Identification of small molecule RXFP3 ligands

松弛素-3是松弛素/胰岛素样家族肽，其主要在未定核中表达。不安核是一种应激反应性脑干核团，广泛投射到涉及焦虑、抑郁、进食、成瘾、疼痛中枢处理和认知的前脑区域。松弛素-3的同源受体是RXFP 3，使用松弛素-3和松弛素-3衍生肽激动剂和拮抗剂对RXFP 3功能的研究表明，RXFP 3是治疗焦虑症、抑郁症和疼痛等的潜在靶标。新的小分子RXFP 3激动剂和拮抗剂将是阐明松弛素-3的功能及其对RXFP 3受体的作用的有价值的工具。 在本报告所述期间，该团队制定了一项研究计划，并接收了表达RXP 3的细胞系，以开始适应一种检测方法，从而实现高通量筛选。

Relaxin-3 is a relaxin/insulin-like family peptide that is expressed predominantly in the nucleus incertus. The nucleus incertus is a stress-responsive brainstem nucleus that projects widely to forebrain regions involved in anxiety, depression, eating, addiction, central processing of pain, and cognition. The cognate receptor for relaxin-3 is RXFP3, and studies of RXFP3 function using relaxin-3 and relaxin-3-derived peptide agonists and antagonists indicate that RXFP3 is a potential target for the treatment of anxiety disorders, depression and pain, among others. Novel small molecule RXFP3 agonists and antagonists will be valuable tools to elucidate the functions of relaxin-3 and its actions at RXFP3 receptors. During the reporting period, the team established a research plan and received RXP3-expressing cell lines to begin adaptation of an assay to enable high-throughput screening.