220725-87-1|EGIS-8332|7-Acetyl-5-(4-aminophenyl)-8-methyl-9H-[1,3]dioxolo[4,5-h][2,3]benzodiazepine-8-carbonitrile|-范德生物科技公司

EGIS-8332

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names：
7-Acetyl-5-(4-aminophenyl)-8-methyl-9H-[1,3]dioxolo[4,5-h][2,3]benzodiazepine-8-carbonitrile
CAS号：
220725-87-1
MDL Number：
MF(分子式)： C20H18N4O3 MW(分子量)： 362.389
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文别名	EGIS-8332
英文别名	EGIS-8332; EGIS 8332; EGIS8332.
CAS号	220725-87-1
Inchi	InChI=1S/C20H18N4O3/c1-12(25)24-20(2,10-21)9-14-7-17-18(27-11-26-17)8-16(14)19(23-24)13-3-5-15(22)6-4-13/h3-8H,9,11,22H2,1-2H3
InchiKey	CBHCOCUJJQDHSR-UHFFFAOYSA-N
分子式 Formula	C20H18N4O3
分子量 Molecular Weight	362.389
溶解度Solubility
性状	Solid powder
储藏条件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

产品说明	EGIS-8332(CAS:220725-87-1):仅限应用于工业或者科学研究过程中非医疗目的，不应用于人类或动物的临床诊断以及治过程疗，该产品非药用，非食用。
Introduction	EGIS-8332 is a potent and selective non-competitive AMPA receptor antagonist. EGIS-8332 inhibits AMPA/kainate ion channels and cell death. EGIS-8332 inhibited AMPA currents in rat cerebellar Purkinje cells and inhibited the AMPA- and quisqualate-induced excitotoxicity in primary cultures of telencephalon neurons (IC(50)=5.1-9.0 microM), in vitro. EGIS-8332 seems suitable for further development for the treatment of epilepsy, ischaemia and stroke based on its efficacy in a variety of experimental disease models, and on its low side effect potential.
Application1
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Application3

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危险性	Warning
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备注

[1]Kovács AD, Saje A, Wong A, Ramji S, Cooper JD, Pearce DA. Age-dependent therapeutic effect of memantine in a mouse model of juvenile Batten disease. Neuropharmacology. 2012 Oct;63(5):769-75. doi: 10.1016/j.neuropharm.2012.05.040. Epub 2012 Jun 6. PubMed PMID: 22683643; PubMed Central PMCID: PMC3408822.

[2]Kovács AD, Saje A, Wong A, Szénási G, Kiricsi P, Szabó E, Cooper JD, Pearce DA. Temporary inhibition of AMPA receptors induces a prolonged improvement of motor performance in a mouse model of juvenile Batten disease. Neuropharmacology. 2011 Feb-Mar;60(2-3):405-9. doi: 10.1016/j.neuropharm.2010.10.010. Epub 2010 Oct 29. PubMed PMID: 20971125; PubMed Central PMCID: PMC3174473.

[3] Cooper JD. Moving towards therapies for juvenile Batten disease? Exp Neurol. 2008 Jun;211(2):329-31. doi: 10.1016/j.expneurol.2008.02.016. Epub 2008 Mar 4. Review. PubMed PMID: 18400221.

[4] Kapus GL, Gacsályi I, Vegh M, Kompagne H, Hegedus E, Leveleki C, Hársing LG, Barkóczy J, Bilkei-Gorzó A, Lévay G. Antagonism of AMPA receptors produces anxiolytic-like behavior in rodents: effects of GYKI 52466 and its novel analogues. Psychopharmacology (Berl). 2008 Jun;198(2):231-41. doi: 10.1007/s00213-008-1121-z. Epub 2008 Mar 25. PubMed PMID: 18363046.

[5] Kovács AD, Pearce DA. Attenuation of AMPA receptor activity improves motor skills in a mouse model of juvenile Batten disease. Exp Neurol. 2008 Jan;209(1):288-91. Epub 2007 Oct 25. PubMed PMID: 17963751; PubMed Central PMCID: PMC4418195.

6: Gigler G, Móricz K, Agoston M, Simó A, Albert M, Benedek A, Kapus G, Kertész S, Vegh M, Barkóczy J, Markó B, Szabó G, Matucz E, Gacsályi I, Lévay G, Hársing LG Jr, Szénási G. Neuroprotective and anticonvulsant effects of EGIS-8332, a non-competitive AMPA receptor antagonist, in a range of animal models. Br J Pharmacol. 2007 Sep;152(1):151-60. Epub 2007 Jul 2. PubMed PMID: 17603549; PubMed Central PMCID: PMC1978282.7: Vegh MG, Kovács AD, Kovács G, Szabó G, Tihanyi K, Hársing LG Jr, Lévay G. The new 2,3-benzodiazepine derivative EGIS-8332 inhibits AMPA/kainate ion channels and cell death. Neurochem Int. 2007 Feb;50(3):555-63. Epub 2006 Dec 4. PubMed PMID: 17147974.8: Matucz E, Móricz K, Gigler G, Benedek A, Barkóczy J, Lévay G, Hársing LG Jr, Szénási G. Therapeutic time window of neuroprotection by non-competitive AMPA antagonists in transient and permanent focal cerebral ischemia in rats. Brain Res. 2006 Dec 6;1123(1):60-7. Epub 2006 Oct 24. PubMed PMID: 17064671.9: Gressens P, Spedding M, Gigler G, Kertesz S, Villa P, Medja F, Williamson T, Kapus G, Levay G, Szenasi G, Barkoczy J, Harsing LG Jr. The effects of AMPA receptor antagonists in models of stroke and neurodegeneration. Eur J Pharmacol. 2005 Sep 5;519(1-2):58-67. PubMed PMID: 16112106.10: Matucz E, Móricz K, Gigler G, Simó A, Barkóczy J, Lévay G, Hársing LG Jr, Szénási G. Reduction of cerebral infarct size by non-competitive AMPA antagonists in rats subjected to permanent and transient focal ischemia. Brain Res. 2004 Sep 3;1019(1-2):210-6. PubMed PMID: 15306255.

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