您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > GYKI 52466(hydrochloride)
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
GYKI 52466(hydrochloride)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GYKI 52466(hydrochloride)图片
CAS NO:192065-56-8
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议

产品介绍
An allosteric AMPA receptor antagonist
Cas No.192065-56-8
别名AMPA受体选择性阻断剂前体
Canonical SMILESCC1=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 tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation 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)