Compounds | Ki, nmol/l (pKi ± S.E.M.) | |||||||
---|---|---|---|---|---|---|---|---|
Pig Striatum (A2A) | PC12 cells (A2A) | HEK-hA2AAdoR | CHO-hA1AdoR | |||||
Affinity | n | Affinity | n | Affinity | n | Affinity | n | |
NECA | N.D. | 297 (6.54 ± 0.06) | 4 | 360 (6.45 ± 0.06) | 3 | 328 (6.49 ± 0.06) | 3 | |
R-PIA | 1106 (5.96 ± 0.06) | 4 | 3476 (5.48 ± 0.10) | 3 | 1656 (5.78 ± 0.02) | 3 | 477 (6.45 ± 0.11) | 3 |
CGS21680 | 157 (6.85 ± 0.23) | 5 | 210 (6.74 ± 0.09) | 3 | 609 (6.22 ± 0.06) | 3 | 3540 (5.47 ± 0.20) | 3 |
CVT-2995 | 14.4 (7.86 ± 0.12) | 4 | 53 (7.28 ± 0.05) | 4 | 305 (6.52 ± 0.04) | 6 | 866 (6.07 ± 0.05) | 3 |
WRC0470 | 20.7 (7.68 ± 0.04) | 3 | 18 (7.77 ± 0.04) | 8 | 272 (6.55 ± 0.04) | 6 | 7278 (5.16 ± 0.09) | 3 |
CVT-3032 | 1594 (5.80 ± 0.10) | 3 | 5516 (5.26 ± 0.05) | 3 | 13651 (4.87 ± 0.02) | 3 | 6350 (5.22 ± 0.11) | 3 |
CVT-3033 | 1417 (5.67 ± 0.16) | 3 | 3623 (5.45 ± 0.03) | 5 | 2895 (5.54 ± 0.03) | 3 | 5836 (5.24 ± 0.04) | 3 |
CVT-3146 | 1095 (5.95 ± 0.11) | 5 | 1734 (5.76 ± 0.01) | 3 | 1269 (5.90 ± 0.03) | 7 | >16460 (4.59 ± 0.35) | 3 |
YT-146 | 16.3 (7.86 ± 0.33) | 4 | N.D. | N.D. | N.D. | |||
CVT-3003 | 1007 (6.00 ± 0.07) | 3 | N.D. | N.D. | N.D. | |||
CVT-3006 | 64 (7.24 ± 0.26) | 3 | N.D. | N.D. | N.D. | |||
CVT-3100 | 697 (6.16 ± 0.06) | 5 | N.D. | N.D. | N.D. | |||
CVT-3101 | 94 (7.03 ± 0.06) | 3 | N.D. | N.D. | N.D. | |||
CVT-3126 | 1667 (5.78 ± 0.09) | 3 | N.D. | N.D. | N.D. | |||
CVT-3127 | 64 (7.22 ± 0.17) | 3 | N.D. | N.D. | N.D. | |||
CVT-3141 | 1138 (5.95 ± 0.07) | 3 | N.D. | N.D. | N.D. | |||
CVT-3144 | 502 (6.31 ± 0.12) | 3 | N.D. | N.D. | N.D. | |||
HENECA | 7.96 (8.10 ± 0.08) | 10 | N.D. | N.D. | N.D. |
The binding affinities of adenosine receptor agonists for A2AAdoRs and A1AdoRs were determined by their effect to compete with specific binding of [3H]ZM241385 or [3H]CPX, respectively, to membranes from the indicated tissue/cells. Values are means ± S.E.M. of results of at least three experiments (n) performed in triplicate. Numbers in parentheses are means of pKi ± S.E.M. Values of the equilibrium dissociation constant (Kd) for [3H]ZM241385 binding that were used in calculations ofKi values were 0.5, 0.5, and 0.8 nM for pig striatum, PC12, and HEK-hA2AAdoR cells, respectively. AKd value of 1 nM for [3H]CPX binding to CHO-hA1AdoR membrane was used in calculation ofKi values.
N.D., not determined.