Hacksell U, Johansson A M, Arvidsson L, Nilsson J L, Hjorth S, Carlsson A, Wikström H, Sanchez D, Lindberg P
J Med Chem. 1984 Aug;27(8):1003-7. doi: 10.1021/jm00374a012.
C1-Methylated derivatives of the potent dopaminergic agonist 5-hydroxy-2-(di-n-propylamino)tetralin (6) have been synthesized and tested for central dopamine (DA) receptor stimulating activity, by using biochemical and behavioral tests in rats. Both cis- and trans-5-hydroxy-1-methyl-2-(di-n-propylamino) tetralin (4 and 3) may be classified as central DA-receptor agonists, albeit of lower potency than 6. The results obtained indicate that both 4 and 3 display DA-autoreceptor stimulation capacity. However, only one of the isomers, trans-3, is able to elicit clear-cut postsynaptic DA receptor agonist actions at larger doses. 5-Hydroxy-1,1-dimethyl-2-(n-propylamino) tetralin (5) was found to be inactive.
强效多巴胺能激动剂5-羟基-2-(二正丙基氨基)四氢萘(6)的C1-甲基化衍生物已被合成，并通过对大鼠进行生化和行为测试来检测其对中枢多巴胺(DA)受体的刺激活性。顺式和反式5-羟基-1-甲基-2-(二正丙基氨基)四氢萘(4和3)均可归类为中枢DA受体激动剂，尽管其效力低于6。所得结果表明，4和3均具有DA自身受体刺激能力。然而，只有反式异构体3在较大剂量时能够引发明显的突触后DA受体激动作用。5-羟基-1,1-二甲基-2-(正丙基氨基)四氢萘(5)被发现无活性。
