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EJNMMI Research

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

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