双向阿片功能调节剂：胍丁胺

近年研究表明某些药物尽管不能与阿片受体发生相互作用，但能对阿片药理作用产生重要的调节．特别是有些药物能对阿片功能产生双向调节作用，即增强阿片镇痛，对抗阿片耐受和躯体依赖．我们将这些不与阿片受体发生作用，但具有双向调节阿片功能的药物称之为双向阿片功能调节剂(biphasic opioid function modulator，BOFM)．基于我们的研究工作，可以认定胍丁胺就是一个典型的双向阿片功能调节剂．胍丁胺本身有弱的镇痛作用，它能增强吗啡镇痛，对抗吗啡耐受和依赖：胍丁胺产生上述作用的主要机制与抑制阿片长期作用下在阿片受体信号转导系统产生的代偿性适应过程相关．

A biphasic opioid function modulator: agrnatine

Recently it has been revealed that some agents that are not able to interact with opioid receptors play an important role in regulating the pharmacological actions of opioids. Especially, some of them show biphasic modulation on opioid functions, which enhance opioid analgesia, but inhibit tolerance to and substance dependence on opioids. We would like to call these agents which do not interact with opioid receptors, but do have biphasic modulation on opioid functions as biphasic opioid function modulator (BOFM). Mainly based on our results, agmatine is a typical BOFM. Agmatine itself was a weak analgesic which enhanced analgesic action of morphine and inhibited tolerance to and dependence on opioid. The main mechanisms of agmatine were related to inhibition of the adaptation of opioid receptor signal transduction induced by chronic treatment of opioid.