Table 1.
Binding Affinity Constants of Synthetic Compounds to D2-like Receptors.
Compounds | a Binding Data of Compounds, Ki ± SEM (nM) | |||
---|---|---|---|---|
D2 | D3 | D4 | D2/D4 | |
Haloperidol | 1.1±0.07 [ 0.89] | 5.5±3.0[ 4.6] | 12.7±7.2 [10.0] | 0.10 [0.09] |
2a | 1.6 ±0.14 [0.31] | 5.1±3.0 [0.71] | 5.3± 0.99 [12.1] | 0.30 [0.03] |
2b | 1231±145 | >10,000 | 789±363 | 1.60 |
2c | 1050±209 | 172±33 | 1015±179 | 1.03 |
3a | 588±57.6 | 128±13 | 7873±1437 | 0.07 |
3b | 160.3±11.8 | 25.0±1.7 | 3007±561 | 0.05 |
3c | 53.0±6.4 | 18.0±1.6 | 277.5±26.5 | 0.19 |
4 | MPA | 2874±584 | 816.5±194.4 | --- |
5 | MPA | 3074±553 | MPA | --- |
= Data obtained from the NIMH-PDSP and those in square brackets are from ref 15. Ki is the mean value obtained on triplicate or quadruplicate determinations unless otherwise indicated. MPA = Missed primary assay threshold of 50% inhibition.