Agbas A, Simon J, Avni Oktem H, Varga E, Borsodi A
Institute of Biochemistry, Hungarian Academy of Sciences, Szeged.
Neuropeptides. 1988 Oct;12(3):171-6. doi: 10.1016/0143-4179(88)90050-9.
The human placenta contains membrane bound opioid receptors. The binding of the antagonist naloxone and the fairly kappa-selective agonist EKC were studied in the microvillous membrane fraction. In both cases high affinity binding sites were detected with Kd values in the nanomolar range. A series of kappa-selective ligand (PD-117302, EKC, and U-50, 488H) were tested in displacement experiments, and found to be potent inhibitors of agonist and antagonist binding. It was confirmed that large percentage of the binding is associated with the kappa sub-type which is of current interest, in that it shows distinctive pharmacology and distribution and is selective for the natural opioid polypeptide, dynorphin.
人类胎盘含有膜结合阿片受体。在微绒毛膜部分研究了拮抗剂纳洛酮和相当具有κ选择性的激动剂EKC的结合情况。在这两种情况下，均检测到高亲和力结合位点，其解离常数（Kd）值处于纳摩尔范围内。在置换实验中测试了一系列κ选择性配体（PD - 117302、EKC和U - 50,488H），发现它们是激动剂和拮抗剂结合的有效抑制剂。已证实，很大比例的结合与目前所关注的κ亚型相关，因为它显示出独特的药理学和分布特点，并且对天然阿片肽强啡肽具有选择性。
