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. Author manuscript; available in PMC: 2014 Jan 7.
Published in final edited form as: Handb Exp Pharmacol. 2011;(200):10.1007/978-3-642-13443-2_6. doi: 10.1007/978-3-642-13443-2_6

Table 2.

Adenosine receptor affinities of 8-phenyl- and 8-phenylalkyl-substituted xanthines and heteroaromatically substituted derivatives

Ki (nM)a
A1 A2A A2B A3
First-generation 8-phenylxanthine derivatives
23 8-PhenylX 2,500 (r)1 21,000 (r)1 810 (h)2 nd
24 8-Phenyl-theophylline (8-PT) 1,340 (h)3
115 (h)4
86 (r)5
76 (r)6
1,540 (gp)6
7.6 (c)6 		454 (h)3
850 (r)5 		415 (h)7
436 (m)8
249 (rb)8
371 (d)8 		1,250 (h)3
>100,000 (r)9
25 1,3-Diethyl-8-phenylX (DPX) 44 (r)10 860 (r)10
190 (h)11 		62.0 (h)7 nd
26 1,3-Dipropyl-8-phenylX 10 (r)6
0.22 (c)6
20.9 (gp)6 		180 (r)12
2100 (h)13 		18.9 (h)7 nd
27 SPT 1,000 (h)3
4,500 (r)5
1,000 (r)6
10,100 (gp)6
6,460 (d)14
300 (c)6 		7,050 (h)3
14,000 (r)5 		1,330 (h)7
1,590 (r)15
4,990 (m)8
2,190 (gp)15
2,370 (rb)8
7,240 (d)8
224 (d)15 		5,890 (h)16
11,000 (h)17
≫10,000 (r)16
25,300 (d)14
28 DPSPX 210 (r)5
140 (r)9 		1,400 (r)5
790 (r)9 		568 (m)8
200 (rb)8
721 (d)8 		183 (s)18
>100,000 (r)9
22,500 (rb)19
29 12 (r)20 83 (r)20 nd nd
30 XAC 6.8 (h)21
29.1 (h)22
1.2 (r)23
0.49 (r)19
5.49 (gp)19
0.45 (rb)19
0.09 (s)19
0.03 (c)19
159 (d)14 		18 (h)21
1.00 (h)22
63 (r)23 		7.8 (h)23
16.0 (h)7
42.7 (r)15
4.51 (m)8
17.8 (gp)15
4.47 (rb)8
29.8 (d)8
3.55 (d)15 		91.9 (h)22
26 (h)21
71 (h)14
29,000 (r)14
106 (rb)14
180 (s)18,24
138 (d)14
31 PD113,297 5.59 (r)12 70.0 (r)12 nd nd
32 PD115,199 14 (r)25
4.05 (r)20 		16 (r)25
3.86 (rb)26 		160 (m)27 nd
33 NPC-205 3.5 (r)28 48 (h)28 50 (gp)29 nd
34 I-ABOPX (BW-A522) 70 (h)45
37 (r)30
601 (d)14 		95 (h)45
700 (r)30 		30 (h)45 18 (h)24
1,170 (r)31
1,500 (r)14
179 (rb)14
37.5 (d)14
35 BWA1433 20 (r)30
132 (d)14 		nd 15.6 (h)45 54 (h)24
15,000 (r)14
384 (rb)14
1,880 (d)14
36 XCC 175 (h)21
58 (r)23 		2200 (h)21
595 (h)21 		13.6 (h)23
40 (h)7
2,200 (r)23 		3,910 (h)21
75,700 (r)21
A2B-selective 8-phenylxanthine derivatives and heteroaromatically substituted derivatives
37 MRS1754 403 (h)21
16.8 (r)21 		503 (h)21
612 (r)21 		1.97 (h)21
12.8 (r)21
16.6 (r)15
3.39 (m)8
9.12 (gp)15
1.79 (rb)8
12.8 (d)8
12.3 (d)15 		570 (h)21
38 MRS1706 157 (h)21
38 (r)21 		112 (h)21
548 (r)21 		1.4 (h)21 230 (h)21
39 MRS1765 152 (h)21
15.7 (r)21 		293 (h)21
1640 (r)21 		2.13 (h)21 1270 (h)21
40 CVT-5440 >10,000 (h)32 >10,000 (h)32 50 (h)32 >10,000 (h)32
41 MRS1595 3,030 (h)21
11.1 (r) 21 		1,970 (h) 21
126 (r) 21 		26.6 (h) 21 670 (h) 21
42 100 (r)33 97.7 (h)33 2.88 (h)33 1,290 (h)33
43 PSB-1115 >10,000 (h) 2
2,200 (r)1 		24,000 (r)1 53.4 (h) 2 >10,000 (h) 2
44 PSB-50 60 (r)2 199 (r)2 6.8 (h) 2 477 (h) 2
45 PSB-53 1,181 (h)2
481 (r)2 		ca. 10,000 (h)2
3,800 (r)2 		24 (h) 2 4,622 (h) 2
46 PSB-55 122 (h)2
37 (r) 2 		ca. 10,000 (r) 2
550 (r) 2 		1.3 (h) 2 475 (h) 2
47 PSB-298 68 (h)2
35 (r) 2 		2,139 (r) 2 1.2 (h) 2
60 (h)34 		422 (h) 2
48 3.6 (r)35 74 (r)35 5.4 (h)35 ≥10,000 (h)35
49 PSB-601 2,067 (h)36
260 (r)36 		484 (h)36
93.7 (r)36 		3.6 (h)36 >1,000 (h)36
50 PSB-09120 >10,000 (h)37
>1,000 (r) 37 		22.7 (h) 37
122 (r) 37 		0.157 (h) 37 >10,000 (h) 37
51 PSB-0788 2,240 (h)37
386 (r) 37 		333 (h) 37
1,730 (r) 37 		0.393 (h) 37 >1,000 (h) 37
52 PSB-603 >10,000 (h)37
>10,000 (r) 37 		>10,000 (h) 37
>10,000 (r) 37 		0.553 (h) 37
KD 0.403 (h) 37
KD 0.351 (m) 37 		>10,000 (h) 37
53 CVT-6694 >6,000 (h)38 >5,000 (h)38 7 (h)38 >9,000 (h)38
54 CVT-7124 >6,000 (h)38 >5,000 (h)38 6 (h)38 >9,000 (h)38
55 CVT-6883 1,940 (h)39 3,280 (h)39 22 (h) 39 1,070 (h) 39
56 MRE-2029-F20 200 (h)40 >1,000 (h) 40 5.5 (h) 40 >1,000 (h) 40
57 ATL 802 369 (h)41
9,583 (m)41 		654 (h)41
8,393 (m)41 		2.36 (h)41
8.58 (m)41 		>1,000 (h)41
>10,000 (m)41
58 ATL 852 nd nd 28.5 (h)c nd
8-Phenylalkyl-substituted xanthines
59 MDL 102,503 6.9 (r)42 157 (r)42 nd nd
60 60.7 (r)42 848 (r)42 nd nd
61 MDL 102,234 23.2 (r)42 3,510 (r)42 nd nd
62 L-97-1 580 (h)43 >100,000 (h)43 >100,000 (h)43 nd
63 102 (r)44 83.2 (h)44 7.41 (h)44 10,000 (h)44
a

h = human; c = cow; d = dog; gp = guinea pig; m= mouse; r = rat; rb = rabbit; a few A2B data are from functional (cAMP) studies; nd = no data available;

c

personal communication (J. Linden), also see 41