Two neighboring residues of loop A of the α1 subunit point towards the benzodiazepine binding site of GABAA receptors

Benzodiazepines are widely used drugs exerting sedative, anxiolytic, muscle relaxant, and anticonvulsant effects by acting through specific high affinity binding sites on some GABAA receptors. It is important to understand how these ligands are positioned in this binding site. We are especially interested here in the conformation of loop A of the α1β2γ2 GABAA receptor containing a key residue for the interaction of benzodiazepines: α1H101. We describe a direct interaction of α1N102 with a diazepam- and an imidazobenzodiazepine-derivative. Our observations help to better understand the conformation of this region of the benzodiazepine pocket in GABAA receptor.