and derivatives:[5]

Methylated xanthines act as both

But different analogues show varying potency at the numerous subtypes, and a wide range of synthetic xanthine derivatives (some nonmethylated) have been developed in the search for compounds with greater selectivity for phosphodiesterase enzyme or adenosine receptor subtypes.[10][11][12][13][14][15][16][17][18][19][20][21][22]

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