Sonesson C, Waters N, Svensson K, Carlsson A, Smith M W, Piercey M F, Meier E, Wikström H
Department of Pharmacology, University of Göteborg, Sweden.
J Med Chem. 1993 Oct 15;36(21):3188-96. doi: 10.1021/jm00073a021.
The (+)-and (-)-enantiomer of compounds 4 and 5 were synthesized and tested for central dopamine (DA) receptor stimulating activity, using biochemical and behavioral tests in rats. Based on the available data the (-)-enantiomers of 4 and 5 are characterized as centrally acting DA autoreceptor antagonists with oral activity. They display a similar pharmacological profile as the prototype DA autoreceptor antagonists (+)-1 and (+)-2 and show a certain preference for the D3 DA receptor antagonist binding site.
合成了化合物4和5的（+）-和（-）-对映体，并利用大鼠的生化和行为测试对其进行了中枢多巴胺（DA）受体刺激活性测试。根据现有数据，4和5的（-）-对映体被表征为具有口服活性的中枢作用DA自身受体拮抗剂。它们表现出与原型DA自身受体拮抗剂（+）-1和（+）-2相似的药理学特征，并对D3 DA受体拮抗剂结合位点表现出一定的偏好。
