. 2018 Jun;365(3):583–601. doi: 10.1124/jpet.117.246660

TABLE 1.

Comparative efficacy of GX and AP for allosteric and direct-gating effect at GABA-A receptors in DGGCs

Compound	GABA-Gated Whole-Cell Current		Tonic Current
	Allosteric Effect: EF_{(2-fold GABA)}^a	Direct Effect: E₃₀ pA	Tonic Current
	Allosteric Effect: EF_{(2-fold GABA)}^a	Direct Effect: E₃₀ pA	E₁ pA	EF_{(2-fold GABA)}^a
	nM	_μ_M^b	_μ_M^c	nM
AP	474	273.5	100.6	80
GX	389	336.1	64.0	290
GABA^d	—	1426.3	19.6	—

^{^a}

EF values represent the effective functional concentration of drug (nanomolars) required to double the 3 μM GABA (EC₁₀) response.

^{^b}

E₃₀ _μ_M values represent the mean tonic current responses of drug at 30 μM concentration.

^{^c}

E₁ _μ_M values represent the mean tonic current responses of drug at 1 μM concentration co-applied with 1 μM GABA. GABA 1 μM tonic current response: 0.66 ± 0.22 pA/pF, 19.6 pA.

^{^d}

GABA median effective concentration (EC₅₀): 18.6 μM. EC₅₀ values represent the concentration required to produce half of its own maximal effect.