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Table 1 BzATP pharmacological parameters on the different P2X 7 SNPs studied

From: Gain and loss of function of P2X7 receptors: mechanisms, pharmacology and relevance to diabetic neuropathic pain

 

Yo-Pro-1 uptake

Ca 2+flux

WT

155Tyr

348Thr

496Ala

496Ala 155Tyr

WT

155Tyr

348Thr

496Ala

496Ala 155Tyr

EC50 (uM)

46.64 ± 5.32

56.65 ± 2.05

45.24 ± 0.54

34.56 ± 5.12

53.18 ± 5.28

67.48 ± 2.1

71.04 ± 4.6

58.22 ± 1.54

96.66 ± 5.88 (*)

89.23 ± 3.45 (**)

Hill slope

1.27 ± 0.10

1.72 ± 0.04

1.77 ± 0.24

1.2 ± 0.51

2.01 ± 0.47

2.77 ± 0.25

2.52 ± 0.17

2.67 ± 0.42

2.67 ± 0.28

2.73 ± 0.34

Efficacy (%)

100

177.68 ± 6.18 (*)

218.06 ± 19.49 (*)

23.56 ± 2.5 (*)

33.46 ± 5.78 (*)

100

125.83 ± 11.74 (*)

137.23 ± 16.06 (*)

46.2 ± 6.87 (*)

54.14 ± 3.6 (*)

n

13

3

4

3

3

15

3

3

6

3

  1. The EC50 and Hill slope values for the WT variant represent averages obtained from all data. The efficacy values are normalized to control experiments on the WT receptors evaluated at the same time. (*) = p < 0.001; (**) = p < 0.005.