Abstract |
Cilostazol(6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)-butoxy]-3,4- dihydro-2(1H)- quinolinone) selectively inhibits cGMP-inhibited phosphodiesterase (PDE3) and is a potent inhibitor of platelet aggregation induced by various agonists. Effect of cilostazol on shear stress-induced human platelet aggregation (SIPA) was examined in vitro and ex vivo. Cilostazol inhibited SIPA dose-dependently in vitro. The IC50 value of cilostazol for inhibition of SIPA was 15 +/- 2.6 microM (m +/- SE, n=5), which was very similar to that (12.5 +/- 2.1 microM) for inhibition of ADP-induced platelet aggregation. Cilostazol potentiates the inhibition of SIPA by PGE1 and enhances its ability to increase cAMP concentrations. A single oral adminstration of 100 mg cilostazol to healthy volunteers produced a significant inhibition of SIPA. This study demonstrates that cilostazol is an effective inhibitor of SIPA, which may be important for the prevention and the treatment of arterial occlusive diseases.
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Authors | N Minami, Y Suzuki, M Yamamoto, H Kihira, E Imai, H Wada, Y Kimura, Y Ikeda, H Shiku, M Nishikawa |
Journal | Life sciences
(Life Sci)
Vol. 61
Issue 25
Pg. PL 383-9
( 1997)
ISSN: 0024-3205 [Print] Netherlands |
PMID | 9416770
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Enzyme Inhibitors
- Platelet Aggregation Inhibitors
- Tetrazoles
- Cyclic AMP
- 3',5'-Cyclic-AMP Phosphodiesterases
- Cyclic Nucleotide Phosphodiesterases, Type 3
- Cilostazol
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Topics |
- 3',5'-Cyclic-AMP Phosphodiesterases
(antagonists & inhibitors)
- Administration, Oral
- Adult
- Blood Platelets
(drug effects, metabolism)
- Cilostazol
- Cyclic AMP
(metabolism)
- Cyclic Nucleotide Phosphodiesterases, Type 3
- Enzyme Inhibitors
(blood, pharmacokinetics, pharmacology)
- Humans
- Male
- Platelet Aggregation Inhibitors
(blood, pharmacokinetics, pharmacology)
- Stress, Mechanical
- Tetrazoles
(blood, pharmacokinetics, pharmacology)
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