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.
D000818:Animals; D000928:Antidepressive Agents; D014150:Antipsychotic Agents / Q000378:metabolism / Q000494:pharmacology*; D001058:Apomorphine / Q000494:pharmacology; D001667:Binding, Competitive / Q000187:drug effects; D001923:Brain Chemistry / Q000187:drug effects; D003024:Clozapine / Q000494:pharmacology*; D003984:Dibenzazepines / Q000494:pharmacology*; D004298:Dopamine / Q000378:metabolism; D004569:Electroencephalography; D006719:Homovanillic Acid / Q000378:metabolism; D006801:Humans; D011388:Prolactin / Q000097:blood; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000378:metabolism; D013134:Spiperone / Q000378:metabolism; D013239:Stereotyped Behavior / Q000187:drug effects
D000928:Antidepressive Agents; D014150:Antipsychotic Agents; D003984:Dibenzazepines; D011954:Receptors, Dopamine; D013134:Spiperone; D011388:Prolactin; C041528:fluperlapine; D003024:Clozapine; D001058:Apomorphine; D004298:Dopamine; D006719:Homovanillic Acid