Table 1. Affinity of clozapine and its metabolites to NMS binding site.
Compound | hM1 | hM2 | hM3 | hM4 | hM5 |
---|---|---|---|---|---|
Acetylcholine | 14 ± 1.8 μM | 1.8 ± 0.2 μM | 9.5 ± 0.8 μM | 12 ± 1.9 μM | 15 ± 0.9 μM |
Clozapine | 13 ± 2 | 51 ± 4 | 25 ± 2 | 33 ± 4 | 26 ± 3 |
N-desmethylclozapine | 55 ± 5 | 1,650 ± 101 | 223 ± 30 | 344 ± 25 | 105 ± 8 |
Clozapine-N-oxide | 2.5 ± 0.3 μM | 33 ± 3 μM | 8 ± 0.7 μM | 4 ± 0.3 μM | 2.5 ± 0.2 μM |
IC50 values are the mean ± SEM of three experiments performed in quadruplicate. IC50 are expressed in nM except otherwise indicated. [3H] NMS concentration was 200 pM.