[Selective antidopaminergic properties of remoxiprid, a new potential antipsychotic agent].
The pharmacology of S-(-)-3-bromo-2, 6-dimethoxy-N-(1-ethyl-2-pyrrolidinylone-ethyl)-benzamide (remoxipride), a new neuroleptic compound belonging to the benzamide group, has been thoroughly investigated using a number of different techniques. The compound blocks apomorphine-induced stereotypies and hyperactivity, indicating potent antidopaminergic activity. However, in contrast to many other antidopaminergic compounds, remoxipride induces only weak and atypical catalepsy, which indicates that remoxipride might exert less antidopaminergic side effects than other neuroleptic drugs. In vivo receptor binding studies using 3H-spiperone show that remoxipride preferentially blocks dopamine receptors only are blocked to 60% even at very high doses. In vitro receptor binding studies show that remoxipride is devoid of affinity for receptors other than the dopamine D2 receptors except at higher concentrations. These results indicate that remoxipride should be a clinically effective neuroleptic compound exerting less extrapyramidal side effects than the neuroleptics currently used.
Ogren
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SO
Hall
H
H
Köhler
C
C
Magnusson
O
O
Florvall
L
L
D000818:Animals; D014150:Antipsychotic Agents / Q000494:pharmacology*; D001058:Apomorphine / Q000037:antagonists & inhibitors; D001549:Benzamides / Q000494:pharmacology*; D002375:Catalepsy / Q000139:chemically induced; D055598:Chemical Phenomena; D002621:Chemistry; D004298:Dopamine / Q000378:metabolism; D008297:Male; D009043:Motor Activity / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000187:drug effects*; D017330:Remoxipride; D013239:Stereotyped Behavior / Q000187:drug effects
D014150:Antipsychotic Agents; D001549:Benzamides; D011954:Receptors, Dopamine; D017330:Remoxipride; D001058:Apomorphine; D004298:Dopamine
Die selektiven antidopaminergen Eigenschaften von Remoxiprid, einem neuen möglichen antipsychotischen Wirkstoff.