Inhibitory effect of 2,4-dihydroxyphenylacetylasparagine, a common moiety of spider toxin, on glutamate binding to rat brain synaptic membranes

Abstract

2,4-Dihydroxyphenylacetylasparagine (2,4-DHPA-ASN), a common moiety of molecules of spider toxins, was shown to inhibit l-[ 3H]glutamic acid binding to rat brain synaptic membranes in a dose-dependent manner. The inhibitory effect of 2,4-DHPA-ASN was almost the same as that of intact spider toxin isolated from Nephila clavata, but significantly higher than that of 2,4-dihydroxyphenylacetic acid (2,4-DHPA). In addition, neither 2,4-dihydroxybenzoic acid nor the isomers of 2,4-DHPA suppressed the glutamate binding. These results suggested that 2,4-DHPA might be the functional part and asparagine in the molecules of spider toxins seemed to cause increasing affinity toward the recognition site of glutamate binding.