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

BMC Neurology

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

4-chloropropofol	positive allosteric modulation
	EC₅₀± SEM	n_H± 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

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.

ISSN: 1471-2377