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Table 1 Affinity constants indicated as IC50 in nM (and the corresponding pIC50) for the compounds used in the present study

From: Characterization of the trigeminovascular actions of several adenosine A2A receptor antagonists in an in vivo rat model of migraine

Compound

A2A

A1

Fold selectivity

   

Selectivity A2A vs. A1

CGS2168033

22 nM (7.6)

3100 nM (5.5)

141

Caffeine28

8100 nM (5.1)

20,000 nM (4.7)

2.5

JNJ-39928122a

7.9 nM λ (8.1)

55.1 nM λ (7.3)

7

JNJ-40529749a

4.9 nM (8.3)

89.1 nM (7.1)

18

JNJ-41942914a

8.3 nM (8.1)

1093 nM (6.0)

132

JNJ-40064440a

8.2 nM (8.1)

1240 nM (5.9)

151

JNJ-41501798a

11.5 nM (7.9)

7997 nM (5.1)

695

  1. The JNJ antagonists were developed by Johnson & Johnson Pharmaceutical Research & Development, L.L.C
  2. Hutchison et al. 1989 [33]; Fredholm et al. 1999 [28]; a, Paul Jackson (Janssen Research & Development, personal communication); λ, Indicates Ki values