Two neighboring residues of loop A of the a1 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 a1b2c2 GABAA receptor containing a key residue for the interaction of benzodiazepines: a1H101. We describe a direct interaction of a1N102 with a diazepamand an imidazobenzodiazepine-derivative. Our observations help to better understand the conformation of this region of the benzodiazepine pocket in GABAA receptor. 2007 Federation of European Biochemical Societies. Published by Elsevier B.V. All rights reserved.

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