Horváth K, Wollemann M
Institute of Biochemistry Biological Research Center of Hungarian Academy of Sciences, Szeged.
Neurochem Res. 1986 Nov;11(11):1565-9. doi: 10.1007/BF00965775.
Azidomorphine at low concentration (10(-9) M) inhibits the high-affinity binding site of labeled naloxone in rat brain membrane preparations. In the presence of Na+ and guanine nucleotides the displacement curves of azidomorphine are increased toward high concentrations, whereas Mg2+ ions decrease the IC50 values; This demonstrates the agonist behavior of azidomorphine in binding experiments. When compared with morphine, azidomorphine displayed five-fold lower IC50 values. Based on the presented results, azidomorphine appears to be a good candidate for photoaffinity labeling of opiate receptors.
低浓度（10⁻⁹ M）的叠氮吗啡可抑制大鼠脑膜制剂中标记纳洛酮的高亲和力结合位点。在存在Na⁺和鸟嘌呤核苷酸的情况下，叠氮吗啡的置换曲线向高浓度方向增加，而Mg²⁺离子会降低IC50值；这证明了叠氮吗啡在结合实验中的激动剂行为。与吗啡相比，叠氮吗啡的IC50值低五倍。基于所呈现的结果，叠氮吗啡似乎是阿片受体光亲和标记的良好候选物。
