[The neuroleptic efficiency of some butyrophenone and fluorinated phenothiazine derivatives (author's transl)].
The action of butaperazine was diminished and simultaneously prolonged by fluorination in the position 3 or 7 as evidenced by a number of tests (prolongation of the resting time, catalepsy, apomorphine and dexphenmetrazine antagonism, conditioned escape reflex, aggressivity, algesimetry) on the rat and the mouse. The same seems to apply, in principle, to promazine and prochlorperazine. In contrast, the action of 7-fluorperphenazine and its esters with adamantanic acid and decanoic acid was markedly increased, but not prolonged, as demonstrated by a test (conditioned escape reflex) on the rat. The potency of fluphenazine is reached, but not its duration of action. This finding still needs confirmation by other tests. The duration of action of the butyrylphenazine esters was scarcely longer than that of butyrylphenazine. Considerable irritation has been seen at the site of injection. The esters of long-chained fatty acids and fluperidol and trifluperidol seem to be more potent than the parent substances. There is obviously no prolongation of the duration of action. The activity of the haloperidol oxime ethers (and probably of the esters, too) is weak as compared to that of haloperidol. The duration of action is not prolonged.
D000818:Animals; D014150:Antipsychotic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001058:Apomorphine / Q000037:antagonists & inhibitors; D001522:Behavior, Animal / Q000187:drug effects; D002375:Catalepsy / Q000139:chemically induced; D006220:Haloperidol / Q000031:analogs & derivatives; D006801:Humans; D010640:Phenothiazines; D051381:Rats
D014150:Antipsychotic Agents; D010640:Phenothiazines; D006220:Haloperidol; D001058:Apomorphine
Neuroleptische Wirksamkeit einiger Butyrophenon- und fluorierter Phenothiazinderivate.