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. Author manuscript; available in PMC: 2016 Apr 29.
Published in final edited form as: Drug Dev Res. 2001 Oct 18;53(4):281–291. doi: 10.1002/ddr.1197

TABLE 2.

Antagonist Activity at Group 1 P2X Receptors

Compound rP2X1
rP2X3
IC50 (nM) CI (nM) nH IC50 (nM) CI (nM) nH
PPADS 68.5 45.9 – 102.2 −1.87 213.6 173.0 – 263.7 −1.17
isoPPADS 34.5 25.3 – 47.1 −1.48 78.8 57.4 – 108.0 −1.46
MRS 2143 32.4 26.5 – 40.4 −0.97 345.3 240.6 – 495.4 −0.88
MRS 2159 9.4 6.6 – 13.4 1.08 117.7 93.4 – 148.3 −1.02
MRS 2191 8.9 5.9 – 13.6 −0.84 228.6 171.0 – 305.5 −1.01
MRS 2257 5.1 3.6 – 7.3 −1.02 21.8 13.8 – 34.5 −1.13
MRS 2273 11.3 7.5 – 17.1 −0.86 32.9 25.8 – 41.9 −1.15
MRS 2284 7.1 6.0 – 8.4 −1.98 139.0 114.1 – 169.3 −1.33
MRS 2285 21.9 17.4 – 27.5 −1.9 259.8 222.3 – 303.8 −1.34
Ip5I 3.13 2.09 – 4.69 −0.94 2059.0 1252.0 – 3388.0 −1.43
TNP-ATP 1.01 0.69 – 1.47 −0.78 0.34 0.25 – 0.46 −0.82

Each compound was tested against ATP-responses (rP2X1, 1 μM; rP2X3, 3 μM). Antagonist activity is expressed as mean IC50 value (nM, for four determinations) with confidence intervals for the mean at the 95% level (CI, nM). The mean Hill coefficient (nH) is also given for each set of inhibition curves.