Edaravon

Edaravon
(IUPAC) ime
	5-metil-2-fenil-2,4-dihidro-3H-pirazol-3-on
Klinički podaci
Identifikatori
CAS broj	89-25-8
ATC kod	nije dodeljen
PubChem	4021
ChemSpider	3881
UNII	S798V6YJRP
KEGG	D01552
ChEBI	CHEBI:31530
ChEMBL	CHEMBL290916
Hemijski podaci
Formula	C10H10N2O
Mol. masa	174,20 g/mol
SMILES	eMolekuli & PubHem
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
Sinonimi	MCI-186
Farmakoinformacioni podaci
Trudnoća	?
Pravni status	℞ Prescription only
Način primene	Oralno

Edaravon (Radicut) je neuroprotektivni lek koji pomaže u neurološkom oporavku nakon akutne ishemije mozga i naknadne cerebralne infarkcije.^[6] On deluje kao potentan antioksidans i jak sakupljaš slobodnih radikala, koji štiti od oksidativnog stresa i neuronalne apoptoze.^[7]^[8]^[9] On je u prodaji u Japanu (od 2001.)^[6] i u Indiji.

Edaravon umanjuje dejstvo metamfetamina i 6-OHDA indukovanu dopaminergičku neurotoksičnost u strijatumu i substantia nigra, a nema efekta na metamfetaminom indukovano otpuštanje dopamina ili hipertermiju.^[10]^[11] On takođe štiti protiv MPTP-posredovane dopaminergičke neurotoksičnosti u substantia nigra, mada ne i u strijatumu.^[12]^[13]^[14]

Reference

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit
↑ Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H.
↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit
↑ ^6,0 ^6,1 Doherty, Annette M. (2002). Annual Reports in Medicinal Chemistry, Volume 37 (Annual Reports in Medicinal Chemistry). Boston: Academic Press. ISBN 0-12-040537-7.
↑ Watanabe T, Tanaka M, Watanabe K, Takamatsu Y, Tobe A (March 2004). „[Research and development of the free radical scavenger edaravone as a neuroprotectant”] (Japanese). Yakugaku Zasshi 124 (3): 99–111. 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. 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.

Literatura

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

Spoljašnje veze

	Portal Medicina
	Portal Hemija

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[3] Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit

[4] Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H.

[5] Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit

[isbn0-12-040537-7-6] 6,0 ^6,1 Doherty, Annette M. (2002). Annual Reports in Medicinal Chemistry, Volume 37 (Annual Reports in Medicinal Chemistry). Boston: Academic Press. ISBN 0-12-040537-7.

[pmid15049127-7] Watanabe T, Tanaka M, Watanabe K, Takamatsu Y, Tobe A (March 2004). „[Research and development of the free radical scavenger edaravone as a neuroprotectant”] (Japanese). Yakugaku Zasshi 124 (3): 99–111. PMID 15049127.

[pmid18221078-8] 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. PMID 18221078.

[pmid16834755-9] 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.

[pmid18671880-10] 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.

[pmid16784740-11] 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.

[pmid17429058-12] 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.

[pmid18235988-13] 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.

[pmid18648914-14] 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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