Summary of Ki values of lorcaserin using radioligand binding competition with human recombinant 5-HT receptors and neurotransmitter transporters
Data represent Ki values derived from one determination in which eight test lorcaserin concentrations and eight reference compound concentrations were used. Triplicate determinations were made at each compound concentration. Ki values were determined for lorcaserin and the respective reference compounds.
Receptor | Lorcaserin Ki | Reference Compound (Ki) |
|---|---|---|
| nM | ||
| Human 5-HT1A | 700 | 8-Hydroxy-2-dipropylaminotetralin (0.9) |
| Human 5-HT3 | 4430 | MDL 72222 (7) |
| Human 5HT4e | 18,900 | 5-HT (330) |
| Human 5-HT5A | 3710 | 5-HT (69) |
| Human 5-HT6 | 1980 | 5-HT (110) |
| Human 5-HT7 | 636 | 5-HT (0.4) |
| Human norepinephrine transporter | 1400 | Protriptyline (15) |
| Human dopamine transporter | 33,000 | 1-[1-(2-Benzo[b]thienyl)cyclohexyl]piperidine (6.8) |
| Human 5-HT transporter | 990 | Imipramine (1.3) |