Preparation of 7-oxaaporphine derivatives and evaluation of their dopaminergic activity.
A series of 7-oxaaporphine derivatives was prepared. The compounds were evaluated as dopaminergic agents. None of them showed either affinity for dopamine receptors or activity in vivo in the climbing behavior (mice) and turning behavior (6-hydroxydopamine-lesioned rats) tests. The lack of activity is tentatively related to the effect of the oxygen atom on the pKa of these molecules.
Banzatti
C
C
Farmitalia Carlo Erba R & D, CNS Line, Milano, Italy.
Carfagna
N
N
Commisso
R
R
Heidempergher
F
F
Pegrassi
L
L
Melloni
P
P
D000818:Animals; D001060:Aporphines / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D001522:Behavior, Animal / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D006863:Hydrogen-Ion Concentration; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D009043:Motor Activity / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000187:drug effects* / Q000502:physiology; D017448:Receptors, Dopamine D2; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship
D001060:Aporphines; D011954:Receptors, Dopamine; D017448:Receptors, Dopamine D2