Affinities (pKi values) of S18616 , dexmedetomidine, and clonidine at diverse adrenoceptor subtypes and related sites
| Receptor | Species | Tissue | Radioligand (nM) | S18616 | Dexmedetomidine | Clonidine |
|---|---|---|---|---|---|---|
| α2 | Rat | Cortex | [3H]RX821,002 (0.4) | 9.8 | 9.0 | 7.5 |
| α2A | Rat | Salivary gland | [3H]RX821,002 (0.5) | 9.6 | NT | 7.6 |
| α2A | Human | CHO | [3H]RX821,002 (0.8) | 9.5 | 8.5 | 7.5 |
| α2A | Human | Sf9 | [3H]MK912 (0.7) | 9.2 | 7.8 | 7.3 |
| α2B | Human | CHO | [3H]RX821,002 (4.0) | 9.6 | 8.7 | 7.4 |
| α2C | Human | CHO | [3H]RX821,002 (0.6) | 9.5 | 8.6 | 7.2 |
| α1 | Rat | Frontal cortex | [3H]Prazosin (0.2) | 7.1 | 6.5 | 6.3 |
| α1A | Rat | Salivary gland | [3H]Prazosin (0.04) | 8.2 | 7.2 | 7.0 |
| α1A | Human | CHO | [3H]Prazosin (0.1) | 8.4 | 6.7 | 6.5 |
| α1B | Rat | Liver | [3H]Prazosin (0.04) | 7.0 | 6.5 | 6.5 |
| α1B | Human | CHO | [3H]Prazosin (0.1) | 7.7 | 6.5 | 6.5 |
| α1D | Human | CHO | [3H]Prazosin (0.1) | 7.6 | 7.1 | 6.9 |
| β1 | Human | Sf9 | [3H]CGP12177 (0.15) | <6.0 | NT | NT |
| β2 | Human | Sf9 | [3H]CGP12177 (0.15) | <6.0 | NT | NT |
| I1 | Bovine | AM | [3H]Clonidine (7.0) | 7.4 | 6.7 | 7.5 |
| I2 | Rat | Cortex | [3H]Idazoxan (2.0) | 7.1 | 7.3 | 6.0 |
| NET | Human | CHO | [3H]Nisoxetine (2.0) | <6.0 | <6.0 | <6.0 |
| MAO A | Rat | Brain | [3H]RO41-1049 (5.0) | <6.0 | <6.0 | <6.0 |
| MAO B | Rat | Brain | [3H]RO19-6327 (15) | <6.0 | <6.0 | <6.0 |
Data are means of two to four determinations. In all cases, the S.E.M. (n ≥ 3) or range (n = 2) was ≤10% of the mean; i.e., ≤0.2 log units (pKi).
I, imidazoline; NET, NE transporter; NT, not tested; AM, adrenal medulla.