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XB-ART-12594
Neurosci Lett 1999 Jul 09;2692:63-6. doi: 10.1016/s0304-3940(99)00431-0.
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EDPC: a novel high affinity ligand for the benzodiazepine site on rat GABA(A) receptors.

Thomet U , Furtmüller R , Sieghart W , Le Hyaric-Almeida M , Rousseau JF , Dodd RH , Venault P , Chapouthier G , Sigel E .


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Rat recombinant alpha1beta2gamma2 gamma-aminobutyric acid type A (GABAA) receptors were functionally expressed in Xenopus laevis oocytes and analyzed for the action of EDPC (Ethyl 3-(1,3-dithian-2-yl)-1H-pyrrolo[2,3-c]pyridine-5-carboxylate) using electrophysiological techniques. EDPC inhibited GABA currents at low concentrations (IC50 approximately/= 2 nM). The inhibition by 100 nM EDPC could be reversed by 1 microM of the benzodiazepine antagonistflumazenil (Ro 15-1788), indicating a negative allosteric modulation via the benzodiazepine binding site. In line with this conclusion are radioactive ligand binding studies. EDPC inhibited the binding of 2 nM [3H]flunitrazepam to membranes from the cerebellum or the cortex with IC50 values of about 8 and 25 nM, respectively.

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Species referenced: Xenopus laevis
Genes referenced: gabarap