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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/02/13 21:08:44」(JST)

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Edaravone (brand name Radicut) is a nootropic and neuroprotective agent used for the purpose of aiding neurological recovery following acute brain ischemia and subsequent cerebral infarction.^[1] It acts as a potent antioxidant and strongly scavenges free radicals, protecting against oxidative stress and neuronal apoptosis.^[2]^[3]^[4] It has been marketed solely in Japan by Mitsubishi Pharma since 2001.^[1] and marketed in India by Edinburgh Pharmaceuticals by the brand name Arone

Edaravone has been shown to attenuate methamphetamine- and 6-OHDA-induced dopaminergic neurotoxicity in the striatum and substantia nigra, and does not affect methamphetamine-induced dopamine release or hyperthermia.^[5]^[6] It has also been demonstrated to protect against MPTP-mediated dopaminergic neurotoxicity to the substantia nigra, though notably not to the striatum.^[7]^[8]^[9]

References

^ ^a ^b Doherty, Annette M. (2002). Annual Reports in Medicinal Chemistry, Volume 37 (Annual Reports in Medicinal Chemistry). Boston: Academic Press. ISBN 0-12-040537-7.
^ Watanabe T, Tanaka M, Watanabe K, Takamatsu Y, Tobe A (March 2004). "[Research and development of the free radical scavenger edaravone as a neuroprotectant]". Yakugaku Zasshi (in Japanese) 124 (3): 99–111. doi:10.1248/yakushi.124.99. PMID 15049127.
^ Higashi Y, Jitsuiki D, Chayama K, Yoshizumi M (January 2006). "Edaravone (3-methyl-1-phenyl-2-pyrazolin-5-one), a novel free radical scavenger, for treatment of cardiovascular diseases". Recent Patents on Cardiovascular Drug Discovery 1 (1): 85–93. doi:10.2174/157489006775244191. PMID 18221078.
^ Yoshida H, Yanai H, Namiki Y, Fukatsu-Sasaki K, Furutani N, Tada N (2006). "Neuroprotective effects of edaravone: a novel free radical scavenger in cerebrovascular injury". CNS Drug Reviews 12 (1): 9–20. doi:10.1111/j.1527-3458.2006.00009.x. PMID 16834755.
^ Yuan WJ, Yasuhara T, Shingo T, et al. (2008). "Neuroprotective effects of edaravone-administration on 6-OHDA-treated dopaminergic neurons". BMC Neuroscience 9: 75. doi:10.1186/1471-2202-9-75. PMC 2533664. PMID 18671880.
^ Kawasaki T, Ishihara K, Ago Y, et al. (August 2006). "Protective effect of the radical scavenger edaravone against methamphetamine-induced dopaminergic neurotoxicity in mouse striatum". European Journal of Pharmacology 542 (1-3): 92–9. doi:10.1016/j.ejphar.2006.05.012. PMID 16784740.
^ Kawasaki T, Ishihara K, Ago Y, Baba A, Matsuda T (July 2007). "Edaravone (3-methyl-1-phenyl-2-pyrazolin-5-one), a radical scavenger, prevents 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced neurotoxicity in the substantia nigra but not the striatum". The Journal of Pharmacology and Experimental Therapeutics 322 (1): 274–81. doi:10.1124/jpet.106.119206. PMID 17429058.
^ Yokoyama H, Takagi S, Watanabe Y, Kato H, Araki T (June 2008). "Role of reactive nitrogen and reactive oxygen species against MPTP neurotoxicity in mice". Journal of Neural Transmission (Vienna, Austria : 1996) 115 (6): 831–42. doi:10.1007/s00702-008-0019-6. PMID 18235988.
^ Yokoyama H, Yano R, Aoki E, Kato H, Araki T (September 2008). "Comparative pharmacological study of free radical scavenger, nitric oxide synthase inhibitor, nitric oxide synthase activator and cyclooxygenase inhibitor against MPTP neurotoxicity in mice". Metabolic Brain Disease 23 (3): 335–49. doi:10.1007/s11011-008-9096-3. PMID 18648914.

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English Journal

Edaravone abrogates LPS-induced behavioral anomalies, neuroinflammation and PARP-1.

Sriram CS1, Jangra A1, Gurjar SS2, Mohan P3, Bezbaruah BK4.
Physiology & behavior.Physiol Behav.2016 Feb 1;154:135-44. doi: 10.1016/j.physbeh.2015.10.029. Epub 2015 Oct 30.
Poly(ADP-ribose) polymerase-1 (PARP-1) is a DNA nick-sensor enzyme that functions at the center of cellular stress response and affects the immune system at several key points, and thus modulates inflammatory diseases. Our previous study demonstrated that lipopolysaccharide (LPS)-induced depressive-
PMID 26522738

Thrombolysis with Low-Dose Tissue Plasminogen Activator 3-4.5 h After Acute Ischemic Stroke in Five Hospital Groups in Japan.

Morihara R1, Kono S1, Sato K1, Hishikawa N1, Ohta Y1, Yamashita T1, Deguchi K1, Manabe Y2, Takao Y3, Kashihara K4, Inoue S5, Kiriyama H5, Abe K6.
Translational stroke research.Transl Stroke Res.2016 Jan 27. [Epub ahead of print]
Clinical data from Japan on the safety and real-world outcomes of alteplase (tPA) thrombolysis in the extended therapeutic window are lacking. The aim of this study was to assess the safety and real-world outcomes of tPA administered within 3-4.5 h of stroke onset. The study comprised consecutive a
PMID 26815291

Protection by Edaravone, a Radical Scavenger, against Manganese-Induced Neurotoxicity in Rats.

