地佐辛、吗啡、芬太尼、布托啡诺和纳布啡与阿片受体的结合。

The opioid receptor binding of dezocine, morphine, fentanyl, butorphanol and nalbuphine.

作者信息

Chen J C, Smith E R, Cahill M, Cohen R, Fishman J B

机构信息

Department of Pharmacology, University of Massachusetts Medical Center, Worcester 01655.

出版信息

Life Sci. 1993;52(4):389-96. doi: 10.1016/0024-3205(93)90152-s.

DOI:10.1016/0024-3205(93)90152-s

PMID:8093631

Abstract

The ability of morphine, fentanyl, butorphanol, nalbuphine, and dezocine to compete with radiolabeled ligands for binding at the mu1, mu2, kappa1, and delta opioid receptors and the sigma receptor was characterized. In the absence of sodium, the potency of opioid receptor competition at each receptor site was found to be: mu1-fentanyl > butorphanol > morphine > or = dezocine = nalbuphine; mu2-butorphanol > fentanyl > nalbuphine > morphine = dezocine; kappa1-butorphanol > nalbuphine >> morphine > or = dezocine > fentanyl; and delta-butorphanol > nalbuphine > or = dezocine > morphine > fentanyl. For all five compounds, competition at the sigma receptor was weak, with nalbuphine and dezocine having Kis of approximately 0.5 microM and the other opioids having Kis of greater than 1 microM. Since the presence of 100 mM NaCl during the competitive binding decreased the K(i), to varying degrees, of all five opioids at the mu1 and delta receptors and of some of the opioids at the mu2 and kappa1 receptors, the five compounds studied appear to differ in efficacy at the five receptor sites.

摘要

研究了吗啡、芬太尼、布托啡诺、纳布啡和地佐辛与放射性标记配体竞争结合μ1、μ2、κ1、δ阿片受体及σ受体的能力。在无钠条件下，发现各受体位点上阿片受体竞争的效力为：μ1-芬太尼＞布托啡诺＞吗啡≥地佐辛=纳布啡；μ2-布托啡诺＞芬太尼＞纳布啡＞吗啡=地佐辛；κ1-布托啡诺＞纳布啡＞＞吗啡≥地佐辛＞芬太尼；δ-布托啡诺＞纳布啡≥地佐辛＞吗啡＞芬太尼。对于所有这五种化合物，其在σ受体上的竞争较弱，纳布啡和地佐辛的Kis约为0.5微摩尔，其他阿片类药物的Kis大于1微摩尔。由于在竞争性结合过程中存在100毫摩尔氯化钠会不同程度地降低所有五种阿片类药物在μ1和δ受体以及部分阿片类药物在μ2和κ1受体上的K(i)，因此所研究的这五种化合物在五个受体位点上的效力似乎有所不同。