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.