GYKI 52466 (hydrochloride)
An allosteric AMPA receptor antagonist
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包装价格促销价数量
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10mg￥2425.001940.00- +
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25mg￥7200.005760.00- +
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50mg￥10812.008650.00- +
- 货号: ajcx25476
- CAS: 192065-56-8
- 别名: AMPA受体选择性阻断剂前体
- 分子式: C17H15N3O2·HCl
- 分子量: 329.8
- 纯度: ＞98%
- 溶解度: Methanol: 1 mg/ml
- 储存: -20°C
- 库存: 现货
Background
GYKI 52466 is an allosteric AMPA receptor antagonist.1 It selectively inhibits AMPA-induced inward currents (IC50 = 7.5 µM) over NMDA- or GABA-induced inward currents in primary rat hippocampal neurons at 50 µM but also inhibits kainate-induced inward currents in the same cells (IC50 = 11 µM).2 GYKI 52466 (10 µM) reduces the amplitude of spontaneous excitatory postsynaptic currents (EPSCs) in the same cells. It increases the latency to seizure onset and reduces mortality in a rat model of generalized tonic-clonic seizures induced by 4-aminopyridine when administered at doses of 25 and 50 mg/kg.1 GYKI 52466 (30 mg/kg) prevents neuronal damage in the CA1 region of the hippocampus in a rat model of global ischemia-reperfusion injury induced by four-vessel occlusion.3
1.Weiczner, R., Krisztin-Péva, B., and Mihály, A.Blockade of AMPA-receptors attenuates 4-aminopyridine seizures, decreases the activation of inhibitory neurons but is ineffective against seizure-related astrocytic swellingEpilepsy Res.78(1)22-32(2008) 2.Donevan, S.D., and Rogawski, M.A.GYKI 52466, a 2,3-benzodiazepine, is a highly selective, noncompetitive antagonist of AMPA/kainate receptor responsesNeuron10(1)51-59(1993) 3.Block, F., Schmitt, W., and Schwarz, M.Pretreatment but not posttreatment with GYKI 52466 reduces functional deficits and neuronal damage after global ischemia in ratsJ. Neurol. Sci.139(2)167-172(1996)
