Synthesis and dopamine receptor affinities of 6-amino-5,6,7,8-tetrahydroquinoline derivatives.
Some N,N-dialkylderivatives of 6-amino-5,6,7,8-tetrahydroquinoline were synthesized. The affinity of new compounds for dopamine binding sites was measured in a test involving displacement of [3H]SCH 23390 (D-1 selective) and [3H]spiperone (D-2 selective) from homogenized rat striatal tissue. While no compound was effective in displacing [3H]SCH 23390, in the binding assays on the D-2 receptor all tetrahydroquinolines displaced [3H]spiperone from specific binding sites, the compounds with a N-n-propyl-N-phenylethylamino group (18) or N,N-di n-propylamino group (16) being the most potent.
Claudi
F
F
Dipartimento di Scienze Chimiche, Università di Camerino, Italy.
Cingolani
G M
GM
Giorgioni
G
G
Cattabeni
F
F
Cimino
M
M
Di Luca
M
M
D015647:2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine; D000634:Aminoquinolines / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D001552:Benzazepines / Q000494:pharmacology; D001667:Binding, Competitive / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D003342:Corpus Striatum / Q000187:drug effects / Q000378:metabolism; D015259:Dopamine Agents / Q000494:pharmacology; D066298:In Vitro Techniques; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000187:drug effects*
D000634:Aminoquinolines; D001552:Benzazepines; D015259:Dopamine Agents; D011954:Receptors, Dopamine; D015647:2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine