Inhibition of heart and brain cyclic adenosine 3',5'-monophosphate phosphodiesterase by new non-steroidic compounds structurally related to natural cardenolides

Nemoz, G.; Prigent, A.F.; Pacheco, H.

Biochemical Pharmacology 27(24): 2769-2774

1978


ISSN/ISBN: 0006-2952
PMID: 216370
DOI: 10.1016/0006-2952(78)90188-0
Accession: 068524377

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Abstract
AP 10 and papaverine. Its affinity for the heart enzyme was 8-10 times higher than for the brain enzyme. The inhibition produced by AP 10 was competitive, reversible and was not reversed by high concentrations of Mg ions. AP 10 slightly affected the binding of cAMP with specific binding protein, but it had a far lower affinity for the binding sites than cAMP. The possibility that inhibition of the low Km phosphodiesterase by AP 10 and related compounds may contribute to their cardiotonic action is discussed.