Table 1.
Affinity of MEL-9, LP-211 and methiothepin for human 5-HT7 receptors expressed in HEK293 cells from [3H]-SB-269970 competitive binding experiments
| 5-HT7 affinity (membrane homogenate radioligand binding) | 5-HT7 affinity (whole-cell radioligand binding) | ||||
|---|---|---|---|---|---|
| Compound | Ki (nmol/L) | pKi | nH | Ki (nmol/L) | pKi |
| MEL-9 | 16.60 ± 0.99 | 7.78 | 1.34 ± 0.14 | 13.77 ± 0.24 | 7.86 |
| LP-211 | 22.52 ± 3.60 | 7.65 | 1 | 19.01 ± 0.14 | 7.72 |
| Methiothepin | 2.31 ± 0.02 | 8.64 | 1 | 2.51 ± 0.73 | 8.62 |
The data are the mean values ± SEM from three independent experiments performed in duplicate. MEL-9, N-benzyl-4-(2-diphenyl)-1-piperazinehexanamide; LP-211, N-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide; HEK293, human embryonic kidney cells; 5-HT7, 5-hydroxytryptamine (serotonin) type 7 receptor; [3H]-SB-269970, (2R)-1-[(3-hydroxyphenyl)sulfonyl]-2-[2-(4-methyl-1-piperidinyl)ethyl]pyrrolidine.