Cis- and trans-4-n-Propyl-1,2,3,4,4a,5,6,10b-octahydrobenzo(f)quinolines.
Cis- and trans-4-n-Propyloctahydrobenzo(f)quinolines 4a,b were prepared for further assessment of dopaminergic effects of non-oxygenated dopamine congeners. The trans isomer 4b exhibited marked dopamine-like effects in the cat cardioaccelerator nerve assay and in a rat rotation model. Compound 4b produced dose-related lowering of blood pressure in the cat. The cis isomer 4a was inactive in these assays. Both compounds were inactive in a dopamine binding assay, but both appeared active in a spiroperidol binding assay. Both compounds are active alpha 1- and alpha 2-adrenoceptor antagonists. Compound 4b provides evidence that alpha 2-adrenoceptors and dopamine receptors are different entities, since this compound is an alpha 2 antagonist and a dopamine receptor agonist at presynaptic sites.
D000818:Animals; D001058:Apomorphine / Q000494:pharmacology; D001667:Binding, Competitive / Q000187:drug effects; D001794:Blood Pressure / Q000187:drug effects; D002319:Cardiovascular System / Q000187:drug effects; D002415:Cats; D002421:Caudate Nucleus / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D002851:Chromatography, High Pressure Liquid; D004298:Dopamine / Q000378:metabolism; D004837:Epinephrine / Q000494:pharmacology; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D007536:Isomerism; D011804:Quinolines / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000187:drug effects* / Q000378:metabolism; D013239:Stereotyped Behavior / Q000187:drug effects
D011804:Quinolines; D011954:Receptors, Dopamine; D001058:Apomorphine; D004298:Dopamine; D004837:Epinephrine