设计、合成了一种新的吗啡受体显像剂。选用吗啡拮抗剂特培洛啡（ｄｉｐｒｅｎｏｒｐｈｉｎｅ，ＤＰＮ），经乙酰化选择性保护苯环３位—ＯＨ，将乙烯锡烷作为弥补基引入ＤＰＮ分子７α支链淑醇基团位置，采用碘代锡烷标记法一步合成碘烷ＤＰＮ（７αｏｉｏｄｏａｌｙｌｄｉｐｒｅｎｏｒｐｈｉｎｅ，即７αｏＩＡＤＰＮ）。其标记率达９０％，比活度为８０ＴＢｑ／ｍｍｏｌ，放化纯度大于９５％。体外吗啡受体结合分析表明其具有很高的亲和力（Ｋｉ＝０．４ｎｍｏｌ／Ｌ）。结果表明：新合成的碘标记吗啡配体适合于ＳＰＥＣＴ活体吗啡受体显像研究。 Design and synthesis of a new morphine receptor imaging agent. The morphine antagonist diprenorphine (DPN) was selected to selectively protect the 3-position of the benzene ring through acetylation. The vinylstannane was introduced into the 7α-branch chain of DPN molecule as a prosthetic group, Alkane marker synthesis of one-step iodine DPN (7α  o-iodoalyldiprenorphine, 7α  o  IA  DPN). The labeling rate of 90%, specific activity of 80TBq / mmol, radiochemical purity greater than 95%. In vitro morphine receptor binding assay showed high affinity (Ki = 0.4 nmol / L). The results showed that the newly synthesized iodine labeled morphine ligand was suitable for SPECT morphine receptor imaging.