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目的：观察二氢埃托啡（ＤＨＥ）与阿片受体的结合情况．方法：采用放射配体受体结合实验，观察了［３Ｈ］ＤＨＥ与大鼠脑膜阿片受体的结合．结果：饱和实验显示［３Ｈ］ＤＨＥ的结合呈高亲和力单一位点，Ｋｄ＝０１９±００５ｎｍｏｌ·Ｌ－１，Ｂｍａｘ＝１１５±２１ｐｍｏｌ／ｇｐｒｏｔｅｉｎ．动力学实验表明［３Ｈ］ＤＨＥ与阿片受体结合极快，解离很慢．ＮａＣｌ１００ｍｍｏｌ·Ｌ－１＋鸟苷三磷酸（ＧＴＰ）５０μｍｏｌ·Ｌ－１可使［３Ｈ］ＤＨＥ的Ｋｄ值提高为７８７ｎｍｏｌ·Ｌ－１，Ｂｍａｘ值不变．激动剂和拮抗剂的竞争抑制实验均表明［３Ｈ］ＤＨＥ与μ阿片受体的亲和力大于δ和κ受体．结论：ＤＨＥ对μ阿片受体具有一定选择性．
Objective: To observe the binding of dihydroetorphine (DHE) to opioid receptors. Methods: Radioligand binding experiments were performed to observe the binding of [3H] DHE to the rat cerebellar opiate receptors. Results: Saturation experiments showed that the binding of [3H] DHE showed a high affinity single site with Kd = 019 ± 005 nmol·L-1 and Bmax = 115 ± 21 pmol / gprotein. Kinetic experiments show that [3H] DHE binds to opioid receptors very fast and dissociates very slowly. The Kd value of [3H] DHE increased to 787 nmol·L-1 with 100 mmol·L -1 NaCl and 50 μmol·L -1 guanosine triphosphate (GTP). Competition inhibition experiments with agonists and antagonists both showed that [3H] DHE had greater affinity for mu opioid receptors than both δ and κ receptors. Conclusion: DHE has a certain selectivity for mu opioid receptor.