Table 1. Chemical Structures and Pharmacological Profile of Quinoxaline-2,3-dione Analogues 1.1−1.3^a.

	AMPA	KA	NMDA	GluK1		GluK2		GluK3	GluK2/5
cmpd	func.b	func.b	func.b	bind.c	func.d	bind.e	func.d	bind.c	bind.c	func.d
1.1 (DNQX)	0.25f	0.53f	4.1f	−h	−h	0.35	−h	−h	−h	−h
1.2 (CNQX)	0.40f	0.27f	13f	−h	8.0	0.53	18	−h	−h	72
1.3 (NBQX)	0.063g	0.078g	>300g	12	25	0.87	21	24	0.6	87

^aData for KA receptor subunits were obtained in the presence of ConA. All values in [μM].

^bK_i values for inhibition of currents activated by kainate (100 μM), AMPA (30 μM), or NMDA (30 μM/glycine (3 μM)) in Xenopus oocytes injected with mRNA from rat cortex.

^cK_i values for displacement of [³H]KA radioligand at human KA receptors expressed in HEK293 cells; from ref (56).

^dIC₅₀ values for inhibition of 100 μM glutamate-induced Ca²⁺ influx in HEK293 cells expressing human KA receptors; from ref (50).

^eK_i values for displacement of [³H]KA radioligand at homomeric receptors in BHK cells; from ref (51).

^fFrom ref (57).

^gFrom ref (58).

^hNot tested.