Table 1. BzR Affinity for Compounds 14–16^a.

			Ki (nM) or % inhibition (10 μM)b,c
cpd	R1	X	bovine brain membranes	α1β2γ2	α2β2γ2	α5β3γ2
14c	H	H	120 ± 11	346 ± 29	39% ± 3	46% ± 5
15d	NO2	H	117 ± 12	65 ± 5	32% ± 3	44% ± 4
16e	NO2	CH3	88 ± 6	31.3 ± 2	0%	0%
diazepam			10 ± 1
flumazenil			0.90 ± 0.05
clonazepam			0.85 ± 0.02

^aK_i (nM) or % inhibition (10 μM) data of indol-3-ylglyoxylylamide derivatives 14–16.

^bK_i represents the means ± SEM of three determinations performed in triplicate.

^cInhibition percentages of specific [³H]-flumazenil binding at 10 μM represent the means ± SEM of three determinations performed in triplicate.

^dData are from Da Settimo et al.⁵⁰

^eData are from Primofiore et al.⁵²