Table 3.
Affinity of aminothiazole analogues at 5-HT receptors
 |
||||||
|---|---|---|---|---|---|---|
| Ki (nM)a | ||||||
| Cmpd # | R1 | 5-HT1ARb | 5-HT2ARc | 5-HT6Rd | 5-HT7ARd | clogPe |
| 33a | Me | 187±24 | 1040±130 | naf | 9.9±1.3 | 3.5 |
| 33b | Pr | 93±12 | na | na | 150±19 | 4.5 |
| 34a | Me | 23±3.0 | na | na | 6.5±0.8 | 3.5 |
| 34b | Pr | 7.5±0.97 | na | na | 132±17 | 4.5 |
| 8-OH DPAT | 0.8 ±0.01 | |||||
| Clozapine | 3.0±0.4 | 4.0±0.5 | 11.4±1.5 | |||
a
Experiments carried out in triplicate;
b
[3H]WAY100635 used as radioligand;
c
[3H]Ketanserin used as radioligand;
d
[3H]LSD used as radioligand;
e
calculated with ChemDraw Professional v. 16.0.1.4;
f
na – not active (compounds displayed < 50% inhibition in a primary assay)