ES-242-2, -3, -4, -5, -6, -7, and -8, novel bioxanthracenes produced by Verticillium sp., which act on the N-methyl-D-aspartate receptor.
Verticillium sp. SPC-15898 was found to produce novel metabolites, designated ES-242-2-(-)8, which were structurally related to ES-242-1. These compounds were isolated from the culture broth and the physico-chemical and biochemical properties were examined. ES-242-2-(-)8 inhibited [3H]thienyl cyclohexypiperidine ([3H]TCP) binding to rat crude synaptic membranes (CSM) with IC50 values of 0.116, 2.9, ca. 2.9, 25.3, 1.0, 59, 24, and 13 microM, respectively. None of these compounds showed inhibitory effects against the binding of [3H]kainate to its receptor, which is another subtype of the excitatory amino acid receptor.
Toki
S
S
Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Japan.
Ando
K
K
Kawamoto
I
I
Sano
H
H
Yoshida
M
M
Matsuda
Y
Y
D000818:Animals; D001921:Brain / Q000187:drug effects; D066298:In Vitro Techniques; D007608:Kainic Acid / Q000378:metabolism; D003904:Mitosporic Fungi / Q000378:metabolism; D010622:Phencyclidine / Q000378:metabolism* / Q000031:analogs & derivatives; D010880:Piperidines; D011714:Pyrans / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D051381:Rats; D016194:Receptors, N-Methyl-D-Aspartate / Q000187:drug effects*; D013329:Structure-Activity Relationship; D014316:Tritium
D010880:Piperidines; D011714:Pyrans; D016194:Receptors, N-Methyl-D-Aspartate; D014316:Tritium; C012058:tenocyclidine; D010622:Phencyclidine; D007608:Kainic Acid