胍丁胺的镇痛作用及拮抗吗啡的耐受性和物质依赖性

目的：探讨胍丁胺对阿片类药物的耐受和物质依赖的拮抗作用。方法：利用行为药理学实验观察胍丁胺对上述作用的影响，使用受体阻滞剂，测定cAMP浓度的改变、一氧化氮合酶（NOS）活性。结果：胍丁胺具有镇痛作用；增强吗啡的镇痛作用；及拮抗吗啡的耐受性和物质依赖性作用；咪唑克生可阻断其作用。胍丁胺能阻止cAMP的上调和戒断时的超射，并抑制NOS的活性。结论；胍丁胺可抑制吗啡的戒断症状，其可能的机制是通过激活咪唑啉受体抑制cAMP的上调和戒断时的超射及抑制NOS的活性。

Analgesic effect of agmatine and its antagonism on morphine tolerance and substance dependence

Objective:To investigate the antagonism effects of agmatine on morphine tolerance and substance dependence.Methods:The antagonism effects of agmatine on morphine tolerance and substance dependence were observed by behavioral pharmacological approches use of receptor antagonists,measurements of concentration of cAMP and NOS activity.Results:Agmatine has analgesic effects,potentiates morphine analgesia,prevents the tolerance and substance dependence induced by morphine.These effects of agmatine are antagonized by idazoxan.Agmatine prevents the up-regulation and over-shooting of cAMP after morphine withdrawal and inhibits NOS activity.Conclusion:The results suggest that agmatine may inhibit morphine abstinence syndrome,the possible mechanisms include activation of imidazoline receptors,prevention of cAMP up-regulation and over-shooting,and inhibition of NOS activity.