Ki | |||||
---|---|---|---|---|---|
A1 | A2A | A2B | A3 | ||
nM | |||||
Nonselective agonists | |||||
1 | Adenosinea | ∼100 (h)b | 310 (h)b | 15,000 (h)b | 290 (h)b |
73 (r)b | 150 (r)b | 5100 (r)b | 6500 (r)b | ||
2 | 2-Chloro-adenosine | 6.7 (r)c | 76 (r)c | 24,000 (h)d | 1890 (r)e |
3 | NECA | 14 (h)b | 20 (h)b | 140 (h)b | 25 (h)b |
5.1 (r)f | 9.7 (r)f | 1890 (h)g | 113 (r)f | ||
1900 (m)f | |||||
A1-selective agonists | |||||
4 | R-PIA | 2.04 (h)h | 220 (r)c | 150,000 (h)d | 33 (h)u |
1.2 (r)c | 19,000 (m)j | 158 (r)e | |||
5 | GW493838 | N.D. | N.D. | N.D. | N.D. |
6 | CHA | 0.85 (r)c | 460 (r)c | 160,000 (h)d | 1025 (h)k |
176 (r)e | |||||
7 | CPA | 2.3 (h)l | 794 (h)l | 18,600 (h)l | 72 (h)l |
8 | CCPA | 0.83 (h)l | 2270 (h)l | 18,800 (h)l | 38 (h)l |
1.3 (r)m | 950 (r)m | 237 (r)m | |||
0.1 (rb)m | 37.7 (rb)m | ||||
9 | TCPA | 2.8 (h)n | 210 (h)n | >10,000 (h)n | 600 (h)n |
10 | 2′-Me-CCPA | 1.8 (c)o | 3900 (c)o | N.D. | 5000 (r)o |
11 | Selodenoson (DTI-0009) | N.D. | N.D. | N.D. | N.D. |
12 | GR79236 | 3.1 (r)l | 1300 (h)l | N.D. | N.D. |
13 | Tecadenoson | 6.5 (p)l | 2315 (h)l | N.D. | N.D. |
14 | GS9667 (CVT-3619) | 55 (h)p | >10,000 (h)p | >50,000 (h)p | >1000 (h)p |
15 | Capadenoson (BAY 68-4986) | N.D. | N.D. | N.D. | N.D. |
A2A-selective agonists | |||||
16 | CGS21680 | 289 (h)l | 27 (h)l | >10,000 (h)l | 67 (h)l |
1800 (r)m | 19 (r)m | >10,000 (r)m | 584 (r)m | ||
120 (rb)m | 673 (rb)m | ||||
17 | Apadenoson (ATL-146e) | 77 (h)l | 0.5 (h)l | N.D. | 45 (h)l |
18 | ATL-313 | N.D. | N.D. | N.D. | N.D. |
19 | UK-432097 | N.D. | 4 (h) | N.D. | N.D. |
20 | Sonedenoson (MRE-0094) | N.D. | N.D. | N.D. | N.D. |
21 | Binodenoson (WRC-0470) | 48,000 (h)l | 270 (h)l | 430,000 (h)l | 903 (h)l |
22 | Regadenoson (CV-3146) | >10,000 (h)l | 290 (h)l | >10,000 (h)l | >10,000 (h)l |
A2B-selective agonists | |||||
23 | A2B agonist | 1050 (h)q | 1550 (h)q | 82 (h)q | >5000 (h)q |
24 | BAY 60-6583 | >10,000 (h)a,r | >10,000 (h)a,r | 3–10 (h)r | >10,000 (h)a,r |
330 (m)s | |||||
750 (d)s | |||||
340 (rb)s | |||||
A3-selective agonist | |||||
25 | IB-MECA (CF101) | 51 (h)l | 2900 (h)l | 11,000 (h)l | 1.8 (h)l |
26 | Cl-IB-MECA | 220 (h)l | 5360 (h)l | >10,000 (h)m | 1.4 (h)l |
CF102 | 280 (r)m | 470 (r)m | >10,000 (m)m | 0.33 (r)m | |
35 (m)m | ∼10,000 (m)m | 0.18 (m)m | |||
27 | CP608,039 | 7300 (h)t | N.D. | N.D. | 5.8 (h)t |
1750 (rb)t | 83 (rb)t | ||||
28 | HEMADO | 330 (h)u | 1200 (h)u | >30,000 (h)u | 1.10 (h)u |
29 | 2-Phenylethynyl-adenosine derivative | 32,800 (h)v | 41,700 (h)v | >30,000 (h)v | 0.44 (h)v |
30 | MRS3558 (CF502) | 260 (h)l | 2330 (h)l | >10,000 (h)l | 0.29 (h)l |
105 (r)m | 1080 (r)m | 1.0 (r)m | |||
15.8 (m)m | 10,400 (m)m | 1.49 (m)m | |||
31 | MRS5151 | 14,900 (h)w | ∼10,000 (h)w | N.D. | 2.38 (h)w |
10,500 (m)w | >10,000 (m)w | 24.4 (m)w |
h, human; c, cow; d, dog; m, mouse; p, pig; r, rat; rb, rabbit; R-PIA, (R)-N6-phenylisopropyladenosine; N.D., no data available; CHA, N6-cyclohexyladenosine; CCPA, 2-chloro-N6-cyclopentyladenosine; TCPA, N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine; ATL-313, 4-{3-[6-amino-9-(5-cyclopropylcarbamoyl-3,4-dihydroxytetrahydrofuran-2-yl)-9H-purin-2-yl]prop-2-y nyl}piperidine-1-carboxylic acid methyl ester; CP608,039, (2S,3S,4R,5R)-3-amino-5-{6-[5-chloro-2-(3-methylisoxazol-5-ylmethoxy)benzylamino]purin-9-yl}-4-hydroxytetrahydrofuran-2-carboxylic acid methylamide; HEMADO, 2-(1-hexynyl)-N-methyladenosine; MRS3558, (1′S,2′R,3′S,4′R,5′S)-4′-{2-chloro-6-[(3-chlorophenylmethyl)amino]purin-9-yl}-1-(methylaminocarbonyl)bicyclo[3.10.0]hexane-2,3-diol; MRS5151, (1′S,2′R,3′S,4′R,5′S)-4′-[6-(3-chlorobenzylamino)-2-(5-hydroxycarbonyl-1-pentynyl)-9-yl]-2′,3′-dihydroxybicyclo[3.10.0]hexane-1′-carboxylic acid N-methylamide.
↵a Data are from functional studies.
↵d Bruns, 1980.
↵g Data from radioligand binding studies versus the antagonist radioligand [3H]PSB-603 (S. Hinz and C. E. Müller, unpublished data).
↵s Data from radioligand binding studies versus the antagonist radioligand [3H]MRS1754 (Auchampach et al., 2009).