Ibudilast
Neuroinflammation inhibitor (PDE pan-inhibitor) / Phosphodiesterase inhibitor with some selectivity for PDE4 and 5. (IC50s= 53, 35, 48,12 and10 μM for PDE 1a, 2, 3, 4 and 5 respectively1). Acts as a cerebral vasodilator by selectively inducing a cGMP-independent relaxation of the intracranial vertebrobasilar artery.2 Attenuates neuroinflammation and enhances retinal ganglion cell viability in glaucoma via PKA signaling.3 A glial cell activation inhibitor.4 Enhances morphine analgesia and attenuates tolerance and withdrawaI.5 Orally active and crosses the blood-brain barrier.5
Biochemicals & reagents
50847-11-5
2-Methyl-1-[2-(1-methylethyl)pyrazolo[1,5-a]pyridine-3-yl 1-propanone; KC-404; AV411
1) Kishi et al. (2001), Ibudilast: a mom-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 ibidilast 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
RT
TARGET: PDE (Phosphodiesterase) -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Inflammation; NeurodegenerationPain