Sigma（σ）受体与CNS许多神经精神疾病、可卡因成瘾以及学习记忆等密切相关，目前已成为发展神经精神疾病药物的新靶点。同时，σ受体还在许多肿瘤细胞系中高度表达，为肿瘤的早期诊断提供了灵敏的分子探针。本文设计了125I、18F标记的吲哚类σ2受体放射性示踪剂，合成了相应的稳定配体，并对其进行了体外生物评价。此外，在以往研究的基础上，进一步优化了苯并螺环哌啶化合物Spiro-I的合成条件以及[125I]Spiro-I的标记条件，并对其进行了一系列体内生物评价。

Sigma (σ) receptors have been involved in neuropsychiatric disorders, drug-abuse as well as learning and memory process. In addition, σ receptors also have high expression in many tumor cells, which provide sensitive molecular probes to the early diagnosis of the tumors. In this paper, the design of 125I- and 18F-labelled σ2 receptor indole radiotracers, synthesis of the corresponding reference compounds, and biological evaluation in vitro of them were performed. Moreover, on the base of the previous studies, the synthetic method of Spiro-I and the labelling condition of [125I]Spiro-I were further optimized. A series of biological evaluations of [125I]Spiro-I in vivo were performed.