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. 2003 Oct 31;100(23):13674–13679. doi: 10.1073/pnas.1835612100

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.