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XB-ART-22092
Neuroreport 1993 Oct 25;51:93-4. doi: 10.1097/00001756-199310000-00026.
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Binding of the AMPA receptor antagonist [3H]GYKI 53405 to Xenopus brain membranes.

Szabó G , Henley JM .


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GYKI 52466 and related 2,3-benzodiazepines are highly selective antagonists of AMPA-evoked responses in rat CNS. However, these compounds do not compete with [3H]AMPA binding and their site of action remains unclear. Here we show that [3H]GYKI 53405 binds specifically to Xenopus brain membranes with KD and Bmax values of 4.5 microM and 35 pmol mg-1 protein respectively. Binding is increased in the presence of Mg2+ and is unaffected by AMPA or kainate. This is the first report of the binding of a GYKI 52466-related radioligand to any tissue and these results provide an initial step towards the characterization of novel recognition sites which are of considerable therapeutic potential.

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