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.
نویسندگان
چکیده
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.
منابع مشابه
The ES-242s, novel N-methyl-D-aspartate antagonists of microbial origin, interact with both the neurotransmitter recognition site and the ion channel domain.
ES-242-1 approximately 5 are novel microbial bioxanthracenes which do not contain nitrogen. The ES-242s inhibited the binding of [3H]TCP and [3H]CGS19755 to the N-methyl-D-aspartate (NMDA) receptor complex. They had no effect on the binding of the specific ligands for the non-NMDA receptor. The biochemical and pharmacological properties of ES-242-1 were fully examined since it is the most poten...
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ورودعنوان ژورنال:
- The Journal of antibiotics
دوره 45 1 شماره
صفحات -
تاریخ انتشار 1992