CAS NO: | 192065-56-8 |
包装 | 价格(元) |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
Cas No. | 192065-56-8 |
别名 | AMPA受体选择性阻断剂前体 |
Canonical SMILES | CC1=NN=C(C2=CC=C(N)C=C2)C3=C(C=C4OCOC4=C3)C1.Cl |
分子式 | C17H15N3O2·HCl |
分子量 | 329.8 |
溶解度 | Methanol: 1 mg/ml |
储存条件 | -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | GYKI 52466 is an allosteric AMPA receptor antagonist.1It 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).2GYKI 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.1GYKI 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) |