TABLE 1

Homologous competition displacement studies yielding K_D values (nanomolar) for [³H]NECA and [³H]ZM241385 binding to wild-type human A_2AAR and single point mutants D52A^2.50, S91A^3.39, W246A^6.48, N280A^7.45, and N284A^7.49, transiently expressed on HEK293 cell membranes

Values are means ± S.E.M. of at least three separate assays performed in duplicate.

	[³H]NECA		[³H]ZM241385
	K_D	Change^a	K_D	Change^a
	nM		nM
Wild type	81 ± 5	1.0	4.6 ± 0.5	1.0
D52A^2.50	77 ± 8	1.0	3.5 ± 0.5	0.75
S91A^3.39	258 ± 24***	3.2	7.0 ± 0.2	1.5
W246A^6.48	1942 ± 124***	24	23.2 ± 4.3***	5.0
N280A^7.45	752 ± 147***	9.3	8.4 ± 1.3*	1.8
N284A^7.49	237 ± 27***	2.9	7.0 ± 0.7	1.5

↵^a Change in fold over wild type.
Significantly different from wild type with *P < 0.05 or ***P < 0.001 [one-way analysis of variance with Dunnett’s posttest performed on corresponding pK_D values].