TABLE 2
Effects of TM2 L9′T mutation on the functional effects of ACh on HS α 4β 2 nAChRs
Oocytes were injected with a 1:10 α4/β2 cDNA ratio to produce HS α4β2 nAChRs. EC50 values are the means of EC50 estimates obtained by fitting separately each concentration-response curve with a one-component sigmoidal equation, which gave the best fit for all data sets. Potency ratios were calculated from fits in which curves were constrained to slope equal to 1 and are expressed in relation to receptors containing 5 L9′ (which therefore have dose ratio values of 1). Results are from four or five independent experiments (n).
| EC50 (95% CI) | Potency Ratio | 2
| 3
| 5
| n | |
|---|---|---|---|---|---|---|
| μM | ||||||
| α4β2wt | 4 (3.3-4.8) | 1 | 5 | |||
| α4LTβ2 | 1 (0.8-1.1) | 4.18 | 2.1 | 4 | ||
| α4β2LT | 0.2 (0.1-0.3) | 18.05 | 2.6 | 4 | ||
| α4LTβ2LT | 0.03 (0.02-0.04) | 136.89 | 2.7 | 4 |
-
CI, confidence interval; HS, high sensitivity.