Neil A, Terenius L
Eur J Pharmacol. 1981 Jan 5;69(1):33-9. doi: 10.1016/0014-2999(81)90599-9.
The actions of d-propoxyphene and morphine on opioid receptor mechanisms were compared. In assay measuring receptor binding selectivity in vitro, with dihydromorphine, naloxone and an enkephalin analogue as radioactive ligands, d-propoxyphene differed from morphine in having a higher relative affinity for sites occupied by the peptide. Naloxone was more potent in antagonizing morphine- than d-propoxyphene-induced antinociception in the mouse hot-plate test. In morphine-tolerant mice showing three-fold lower morphine sensitivity the antinociceptive efficacy of d-propoxyphene was unchanged. The results indicate differences in receptor-effector mechanisms between d-propoxyphene and morphine.
比较了右旋丙氧芬和吗啡对阿片受体机制的作用。在体外测定受体结合选择性的实验中,以二氢吗啡、纳洛酮和脑啡肽类似物作为放射性配体,右旋丙氧芬与吗啡不同,它对肽占据的位点具有更高的相对亲和力。在小鼠热板试验中,纳洛酮拮抗吗啡诱导的镇痛作用比拮抗右旋丙氧芬诱导的镇痛作用更有效。在吗啡敏感性降低三倍的吗啡耐受小鼠中,右旋丙氧芬的镇痛效果未改变。结果表明右旋丙氧芬和吗啡在受体 - 效应器机制上存在差异。