咪唑啉I_2受体研究进展

Progress in study of imidazoline I_2 receptors

咪唑啉I2 受体是新近发现的一种咪唑啉受体 ,根据其与阿米洛利的亲和力可进一步将其分为I2A和I2B两个亚型 ,主要分布于肾、脑和肝细胞的线粒体外膜上 ,其内源性配体是胍丁胺。许多证据提示咪唑啉I2 受体与单胺氧化酶 B具有高度同源性 ,但其与配体的结合位点不同于该酶的催化位点。激活咪唑啉I2 受体可能产生神经元保护、抗血管平滑肌增生及调节阿片功能等多种药理作用。咪唑啉I2 受体与抑郁症、帕金森病、亨廷顿病、阿片成瘾及阿尔茨海默病等疾病的发生有关。

Imidazoline I 2 receptor is one of newly found imidazoline receptors. Based on its binding characteristics with amiloride, I 2 receptor is further divided into I 2A and I 2B subtypes. I 2 receptor is located mainly on the outer membrane of mitochondria in kidney, brain and liver. The endogenous ligand of I 2 receptor is agmatine. Many studies indicate that I 2 receptor is structurally related to monoamine oxidase B (MAO B), but the binding site of I 2 receptor with its ligand is different from the catalyzed site of MAO B. Many pharmacological effects include neuro protective effect, inhibition of vascular smooth muscle proliferation and modulation of opioids functions are produced under activation of I 2 receptor. I 2 receptor is related to some diseases, such as depression, Parkinson′s disease, Huntington′s disease, opioid addiction and Alzheimer′s disease.