TABLE 1

Structures of adenosine receptor antagonists and affinities at adenosine receptor subtypesEmbedded Image

No.
Compound
Ki (nM) (Species)a
A2B
 A1
 A2A
 A3
1 Caffeine 13,000 (m)d1 41,000 (r)2 43,000 (r)2 >100,000 (r)3
10,400 (h)4 44,900 (h)c 23,400 (h)c 13,300 (h)5
2 DMPX 2500 (m)d1 45,000 (r)6 16,000 (r)6 >10,000 (h)c
4130 (h)4
3 Enprofylline 4730 (h)4 32,000 (r)7 135,000 (r)7 158,000 (h)8
4 8-SPT 2200 (r)9 3200 (r)9 57,000 (r)9 >100,000 (r)9
5890 (h)5
5 8-SPC »10,000 (h)c >100,000 (r)10 57,000 (r)10 »10,000 (h)c
6 DPCPX 186 (r)4 1.0 (r)4 500 (r)4 >10,000 (r)3
63.8 (h)4 795 (h)11
7 PSB-36c 187 (h) 0.12 (r) 552 (r) 6500 (r)
2300 (h)
8ab MSX-212 >10,000 (h) 900 (r) 8 (r) >10,000 (h)
9 PSB-10 30,000 (h)c 805 (r)13 6040 (r)13 0.441 (h)13
10 PSB-1115 53 (h)11 2200 (r)11 24,000 (r)11 >10,000 (h)c
11 PSB-5311 24 (h) 481 (r) 3800 (r) 4622 (h)
12 PSB-5011 6.8 (h) 60 (r) 199 (r) 477 (h)
13
PSB-5511
1.3 (h)
37 (r)
550 (r)
475 (h)

  • ↵ a r = rat; m = mouse; h = human

  • ↵ b MSX-3 (8a) is a water-soluble phosphate prodrug of MSX-2 (8b)

  • ↵ c Results from our laboratory

  • ↵ d Data obtained from adenylate cyclase assays at NIH 3T3 intact cells

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