From: Dibenzazecine compounds with a novel dopamine/5HT2A receptor profile and 3D-QSAR analysis
 | pK i app | |||||
---|---|---|---|---|---|---|
Compound | [cAMP]i | [Ca2+]i | [35S]-GTPγ S binding | |||
 | hD1 | hD2L | hD1 | hD2L | hD1 | hD2L |
Haloperidol | 6.80 ± 0.10 | 9.88 ± 0.07 | 6.61 ± 0.09 | 10.0 ± 0.13 | 7.10 ± 0.91 | 9.10 ± 0.07 |
Clozapine | 6.46 ± 0.05 | 7.30 ± 0.07 | 6.54 ± 0.15 | 6.92 ± 0.11 | 7.47 ± 0.29 | 7.48 ± 0.08 |
LE300 | 7.55 ± 0.13 | 8.73 ± 0.10 | 7.22 ± 0.15 | 7.93 ± 0.12 | 7.75 ± 0.12 | 8.14 ± 0.11 |
LE400 | 5.35 ± 0.17 | 6.88 ± 0.09 | < 5.00a) | < 5.00a) | 6.25 ± 0.13 | 6.39 ± 0.14 |
LE401 | 5.00 ± 0.13 | < 5.00a) | < 5.00a) | < 5.00a) | < 5.00a) | < 5.00a) |
LE403 | 7.02 ± 0.09 | 7.23 ± 0.12 | 7.57 ± 0.11 | 7.14 ± 0.08 | 7.48 ± 0.12 | 7.20 ± 0.15 |
LE404 | 7.95 ± 0.09 | 8.01 ± 0.08 | 8.20 ± 0.15 | 7.71 ± 0.01 | 8.10 ± 0.13 | 8.13 ± 0.08 |
LE410 | 7.35 ± 0.12 | 8.63 ± 0.07 | 7.39 ± 0.07 | 8.13 ± 0.11 | 8.02 ± 0.08 | 8.13 ± 0.09 |
LE420 | 6.44 ± 0.21 | 7.69 ± 0.08 | 6.73 ± 0.09 | 7.08 ± 0.12 | 7.17 ± 0.11 | 7.51 ± 0.08 |