产品
编 号：F193254
分子式：C18H11Cl2NO4
分子量：376.19
分子式：C18H11Cl2NO4
分子量：376.19
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 161230-88-2
产品详情
生物活性：
MDL 105519 is a potent and selective antagonist of glycine binding to the NMDA receptor.
体内研究：
MDL 105519 is an NMDA receptor antagonist in vivo. Intravenously administration of MDL 105519 prevents harmaline-stimulated increases in cerebellar cyclic GMP content, providing biochemical evidence of NMDA receptor antagonism in vivo. This antagonism is associated with anticonvulsant activity in genetically based, chemically induced, and electrically mediated seizure models. Anxiolytic activity is observed in the rat separation-induced vocalization model, but muscle-relaxant activity is apparent at lower doses. Higher doses impair rotorod performance, but are without effect on mesolimbic dopamine turnover or prepulse inhibition of the startle reflex.
体外研究：
MDL 105519 is a potent and selective ligand for the glycine recognition site that completely inhibit the binding of [3H]glycine to rat brain membranes with a Ki value of 10.9 nM. MDL 105519 is approximately 10,000-fold selective for the glycine recognition site relative to the other receptor types investigated. MDL 105519 inhibits NMDA-dependent responses, such as elevations of [3H]TCP binding in brain membranes, cyclic GMP accumulation in brain slices, and alterations in cytosolic Ca2+ and Na+-Ca2+ currents in cultured neurons. Inhibition is non-competitive with respect to NMDA and could be nullified with D-serine.
MDL 105519 is a potent and selective antagonist of glycine binding to the NMDA receptor.
体内研究：
MDL 105519 is an NMDA receptor antagonist in vivo. Intravenously administration of MDL 105519 prevents harmaline-stimulated increases in cerebellar cyclic GMP content, providing biochemical evidence of NMDA receptor antagonism in vivo. This antagonism is associated with anticonvulsant activity in genetically based, chemically induced, and electrically mediated seizure models. Anxiolytic activity is observed in the rat separation-induced vocalization model, but muscle-relaxant activity is apparent at lower doses. Higher doses impair rotorod performance, but are without effect on mesolimbic dopamine turnover or prepulse inhibition of the startle reflex.
体外研究：
MDL 105519 is a potent and selective ligand for the glycine recognition site that completely inhibit the binding of [3H]glycine to rat brain membranes with a Ki value of 10.9 nM. MDL 105519 is approximately 10,000-fold selective for the glycine recognition site relative to the other receptor types investigated. MDL 105519 inhibits NMDA-dependent responses, such as elevations of [3H]TCP binding in brain membranes, cyclic GMP accumulation in brain slices, and alterations in cytosolic Ca2+ and Na+-Ca2+ currents in cultured neurons. Inhibition is non-competitive with respect to NMDA and could be nullified with D-serine.
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