反向激动剂：受体研究中的一个新发现

静息时就有一部分受体处于激活性状它们与非激活状态的受体处于动态平衡状态之中。某些原来认为的受体拮抗对Ｒ的亲和性远远高于对Ｒ的亲和性,导致动态平衡中的Ｒ数量减少,因而产生生物效应,对某些受体突变或爱 体过度表达引起的疾病,反向激动剂具有应用前景。

Inverse agonist: a novel discovery in receptor research

There is a part of unligated receptors in a state of activity (R*). The active (R*) and inactive (R) receptors exist in equilibrium. Some antagonists have a higher affinity with R as compared with R*, resulting in a decrease in the proportion of R* in the equilibrium, and inducing a biological response opposite to those of agonist. These antagonists are termed inverse agonists. In some diseases caused by receptor mutation or over expression, the therapeatic benefits of inverse agonist encourage further exploration.