The selective p 38 inhibitor SB - 239063 protects primary neurons from 2 mild to moderate excitotoxic injury 3 Jeffrey
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چکیده
5 In Vivo Pharmacology, High Throughput Biology, Discovery Research, GlaxoSmithKline, PO Box 1539, Mail Code UW 2523, 709 Swedeland Road, 6 King of Prussia, PA 19406, USA 7 Department of Neurobiology, University of Pittsburgh School of Medicine, Pittsburgh, PA, USA 8 Neurology Centre of Excellence for Drug Discovery, GlaxoSmithKline, Harlow, UK 9 Cardiovascular and Urogenital Center of Excellence for Drug Discovery, GlaxoSmithKline, King of Prussia, PA, USA 10 11 Received 5 April 2002; received in revised form 23 May 2002; accepted 24 May 2002
منابع مشابه
SB 239063, a second-generation p38 mitogen-activated protein kinase inhibitor, reduces brain injury and neurological deficits in cerebral focal ischemia.
The stress-activated mitogen-activated protein kinase (MAPK) p38 has been linked to the production of inflammatory cytokines/mediators/inflammation and death/apoptosis following cell stress. In these studies, a second-generation p38 MAPK inhibitor, SB 239063 (IC(50) = 44 nM), was found to exhibit improved kinase selectivity and increased cellular (3-fold) and in vivo (3- to 10-fold) activity ov...
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The MAPK family member p38 is activated in the heart after ischemia-reperfusion (I/R) injury. However, the cardioprotective vs. proapoptotic effects associated with p38 activation in the heart after I/R injury remain unresolved. Another issue to consider is that the majority of past studies have employed the rodent as a model for assessing p38's role in cardiac injury vs. protection, while the ...
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BACKGROUND AND PURPOSE Mitogen-activated protein kinases (MAPK) are centrally involved in several mechanisms important for heart failure such as apoptosis, activation of inflammatory responses and cell proliferation. We therefore evaluated the effect of the selective p38 MAPK inhibitor SB 239063 on progression of left ventricular remodelling after myocardial infarction (MI) in rats. EXPERIMEN...
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BACKGROUND In vitro evidence suggests that the p38 mitogen-activated protein kinase (p38 MAPK) plays a crucial role in PMN activation and inflammatory cytokine production. However, the effect of p38 MAPK on myocardial reperfusion injury, a pathologic condition involving a typical inflammatory response, has not been fully examined. In the present study, we investigated the effect of SB 239063, a...
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Extracellular glutamate is elevated following brain ischemia or trauma and contributes to neuronal injury. We tested the hypothesis that magnesium sulfate (MgSO4, 3 mM) protects against metabolic failure caused by excitotoxic glutamate exposure. Rat cortical neuron preparations treated in medium already containing a physiological concentration of Mg(2+) (1 mM) could be segregated based on their...
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تاریخ انتشار 2002