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XB-ART-24809
Sheng Li Xue Bao 1991 Jun 01;433:227-35.
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[Fungal toxin dihydroxyaflavinine inhibits non-competitively GABAA receptor channel expressed in Xenopus oocytes].

Yao Y , Li Y .


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Dihydroxyaflavinine is an indole-derived metabolite of Aspergillus flavus. Its action on GABA-induced response was quantitatively studied on the GABAA receptor expressed in Xenopus oocytes after injection of chick brain mRNA under voltage-clamp conditions. Dihydroxyaflavinine inhibits GABA-induced current non-competitively with KI = 12 mumol/L. This blockage is rapidly reversible. In comparison, the inhibitory effect of penicillin on GABAA receptor is enhanced by increasing GABA concentration. Ro 15-1788 (a benzodiazepine ligand with KD = 0.6--2 nmol/L) of concentration as high as 1 mumol/L, does not mask the action of 10 mumol/L dihydroxyaflavinine, indicating that dihydroxyaflavinine acts on a site different from benzodiazepines. Dihydroxyaflavinine appears to expedite desensitization of the receptor, which is similar to the action of picrotoxin and in contrast with that of penicillin and bicuculline.

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Species referenced: Xenopus laevis
Genes referenced: gabarap