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  • SDZ 220-581 hydrochloride
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SDZ 220-581 hydrochloride

SDZ 220-581 hydrochloride 是一种口服有效的竞争性 NMDA 受体拮抗剂,pKi 值为 7.7。

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¥1300-5450
价格
1040-4360
SDZ 220-581 hydrochloride的二维码

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  • 货号: ajci18214
  • CAS: 179411-93-9
  • 别名: (S)-ALPHA-氨基-2'-氯-5-(膦酰甲基)-[1,1'-联苯]-3-丙酸盐酸盐
  • 分子式: C16H18Cl2NO5P
  • 分子量: 406.2
  • 纯度: >98%
  • 溶解度: Soluble in DMSO
  • 储存: Store at -20°C
  • 库存: 现货

Background

SDZ 220-581 hydrochloride is a potent and competitive antagonist of NMDA receptor with pKi value of 7.7 [1].


SDZ 220-581 is a biphenyl-AP7-derivative. It is potent both in vitro and in vivo. SDZ 220-581 binds with high affinity to the recognition site of NMDA receptor. It does not bind to the strychnine-insensitive glycine site or the MK-801 site within the NMDA receptor. In addition, SDZ 220-581 shows no effect on a variety of other binding assays such as for dopamine, serotonin and adenosine [1].


In the in vivo assay, the administration of SDZ 220-581 protects the mice against the maximal electroshock-induced seizures (MES). In the rat MES model, SDZ 220-581 also shows potent efficacy. Moreover, SDZ 220-581 can protect brain against quinolinic acid induced neuronal degeneration in rat. Furthermore, a dose of 1.25mg/kg SDZ 220-581 markedly reduces the cerebral infarct size in the focal cerebral ischemia model in rat [2].

参考文献:
[1] Urwyler et al .Biphenyl-derivatives of 2-amino-7-phosphono-heptanoic acid, a novel class of potent competitive N-methyl-D-aspartate receptor antagonists - II. Pharmacological characterization in vivo. Neuropharmacology 1996, 35 655.
[2] Urwyler S, Campbell E, Fricker G, et al. Biphenyl-derivatives of 2-amino-7-phosphono-heptanoic acid, a novel class of potent competitiveN-Methyl-D-aspartate receptor antagonists—II. Pharmacological characterization in vivo[J]. Neuropharmacology, 1996, 35(6): 655-669.

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