Table 2c.
Affinity of analogs at α-adrenergic receptors
| Ki (nM)a. | ||||||||
|---|---|---|---|---|---|---|---|---|
| Cmpd # | R1 | R2 | R3 | α1Ab | α1Bb | α2Ac | α2Bc | α2Cc |
| 10 | OMe | OMe | H | 545 | 2592 | 1603 | 1120 | 774 |
| 11 | OH | OH | H | 3197 | NAd | 2590 | 2197 | 1106 |
| 12 | OMe | OMe | Me | 2863 | 5874 | 1174 | NA | 472 |
| 13 | OH | OH | Me | >10,000 | NA | NA | 5822 | 1959 |
| prazosin | 0.38 | 0.39 | ||||||
| oxymetazoline | 9.30 | 65.58 | ||||||
| yohimbine | 10.85 | |||||||
Experiments conducted in triplicate; SEM values are within 15% of reported values;
[3H]Prazosin used as radioligand;
[3H]Rauwolscine used as radioligand;
NA- not active- ligands displayed <10% inhibition in a primary assay at a ligand concentration of 10 μM