Table 1. IC50 values for PhTX-343 inhibition of nAChR subunit combinations.
VH (mV) | n | PhTX-343 IC50 (95% CI), μM | ||||
---|---|---|---|---|---|---|
Peak | Late | |||||
α4β2 | −60 | 7 | 1.90 | (1.01–3.60) | 0.46 | (0.28–0.75) |
−80 | 7 | 0.93 | (0.41–2.09) | 0.31 | (0.18–0.54) | |
−100 | 7 | 0.14 | (0.09–0.22) | 0.08 | (0.049–0.132) | |
α4β2(V253F) | −60 | 14 | 0.62 | (0.30–1.28) | 0.063 | (0.045–0.089) |
−80 | 10 | 0.75 | (0.46–1.23) | 0.12 | (0.06–0.23) | |
−100 | 8 | 0.11 | (0.07–0.17) | 0.014 | (0.011–0.016) | |
α4β4 | −60 | 9 | 0.97 | (0.60–1.58) | 0.17 | (0.12–0.24) |
−80 | 9 | 0.35 | (0.24–0.50) | 0.065 | (0.047–0.089) | |
−100 | 6 | 0.29 | (0.18–0.46) | 0.027 | (0.020–0.036) | |
α3β4 | −60 | 7 | 0.29 | (0.21–0.40) | 0.088 | (0.065–0.120) |
−80 | 8 | 0.080 | (0.062–0.104) | 0.012 | (0.010–0.014) | |
−100 | 9 | 0.077 | (0.059–0.102) | 0.0077 | (0.0063–0.0093) | |
α3β4(F255V) | −60 | 7 | 0.31 | (0.23–0.42) | 0.074 | (0.060–0.091) |
−80 | 9 | 0.038 | (0.029–0.048) | 0.012 | (0.010–0.014) | |
−100 | 8 | 0.017 | (0.011–0.024) | 0.005 | (0.0036–0.0068) | |
α3β2 | −60 | 7 | 64.5 | (7.8–532) | 1.59 | (1.20–2.11) |
−80 | 12 | 9.26 | (5.90–14.6) | 1.37 | (1.12–1.69) | |
−100 | 8 | 3.59 | (1.58–8.19) | 0.37 | (0.29–0.48) | |
α7 | −60 | 6 | 6.71 | (5.39–8.35) | 6.56† | (5.30–8.12) |
−80 | 7 | 6.48 | (5.12–8.21) | 5.06† | (3.95–6.48) | |
−100 | 9 | 8.80 | (6.92–11.18) | 6.77† | (5.44–8.42) | |
α1β1γδ | −60 | 8 | 27.1 | (19.1–38.4) | 18.0 | (12.8–25.4) |
−80 | 8 | 15.1 | (9.5–24.0) | 11.9 | (9.2–15.4) | |
−100 | 9 | 3.26 | (2.54–4.17) | 2.44 | (1.50–3.97) |