Table 1

Affinity and selectivity of MRE 3008F20 to adenosine receptor subtypes

Species[3H]DPCPX A1[3H]SCH 58261 A2A[3H]DPCPX A2B[125I]AB-MECA A3[3H]MRE 3008F20 A3A1/A3A2A/A3A2B/A3
Human1100 ± 100140  ± 152100 ± 3000.29 ± 0.030.85 ± 0.0212941652471
Rat>100001993  ± 224NT1-a >10000ND

Human A2B receptors were expressed in HEK-293 cells; all other human receptors and rat A3 receptors were expressed in CHO cells. Rat A1 and A2A receptors were characterized in cortical and striatal membranes, respectively. Kivalues (nM) are shown and represent the mean ± S.E. of three independent determinations performed in duplicate. The radioligand used is stated along with the receptor subtype. The selectivity values versus A3 receptors were calculated with respect to theKi value obtained using [3H]MRE 3008F20 as radioligand.

  • 1-a NT, not tested; ND, not determinable.