别名 κ阿片样受体、K-OR-1、Kappa-type opioid receptor + [6] |
简介 G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synthetic opioids and for the psychoactive diterpene salvinorin A. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Plays a role in the perception of pain. Plays a role in mediating reduced physical activity upon treatment with synthetic opioids. Plays a role in the regulation of salivation in response to synthetic opioids. May play a role in arousal and regulation of autonomic and neuroendocrine functions. |
作用机制 κ opioid receptor激动剂 |
最高研发阶段批准上市 |
首次获批国家/地区 美国 |
首次获批日期2021-08-23 |
作用机制 κ opioid receptor激动剂 [+1] |
原研机构 |
非在研适应症 |
最高研发阶段批准上市 |
首次获批国家/地区 中国台湾 |
首次获批日期2016-07-11 |
作用机制 δ opioid receptor拮抗剂 [+2] |
在研机构 |
原研机构 |
最高研发阶段批准上市 |
首次获批国家/地区 美国 |
首次获批日期2015-05-27 |
开始日期2025-04-01 |
开始日期2025-02-01 |
申办/合作机构 |
开始日期2025-01-31 |