Table 2b.
Affinity of analogs at serotonin receptors
| Ki (nM)a | ||||||||
|---|---|---|---|---|---|---|---|---|
| Cmpd # | R1 | R2 | R3 | 5-HT1Ab | 5-HT1Bc | 5-HT2Ad | 5-HT5Ae | 5-HT6e |
| 10 | OMe | OMe | H | 110 | 255 | 1680 | 578 | 5 |
| 11 | OH | OH | H | 151 | 451 | 1564 | 244 | 38 |
| 12 | OMe | OMe | Me | NAf | NA | 811 | 286 | 5 |
| 13 | OH | OH | Me | 393 | 1032 | 352 | 363 | 123 |
| 8-OH-DPAT | 0.81 | |||||||
| ergotamine | 9.28 | 6.92 | ||||||
| clozapine | 3.91 | 3.88 | ||||||
Experiments conducted in triplicate; SEM values are within 15% of reported values;
[3H]-WAY100635 used as radioligand;
[3H]GR125743 used as radioligand;
.[3H]ketanserin used as radioligand;
[3H]LSD used as radioligand;
NA- not active- ligands displayed <10% inhibition in a primary assay at a ligand concentration of 10 μM