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  • Title: Dihydropyridine Ca2+ entry blockers selectively inhibit peak I cAMP phosphodiesterase.
    Author: Norman JA, Ansell J, Phillips MA.
    Journal: Eur J Pharmacol; 1983 Sep 16; 93(1-2):107-12. PubMed ID: 6313398.
    Abstract:
    The vasodilatory action of Ca2+ entry blockers is due primarily to slow Ca2+ channel inhibition; however, these drugs may have additional sites of action that contribute to vasodilation. Eleven Ca2+ entry blockers were evaluated for their inhibition of the two major forms of bovine heart cAMP phosphodiesterase which were separated by DEAE cellulose chromatography. Nifedipine and four other dihydropyridine Ca2+ entry blockers selectively inhibited peak I phosphodiesterase activity with IC50 values between 2 and 3 microM but were weak inhibitors of peak II phosphodiesterase with IC50 values of 100 microM or greater. The selective inhibition of peak I phosphodiesterase activity by these dihydropyridine Ca2+ entry blockers may be an intracellular mechanism for producing vasodilation in addition to slow Ca2+ channel inhibition.
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