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Screening of putative GABA(A) receptor ligands specific for the alpha3beta2gamma2 subunit combination

Laufzeit: 01.01.2005 - 31.12.2006

Kurzfassung


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.

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