The sigma receptor (σR) family has been considered mysterious for a long time. In fact, the σ2R subtype has been cloned only recently, revealing its identity as TMEM97, a NPC1-binding protein involved in cholesterol biosynthesis and implicated in the pathogenesis of cancer and neurologic disorders. With the aim of developing new chemical entities gifted with σR affinity, herein we report the design and synthesis of new piperidine-based alkylacetamide derivatives with mixed affinity towards both σ1 and σ2R subtypes.

中文翻译：

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新的基于哌啶的衍生物作为sigma受体配体。合成与药理评价

长期以来，人们一直认为sigma受体（σR）家族是神秘的。实际上，σ2R亚型直到最近才被克隆，揭示了其与TMEM97的同一性，TMEM97是一种NPC1结合蛋白，参与胆固醇的生物合成，并与癌症和神经系统疾病的发病机理有关。为了开发具有σR亲和力的新化学实体，我们在此报告了对σ1和σ2R亚型具有混合亲和力的新哌啶基烷基乙酰胺衍生物的设计和合成。