The inhibitory profile of Ibudilast against the human phosphodiesterase enzyme family.
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.
Gibson
Lucien C D
LC
Kyorin Scotland Research Laboratories, Scottish Biomedical, Todd Campus, West of Scotland Science Park, Glasgow, Scotland, G20 0XA, UK.
Hastings
Stuart F
SF
McPhee
Ian
I
Clayton
Robert A
RA
Darroch
Claire E
CE
Mackenzie
Alison
A
Mackenzie
Fiona L
FL
Nagasawa
Michiaki
M
Stevens
Patricia A
PA
Mackenzie
Simon J
SJ