Ki | |||||
---|---|---|---|---|---|
A1 | A2A | A2B | A3 | ||
nM | |||||
Nonselective antagonists | |||||
32 | Caffeine | 10,700 (h)a | 23,400 (h)b | 33,800 (h)c | 13,300 (h)a |
44,900 (h)b | 9560 (h)a | 10,400 (h)d | >100,000 (r)e | ||
41,000 (r)f | 45,000 (r)g | 20,500 (h)h | |||
44,000 (r)g | 32,500 (r)u | 30,000 (r)j | |||
47,000 (gp)k | 48,000 (r)a | 13,000 (m)j | |||
44,000 (c)k | |||||
33 | Theophylline | 6770 (h)l | 1710 (h)l | 9070 (h)d | 22,300 (h)a |
14,000 (r)m | 6700 (h)a | 74,000 (h)h 15,100 (r)d | 86,400 (h)l | ||
8740 (r)a | 22,000 (r)m | 5630 (m)n | >100,000 (r)e | ||
7060 (gp)o | 25,300 (r)a | 11,000 (gp)p | 85,000 (r)q | ||
4710 (rb)o | 17,700 (rb)n | >100,000 (d)r | |||
9050 (s)o | 38,700 (d)n | ||||
6330 (c)o | |||||
34 | CGS15943 | 3.5 (h)s | 1.2 (h)s | 32.4 (h)n | 35 (h)s |
6.4 (r)s | 9.07 (m)n | ||||
A1-selective antagonists | |||||
35 | DPCPX (CPX) | 3.0 (h)t | 129 (h)l | 51 (h)t | 795 (h)u |
0.50 (r)t | 60 (h)t | 63.8 (h)d | 243 (h)t | ||
1.0 (r)d | 157 (r)u | 186 (r)d | 509 (h)r | ||
0.18 (r)o | 500 (r)d | 200 (r)p | 3960 (h)l | ||
1.06 (gp)o | 86.2 (m)n | >10,000 (r)t | |||
3.9 (gp)k | 145 (gp)p | 43,000 (r)r | |||
0.21 (rb)o | 96.0 (rb)n | 708 (rb)r | |||
0.10 (s)o | 147 (d)n | 115 (d)c | |||
0.05 (c)o | 132 (d)p | ||||
0.29 (c)k | |||||
11.4 (d)r | |||||
36 | CPFPX | 1.26 (h)v | 940 (h)v | ndb | N.D. |
0.63 (r)v | 812 (r)v | ||||
1.37(p)v | |||||
0.18 (c)v | |||||
37 | Rolofylline (KW-3902, NAX) | 0.72 (h)w | 108 (h)w | 296 (h)x | 4390 (h)x |
8.0 (h)x | 673 (h)x | ||||
0.19 (r)y | 380 (r)y | ||||
12.6 (r)w | 510 (r)w | ||||
38 | PSB-36 | 0.7 (h)t | 980 (h)t | 187 (h)t | 2300 (h)t |
0.124 (r)t | 552 (r)t | 6500 (r)t | |||
39 | Toponafylline (BG-9928) | 7.4 (h)x | 6410 (h)x | 90 (h)x | >10,000 (h)x |
3.9 (mk)z | 943 (mk)z | ||||
1.3 (r)x | 2440 (r)x | ||||
29 (d)z | 4307 (d)z | ||||
40 | FK-453 | 18 (h)aa | 1300 (h)aa | 980 (h)aa | >10,000 (h)aa |
41 | SLV320 | 1.00 (h)bb | 398 (h)bb | 3981 (h)bb | 200 (h)bb |
2.51 (r)bb | 501 (r)bb | ||||
42 | LUF5981 | 0.90 (h)cc | 194 (h)cc | >300 (h)cc | 637 (h)cc |
A2A-selective antagonists | |||||
43 | Istradefylline (KW6002) | 841 (h)dd | 12 (h)ee | >10,000 (h)dd | 4470 (h)dd |
230 (r)dd | 91.2 (h)dd | ||||
2.2 (r)ff | |||||
4.46 (r)gg | |||||
44 | CSC (Ki MAO-B = 80.6 nM)gg | 28,000 (r)hh | 54 (r)hh | 8200ii | >10,000 (r)e |
45 | MSX-2 | 900 (r)jj | 8.04 (r)u,jj | >10,000 (h)jj | >10,000 (h)jj |
2500 (h)jj | 5.38 (h)jj,kk | 2900 (h)ll | |||
14.5 (h)jj,mm | |||||
