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. 2019 May 22;4(5):8846–8851. doi: 10.1021/acsomega.9b00434

Table 1. Obtained PAM EC50 Values for 1 and DS2 at Selected GABAA Receptor Subtypesa.

  EC50 (μM) (pEC50 0ESEM, n)
EC20 (μM)
  1b DS2b GABA GABA
α1β2δ 3.68 (5.43 ± 0.055, 4) 2.97 (5.53 ± 0.13, 3) 6.71 (5.17 ± 0.087, 4) 1.6–2.0
α4β2δ 2.91 (5.54 ± 0.069, 3) 1.41 (5.85 ± 0.085, 3) 0.25 (6.61 ± 0.030, 3) 0.08
α6β2δ 2.25 (5.65 ± 0.0038, 3) 2.02 (5.69 ± 0.10, 3) 0.21 (6.68 ± 0.13, 3) 0.05
α6β2γ2s no modulation (n = 3) no modulation (n = 3) 0.50 (6.30 ± 0.091, 3) 0.1–0.2
a

GABA agonist EC50 values are given for reference and GABA EC20 used for PAM testing is also given. No modulation means no activity at 10 μM.

b

Tested as PAMs in the presence of the stated GABA EC20.