3-Phenylpiperidines. Central dopamine-autoreceptor stimulating activity
作者:Uli Hacksell、Lars Erik Arvidsson、Uno Svensson、J. Lars G. Nilsson、Domingo Sanchez、Hakan Wikstroem、Per Lindberg、Stephan Hjorth、Arvid Carlsson
DOI:10.1021/jm00144a021
日期:1981.12
Thirty compounds related to the selective dopamine-autoreceptor agonist 3-(3-hydroxyphenyl)-N-n-propylpiperidine have been synthesized and tested for central dopamine-autoreceptor stimulating activity. The 3-(3-hydroxyphenyl)piperidine moiety seems indispensable for high potency and selectivity. Introduction of an additional hydroxyl group into the 4 position of the aromatic ring gives a compound with
已经合成了三十种与选择性多巴胺-自身受体激动剂3-(3-羟苯基)-Nn-丙基哌啶有关的化合物,并测试了其对中央多巴胺-自身受体的刺激活性。3-(3-羟苯基)哌啶部分似乎对于高效力和选择性是必不可少的。将另外的羟基引入芳族环的4位得到具有多巴胺能活性但对自体受体缺乏选择性的化合物。3-(3-羟基苯基)-Nn-丙基吡咯烷,3-(3-羟基)-Nn-丙基全氢a庚因和3-(3-羟基苯基)喹核苷均无活性。最有效的化合物是N-异丙基,Nn-丁基,Nn-戊基和N-苯乙基取代的3-(3-羟苯基)哌啶衍生物。