Screening of putative GABA(A) receptor ligands specific for the alpha3beta2gamma2 subunit combination
Laufzeit: 01.01.2005 - 31.12.2006
Laufzeit: 01.01.2005 - 31.12.2006
19 elbion compounds have been tested together with diazepam as control for their binding to the benzodiazepine site of recombinant alpha3beta2gamma2S GABA(A) receptors at concentrations of 100 nM and 1 µM. At a concentration of 1 µM, five compounds (E034-00117, E034-00138, E034-00139, E034 00141, E034-00163) inhibited the binding of the ligand [3H]Ro15-4513 with more than 50%. E034-00138 was the most potent inhibitor of this group as indicated by 46% inhibition at a concentration of 100 nM.