Sheehan M J, Hayes A G, Tyers M B
Eur J Pharmacol. 1986 Oct 14;130(1-2):57-64. doi: 10.1016/0014-2999(86)90183-4.
Electrically evoked contractions of the hamster isolated vas deferens are inhibited only by opioid drugs which have agonist activity at delta-opioid receptors. Opioids which are mu-, kappa- or sigma-selective were either inactive or were antagonists. The compound beta-funaltrexamine, which irreversibly blocks mu- and delta-opioid receptors, caused a flattening of the dose-response curve and a reduced maximum inhibition available to delta-opioid agonists. Analysis of the curves by the double-reciprocal null method enabled the affinity of these agonists at delta-opioid receptors to be calculated.
仓鼠离体输精管的电诱发收缩仅被对δ-阿片受体具有激动剂活性的阿片类药物所抑制。对μ-、κ-或σ-受体具有选择性的阿片类药物要么无活性,要么是拮抗剂。不可逆地阻断μ-和δ-阿片受体的化合物β-芬太尼丁胺导致剂量反应曲线变平,且δ-阿片受体激动剂的最大抑制作用降低。通过双倒数归零法对曲线进行分析,能够计算出这些激动剂对δ-阿片受体的亲和力。