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阿片受体研究自1992年δ受体克隆成功；发展迅速，1993年μ、κ受体也克隆成功。1994年发现阿片孤儿受体ORL－1，1995年即找到ORL－1的内源性配体Nociceptin（OrphaninFQ）。1996年成功地应用基因敲出技术制成缺乏μ受体基因的小鼠，证明吗啡镇痛及成痛形成通过μ受体。1997年又发现了μ受体内源性配体endomorphine－1和endomorphine－2。我国学者研究成功的羟甲芬太尼的八个立体异构体合成，发现F－9202和F－9204是当前μ受体选择性最高的配体。计算机模拟μ受体三维结构及定点突变工作证明Tyr－148及His－319是羟甲芬太尼的结合位点。这些进展反映了当前神经分子药理研究的动向。
Opioid receptor research since 1992 δ receptor cloning success; rapid development in 1993, μ, κ receptor cloning success. Opposed opiate orphan receptor ORL-1 was found in 1994 and was identified as Nociceptin (OrphaninFQ) by OriGene in 1995. The successful application of gene knockout technology in 1996 to mice lacking the mu receptor gene demonstrated morphine analgesia and pain formation through the mu receptor. In 1997, we found endomorphine-1 and endomorphine-2, which are endogenous ligands of μ receptor. Our scholars study the successful synthesis of eight stereoisomers of oxymetazidine and found that F-9202 and F-9204 are the most selective ligands for μ receptor. Computer simulation of the three-dimensional structure of μ receptor and site-directed mutagenesis proved that Tyr-148 and His-319 are the binding sites for oxymetazidine. These advances reflect the current trend of neural molecular pharmacology.