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Table 2 Effects of selective P2X 7 antagonists at GOF and LOF P2X 7 variants

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

 

Yo-Pro-1 uptake (IC 50, nM)

Ca 2+flux (IC 50, nM)

WT

155Tyr

348Thr

496Ala

WT

155Tyr

348Thr

496Ala

A-804598

21.77 ± 2.8

21.50 ± 5.8

15.5 ± 0.6

ND

20.81 ± 7.6

19.36 ± 6.9

40.7 ± 14.2

25.57 ± 1.6

A740003

332.83 ± 12.3

449.2 ± 12.7

415.9 ± 98.2

ND

507.87 ± 91.1

379.43 ± 135.1

720.75 ± 27.9

405.50 ± 81.7

AZ11645373

198.2 ± 42

342.6 ± 48.3

218.75 ± 113.5

ND

296.3 ± 98.5

510 ± 39.9

806.75 ± 249.3

412.40 ± 1.7

  1. IC50 values reported here represent the averages ± SEM of 3 separate experiments. For simplicity Hill slope were not included in the table. Data for Yo-Pro-1 uptake assay for 496Ala variant could not be determined (ND) due to the low amplitude of responses obtained with this variant.
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Molecular Pain

ISSN: 1744-8069

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