Affinities of S18327 at multiple adrenergic receptors and NE reuptake sites
| Receptor | Species | Tissue | Radioligand | pKi |
|---|---|---|---|---|
| nM | ||||
| α1 | Rat | Frontal cortex | [3H]Prazosin (0.2) | 8.95 ± 0.09 |
| α1A | Rat | Salivary gland | [3H]Prazosin (0.04) | 8.88 ± 0.09 |
| α1B | Rat | Liver | [3H]Prazosin (0.04) | 9.34 ± 0.03 |
| α1A | Human | CHO cell line | [3H]Prazosin (0.1) | 9.00 ± 0.09 |
| α1B | Human | CHO cell line | [3H]Prazosin (0.1) | 9.11 ± 0.08 |
| α1D | Human | CHO cell line | [3H]Prazosin (0.1) | 8.56 ± 0.12 |
| α2A | Rat | Cortex | [3H]RX821002 (0.4) | 6.68 ± 0.04 |
| α2A | Human | Sf9 cells | [3H]MK912 (0.7) | 7.42 ± 0.02 |
| α2A | Human | CHO cell line | [3H]RX821002 (0.8) | 7.07 ± 0.11 |
| α2B | Human | CHO cell line | [3H]RX821002 (4.0) | 7.56 ± 0.13 |
| α2C | Human | CHO cell line | [3H]RX821002 (0.6) | 7.30 ± 0.13 |
| β1 | Human | Sf9 cells | [3H]CGP12177 (0.16) | <6 |
| β2 | Human | Sf9 cells | [3H]CGP12177 (0.2) | <6 |
| NE reuptake site | Rat | Frontal cortex | [3H]Nisoxetine (1) | <6 |
| NE reuptake site | Human | CHO cell line | [3H]Nisoxetine (2) | <6 |
Data are means ± S.E. of ≥3 determinations performed in triplicate. For details of methods, see Millan et al., 1998b.