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通过受体发挥作用的药物,据其效应,可分为激动剂、部分激动剂和拮抗剂。其中,激动药能激活受体,产生生物效应;拮抗剂不能引起效应,却可阻滞激动剂(递质或药物)的作用。那么,决定药物归属的因素是什么?是药物本身的固有特性,即内在活性,或叫药物与受体结合后激动受体的能力。 按照Ariens修改的受体占领学说,在理论上,完全激动剂具有强的内在活性,以1表示;部分激动剂在0～1之间;拮抗剂内在活性为0。与完全激动剂不同,部分激动剂具有激动剂和拮抗剂两种特性。部分激动剂与完全激动剂相互作
Drugs that act through receptors, depending on their effects, can be classified as agonists, partial agonists and antagonists. Among them, agonists can activate receptors, resulting in biological effects; antagonists can not cause effects, but can block the agonist (transmitter or drug) role. So what are the factors that determine drug attribution? It is the intrinsic property of the drug itself, that is intrinsic activity, or the ability of the drug to agonize receptors upon binding to the receptor. According to Ariens modified receptor occupational theory, in theory, full agonists have a strong intrinsic activity, expressed as 1; partial agonists in the 0 to 1; antagonist intrinsic activity of 0. Unlike full agonists, partial agonists have both agonist and antagonist properties. Partial agonists interact with complete agonists