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Effects of Depogen on Various Isozymes of Cyclic Nucleotide Phosphodiesterase Isolated from Porcine Aorta
http://hdl.handle.net/10191/33208
http://hdl.handle.net/10191/3320893ba0a50-7505-4c76-9c91-9b6ec9e8222a
名前 / ファイル | ライセンス | アクション |
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43(3)_127-134.pdf (833.4 kB)
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Item type | 紀要論文 / Departmental Bulletin Paper(1) | |||||
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公開日 | 2015-08-31 | |||||
タイトル | ||||||
タイトル | Effects of Depogen on Various Isozymes of Cyclic Nucleotide Phosphodiesterase Isolated from Porcine Aorta | |||||
タイトル | ||||||
言語 | en | |||||
タイトル | Effects of Depogen on Various Isozymes of Cyclic Nucleotide Phosphodiesterase Isolated from Porcine Aorta | |||||
言語 | ||||||
言語 | eng | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | depogen | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | PDE | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | vascular smooth muscle | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | cAMP | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | cGMP | |||||
資源タイプ | ||||||
資源 | http://purl.org/coar/resource_type/c_6501 | |||||
タイプ | departmental bulletin paper | |||||
著者 |
Cai, Ji-Qun
× Cai, Ji-Qun× Yoshida, Yutaka× Imai, Shoichi |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | Cyclic nucleotide phosphodiesterase (PDE) isozymes were separated from the soluble fraction of porcine aortic smooth muscle by DEAE-Sepharose Fast Flow ion exchange chromatography, and the effects of depogen (a theophilline-7 -acetice acid salt of drotaverine) on the isozymes were investigated in comparison with those of various selective or nonselective PDE inhibitors. Five PDE isozymes (Types I-V) were identified on the basis of their regulatory and kinetic properties and their sensitivities to selective PDE inhibitors. Type I (calmodulin-stimulated) preferentially hydrolyzed cGMP. The presence of Type II was demonstrated by a marked stimulation of activity by cGMP. Because of an insufficient amount of the isozyme and the unavailability of specific inhibitors, no further study of the Type II PDE was conducted. The Type III (cGMP-inhibited) and Type IV(cAMP-specific) isozymes preferentially hydrolyzed cAMP. The Type V PDE (cGMP-specific) hydrolyzed cGMP with a high selectivity. Depogen inhibited Types I, III and V PDE isozymes with potencies much weaker than selective inhibitors of each PDE isozyme as well as a nonselective PDE inhibitor, 3-isobutyl- 1-methylxanthine. In contrast, the inhibitory action of depogen was most potent toward Type IV PDE (IC_<50> =17μM), being more potent than that of RO20-1724, a Type IV-specific inhibitor (IC_<50>=32μM). Theophilline-7-acetic acid produces only a minimal inhibition while the inhibitory activities of drotaverine were very much like those of depogen. These results suggest that depogen is a selective inhibitor of Type IV PDE isozyme and that the inhibitory activity of depogen is mainly attributable to drotaverine. | |||||
書誌情報 |
Acta medica et biologica en : Acta medica et biologica 巻 43, 号 3, p. 127-134, 発行日 1995-09 |
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出版者 | ||||||
出版者 | Niigata University School of Medicine | |||||
ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 05677734 | |||||
書誌レコードID | ||||||
収録物識別子タイプ | NCID | |||||
収録物識別子 | AA00508361 | |||||
著者版フラグ | ||||||
値 | publisher |