title: 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.
authors.affiliation: Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Tokyo, Japan.
authors.forename: S
authors.initials: S
authors.lastname: Toki
authors.forename: K
authors.initials: K
authors.lastname: Ando
authors.forename: M
authors.initials: M
authors.lastname: Yoshida
authors.forename: I
authors.initials: I
authors.lastname: Kawamoto
authors.forename: H
authors.initials: H
authors.lastname: Sano
authors.forename: Y
authors.initials: Y
authors.lastname: Matsuda
mesh_terms: D000818:Animals; D001419:Bacteria / Q000187:drug effects; D001667:Binding, Competitive; D002498:Centrifugation; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D046508:Culture Techniques; D016291:Dizocilpine Maleate / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D005285:Fermentation; D007608:Kainic Acid / Q000378:metabolism; D007649:Ketamine / Q000494:pharmacology; D003904:Mitosporic Fungi / Q000378:metabolism*; D015394:Molecular Structure; D010622:Phencyclidine / Q000031:analogs & derivatives / Q000378:metabolism; D011714:Pyrans / Q000737:chemistry / Q000302:isolation & purification / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D016194:Receptors, N-Methyl-D-Aspartate / Q000378:metabolism*; D012988:Soil Microbiology; D012995:Solubility; D013570:Synaptic Membranes / Q000378:metabolism*
chemical_list: D011714:Pyrans; D016194:Receptors, N-Methyl-D-Aspartate; C073561:ES 242-1; D007649:Ketamine; D016291:Dizocilpine Maleate; C012058:tenocyclidine; D010622:Phencyclidine; D007608:Kainic Acid