Table 2. Functional properties of clobazam, N-desmethylclobazam, and clonazepam at the human α₁β₂γ_2S, α₂β₂γ_2S, α₃β₂γ_2S, α₅β₂γ_2S, α₆β₂δ and α₆β₂GABA_ARs expressed in Xenopus oocytes.

Receptor	EC50 [pEC50 ± S.E.M.]	Imax ± S.E.M. (%)	N
Clobazam
α1β2γ2S	132 [6.88 ± 0.05]	256 ± 12	5
α2β2γ2S	138 [6.86 ± 0.04]	261 ± 6.7	6
α3β2γ2S	240 [6.62 ± 0.10]	269 ± 0.8	4
α5β2γ2S	174 [6.76 ± 0.03]	216 ± 7.0	6
α6β2δ	55,000 [4.26 ± 0.04]	528 ± 46	6
N-desmethylclobazam
α1β2γ2S	151 [6.82 ± 0.07]	203 ± 8.5	6
α2β2γ2S	138 [6.86 ± 0.18]	270 ± 20	6
α3β2γ2S	282 [6.55 ± 0.11]	270 ± 27	5
α5β2γ2S	98 (123 and 79) b	233 (248 and 217) b	2
α6β2δ	∼300,000 [∼3.5] a	2420 ± 210 a	5
α6β2	∼300,000 [∼3.5] a	2350 ± 200 a	4
Clonazepam
α1β2γ2S	15 [7.81 ± 0.12]	209 ± 14	4
α2β2γ2S	7.4 [8.13 ± 0.04]	253 ± 17	5
α3β2γ2S	16 (20 and 13) b	316 (334 and 297) b	2
α5β2γ2S	21 [7.68 ± 0.17]	255 ± 25	5
α6β2δ	29,000 [4.53 ± 0.10]	283 ± 38	5

^a The concentration-response curves for N-desmethylclobazam at the α₆β₂δ and α₆β₂GABA_ARs were not saturated at the maximal concentration used (1 mM). Thus, for this receptors the EC₅₀ and pEC₅₀ values for N-desmethylclobazam are estimated from the data, and the currents evoked by 1 mM N-desmethylclobazam (in % of the GABA EC₂₀ response) is given instead of I_max.

^b The properties for N-desmethylclobazam at α₅β₂γ_2S and for clonazepam at α₃β₂γ_2S are based on two independent experiments (n = 2), and thus the mean EC₅₀ and I_max values for the modulators are given with specific EC₅₀ and I_max values determined in the two experiments in parantheses.