Synthesis and dopaminergic activity of 2-substituted octahydrobenzo[f]quinolines.
A series of 2-substituted octahydrobenzo[f]quinolines has been synthesized and assayed for dopamine agonist activity. Only the compounds corresponding to the beta-rotameric conformation of dopamine showed biphasic activity in competition binding studies with the radioligand [3H]spiroperidol. These findings suggest that the congeners possessing the beta-rotamer conformation show receptor-binding characteristics that resemble those of the ergolines more closely than do those of the corresponding alpha-rotamer congeners.
Craig
J C
JC
Department of Pharmaceutical Chemistry, School of Pharmacy, University of California, San Francisco 94143.
Torkelson
S M
SM
Findell
P R
PR
Weiner
R I
RI
D000818:Animals; D002417:Cattle; D015259:Dopamine Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004873:Ergolines / Q000494:pharmacology; D066298:In Vitro Techniques; D008968:Molecular Conformation; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D015259:Dopamine Agents; D004873:Ergolines; D011804:Quinolines