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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 3.

Adenosine receptor affinities of 8-cycloalkylxanthines

Ki (nM)a
A1 A2A A2B A3
64 8-Cyclopentyl-theophylline 24 (r)1
6.3 (r)3
26.1 (gp)3
6.4 (rb)3
2.9 (s)3
1.4 (c)3 		1,400 (r)1
3,170 (r)27 		710 (h)2
902 (h)27 		~100,000 (h)1
>10,000 (r)27
65 DPCPX (CPX) 3.0 (h)4
0.50 (r)4
1.0 (r)5
0.18 (r)3
1.06 (gp)3
3.9 (gp)6
0.21 (rb)3
0.10 (s)3
0.05 (c)3
0.29 (c)6
11.4 (d)7 		129 (h)8
60 (h)9
157 (r) 10
500 (r)5 		51 (h)4
63.8 (h)5
186 (r)5
200 (r)11
86.2 (m)12
145 (gp)11
96.0 (rb)12
147 (d)12
132 (d)11 		795 (h)13
243 (h)4
509 (h)7
3,960 (h)8
>10,000 (r)9
43,000 (r)7
708 (rb)7
115 (d)7
66 2-Thio-CPX 0.655 (r)14 314 (r)14 2800 (h)15 nd
67
KFM19 (rac.)
BIIP-20 (S-(−))		 Apaxifylline (S-(−)-configurated enantiomer) 10.5 (mk)16,b
3 (r)17 		1,512 (mk)16,b
2,640 (r)17 		nd nd
68
IRFI117		 Midaxifylline (8-(1-Aminocyclo-pentyl)-1,3-dipropylX 2618 54,60018 nd nd
69 KW3902 (NAX) Rolofylline 1,3-Dipropyl-8-(3-noradamantyl)X 0.72 (h)19
8.0 (h)20
0.19 (r)21
12.6 (r)19 		108 (h)19
673 (h)20
380 (r)21
510 (r)19 		296 (h)20 4,390 (h)20
70 1-Propyl-3-(S)-1-methylbenzyl-8-cyclopentylX 10.1 (r)9 3,500 (r)9 8,000 (h)9 85 (h)9
>10,000 (r)9
71 1-Propyl-3-(R)-1-methylbenzyl-8-cyclopentylX 23.8 (r)9 2,400 (r)9 2,960 (h)9 370 (h)9
72 1-Propyl-3-benzyl-8-cyclopentylX 24.3 (h)9
8.70 (r)9 		511 (r)9 8,000 (h)9 54.6 (h)9
73 1-Propyl-3-phenyl-8-cyclopentylX 7.1 (h)9
1.01 (r)9 		1,200 (h)9
492 (r)9 		625 (h)9 395 (h)9
74 PSB-16 1-Propyl-3-(3-hydroxypropyl)-8-cyclopentylX 5.74 (h)9
0.57 (r)9 		664 (r)9 194 (h)9 3,100 (h)9
75 1-Butyl-3-(3-hydroxypropyl)-8-cyclopentyl X 0.45 (r)9 582 (r)9 nd 1,190 (h)9
77 PSB-36 1-Butyl-3-(3-hydroxypropyl)-8- (3-noradamantyl)X 0.7 (h)9
0.124 (r)9 		980 (h)9
552 (r)9 		187 (h)9 2,300 (h)9
6,500 (r)9
78 49 (h)22
55 (r)22 		>10,000 (h)22
>10,000 (r)22 		nd 3,550 (h)22
79 29 (h)22
21 (r)22 		>10,000 (h)22
>10,000 (r)22 		nd >10,000 (h)22
80 BG-9719 (CVT-124) Naxifylline 0.45 (h)19
12 (h)21
0.67 (r)19 		1,100 (h)19
1,660 (h)21
1,250 (r)19 		611 (h)21
1,010 (m)12
470 (rb)12
742 (d)12 		4,810 (h)21
81 18 (h)21
3.0 (r)21 		657 (h)21
264 (r)21 		802 (h)21 >1,000 (h)21
82 BG-9928 Toponafylline 7.4 (h)20
3.9 (mk)23
1.3 (r)20
29 (d)23 		6,410 (h)20
943 (mk)23
2,440 (r)20
4307 (d)23 		90 (h)20 >10,000 (h)20
83 MPDX (1-Methyl analog of KF 15372) 4.2 (r)24 >100 (r)24 nd nd
84 KF 15372 0.99 (r) 25
3.0 (r)26
3.0 (gp)25 		430 (r) 25 nd nd
a

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

b

data for the racemate (KFM-19)