TABLE 1

Parameters [log IC50 (molar) and extent of inhibition (ExIn; percentage of control specific binding) ± S.E.M.] for EBDN or Bgt competition toward specific [3H]EBDN or I-Bgt binding to α7-nAChR

Radioligand binding competition assays were conducted as described under Materials and Methods and in the legends to Figs. 9 and 10. Results were fit to the logistic equation with Hill coefficients set to -1 to determine log IC50 values and maximum or minimum levels of binding relative to control specific binding. Maximum binding was within one standard error of 100% for all samples, and minimum binding was within one standard error of 0% for samples unless the extent of inhibition (ExIn) is shown (ExIn for EBDN versus I-Bgt binding for SH-EP1-Toff-hα7 cells is >73% because a full dose-response was not conducted).

Preparation
EBDN vs. 10 nM I-Bgt
Bgt vs. 10 nM I-Bgt log IC50a
EBDN vs. 1 nM [3H]EBDN log IC50a
Bgt vs. 1 nM [3H]EBDN
Bgt vs. 10 nM [3H]EBDN ExIn
log IC50
 ExIn
log IC50
 ExIn
SH-EP1-pCEP4-hα7 -7.87 ± 0.07 80 ± 3* -7.45 ± 0.07 -8.50 ± 0.08 -7.34 ± 0.07 81 ± 3* ND
SH-EP1-Toff-hα7 -7.87 ± 0.12 >73 ± 6* ND ND -7.33 ± 0.07 83 ± 3* ND
SH-SY5Y-pCEP4-hα7 -7.66 ± 0.04 100 ± 2 -7.67 ± 0.14 -8.16 ± 0.04 -8.03 ± 0.20 56 ± 4* ND
SH-SY5Y-pCEP4-rα7 -7.44 ± 0.06 94 ± 4 -7.70 ± 0.13 -8.08 ± 0.08 -8.09 ± 0.26 35 ± 4* 85 ± 5*
SH-SY5Y -7.77 ± 0.11 90 ± 5 -7.58 ± 0.06 -8.56 ± 0.08 -9.12 ± 1.16 6 ± 9* 20 ± 4*
Rat brain
-8.18 ± 0.11
87 ± 4*
-7.26 ± 0.26
-8.66 ± 0.09
-7.85 ± 1.07
8 ± 6*
31 ± 4*

  • ND, not determined.

  • ↵* Extent of inhibition is different from 100% at the 95% confidence level or better.

  • ↵ a Extent of inhibition (ExIn) is ∼100% for all preparations in this data set.