Troponoids. 6. Troponylpiperazines: a new class of dopamine agonists.
A series of alkyltroponylpiperazine derivatives was synthesized and evaluated for dopaminergic activity in rats rendered hypokinetic by the bilateral injection of 6-hydroxydopamine (6-OHDA) into the anterolateral hypothalamus. Several members of the series were active, and a structure-activity relationship is presented. A few selected compounds were also evaluated with regard to their ability to induce contralateral rotational behavior in rats with a unilateral 6-OHDA-induced lesion of the nigrostriatal dopamine pathway. The compounds were compared to bromocriptine. The results indicate that dopaminergic activity is very sensitive to small changes in the troponylpiperazine moiety.
D000818:Animals; D001971:Bromocriptine / Q000494:pharmacology; D003508:Cycloheptanes / Q000138:chemical synthesis*; D004195:Disease Models, Animal; D006892:Hydroxydopamines / Q000494:pharmacology; D008297:Male; D016627:Oxidopamine; D010300:Parkinson Disease / Q000188:drug therapy; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000378:metabolism*; D013329:Structure-Activity Relationship; D014334:Tropolone / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology
D003508:Cycloheptanes; D006892:Hydroxydopamines; D010879:Piperazines; D011954:Receptors, Dopamine; D001971:Bromocriptine; D014334:Tropolone; D016627:Oxidopamine