Dopaminergic effects of non-hydroxylated rigid analogs of apomorphine.
A series of rigid analogs of apomorphine lacking aromatic hydroxyl substitutents were evaluated for dopaminergic properties. Three compounds, N-methyl-N-propyl-2-aminotetralin (Me-Pr-2-AT), N-N-dipropyl-2-aminotetralin (Di-pr-2-AT) and N,N-dipropyl-2-aminoindane (Di-Pr-2-AI) induced emesis in dogs, contralateral circling in unilaterally lesioned rats, and inhibited prolactin secretion. The induced circling responses, however, were attenuated by prior treatment with alpha-methyl-p-tyrosine methyl ester (AMPTME) and the compounds were weak inhibitors of 3-H-dopamine binding in calf caudate homogenates. The possibility that these agents may be metabolically activated in vivo is discussed.
D000818:Animals; D001058:Apomorphine / Q000031:analogs & derivatives* / Q000494:pharmacology; D002417:Cattle; D002421:Caudate Nucleus / Q000378:metabolism; D004285:Dogs; D004298:Dopamine / Q000378:metabolism / Q000502:physiology*; D004639:Emetics; D005260:Female; D006220:Haloperidol / Q000494:pharmacology; D006801:Humans; D006892:Hydroxydopamines; D066298:In Vitro Techniques; D008297:Male; D008781:Methyltyrosines / Q000494:pharmacology; D011388:Prolactin / Q000097:blood; D051381:Rats; D013239:Stereotyped Behavior / Q000187:drug effects
D004639:Emetics; D006892:Hydroxydopamines; D008781:Methyltyrosines; D011388:Prolactin; D006220:Haloperidol; D001058:Apomorphine; D004298:Dopamine