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Inhibition of beef heart and rat brain nucleoside-3′:5′-monophosphate phosphodiesterase by 3β-14-dihydroxy-21-oxo-23-desoxo-5-β-card-20(22)-enolide 3-acetate (AY-17,605) and structurally related compounds

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Résumé

Des composés isomères aux glycosides cardiaques naturels ont démontré l'inhibition in vitro de l'enzyme nucleoside-3′:5′-monophosphate phosphodiesterase (PDE) d'origine cœur du bœuf exercée sur le cyclic-AMP, le composé le plus actif étant un dérivé de la lactone isomérique contenant une fraction 3-acetyl (AY-17,605); leK i du composé AY-17,605 était de 0.64×10−4 M et le procédé inhibiteur était d'une nature non-compétitive. Aucun des composés n'a exhibé une activité supérieure autre qu'une inhibition modérée du PDE dans le cerveau du rat.

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Acknowledgment. The author wishes to acknowledge the technical assistance of MissG. Carew-Gibson.

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Lippmann, W. Inhibition of beef heart and rat brain nucleoside-3′:5′-monophosphate phosphodiesterase by 3β-14-dihydroxy-21-oxo-23-desoxo-5-β-card-20(22)-enolide 3-acetate (AY-17,605) and structurally related compounds. Experientia 30, 237–239 (1974). https://doi.org/10.1007/BF01934800

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