<Original Article> Effects of Sildenafil (Viagra TM) on the Cyclic AMP Hydrolyzing Phosphodiesterase Activity in the Canine Heart Assessed Using a Modified Enzymatic Fluorometric Assay Technique
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- SUGIYAMA Atsushi
- Departments of Pharmacology, Yamanashi Medical University
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- SAEGUSA Yoshiki
- Departments of Pharmacology, Yamanashi Medical University
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- TAKAHARA Akira
- Departments of Pharmacology, Yamanashi Medical University
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- SUGITA Masao
- Departments of Neurosurgery, Yamanashi Medical University
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- HASHIMOTO Keitaro
- Departments of Pharmacology, Yamanashi Medical University
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説明
Sildenafil is a phosphodiesterase type-5(PDE5) inhibitor, but has stimulatory effects on heart in vivo and in vitro. We evaluated the effects of sildenafil on the cyclic AMP hydrolyzing PDE activity in a crude enzyme preparation made from the intact canine heart using the modified enzymatic fluorometric assay technique. The basal PDE activity was 485±47pmol/min/mg protein (n=6).Sildenafil as well as a non-specific PDE inhibitor, 3-isobutyl-1-methylxanthine (IBMX) inhibited the PDE activity in a concentration-related manner. Significant inhibition at 1-10μmol/L of sildenafil was almost equivalent to that of the same concentration of IBMX. These results suggest that supra-therapeutic concentration of sildenafil may directly inhibit cyclic AMP hydrolyzing PDEs in the intact heart.
収録刊行物
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- 山梨医科大学雑誌
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山梨医科大学雑誌 17 (3), 69-74, 2002
山梨医科大学医学会
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詳細情報 詳細情報について
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- CRID
- 1390853649746905344
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- NII論文ID
- 110004746865
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- NII書誌ID
- AN10044054
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- ISSN
- 09120025
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- IRDB
- CiNii Articles