| Assay Method Information | |
| | Electrophysical Characterization Assay |
| Description: | Human embryonic kidney (HEK) 293 cells (ATCC CRL 1573) and/or Xenopus laevis oocytes were used for expressing the human a1-3 glycine receptor subunit as well as human a1, b3, g2 GABA receptor subunit cDNAs inserted into mammalian expression vectors. Patch- and voltage-clamp recording from receptor expressing cells was performed at a holding potential of −70 mV in normal Ringer solution and digitized for analyses. Dose-response curves of agonist induced peak currents (I) were normalized to the maximal current value obtained and fitted with the sigmoidal Hill equation using a Gauss Marquardt iteration, where EC50 represents the glycine/GABA concentration resulting in a half maximal response. Effects of the compounds tested on agonist induced currents were analysed after superfusing the cells with the respective compound for 5 seconds prior to and during agonist application and dose-response curves of modulated currents were determined in the presence of agonist concentrations eliciting a response corresponding to 20% of the maximal inducible current (EC20 value). |
| Affinity data for this assay | |
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