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. Author manuscript; available in PMC: 2013 Oct 10.
Published in final edited form as: J Med Chem. 2011 May 6;54(11):3926–3934. doi: 10.1021/jm2002487

Table 2.

Modulation of Rat α1β2γ2L GABAA Receptor Function by Steroids 1, 2 and Structural Analogues.

Compound oocyte electrophysiologya
0.1 µM 1 µM 10 µM (gating) 10 µM
1b 2.91 ± 0.57 4.70 ± 1.11 19.64 ± 4.04 0.11 ± 0.02
2b 0.94 ± 0.04 0.97 ± 0.05 1.87 ± 0.14 0.08 ± 0.07
3b 1.12 ± 0.03 4.59 ± 0.42 21.14 ± 2.14 0.14 ± 0.03
4b 1.49 ± 0.44 4.07 ± 1.09 23.75 ± 3.61 0.21 ± 0.04
5a 0.77 ± 0.06 1.57 ± 0.15 10.78 ± 0.64 0.02 ± 0.01
5b 0.87 ± 0.02 1.44 ± 0.02 8.22 ± 0.14 0.04 ± 0.01
5c 0.91 ± 0.03 1.13 ± 0.08 4.67 ± 0.14 0.01 ± 0.01
6a 1.17 ± 0.04 5.06 ± 0.6 21.51 ± 7.07 0.17 ± 0.00
6b 0.79 ± 0.05 0.77 ± 0.04 1.82 ± 0.21 0.02 ± 0.01
6c 0.90 ± 0.05 1.52 ± 0.24 5.02 ± 0.62 0.04 ± 0.01
6d 0.90 ± 0.01 0.86 ± 0.04 1.53 ± 0.02 0.05 ± 0.02
a

The GABA concentration used for the control response was 2 µM. Each compound was evaluated on at least four different oocytes at the concentrations indicated, and the results reported are the ratio of currents measured in the presence/absence of added compound. Gating represents direct current gated by 10 µM compound in the absence of GABA, and this current is reported as the ratio of compound only current/2 µM GABA current. Error limits are calculated as standard error of the mean (N ≥ 4). Methods were as reported previously. 25

b

These values are from the literature.21