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- Title
An updated unified pharmacophore model of the benzodiazepine binding site on gamma-aminobutyric acid(a) receptors: correlation with comparative models.
- Authors
Clayton, T; Chen, J L; Ernst, M; Richter, L; Cromer, B A; Morton, C J; Ng, H; Kaczorowski, C C; Helmstetter, F J; Furtmüller, R; Ecker, G; Parker, M W; Sieghart, W; Cook, J M
- Abstract
A successful unified pharmacophore/receptor model which has guided the synthesis of subtype selective compounds is reviewed in light of recent developments both in ligand synthesis and structural studies of the binding site itself. The evaluation of experimental data in combination with a comparative model of the alpha1beta2gamma2 GABA(A) receptor leads to an orientation of the pharmacophore model within the Bz BS. Results not only are important for the rational design of selective ligands, but also for the identification and evaluation of possible roles which specific residues may have within the benzodiazepine binding pocket.
- Publication
Current medicinal chemistry, 2007, Vol 14, Issue 26, p2755
- ISSN
0929-8673
- Publication type
Journal Article
- DOI
10.2174/092986707782360097