ES-242-1, A NOVEL COMPOUND FROM Verticillium sp., BINDS TO A SITE ON N-METHYL-D-ASPARTATE RECEPTOR THAT IS COUPLED TO THE CHANNEL DOMAIN

Abstract

A novel compound, ES-242-1, which binds to a site on N-methyl-D-aspartate (NMDA) receptor that is coupled to the channel domain, was isolated from the culture broth of a fungus, Verticillium sp. SPC-15898. ES-242-1 inhibited the [³H]thienyl cyclohexylpiperidine ([³H]TCP) binding to rat crude synaptic membrane fractions with an IC₅₀ value of 116 nM, but did not inhibit the [³H]kainate binding to its receptor, which is another subtype of the excitatory amino acid receptor.