Table 2.
Binding affinities (Ki) of SSRIs with resting and desensitized nAChRs.
| Radioligand | nAChR Subtype | SSRI | Ki (μM) a | Reference | |
|---|---|---|---|---|---|
| Resting State | Desensitized State | ||||
| [3H]Imipramine | hα4β2 | Fluoxetine | 3.2 ± 0.4 | 1.0 ± 0.1 | [70] |
| Paroxetine | 16.1 ± 1.3 | 6.7 ± 0.9 | [70] | ||
| Citalopram | ND | 4.1 ± 0.3 | [68] | ||
| hα3β4 | Citalopram | ND | 1.8 ± 0.1 | [68] | |
| Fluoxetine | 14.9 ± 1.4 | 4.8 ± 0.5 | [70] | ||
| Paroxetine | 24.0 ± 1.8 | 6.9 ± 0.6 | [70] | ||
| hα7 | Fluoxetine | 16.9 ± 1.4 | 11.0 ± 1.0 | [70] | |
| Paroxetine | 8.9 ± 0.8 | 8.7 ± 0.6 | [70] | ||
| [3H]TCP |
Torpedo α1β1γδ |
Fluoxetine | 1.9 ± 0.2 | 0.96 ± 0.04 | [77] |
| Paroxetine | 34 ± 2 | 2.5 ± 0.1 | [77] | ||
a The inhibition constant (Ki) represents the ligand affinity for the tested radioligand binding site(s) in the desensitized (agonist-bound) and resting (bungarotoxin-bound) states, respectively. h, human.