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