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2-或/和8-取代腺苷衍生物对腺苷脱氨酶和钙调蛋白依赖性磷酸二酯酶的抑制作用。

Inhibition by 2- or/and 8-substituted adenosine derivatives of adenosine deaminase and calmodulin-dependent phosphodiesterase.

作者信息

Sasaki Y, Ono Y

出版信息

Nucleic Acids Symp Ser. 1980(8):s163-6.

PMID:6265879
Abstract

Several 2- or/and 8-substituted adenosine derivatives were tested for their ability to inhibit the adenosine deaminase activity in hog heart and Ca++, calmodulin-dependent phosphodiesterase activity in hog brain. Among these derivatives, 2-piperidyladenosine competitively inhibited not only the adenosine deaminase activity but also the phosphodiesterase activity. Further substitution of this compound with a bulky group at 8-position, 2-piperidyl-8-(8-aminooctylamino)-adenosine, abolished its ability to inhibit the adenosine deaminase activity, but progressively increased in the ability to inhibit the phosphodiasterase activity. On the other hand, 8-monosubstituted adenosine derivatives did not inhibit the adenosine deaminase activity.

摘要

测试了几种2-或/和8-取代的腺苷衍生物抑制猪心脏腺苷脱氨酶活性以及猪脑钙调蛋白依赖性磷酸二酯酶活性的能力。在这些衍生物中,2-哌啶基腺苷不仅竞争性抑制腺苷脱氨酶活性,还抑制磷酸二酯酶活性。该化合物在8位进一步被一个庞大基团取代,即2-哌啶基-8-(8-氨基辛基氨基)-腺苷,消除了其抑制腺苷脱氨酶活性的能力,但抑制磷酸二酯酶活性的能力却逐渐增强。另一方面,8-单取代的腺苷衍生物不抑制腺苷脱氨酶活性。

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