EDPC: a novel high affinity ligand for the benzodiazepine site on rat GABAA receptors
| Autor: | Patrice Venault, Jean-François Rousseau, Robert H. Dodd, Erwin Sigel, Georges Chapouthier, Roman Furtmüller, Werner Sieghart, Mireille Le Hyaric-Almeida, Urs Thomet |
|---|---|
| Rok vydání: | 1999 |
| Předmět: |
Flumazenil
Male Pyridines medicine.drug_class Allosteric regulation In Vitro Techniques Ligands Mice Radioligand Assay Xenopus laevis chemistry.chemical_compound Prosencephalon Allosteric Regulation Seizures Cerebellum DMCM medicine Animals GABA Modulators Receptor Benzodiazepine Binding Sites GABAA receptor General Neuroscience Receptors GABA-A Ligand (biochemistry) Recombinant Proteins Rats chemistry Biochemistry Oocytes Biophysics Flunitrazepam medicine.drug |
| Zdroj: | Neuroscience Letters. 269:63-66 |
| ISSN: | 0304-3940 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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