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Table 6 EFB and A-740003 calcium influx inhibition of P2X7 receptor subtypes

From: Design, synthesis and evaluation in an LPS rodent model of neuroinflammation of a novel 18F-labelled PET tracer targeting P2X7

P2X7 isoform Cell line [BzATP] (μM) pIC50 Lit. pIC50 K i (nM) pKi
Human P2X7-HEK293 100 5.74 n/a 2.88 8.54
Rat P2X7-HEK293 100 5.14 n/a 36.1 7.44
Mouse P2X7-B16 200 5.22 n/a 547 6.26
Human P2X7-HEK293 100 7.18 7.36 [32] 0.10 9.98
Rat P2X7-HEK293 100 5.76 7.75 [32] 8.67 8.06
Mouse P2X7-B16 200 5.97 6.57 [34] 97.20 7.01