Perez J, Perez Z, Angel J, Charris J, Torres M, Israel A
Universidad Central de Venezuela, Organic Synthesis Laboratory, Caracas.
Boll Chim Farm. 1995 Jun;134(6):329-32.
We describe the non stereoselective synthesis of (+/-)-1-amino-6,7,8,8a-tetrahydroacenaphthene (14), a novel compound that belongs to the acetanaphtene group, that is presented as a rigid non hydroxylated 2-aminoindan which has a structural disposition of a dopaminergic pharmacophore that possess a phenylethylamine fragment. Intracerebroventricular administration of this compound induces an increase in urinary volume and sodium excretion in conscious rats. The renal actions of 14 were blocked by haloperidol pretreatment, suggesting that 14 acts centrally through a dopaminergic mechanism.
我们描述了（±）-1-氨基-6,7,8,8a-四氢苊（14）的非立体选择性合成，这是一种属于苊类的新型化合物，它呈现为一种刚性的非羟基化2-氨基茚，具有多巴胺能药效团的结构布局，拥有苯乙胺片段。向清醒大鼠脑室内注射该化合物会导致尿量和钠排泄增加。14的肾脏作用可被氟哌啶醇预处理阻断，这表明14通过多巴胺能机制在中枢起作用。
