正确理解反向激动剂  

A correct understanding of inverse agonists

作　　者：于瑞红[1] 曹永孝[1] 

机构地区：[1]西安交通大学医学部药理学系,陕西西安710061

出　　处：《医学争鸣》2016年第2期52-54,共3页Negative

摘　　要：反向激动剂是作用于受体的新的药物类型,对受体有亲和力,而无内在活性。由于其不激动受体,不具备激动剂的特性,因而归类于激动剂欠妥。反向激动剂无内在活性,通过拮抗受体产生效应,因而具有拮抗剂的特性。反向激动剂产生效应的前提是受体的固有活性,正如拮抗剂产生效应必须有激动剂存在一样。反向激动剂拮抗受体的固有活性,拮抗剂拮抗激动剂的效应,均产生与相应激动剂作用方向相反的效应。拮抗剂主要用于激动剂活性增高的情况,而反向激动剂是治疗固有活性增强相关疾病的理想药物。Inverse agonists are a new category of drugs acting on receptors.They have an affinity for receptor,but have no intrinsic activity.Because inverse agonists don’t possess the characteristic of activating receptors,it isn’t proper to classify them as agonist.Because inverse agonists exert effects through antagonizing receptors,they possess the characteristic of antagonist.Constitutive activity of receptors is the premise of inverse agonists’ effects,which is the same as that the existence of agonist is necessary for antagonists’ effects.Inverse agonists antagonize the constitutive activity of receptors,and antagonists antagonize the effect of the corresponding agonists;their effects are all opposite the effects of the corresponding agonists.Antagonists are usually used when the action of agonists increases;however,inverse agonists are the ideal drugs to treat the diseases with enhanced constitutive activity.

关 键 词：反向激动剂 固有活性 受体学说 G蛋白耦联受体 

分 类 号：R961[医药卫生—药理学]