50847-11-5 Usage
Description
Ibudilast is a leukotriene D4 antagonist and phosphodiesterase inhibitor, which plays a significant role in the treatment of bronchial asthma. It effectively antagonizes leukotriene D4-induced contractions of guinea pig ileum and tracheal muscles in vitro, and inhibits eosinophil accumulation in vivo.
Uses
Used in Pharmaceutical Industry:
Ibudilast is used as a phosphodiesterase inhibitor with anti-inflammatory activity for the treatment of bronchial asthma and other inflammatory conditions. Its ability to inhibit PDE4, PDE3, and PDE5 at varying concentrations helps suppress the elaboration of mediators involved in asthma and inflammation.
Used in Respiratory Therapy:
Ibudilast is used as an antiallergic and antiasthmatic agent, providing relief from allergic reactions and asthma symptoms by reducing inflammation and bronchoconstriction.
Used in Neurological Therapy:
Ibudilast is used as a vasodilator in the cerebral context, promoting improved blood flow and potentially offering benefits in the treatment of neurological disorders associated with reduced cerebral blood flow.
Originator
Kyorin (Japan)
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.
Biochem/physiol Actions
Phosphodiesterase IV (PDE4) inhbitor. Inhibits platelet aggregation. Anti-asthma drug.
in vitro
ibudilast could potently inhibit purified human pde4a, 4b, 4c and 4d with ic50 values at 54, 65, 239 and 166 nm, respectively. ibudilast was also able to effectively block lps-induced tumor necrosis factor and n-formyl-metleu-phe-induced leukotriene b4 biosynthesis in human whole blood [1].
in vivo
rats received a daily oral administration of 10, 30 or 60 mg/kg ibudilast. results showed that in the vehicle-treated animals, white matter lesions and microglial activation occurred in the optic tract, internal capsule and corpus callosum. a low dose of ibudilast failed to suppress the white matter lesions and microglial activation, whereas a dose of either 30 or 60 mg/kg ibudilast ameliorated these lesions [2].
IC 50
54-239 nm
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
Check Digit Verification of cas no
The CAS Registry Mumber 50847-11-5 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 5,0,8,4 and 7 respectively; the second part has 2 digits, 1 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 50847-11:
(7*5)+(6*0)+(5*8)+(4*4)+(3*7)+(2*1)+(1*1)=115
115 % 10 = 5
So 50847-11-5 is a valid CAS Registry Number.
InChI:InChI=1/C14H18N2O/c1-9(2)13-12(14(17)10(3)4)11-7-5-6-8-16(11)15-13/h5-10H,1-4H3
50847-11-5Relevant articles and documents
SUBSTITUTED PYRAZOLO [1,5-α] PYRIDINE COMPOUNDS AND THEIR METHODS OF USE
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Page/Page column 43, (2010/11/29)
The present invention is directed to substituted pyrazolo[l,5-α]pyridines and related methods for their synthesis and use.
