Synthesis and evaluation of 1,2,3,4-tetrahydro[1]benzothieno[2,3-h]isoquinolines as dopamine antagonists.
1,2,3,4-Tetrahydro[1]benzothieno[2,3-h]isoquinolines were prepared and evaluated as dopamine antagonists and for potential neuroleptic activity. These compounds, which are analogues of the dopamine agonist apomorphine (2) in which the C-7 methylene has been removed, were found to be dopamine antagonists by in vitro receptor binding studies. However, in vivo evaluation did not suggest potential antipsychotic activity.
D000818:Animals; D001362:Avoidance Learning / Q000187:drug effects; D001522:Behavior, Animal / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D018492:Dopamine Antagonists; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D013876:Thiophenes / Q000138:chemical synthesis* / Q000494:pharmacology
D018492:Dopamine Antagonists; D007546:Isoquinolines; D013876:Thiophenes