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Table 2 Positive allosteric modulation of 4-chloropropofol at GlyR/mutations

From: 4-Chloropropofol enhances chloride currents in human hyperekplexic and artificial mutated glycine receptors

4-chloropropofol positive allosteric modulation
  EC50± SEM nH± SEM N= potentiation [% of peak current amplitude] ± SEM
WT 0.08 ± 0.02 nM 2.0 ± 2.8 4 269 ± 88
R271Q 1.3 ± 0.6μM 0.9 ± 1.3 5 260 ± 52
R271L 0.1 ± 0.2μM 0.7 ± 0.3 6 153 ± 46
R271K 6.0 ± 2.3μM 0.3 ± 0.1 6 231 ± 174
S267I 55.1 ± 28.4μM 0.7 ± 0.3 4 128 ± 14
  1. EC50 values and Hill coefficients for receptor modulation by 4-chloropropofol derived from fits of the Hill equation to the normalized current response as well as values for maximal positive allosteric modulation at WT and mutated glycine receptors.