Seeman P, Van Tol H H
Department of Pharmacology, University of Toronto, Canada.
Eur J Pharmacol. 1993 Mar 16;233(1):173-4. doi: 10.1016/0014-2999(93)90365-o.
In order to identify new atypical antipsychotic drugs which are more selective for the human dopamine D4 receptor than for the human dopamine D2 (long) receptor, we tested enantiomer pairs of dopamine agonists and dopamine antagonists on the expressed proteins of these cloned receptors. The (+)-aporphines ((+)-N-propyl-norapomorphine, 11-OH-N-propyl-norapomorphine and (+)-apomorphine) bound to the dopamine D4 receptor with selectivities up to 20 times greater than to the dopamine D2 receptor, suggesting that these pharmacologically inactive enantiomers may succeed as atypical neuroleptics.
为了鉴定出对人多巴胺D4受体比对人多巴胺D2（长）受体更具选择性的新型非典型抗精神病药物，我们在这些克隆受体的表达蛋白上测试了多巴胺激动剂和多巴胺拮抗剂的对映体对。（+）-阿朴啡类化合物（（+）-N-丙基去甲阿扑吗啡、11-羟基-N-丙基去甲阿扑吗啡和（+）-阿扑吗啡）与多巴胺D4受体结合的选择性比对多巴胺D2受体高20倍，这表明这些药理上无活性的对映体可能会成为成功的非典型抗精神病药物。
