Pharmacology of fluperlapine compared with clozapine.

3-Fluoro-6-(4-methyl-piperazinyl)- 11H -dibenz [b,e]azepine ( fluperlapine , NB 106-689) resembles clozapine qualitatively and quantitatively in that it causes sedation, muscle relaxation, anticholinergic effects, no catalepsy, has little effect on apomorphine- and amphetamine-induced behaviour, does not induce apomorphine supersensitivity, and increases dozing and spindle activity in the rat's EEG. In the striatum of rats, it binds less to dopamine (DA) D2-receptor sites, but it enhances DA-turnover more than clozapine. Like clozapine and unlike haloperidol, it is equally active in the striatum, the nucl . accumbens and the cortex. Unlike clozapine, it does not significantly enhance norepinephrine (noradrenaline, NA)- or 5-hydroxytryptamine turnover and it does not increase prolactin blood levels significantly. Of the two compounds, only fluperlapine has some effects in common with antidepressants, i.e. tetrabenazine-antagonism and NA-uptake inhibition in slices of rat brain in vitro and ex vivo.