Table 5.
Concentration–response data for different sugar-modified agonists
AgonistEC50 (µM)nHImax agonist/Imax ATP (%)n
ATP 32 ± 4 1.4 ± 0.1 n/a 15 
LNA-ATP 27 ± 1 1.8 ± 0.1 66 ± 1 
C2′-F-dATP 52 ± 6** 2.1 ± 0.1*** 60 ± 2 
Ara-ATP >100 ND ND 
C3′-dATP 83 ± 4**** 2.6 ± 0.1**** 67 ± 2 
C2′-dATP >300 ND ND 
C2′-C3′-ddATP ND ND ND ND 
AgonistEC50 (µM)nHImax agonist/Imax ATP (%)n
ATP 32 ± 4 1.4 ± 0.1 n/a 15 
LNA-ATP 27 ± 1 1.8 ± 0.1 66 ± 1 
C2′-F-dATP 52 ± 6** 2.1 ± 0.1*** 60 ± 2 
Ara-ATP >100 ND ND 
C3′-dATP 83 ± 4**** 2.6 ± 0.1**** 67 ± 2 
C2′-dATP >300 ND ND 
C2′-C3′-ddATP ND ND ND ND 

Concentration–response data (EC50) and Hill coefficient (nH) for ATP and a range of sugar-modified nucleoside triphosphate analogues (shown as mean ± SEM). Relative efficacy expressed as maximal current compared to that elicited by 1 mM of ATP and number of experiments (n) and are also shown (n/a: not applicable; ND, not determined). Significant differences were determined by one-way ANOVA with Dunnett’s test. **, P < 0.01; ***, P = 0.0001; ****, P < 0.0001.

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