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产品介绍
产品介绍
产品信息
商品描述
L-689,560 is a very potent antagonist at the glycine-NMDA site. The N-methyl-D-aspartate (NMDA) subtype of excitatorynamino acid receptor has been proved adequately that its relevant antagonists can reduce ischaemic brain damage (particularly in experimental models of focal cerebral ischaemia).
分子量
380.2
纯度
＞97%
可溶性
Soluble in DMSO (25 mM), ethanol (100 mM), and methanol.
外观
White to yellow solid
IC50
Glutamate NMDA receptor: IC50 = 4 nM (rat); Glutamate receptor subunit zeta 1: IC50 = 4 nM (rat)
In vitro(体外研究)
L-689560 is described as one of the most potent NMDA antagonists and [4'-3H]-L-689560 has been thought to be a highly specific radioligand for the glycine site. In consistent with the 5,7-disubstituted kynurenates, the tetrahydroquinolines are selective antagonists of glycine site NMDA, L-689560 exhibiting at least 3 orders of magnitude selectivity versus the glutamate site.
In vivo(体内研究)
MDL100748 with an ED50 of 83 mg kg-1 can prevent audiogenic seizures in susceptible mice after systemic injection. As a standard L689560, its subsequent analogues have been compared; the displacement of [3H] L689560 has often been used to displace that of [3H] glycine as an alternative assay. L701252, a quinones (the retention of a keto grouping at position 3), has been against L689560 binding (IC50 of 420 nM) and against seizures (ED50 of 4.1 mg kg-1) in DBA/2 mice. A group of sulfonamide analogues of kynurenic acid are also in active among the 2-quinolone series. Those of a series of 3,4-dihydroquinolones and tetrahydroquinolines with a nitrosubstituent at 3-position were selective antagonists at the NMDA receptor glycine site if they bore a bulky grouping in the position 4. The compound with no substitution at position 4 was proved to be one of the most effective broad-spectrum antagonists against NMDA and AMPA receptors.
Ki 数据
Glutamate NMDA receptor: Ki= 2 nM (rat)
应用
实验应用
A potent antagonist at the glycine-NMDA receptor site
背景
别名
trans-2-Carboxy-5,7-dichloro-4-phenylaMinocarbonyl aMino-1,2,3,4-tetrahydroquinoline
分子式
C17H15N3O3Cl2
CAS号
139051-78-8
PK值
pKa: 11.16 (Predicted), pKb: 3.19 (Predicted)
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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