Apaydin M1,2, Erbas O3, Taskiran D4.
Journal of biochemical and molecular toxicology.J Biochem Mol Toxicol.2016 Jan 18. doi: 10.1002/jbt.21780. [Epub ahead of print]
Manganese (Mn) is a required element for biological systems; however, its excessive exposure may lead to a neurological syndrome known as manganism. The aim of the present study was to assess the toxic effects of subacute exposure of Mn by measuring weight gain, motor performance, and biochemical pa
PMID 26778341

Japanese Journal

Inhibitory Effects of Edaravone, a Free Radical Scavenger, on Cytokine-induced Hyperpermeability of Human Pulmonary Microvascular Endothelial Cells:A Comparison with Dexamethasone and Nitric Oxide Synthase Inhibitor

Acta Medica Okayama 69(5), 279-290, 2015-10
NAID 120005666066

実験的自己免疫性神経炎ラットにおける末梢神経内ヒドロキシラジカルの産生 (東邦医学会雑誌)

東邦医学会雑誌 1(1), 2-10, 2015-03
NAID 120005614766

片側の椎骨動脈解離により生じた両側延髄内側梗塞の1例

臨床神経学 55(10), 748-752, 2015
NAID 130005103329

「エダラボン」

Edaravone
Systematic (IUPAC) name
	5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one
Clinical data
Legal status	℞ Prescription only;
Routes	Oral
Identifiers
CAS number	89-25-8
ATC code	None
PubChem	CID 4021
ChemSpider	3881
UNII	S798V6YJRP
KEGG	D01552
ChEBI	CHEBI:31530
ChEMBL	CHEMBL290916
Synonyms	MCI-186
Chemical data
Formula	C10H10N2O
Molecular mass	174.20 g/mol
	SMILES O=C1N(/N=C(\C1)C)c2ccccc2;
	InChI InChI=1S/C10H10N2O/c1-8-7-10(13)12(11-8)9-5-3-2-4-6-9/h2-6H,7H2,1H3 ; Key:QELUYTUMUWHWMC-UHFFFAOYSA-N ;
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　　[★]

英: edaravone
商: ラジカット

脳保護薬;ラジカルスカベンジャー

[isbn0-12-040537-7-1] Doherty, Annette M. (2002). Annual Reports in Medicinal Chemistry, Volume 37 (Annual Reports in Medicinal Chemistry). Boston: Academic Press. ISBN 0-12-040537-7.

[pmid15049127-2] Watanabe T, Tanaka M, Watanabe K, Takamatsu Y, Tobe A (March 2004). "[Research and development of the free radical scavenger edaravone as a neuroprotectant]". Yakugaku Zasshi (in Japanese) 124 (3): 99–111. doi:10.1248/yakushi.124.99. PMID 15049127.

[pmid18221078-3] Higashi Y, Jitsuiki D, Chayama K, Yoshizumi M (January 2006). "Edaravone (3-methyl-1-phenyl-2-pyrazolin-5-one), a novel free radical scavenger, for treatment of cardiovascular diseases". Recent Patents on Cardiovascular Drug Discovery 1 (1): 85–93. doi:10.2174/157489006775244191. PMID 18221078.

[pmid16834755-4] Yoshida H, Yanai H, Namiki Y, Fukatsu-Sasaki K, Furutani N, Tada N (2006). "Neuroprotective effects of edaravone: a novel free radical scavenger in cerebrovascular injury". CNS Drug Reviews 12 (1): 9–20. doi:10.1111/j.1527-3458.2006.00009.x. PMID 16834755.

[pmid18671880-5] Yuan WJ, Yasuhara T, Shingo T, et al. (2008). "Neuroprotective effects of edaravone-administration on 6-OHDA-treated dopaminergic neurons". BMC Neuroscience 9: 75. doi:10.1186/1471-2202-9-75. PMC 2533664. PMID 18671880.

[pmid16784740-6] Kawasaki T, Ishihara K, Ago Y, et al. (August 2006). "Protective effect of the radical scavenger edaravone against methamphetamine-induced dopaminergic neurotoxicity in mouse striatum". European Journal of Pharmacology 542 (1-3): 92–9. doi:10.1016/j.ejphar.2006.05.012. PMID 16784740.

[pmid17429058-7] Kawasaki T, Ishihara K, Ago Y, Baba A, Matsuda T (July 2007). "Edaravone (3-methyl-1-phenyl-2-pyrazolin-5-one), a radical scavenger, prevents 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced neurotoxicity in the substantia nigra but not the striatum". The Journal of Pharmacology and Experimental Therapeutics 322 (1): 274–81. doi:10.1124/jpet.106.119206. PMID 17429058.

[pmid18235988-8] Yokoyama H, Takagi S, Watanabe Y, Kato H, Araki T (June 2008). "Role of reactive nitrogen and reactive oxygen species against MPTP neurotoxicity in mice". Journal of Neural Transmission (Vienna, Austria : 1996) 115 (6): 831–42. doi:10.1007/s00702-008-0019-6. PMID 18235988.

[pmid18648914-9] Yokoyama H, Yano R, Aoki E, Kato H, Araki T (September 2008). "Comparative pharmacological study of free radical scavenger, nitric oxide synthase inhibitor, nitric oxide synthase activator and cyclooxygenase inhibitor against MPTP neurotoxicity in mice". Metabolic Brain Disease 23 (3): 335–49. doi:10.1007/s11011-008-9096-3. PMID 18648914.

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edaravone