Synthesis and dopamine receptor affinities of 6-amino-5,6,7,8-tetrahydroquinoline derivatives.

Drug design and delivery Pub Date : 1989-06-01
F Claudi, G M Cingolani, G Giorgioni, F Cattabeni, M Cimino, M Di Luca
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引用次数: 0

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.

6-氨基-5,6,7,8-四氢喹啉衍生物的合成及多巴胺受体亲和性。
合成了6-氨基-5,6,7,8-四氢喹啉的N,N-二基衍生物。通过从匀浆大鼠纹状体组织中置换[3H]SCH 23390 (D-1选择性)和[3H]spiperone (D-2选择性)的实验,测量了新化合物对多巴胺结合位点的亲和力。虽然没有化合物能有效取代[3H] sch23390,但在D-2受体的结合实验中,所有四氢喹啉类化合物都能从特定的结合位点取代[3H]spiperone,具有N-正丙基-N-苯乙基氨基(18)或N,N-二正丙基氨基(16)的化合物是最有效的。
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