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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 5.

Adenosine receptor affinitities of deazaxanthines and azaxanthines

Ki (nM)a
A1 A2A A2B A3
Deazaxanthines
109 9-Deaza-theophylline 5,400 (r)1 12,000 (r)1 nd nd
110 9-Deazacaffeine 32,000 (r)1 72,000 (r)1 nd nd
111 7-Deaza-theophylline 43,000 (r)1 >250,000 (r)1 nd nd
112 1,3-Dimethyl-8-phenyl-9-deazaX 47 (r)1 510 (r)1 nd nd
113 1,3-Dipropyl-8-phenyl-9-daX 13 (r)1 450 (r)1 nd nd
114 1-Methyl-8-phenyl-9-deazaX 97 (r)1 2000 (r)1 520 (h)2 2098 (h)2
115 1-Propyl-8-phenyl-9-daX 45 (h)2
39 (r)1 		>10,000 (h)2
1,200 (r)1 		42 (h)2 380 (h)2
116 1,3-Dimethyl-8-phenyl-7-deazaX 3,1001 12,0001 nd nd
117 14.8 (h)3 64.6 (h)3 3.02 (h)3 >1,000 (h)3
118 >1,000 (h)4 10,000 (h)4 11.0 (h)4 >1,000 (h)4
119 89.1 (h)4 324 (h)4 2.04 (h)4 2,240 (h)4
120 676 (h)4 3,550 (h)4 5.26 (h)4 >1,000 (h)4
121 183 (h)5 nd 1 (h)5 12,260 (h)5
122 Tricyclic 9-DeazaX 346 (h)6 164 (h)6 nd 3.82 (h)6
8-Azaxanthines
123 1,3-Dimethyl-8-cyclopentyl-8-azaX 110,000 (c)7 58,000 (c)7 nd nd
124 1,3-Dipropyl-8-cyclopentyl-8-azaX 1,300 (c)7 13,000 (c)7 nd nd
125 1,3-Dimethyl-7-cyclopentyl-8-azaX 11,000 (c)7 292,000 (c)7 nd nd
126 1,3-Dipropyl-7-cyclopentyl-8-azaX 340 (c)7 10,000 (c)7 nd nd
a

h = human; c = cow; r = rat; a few A2B data may be from functional (cAMP) studies; nd = no data available