咪唑啉I_2受体研究进展

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。

Progress in study of imidazoline I2 receptors

Imidazoline I₂ receptor is one of newly found imidazoline rece ptors. Based on its binding characteristics with amiloride, I₂ receptor is f urth er divided into I_2A and I_2B subtypes. I₂ receptor is located mainly on the outer membrane of mitochondria in kidney, brain and liver. The endogeno us ligand of I₂ receptor is agmatine. Many studies indicate that I₂ receptor is structurally related to monoamine oxidase-B (MAO-B), but the binding site of I₂ receptor with its ligand is different from the catalyzed site of MAO-B. Many pharmacological effects include neuro-protective effect, inhibition of vas cular smooth muscle proliferation and modulation of opioids functions are produced under activation of I₂ receptor. I₂ receptor is related to some diseases, such as depression, Parkinson′s disease, Huntington′s disease, opioid addiction and Alzheimer′s disease.