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].
[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.
