Table 1: Summary of effects of the hexacyclododecylamine derivatives and related compounds on affinity for sigma-1 receptors and voltage gated calcium channel modulation.

Number Structure σ1R Affinity   % Ca2+ Flux Inhibition
  KCl [100 µM]
Ki (µM) IC50 (µM)
Amantadine 7.44 [46] 15.24 3%
NGP1-01 0.869 [33] 1.78 52%**
IC50 = 86 uM
1 0.752 [33] 1.54 89%***
IC50 = 51 uM
2 0.103 [33] 0.211 > 95%***
IC50 = 35 uM
3 0.020 [33] 0.041 > 95%***
IC50 = 8 uM
8 1.132 2.34 nd
12 0.067 0.139 51%**
IC50 = < 100 µM
18 0.132 0.273 26%
21 0.349 0.723 nd
22 0.251 0.518 nd
24 0.215 0.445 97%***
IC50 = 9.28 μM
25 11.855 24.5 25%
27 0.469 0.971 79%***
IC50 = 9.80 μM
Nimodipine - nd nd > 95%***
IC50 = 0.008 μM

aData taken from reference [46]. bData taken from reference [33]. Statistical analysis was performed on raw data, with asterisks indicating significant inhibitory effect [(*) p < 0.05, (**) p < 0.01, (***) p < 0.001] relative to the control. n.d. = not determined.