Table 2.

In vitro pharmacological data for the synthesized analogs of compound 2a at the hP2Y₁R in binding, determined as in Table 1, and in the antagonism increase of intracellular calcium ion concentration induced by 30 nM 2-MeSADP in 1321N1 astrocytoma cells expressing the hP2Y₁R.

Compound No.	R	Binding Ki, µM	% inhibition in Ca2+ assay at 10 µM
2a (F3099-0019)		13 ± 3	36.8 ± 2.2a
15 a		NE	< 5
15b		27 ± 10	17.6 ± 1
15c		≥ 100	21.7 ± 3.5
15d		42 ± 15	31.3 ± 2.5
15e		NE	11.3 ± 2.3
15f		≥ 100	10.2 ± 2.6
15g		45 ± 8	32.7 ± 3.7
15h		NE	9.1 ± 0.4
15i		NE	9.4 ± 0.2b

^aIC₅₀ in the IP Assay: 0.14 ± 0.04 µM;

^bIC₅₀ in the IP Assay: 0.13 ± 0.01 µM; NE – less than 10% inhibition at 20 µM.