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Description
Ibudilast is a leukomene antagonist and phosphodiesterase inhibitor useful in the
treatment of bronchial asthma. It antagonizes leukotriene D4-induced contractions of
guinea pig ileum and tracheal muscles in virro, and inhibits eosinophil accumulation in
vivo.
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Chemical Properties
White Solid
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Originator
Kyorin (Japan)
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Uses
Inhibitors of phosphodiesterase 4 (PDE4), which catalyzes the hydrolysis of cAMP, have potential applications in a variety of diseases, including asthma. Ibudilast is an inhibitor of PDE4 (IC50 = 54-239 nM) that, at higher doses, also inhibits PDE3 and PDE5 (IC50 = 1,600-3,510 nM). Through this action, it suppresses the elaboration of mediators involved in asthma and inflammation.[Cayman Chemical]
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Uses
a phosphodiesterase inhibitor with anti-inflammatory activity
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Uses
A leukotriene D4 antagonist. Used as an antiallergic, antiasthmatic, and vasodilator (cerebral)
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brand name
Ketas
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Biological Activity
Phosphodiesterase inhibitor (IC 50 values are 53, 35, 48, 12 and 10 mM for PDE Ia, II, III, IV and V respectively). Inhibits platelet aggregation and is an orally-active cerebral vasodilator, bronchodilator and antiallergic agent.
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Biochem/physiol Actions
Phosphodiesterase IV (PDE4) inhbitor. Inhibits platelet aggregation. Anti-asthma drug.
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References
1) Kishi et al. (2001), Ibudilast: a non-selective PDE inhibitor with multiple actions on blood cells and the vascular wall; Cardiovasc. Drug Rev., 19 215
2) Yamazaki et al. (2011), Ibudilast. A mixed PDE3/4 inhibitor, causes a selective and nitric oxide/cGMP-independent relaxation of the intracranial vertebrobasilar artery; Eur. J. Pharmacol., 650 605
3) Cueva Vargas et al. (2016), The glial cell modulator ibudilast attenuates neuroinflammation and enhances retinal ganglion cell viability in glaucoma through protein kinase A signaling.; Neurobiol. Dis., 93 156
4) Mizuno et al. (2004), Neuroprotective role of phosphodiesterase inhibitor ibudilast on neuronal cell death induced by activated microglia; Neuropharmacology, 46 404
5) Ledeboer et al. (2007), Ibudilast (AV-411). A class therapeutic candidate for neuropathic pain and opioid withdrawal syndromes; Expert. Opin. Investig. Drugs, 16 935
