TABLE 1. Binding characteristics of wild-type and mutant human A2A-adenosine receptors using the antagonist radioligand [3H]XAC.
Construct |
|||||
---|---|---|---|---|---|
Compound | Wild-type | T88A | T88S | 188R | |
Bmax (pmol/mg) | [3H]XAC | 14.9 ± 1.2 | 6.54 ± 1.61b | 6.26 ± 070b | 5.54 ± 0.47b |
Kd (nM) | [3H]XAC | 8.83 ± 1.46 | 10.8 ± 18d | 5.76 ± l.82d | 4.21 ± 1.17c |
Ki (nM) | Agonists | ||||
CADO | 118 ± 22 | 16,400 ± 3,200c | 776 ± 313c | 9,140 ± 2,590c | |
DPMA | 65.5 ± 0.3 | 5,710 ± 2,520c | 655 ± 134c | 4,090 ± 760c | |
NECA | 19.1 ± 1.7 | 1,590 ± 280c | 778 ± 224c | 2,660 ± 1,390c | |
CGS 21680 | 26.7 ± 6.5 | 22,100 ± 2,900b | 422 ± 180c | 4,620 ± 620b | |
Antagonists | |||||
CGS 15943 | 1.20 ± 0.30 | 7.98 ± 1.71c | 6.28 ± 1.68c | 5.00 ± 052b | |
ZM 241385 | 0.758 ± 0.135 | 3.47 ± 2.41d | 1.16 ± 0.20d | 2.00 ± 0.71d |
p <0.001.
p <0.01.
p <0.05.
Not significant.