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Eur J Pharmacol ; 538(1-3): 39-42, 2006 May 24.
Artigo em Inglês | MEDLINE | ID: mdl-16674936

RESUMO

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.


Assuntos
Inibidores de Fosfodiesterase/farmacologia , Diester Fosfórico Hidrolases/metabolismo , Piridinas/farmacologia , Animais , Linhagem Celular , AMP Cíclico/metabolismo , GMP Cíclico/metabolismo , Humanos , Hidrólise/efeitos dos fármacos , Isoenzimas/genética , Isoenzimas/metabolismo , Cinética , Diester Fosfórico Hidrolases/genética , Spodoptera , Especificidade por Substrato
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