The inhibitory profile of Ibudilast against the human phosphodiesterase enzyme family

被引：116

作者：

Gibson, Lucien C. D.

Hastings, Stuart F.

McPhee, Ian

Clayton, Robert A.

Darroch, Claire E.

Mackenzie, Alison

MacKenzie, Fiona L.

Nagasawa, Michiaki

Stevens, Patricia A.

MacKenzie, Simon J.

机构：

[1] Scottish Biomed, Kyorin Scotland Res Labs, Glasgow G20 0XA, Lanark, Scotland

[2] Kyorin Pharmaceut Co Ltd, Tokyo, Japan

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 2006年 / 538卷 / 1-3期

关键词：

phosphodiesterase; Ibudilast; neurological disease; respiratory disease;

D O I：

10.1016/j.ejphar.2006.02.053

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Ibudilast is widely used in Japan to treat ischemic stroke and bronchial asthma. Its mode of action is through the inhibition of cyclic nucleotide phosphodiesterases (PDEs). Growing evidence suggests this compound has utility in a range of neurological conditions linked to its ability to elevate cellular cyclic nucleotide concentrations, however limited data exists on Ibudilast's action on individual PDE families. We therefore used an extensive panel of human PDE enzymes to define the PDE inhibitory profile of this compound. Ibudilast preferentially inhibits PDE3A, PDE4, PDE10 and PDE11 with lesser inhibition of a number of other families. The significance of these findings is discussed in relation to Ibudilast's observed effects on certain disease states. (c) 2006 Elsevier B.V. All rights reserved.

引用

页码：39 / 42

页数：4

共 32 条

[1] A mouse model of Rubinstein-Taybi syndrome: Defective long-term memory is ameliorated by inhibitors of phosphodiesterase 4 [J].