Molecular Mechanisms of Cardiostimulatory Effects of Sildenafil

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Author(s)

Abstract

To better understand the molecular mechanisms of the previously described cardiostimulatory action of the phosphodiesterase type-5 (PDE5) inhibitor sildenafil, we first evaluated its effects on cyclic AMP level in the canine ventricular membrane preparation. Sildenafil (10 μmol/L) significantly increased the net cyclic AMP production rate, the potency of which was similar to that of 3-isobutyl-1-methylxanthine (IBMX). Next, we assessed the inhibitory effect of sildenafil on PDE of bovine heart. Sildenafil (≥1 μmol/L) as well as IBMX significantly decreased the cyclic AMP hydrolyzing speed of PDE. These results suggest that a supra-therapeutic concentration of sildenafil may directly inhibit cyclic AMP hydrolyzing PDEs in the heart, although indirect inhibition of PDE3 via the “cross-talk” pathway cannot be totally excluded.

Journal

  • The Japanese Journal of Pharmacology

    The Japanese Journal of Pharmacology 88(3), 362-364, 2002-03-01

    The Japanese Pharmacological Society

References:  10

Codes

  • NII Article ID (NAID)
    10008188130
  • NII NACSIS-CAT ID (NCID)
    AA00691188
  • Text Lang
    ENG
  • Article Type
    SHO
  • ISSN
    00215198
  • NDL Article ID
    6119718
  • NDL Source Classification
    ZS51(科学技術--薬学)
  • NDL Call No.
    Z53-D199
  • Data Source
    CJP  NDL  J-STAGE 
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