别名 somatostatin receptor 2、Somatostatin receptor type 2、SRIF-1 + [5] |
简介 Receptor for somatostatin-14 and -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase. In addition it stimulates phosphotyrosine phosphatase and PLC via pertussis toxin insensitive as well as sensitive G proteins. Inhibits calcium entry by suppressing voltage-dependent calcium channels. Acts as the functionally dominant somatostatin receptor in pancreatic alpha- and beta-cells where it mediates the inhibitory effect of somatostatin-14 on hormone secretion. Inhibits cell growth through enhancement of MAPK1 and MAPK2 phosphorylation and subsequent up-regulation of CDKN1B. Stimulates neuronal migration and axon outgrowth and may participate in neuron development and maturation during brain development. Mediates negative regulation of insulin receptor signaling through PTPN6. Inactivates SSTR3 receptor function following heterodimerization. |
靶点 |
作用机制 SSTR2拮抗剂 |
非在研适应症- |
最高研发阶段批准上市 |
首次获批国家/地区 加拿大 |
首次获批日期2022-02-24 |
靶点 |
作用机制 SSTR2拮抗剂 |
在研适应症 |
最高研发阶段批准上市 |
首次获批国家/地区 欧盟 [+3] |
首次获批日期2017-09-26 |
开始日期2025-08-01 |
开始日期2025-05-07 |
申办/合作机构 |