Claudi F, Cingolani G M, Giorgioni G, Cattabeni F, Cimino M, Di Luca M
Dipartimento di Scienze Chimiche, Università di Camerino, Italy.
Drug Des Deliv. 1989 Jun;4(4):279-87.
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.
合成了6-氨基-5,6,7,8-四氢喹啉的一些N,N-二烷基衍生物。在一项涉及从匀浆大鼠纹状体组织中置换[3H]SCH 23390(D-1选择性)和[3H]螺哌隆(D-2选择性)的试验中,测定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置换[3H]SCH 23390,但在D-2受体的结合试验中,所有四氢喹啉都能从特异性结合位点置换[3H]螺哌隆,其中具有N-正丙基-N-苯乙氨基的化合物(18)或N,N-二正丙氨基的化合物(16)活性最强。