Studies on the Mechanism of Action of Substituted Benzamide Drugs
作者:
Christer Köhler,
Sven‐Ove Ögren,
Kjell Fuxe,
期刊:
Acta Psychiatrica Scandinavica
(WILEY Available online 1984)
卷期:
Volume 69,
issue S311
页码: 125-137
ISSN:0001-690X
年代: 1984
DOI:10.1111/j.1600-0447.1984.tb06864.x
出版商: Blackwell Publishing Ltd
关键词: Benzamides;neuroleptics;sulpiride;in vivo binding.
数据来源: WILEY
摘要:
AbstractThe effects of classical neuroleptic drugs (haloperidol, chlorpromazine) and atypical neuroleptics, i.e. substituted benzamides (L‐sulpiride, tiapride, FLA 731(‐)) on specificin vivobinding of the dopamine antagonist3H‐spiperone and the dopamine agonist3H‐n‐propylnorapomorphine (3H‐NPA) was examined in male rats. The atypical neuroleptics were found to be considerably more potent in displacing nigral than striatal3H‐spiperone binding while the classical neuroleptics were about equipotent in the two brain regions. The benzamides also produced considerably less displacement of3H‐spiperone in the striatum than did classical neuroleptics. Furthermore, while the classical neuroleptic drugs block the striatal3H‐spiperone and3H‐NPA binding sites to about the same degree, the substituted benzamides appear to have a higher affinity for the DA receptors labelled by3H‐NPA than those labelled by3H‐spiperone. The behavioural effects of the benzamides were found to differ from classical neuroleptic drugs particularly with regard to induction of catalepsy. Thus, the induction of cataleptic behaviour was found to correlate with displacement of3H‐spiperone in the striatum while blockade of apomorphine induced hyperactivity correlated with the displacement of spipero
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