Figure 3.

Radioligand displacement assay of [³H]-Flunitrazepam by DCBS192 (a) and MTI163 (b). Membranes from rat cerebellum were incubated with 2 nM [³H]-flunitrazepam in the presence of various concentrations of the two ligands. Data shown are the mean ± SEM of three independent experiments performed in duplicates each. (c,d) Superposition of the flumazenil bound 6D6T (green) and the alprazolam bound 6HUO (yellow) in two different perspectives demonstrate that the structurally related molecules do not bind with aligned pharmacophore features at all. The heteroatoms of the molecules are depicted in different colors: blue-nitrogen, red-oxygen, green-chloro. (e) Structures of alprazolam and flumazenil.