The discovery of a highly selective putative sigma-1 (σ1) receptor agonist, PRE-084, has revealed the numerous potential uses of this receptor subtype as a therapeutic target. While much work has been devoted to determining the role of σ1 receptors in normal and pathophysiological states in the nervous system, recent work suggests that σ1 receptors may be important for modulating functions of other tissues. These discoveries have provided novel insights into σ1 receptor structure, function, and importance in multiple intracellular signaling mechanisms. These discoveries were made possible by σ1 receptor-selective agonists such as PRE-084. The chemical properties and pharmacological actions of PRE-084 will be reviewed here, along with the expanding list of potential therapeutic applications for selective activation of σ1 receptors.

高度选择性的推定 sigma-1 (σ1) 受体激动剂 PRE-084 的发现揭示了该受体亚型作为治疗靶点的众多潜在用途。虽然许多工作致力于确定 σ1 受体在神经系统正常和病理生理状态中的作用，但最近的工作表明，σ1 受体可能对调节其他组织的功能很重要。这些发现为 σ1 受体的结构、功能和在多种细胞内信号传导机制中的重要性提供了新的见解。σ1 受体选择性激动剂（如 PRE-084）使这些发现成为可能。本文将回顾 PRE-084 的化学特性和药理作用，以及选择性激活 σ1 受体的潜在治疗应用的扩展列表。