
Journal of Pharmaceutical Sciences p. 672 - 675 (1985)
Update date:2022-09-26
Topics:
Cannon
Koble-Suarez
Long
Ilhan
Bhatnagar
cis- and trans-4-n-Propyloctahydrobenzo(f)quinolines 4a,b were prepared for further assessment of dopaminergic effects of nonoxygenated 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 α1 and α2-adrenoceptor antagonists. Compound 4b provides evidence that α2-adrenoceptors and dopamine receptors are different entities, since this compound is an α2 antagonist and a dopamine receptor agonist at presynaptic sites.
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(1971)