Figure 3
A selective P2X 7 antagonist shows similar activity on both WT and GOF variants. Effects of A-804598 on agonist induced responses were studied in the FLIPR assay for both activation modes (Yo-Pro-1 uptake and Ca2+ flux). Data were normalized to the amplitude of responses elicited by the 100 μM BzATP. Only the results obtained with A-804598 in the WT variant (black symbols) and the 155Tyr (A, B) and 348Thr (C, D) variants (red symbols) are shown. Due to the low responses obtained with 496Ala in the Yo-Pro-1 uptake only data for the Ca2+ flux could be generated (E). Averaged data for A-804598, as well as for the other two selective P2X7 antagonists used in this study, are presented in Table 2.