（+）-顺式-8-羟基-1-甲基-2-（二正丙基氨基）四氢萘：一种强效且高度立体选择性的5-羟色胺受体激动剂。

(+)-cis-8-Hydroxy-1-methyl-2-(di-n-propylamino)tetralin: a potent and highly stereoselective 5-hydroxytryptamine receptor agonist.

作者信息

Arvidsson L E, Johansson A M, Hacksell U, Nilsson J L, Svensson K, Hjorth S, Magnusson T, Carlsson A, Andersson B, Wikström H

机构信息

Department of Organic Pharmaceutical Chemistry, University of Uppsala,Sweden.

出版信息

J Med Chem. 1987 Nov;30(11):2105-9. doi: 10.1021/jm00394a029.

DOI:10.1021/jm00394a029

PMID:2959776

Abstract

C1-Methylated derivatives of the potent 5-hydroxytryptamine (5-HT) receptor agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT, 1) were synthesized and tested for central 5-HT and dopamine receptor activity by use of a biochemical test method in rats. cis-8-Hydroxy-1-methyl-2-(di-n-propylamino)tetralin (8) was found to be a 5-HT receptor agonist. The (+)-enantiomer of 8 had a potency equal to that of 1, whereas (-)-8 and the trans isomer (+/-)-9 were inactive.

摘要

合成了强效5-羟色胺（5-HT）受体激动剂8-羟基-2-（二正丙基氨基）四氢萘（8-OH-DPAT，1）的C1-甲基化衍生物，并通过生化测试方法在大鼠中测试其对中枢5-HT和多巴胺受体的活性。发现顺式-8-羟基-1-甲基-2-（二正丙基氨基）四氢萘（8）是一种5-HT受体激动剂。8的（+）-对映体的效力与1相当，而（-）-8和反式异构体（+/-）-9无活性。