Table 2.

Potency of α,β-methylene analogues of UDP and CDP at the human P2Y₆R and P2Y₁₄R.^a

Compound	hP2Y6R EC50 ± SEM (μM) or %	hP2Y14R IC50 ± SEM (μM)
14a	0.339b	0.011b
14bc	1.99b	0.00092b
16	0.203 ± 0.030	0.362 ± 0.090
17	0.097 ± 0.011	16.6 ± 10.3
20	1.45 ± 0.22	>100
23	1.32 ± 0.08	>100
25	0.571 ± 0.196	>100
28	0.549 ± 0.070	21.5 ± 11.1
30	1.39 ± 0.223	6.66 ± 4.74

^aFLIPR (Ca²⁺) assay in hP2Y₆R-1231N1 astrocytoma cells, expressed as EC₅₀ or % activation at 3 µM, unless noted. Fluorescent antagonist was used as a tracer for flow cytometry of hP2Y₁₄R-CHO cells, unless noted.

^bPotency in a phospholipase C assay of hP2Y₆R activation (Maruoka et al., 2010)⁴ or in a cAMP assay of hP2Y₁₄R activation (Das et al., 2010).⁹

^cStructure of 14b: