Ibudilast
Ibudilast structure
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Common Name | Ibudilast | ||
|---|---|---|---|---|
| CAS Number | 50847-11-5 | Molecular Weight | 230.305 | |
| Density | 1.1±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C14H18N2O | Melting Point | 53-54°C | |
| MSDS | Chinese USA | Flash Point | N/A | |
| Symbol |
GHS07 |
Signal Word | Warning | |
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The glial cell modulators, ibudilast and its amino analog, AV1013, attenuate methamphetamine locomotor activity and its sensitization in mice.
Eur. J. Pharmacol. 679(1-3) , 75-80, (2012) Over 800,000 Americans abuse the psychomotor stimulant, methamphetamine, yet its abuse is without an approved medication. Methamphetamine induces hypermotor activity, and sensitization to this effect is suggested to represent aspects of the addiction process.... |
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Phosphodiesterase inhibitors. Part 1: Synthesis and structure–activity relationships of pyrazolopyridine–pyridazinone PDE inhibitors developed from ibudilast
Bioorg. Med. Chem. Lett. 21(11) , 3307-12, (2011) Ibudilast [1-(2-isopropylpyrazolo[1,5-a]pyridin-3-yl)-2-methylpropan-1-one] is a nonselective phosphodiesterase inhibitor used clinically to treat asthma. Efforts to selectively develop the PDE3- and PDE4-inhibitory activity of ibudilast led to replacement of... |
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Ibudilast, a pharmacologic phosphodiesterase inhibitor, prevents human immunodeficiency virus-1 Tat-mediated activation of microglial cells.
PLoS ONE 6(4) , e18633, (2011) Human Immunodeficiency Virus-1 (HIV-1)-associated neurocognitive disorders (HAND) occur, in part, due to the inflammatory response to viral proteins, such as the HIV-1 transactivator of transcription (Tat), in the central nervous system (CNS). Given the need ... |
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Inhibition of paclitaxel-induced decreases in calcium signaling.
J. Biol. Chem. 287(45) , 37907-16, (2012) Peripheral neuropathy is one of the most severe and irreversible side effects caused by treatment from several chemotherapeutic drugs, including paclitaxel (Taxol®) and vincristine. Strategies are needed that inhibit this unwanted side effect without altering... |
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Ibudilast, a mixed PDE3/4 inhibitor, causes a selective and nitric oxide/cGMP-independent relaxation of the intracranial vertebrobasilar artery.
Eur. J. Pharmacol. 650(2-3) , 605-11, (2011) Ibudilast, a mixed phosphodiesterase (PDE) 3/4 inhibitor, is a cerebral vasodilator widely used in Japan for treating post-stroke dizziness. However, little studies have been conducted on the vasorelaxant effects of PDE inhibitors in the vertebrobasilar arter... |
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Ibudilast, a phosphodiesterase inhibitor with anti-inflammatory activity, protects against ischemic brain injury in rats.
Brain Res. 1431 , 97-106, (2012) Ibudilast, a non-selective phosphodiesterase inhibitor, is clinically used in patients with stroke or dizziness. However, whether the compound exerts a beneficial effect on acute ischemic stroke remains to be established. We used a rat model of transient foca... |
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Cross-species comparisons of the pharmacokinetics of ibudilast.
Xenobiotica 39(12) , 964-77, (2009) To enable clinical development of ibudilast for new indications, its pharmacokinetics were characterized in mice, rats, rabbits, dogs, cynomolgus monkeys, and minipigs. Animal pharmacokinetics were compared with a separate study in healthy volunteers. Followi... |
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Effects of topical application of ibudilast for seasonal allergic conjunctivitis in patients wearing soft contact lenses.
Eye Contact Lens 35(5) , 251-4, (2009) To assess the influence of topical application of ibudilast for seasonal allergic conjunctivitis in patients wearing soft contact lenses (SCLs).There were 16 SCL wearers (32 eyes) with allergic conjunctivitis due to cedar pollen, who were studied from Februar... |
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Vasodilator effects of ibudilast on retinal blood vessels in anesthetized rats.
Biol. Pharm. Bull. 32(11) , 1924-7, (2009) Ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-alpha]pyridine) is clinically used as a cerebral vasodilator in Japan. However, the effects of ibudilast on retinal blood vessels have not been fully examined. The aim of this study, therefore, was to examine th... |
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Determination of ibudilast in human serum by high-performance liquid chromatography for pharmacokinetic study.
Biomed. Chromatogr. 24(3) , 324-8, (2010) A simple, accurate, precise and cost effective reversed-phase HPLC method was developed to determine the concentration of ibudilast in human serum. Ibudilast and an internal standard, butyl 4-hydroxybenzoate, were extracted by liquid-liquid extraction with me... |