Table 2 IC50 values for PhTX-12 inhibition of nAChR subunit combinations.

From: Block of nicotinic acetylcholine receptors by philanthotoxins is strongly dependent on their subunit composition

 

VH (mV)

n

PhTX-12 IC50 (95% CI), μM

Peak

Late

α4β2

−60

8

3.87

(1.47–10.16)

0.23

(0.14–0.38)

−80

9

2.17

(1.30–3.64)

0.28

(0.17–0.45)

−100

11

1.64

(0.74–3.67)

0.044

(0.030–0.064)

α4β2(V253F)

−60

4

2.22

(1.44–3.42)

0.41

(0.28–0.60)

−80

5

4.05

(2.22–7.36)

0.3

(0.25–0.35)

−100

9

3.48

(1.40–8.70)

0.19

(0.13–0.27)

α4β4

−60

9

1.21

(0.70–2.07)

0.25

(0.16–0.40)

−80

12

1.65

(0.96–2.83)

0.29

(0.21–0.40)

−100

9

2.77

(1.30–5.92)

0.19

(0.14–0.27)

α3β4

−60

7

3.09

(2.13–4.47)

0.11

(0.08–0.14)

−80

8

2.62

(1.71–4.01)

0.11

(0.08–0.15)

−100

8

2.03

(1.22–3.36)

0.027

(0.022–0.033)

α3β4(F255V)

−60

5

1.63

(0.74–3.60)

0.52

(0.30–0.90)

−80

5

2.78

(1.13–6.84)

0.36

(0.26–0.50)

−100

5

1.05

(0.54–2.05)

0.068

(0.044–0.105)

α3β2

−60

9

65.2

(36.0–118.0)

3.20

(2.39–4.28)

−80

12

60.6

(21.4–172)

2.57

(2.16–3.06)

−100

10

74.4

(21.3–259.3)

1.38

(1.05–1.82)

α7

−60

12

18.7

(14.9–23.4)

8.32†

(6.55–10.58)

−80

12

11.1

(7.2–17.1)

4.92†

(2.79–8.66)

−100

10

12.1

(9.04–16.2)

5.02†

(3.01–8.40)

α1β1γδ

−60

9

3.16

(2.11–4.74)

0.070

(0.056–0.092)

−80

11

6.18

(4.03–9.46)

0.10

(0.08–0.13)

−100

8

5.02

(2.86–8.83)

0.071

(0.055–0.093)

  1. IC50 values for PhTX-12 inhibition of both peak and late current estimated from concentration-inhibition curves in Figs 2 and 4.
  2. †For α7 this is based on the area under the current trace as there was no stable late current.
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