The influence of ivermectin on agonist-evoked responses was examined on wild-type α7 nAChRs and a series of α7 nAChRs containing single point mutations
In each case, the influence of a maximal concentration of ivermectin (30 μM) was examined on an EC20 concentration of acetylcholine. The effect of ivermectin is expressed either as potentiation or inhibition compared with the magnitude of responses obtained with an EC20 concentration of acetylcholine in the absence of ivermectin.
| Subunit | Location | EC20 ACh | Potentiation | Inhibition | n |
|---|---|---|---|---|---|
| μM | fold | % | |||
| α7 | 50 | 4.6 ± 0.6 | 8 | ||
| G211V | TM1 | 50 | 4.7 ± 0.5 | 6 | |
| S222M | TM1 | 50 | 89.1 ± 6.6*** | 4 | |
| A225D | TM1 | 50 | 1.1 ± 0.1** | 4 | |
| L230Y | TM1 | 50 | 4.7 ± 0.5 | 5 | |
| M253L | TM2 | 50 | 55.6 ± 8.8*** | 3 | |
| M260L | TM2 | 25 | 4.4 ± 0.6 | 5 | |
| Q272V | TM3 | 60 | 1.2 ± 0.1* | 3 | |
| S276V | TM3 | 50 | 84.2 ± 3.5*** | 4 | |
| F445A | TM4 | 50 | 4.6 ± 1.0 | 6 | |
| T456V | TM4 | 50 | 1.2 ± 0.2*** | 7 | |
| C459Y | TM4 | 50 | 1.4 ± 0.2*** | 7 |