TABLE 8.
Binding affinity of agonists and antagonists at rat adenosine receptor subtypes (Ki values with 95% confidence intervals or ±S.E.M. in parentheses)
A1 | A2A | A3 | Reference | |
---|---|---|---|---|
Agonists with unmodified ribose | ||||
R-PIA | 1.2 (±0.16) | 124 (±9) | —a | |
1.3 (1.1–1.6) | 730 (690–770) | —b | ||
0.51 | —c | |||
220 (±43) | —d | |||
160 (±52) | —e | |||
S-PIA | 49 (±2.4) | 1,800 (±380) | —a | |
29 | —f | |||
920 (±310) | —e | |||
CPA | 0.59 (±0.02) | 460 (±15) | —a | |
0.8 (0.6–1.0) | 2,000 (1,400–2,900) | —b | ||
240 (±36) | —e | |||
CCPA | 0.4 (0.2–0.7) | 3,900 (2,500–4,700) | —b | |
0.23 | —c | |||
240 (±71) | —e | |||
ADAC | 0.85 (±0.35) | —w | ||
2-Cl-adenosine | 9.3 (±0.58) | 63 (±7.5) | —a | |
1,900 (±900) | —e | |||
DPMA | 140 (±23) | 4.4 (±0.2) | —u | |
3,600 (±1,700) | —e | |||
(S)-ENBA | 0.3 (±0.02) | 1,400 (±150) | —v | |
Agonists with 5_-modified ribose | ||||
NECA | 6.3 (±0.52) | 10 (±0.5) | —a | |
11 (7.0–17) | 22 (20–25) | —f | ||
3.7 | —c | |||
260 (±36) | —d | |||
CGS 21680 | 3100 (±470) | 22 (±4.3) | —g | |
580 (±32) | —e | |||
HENECA | 136 (95–195) | 3.8 (1.5–9.9) | —f | |
PENECA | 698 (611–798) | 120 (112–128) | —h | |
PHPNECA | 2.5 (2.2–2.9) | 0.9 (0.7–1.3) | —i | |
AB-MECA | 430 (±45) | 1,600 (±180) | 14 (±3) | —j |
IB-MECA | 54 (±5) | 56 (±8) | 1.1 (±0.3) | —j |
IAB-MECA | 18 (±5) | 200 (±84) | 1.3 (±0.18) | —j |
Cl-IB-MECA | 820 (±570) | 470 (±370) | 0.33 (±0.08) | —k |
Antagonists: xanthines | ||||
DPCPX | 0.3 | 340 | —l | |
0.18* (0.16–0.20) | —l | |||
>10,000 | —e | |||
XAC | 2.8 (1.9–4.2) | —m | ||
3.5 | 24 | —l | ||
4 | 50 | —n | ||
>100,000 | —o | |||
MRS1754 | 17 (±3.6) | 610 (±290) | —o | |
MSX-2 | 900 (±10) | 8 (±3) | —p | |
Theophylline | 11,000 | 32,000 | —b | |
>100,000 | —o | |||
Antagonists: non-xanthines | ||||
CGS 15943 | 21 (±3.5) | 3.3 (±1.8) | —q | |
22 | 3 | —n | ||
6.4 (6.2–6.6) | 1.2 (1.1–1.3) | —r | ||
>100,000 | —o | |||
SCH 58261 | 120 (100–140) | 2.3 (2.0–2.7) | —r | |
ZM 241385 | 2,000 (1,500–2,700) | 0.30 (0.10–0.95) | 150,000 (87,000–210,000) | —s |
MRE 3008F20 | >10,000 | 2,000 (±220) | >10,000 | —t |
Data from saturation experiments; where confidence limits are missing, they are within 0.15 log units.
Bruns et al., 1986; brain membranes (A1), striatum (A2A); radioligands [3H]CHA (A1), [3H]NECA (A2A).
Lohse et al., 1988; brain membranes (A1), striatum (A2A); radioligands [3H]PIA (A1), [3H]NECA (A2A).
Klotz et al., 1991; brain membranes; radioligand [3H]DPCPX.
Olah et al., 1994; transfected CHO cells; radioligand 125I-AB-MECA.
van Galen et al., 1994; transfected CHO cells; radioligand 125I-APNEA.
Cristalli et al., 1992; brain membranes (A1), striatum (A2A); radioligands [3H]DPCPX (A1), [3H]NECA (A2A).
Hutchison et al., 1989; rat brain; radioligands [3H]CHA (A1), [3H]NECA (A2A). Given are IC50 values; based on the experimental conditions Ki values should be about 0.5– 0.7 and 0.9 times the IC50 values for A1 and A2A, respectively.
Cristalli et al., 1995; brain membranes (A1), striatum (A2A); radioligands [3H]CHA (A1), [3H]CGS 21680 (A2A).
Camaioni et al., 1997; brain membranes (A1), striatum (A2A); radioligands [3H]CHA (A1), [3H]CGS 21680 (A2A).
Gallo-Rodriguez et al., 1994; rat brain (A1), rat striatum (A2A), transfected CHO cells (A3); radioligand [3H]PIA (A1), [3H]CGS 21680 (A2A), 125I-AB-MECA (A3).
Kim et al., 1994; rat brain (A1), rat striatum (A2A), transfected CHO cells (A3); radioligand [3H]PIA (A1), [3H]CGS 21680 (A2A), 125I-AB-MECA (A3).
Lohse et al., 1987; brain membranes (A1), striatum (A2A); radioligands [3H]PIA (A1), [3H]NECA (A2A).
Jacobson et al., 1986; rat brain, radioligand [3H]XAC.
Jarvis et al., 1989; rat brain; radioligands [3H]CHA (A1), [3H]CGS 21680 (A2A).
Kim et al., 2000; transfected HEK 293 cells (A1), rat striatum (A2A); radioligands [3H]PIA (A1), [3H]CGS 21680 (A2A).
Sauer et al., 2000; brain cortex (A1), striatum (A2A); radioligand [3H]CHA (A1), [3H]CGS 21680 (A2A).
Williams et al., 1987; brain (A1), striatum (A2A); radioligands [3H]CHA (A1), [3H]NECA (A2A). Given are IC50 values; based on the experimental conditions Ki values should be about 0.5– 0.7 and 0.9 times the IC50 values for A1 and A2A, respectively.
Baraldi et al., 1994; rat brain (A1), rat striatum (A2A); radioligand [3H]CHA (A1), [3H]CGS 21680 (A2A).
Poucher et al., 1995; brain cortex (A1), PC 12 cells (A2A), transfected CHO cells (A3); radioligands [3H]PIA (A1), [3H]NECA (A2A) 125I-AB-MECA (A3). Given are IC50 values; based on the experimental conditions Ki values should be about 0.1, 0.2, and 0.5 times the IC50 values for A1, A2A, and A3, respectively.
Varani et al., 2000; brain cortex (A1), striatum (A2A), transfected CHO cells (A3); radioligands [3H]DPCPX (A1), [3H]SCH 58261 (A2A), 125I-AB-MECA (A3).
Bridges et al., 1988; brain (A1), striatum (A2A); radioligand [3H]CHA (A1), [3H]NECA (A2A); DPMA or PD 125944 is compound 16 in this paper.
Trivedi et al., 1989; brain (A1), striatum (A2A); radioligand [3H]CHA (A1), [3H]NECA (A2A).
Jacobson et al., 1987; brain (A1), radioligand [3H]PIA (A1).