Gottschlich R, Krug M, Barber A, Devant R M
Department of Medicinal Chemistry, E. Merck, Darmstadt, Germany.
Chirality. 1994;6(8):685-9. doi: 10.1002/chir.530060814.
The four stereoisomers of the two peripherally selective kappa-opioid agonists EMD 60,400 and EMD 61,753 were synthesized, tested for stereoisomeric purity, and examined for affinity to the kappa opioid receptor. The relationships between the configuration of these molecules and their biological activity are discussed.
合成了两种外周选择性κ-阿片受体激动剂EMD 60,400和EMD 61,753的四种立体异构体，检测了它们的立体异构纯度，并研究了它们与κ-阿片受体的亲和力。讨论了这些分子的构型与其生物活性之间的关系。
