Synthesis and dopamine receptor affinities of 6-amino-5,6,7,8-tetrahydroquinoline derivatives.
Francesco Claudi, G. M. CINGOLANI, Gianfabio Giorgioni, F. Cattabeni, Mauro Cimino, Mónica Di Luca
Abstract
Francesco Claudi, G. M. CINGOLANI, Gianfabio Giorgioni, F. Cattabeni, Mauro Cimino, Mónica Di Luca
Abstract
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.
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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.
Key concepts: SCH-23390, Spiperone, Affinities, Dopamine receptor, Stereochemistry, Dopamine, Dopamine antagonist, Chemistry