46 | SYN-115 | N.D. | N.D. | N.D. | N.D. |
47 | BIIB014 (V2006) | 68 (h)nn | 1.3 (h)nn | 63 (h)nn | 1005 (h)nn |
48 | ZM-241385 | 774 (h)aa | 1.6 (h)aa | 75 (h)aa | 743 (h)aa |
49 | ST-1535 | 71.8 (h)oo | 6.6 (h)oo | 352.3 (h)oo | >1000 (h)oo |
50 | SCH-58261 | 725 (h)aa | 5.0 (h)aa | 1110 (h)aa | 1200 (h)aa |
51 | Preladenant (SCH-420814) | >1000 (h)pp | 0.9 (h)pp | >1000 (h)pp | >1000 (h)pp |
52 | SCH-442416 | 1110 (h)aa | 4.1 (h)qq | >10,000 (h)aa | >10,000 (h)aa |
A2B-selective antagonists | |||||
53 | MRS1754 | 403 (h)rr | 503 (h)rr | 1.97 (h)rr | 570 (h)rr |
16.8 (r)rr | 612 (r)rr | 12.8 (r)rr | |||
16.6 (r)p | |||||
3.39 (m)n | |||||
9.12 (gp)p | |||||
1.79 (rb)n | |||||
12.8 (d)n | |||||
12.3 (d)p | |||||
nM | |||||
54 | MRE-2029-F20 | 200 (h)ss | >1000 (h)ss | 5.5 (h)ss | >1000 (h)ss |
55 | PSB-603 | >10,000 (h)tt | >10,000 (h)tt | 0.553 (h)tt | >10,000 (h)tt |
>10,000 (r)tt | >10,000 (r)tt | KD 0.403 (h)tt | |||
KD 0.351 (m)tt | |||||
56 | CVT-6883 | 1940 (h)uu | 3280 (h)uu | 22 (h)uu | 1070 (h)uu |
57 | PSB-1115 | >10,000 (h)u | 24,000 (r)m | 53.4 (h)u | >10,000 (h)u |
2200 (r)m | |||||
58 | ATL 802 | 369 (h)rr | 654 (h)rr | 2.36 (h)rr | >1000 (h)rr |
9583 (m)rr | 8393 (m)rr | 8.58 (m)rr | >10,000 (m)rr | ||
59 | LAS38096 | 2821 (h)vv | >1000 (h)vv | 17 (h)vv | 1043 (h)vv |
A3-selective antagonists | |||||
60 | KF26777 | 1800 (h)ww | 470 (h)ww | 620 (h)ww | 0.20 (h)ww |
61 | PSB-10 | 1700 (h)xx | 2700 (h)xx | N.D. | 0.441 (h)yy |
805 (r)yy | 6040 (r)yy | ||||
62 | PSB-11 | 1640 (h)xx | 1280 (h)xx | 2100 (m)yy | 2.34 (h)xx |
440 (r)xx | 2100 (r)xx | KD 4.9 (h)zz | |||
63 | MRE-3008-F20 | 1200 (h)aa | 141 (h)aa | 2100 (h)aa | 0.82 (h)aa |
64 | MRS1523 | >10,000 (h)aaa | 3660 (h)aaa | >10,000 (h)aaa | 18.9 (h)aa |
15,600 (r)aaa | 2050 (r)aaa | >10,000 (m)aaa | 113 (r)aaa | ||
731 (m)aaa | |||||
65 | MRS1191 | >10,000 (h)aaa | >10,000 (h)aaa | >10,000 (h)aaa | 31.4 (h)aaa |
40,100 (r)aaa | >10,000 (r)aaa | 1850 (r)aaa | |||
66 | VUF-5574 | ≤10,000 (r)bbb | ≤10,000 (r)bbb | N.D. | 4.03 (h)bbb |
h, human; c, cow; d, dog; gp, guinea pig; m, mouse; r, rat; rb, rabbit; N.D., no data available; LUF5981, 8-cyclohexyl-2,6-diphenyl-1-deazapurine; CSC, 8-(3-chlorostyryl)caffeine; KF26777, 2-(4-bromophenyl)-4-ethyl-4,5,7,8-tetrahydro-1H-imidazo[2.1-i]purin-5-one.
↵dd Müller et al., unpublished data.
↵kk Recombinant receptors (expressed in CHO cells).
↵mm Native receptors (post mortem brain).
↵aaa Liang et al., 2010.