Table 3.

Agonist binding affinities determined in saturation and competition experiments and basal cAMP production in COS-7 cells that express WT and mutant human A₃ ARs (n = 3-4).

	[125I]AB-MECA (Kd. nM)	Cl-IB-MECA (Ki binding, nM)	Basal cAMP (pmol/ml)
WT	1.2 ± 0.2	3.8 ± 0.6	256 ± 32
N30A	9.8 ± 2.3	137 ± 46	232 ± 28
C88F	8.3 ± 2.1	53.6 ± 7.8	240 ± 44
D107N	0.55 ± 0.13	1.3 ± 0.4	248 ± 34
D107K	0.90 ± 0.24	2.1 ± 0.5	220 ± 30
D107R	0.86 ± 0.11	1.8 ± 0.3	216 ± 52
R108K	0.95 ± 0.08	4.1 ± 1.0	149 ± 42*
R108A	0.70 ± 0.12	0.9 ± 0.1	101 ± 22*
R108N	0.68 ± 0.07	2.4 ± 0.4	238 ± 50
R108E	0.86 ± 0.09	5.4 ± 0.8	232 ± 58
R108H	0.85 ± 0.14	3.7 ± 1.1	252 ± 39
Y109F	2.0 ± 0.21	17 ± 4.6	236 ± 48
D107K/R108K	a		224 ± 43
D107K/R108E	a		242 ± 32
A229E	0.64 ± 0.08	2.7 ± 0.4	69 ± 12*
Y282F	9.3 ± 2.7	33.6 ± 4.7	250 ± 48

^aspecific binding of radioligand at 1 nM <20% of WT.

^*basal value significantly lower than WT (p < 0.05).