. 2010 Sep;62(3):405–496. doi: 10.1124/pr.109.002451

TABLE 12.

IC₅₀ values in micromolar for noncompetitive AMPA and kainate receptor antagonists

Noncompetitive Antagonist	GluA1	GluA2	GluA3	GluA4	GluK1	GluK2	GluK3	GluK2/GluK5
	μM
GYKI 52466	18–117^a,b		34^c	22–66^a,b		>100^a		>100^a
GYKI 53405 (LY 293606)	24^a			28^a		>100^a		>100^a
GYKI 53773 (LY 300164)^d	21^e	18^e	19^e	18^e		>100^a
GYKI 53655 (LY 300168)	6^a			5^a	>100^a	198^f	63^f	>100^a
GYKI 53784 (LY 303070)^d	3^a			3^a	>100^a	>100^a		>100^a
CP-465,022	0.5^g		0.5^g	0.3^g		>100^g		>1^h
NS-3763					1.6ⁱ	>30ⁱ		N.E.^j

GYKI 52466, 1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine; GYKI 53405, 1-(4-aminophenyl)-3-acetyl-4-methyl-3,4-dihydro-7,8-methylenedioxy-5H-2,3-benzodiazepine; GYKI 53655, 1-(4-aminophenyl)-3-methylcarbamoyl-4-methyl-3,4-dihydro-7,8-methylenedioxy-5H-2,3 benzodiazepine; GYKI 53784, (−)-1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-4,5-dihydro-3-methylcarbamoyl-2,3-benzodiazepine.

Bleakman et al. (1996).

Johansen et al. (1995).

IC₅₀ value was determined from inhibition of Ca²⁺ influx activated by 30 μM glutamate at human GluA3 expressed in HEK69–8 cells (Varney et al., 1998).

This compound is the active enantiomer of the compound directly above it.

Cotton and Partin (2000).

Perrais et al. (2009).

Balannik et al. (2005).

Lazzaro et al. (2002).

ⁱ

Values are for inhibition of Ca²⁺ influx evoked by domoate (2 μM for GluK1 and 0.2 μM for GluK2) in HEK293 cells expressing recombinant human receptors (Christensen et al., 2004b).

Values are for inhibition of glutamate-evoked currents at HEK293 cells expressing recombinant receptors (Christensen et al., 2004b).