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. Author manuscript; available in PMC: 2020 Apr 6.
Published in final edited form as: Neuropharmacology. 2016 Mar 5;107:160–167. doi: 10.1016/j.neuropharm.2016.03.010

Table 1.

Overview of the affinity and the biophysical properties of different chimeras. Vact 1/2 are the midpoint potentials and k the slope factors of the GV curves, respectively. ΔV1/23.1 are the shifts in the voltage dependence of channel activation compared to WT Kv3.1 (ΔV1/23.1=Vact 1/2 of channel - Vact 1/2 of Kv3.1). IC50 is the concentration that induces 50% current inhibition and IC50/IC503.1 the fold difference in gambierol affinity of the channel compared to WT Kv3.1.

Channel IC50 (nM) Vact 1/2 (mV) k (mV) IC50/IC503.1 ΔV1/23.1(mV)
Kv3.1 1.2 ± 0.2 23.5 ± 1.0 5.6 ± 0.3 - -
Kv2.1 >10,000 12.2 ± 1.4 9.5 ± 0.6 >10,000 −11
Kv3.1_EMcoupling_2.1 2.4 ± 0.2 1.1 ±1.5 5.9 ± 0.2 2.0 −23
Kv3.1_S1-S4_2.1 280 ± 40 34.8 ± 3.0 9.1 ± 0.4 233 12
Kv3.1_S1-S3a_2.1 1.9 ± 0.2 44.3 ± 2.4 9.1 ± 0.9 1.6 21
Kv3.1 S3b-S4 2.1 143 ± 28 52.0 ± 0.8 9.4 ± 1.1 119 28
Kv2.1 V404T 504 ± 28 28.7 ± 1.5 16.7 ± 1.5 420 5
Kv2.1 V404T_S3b-S4_3.1 900 ± 41 115.6 ± 9.1 31.5 ± 7.0 750 92