胍丁胺在体外对豚鼠回肠的吗啡耐受性和依赖性具有抑制作用。
Agmatine inhibited tolerance to and dependence on morphine in guinea pig ileum in vitro.
作者信息
Li J, Li X, Pei G, Qin B Y
机构信息
Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing, China.
出版信息
Zhongguo Yao Li Xue Bao. 1998 Nov;19(6):564-8.
AIM
To observe effect of agmatine (Agm) on tolerance to and substance dependence on morphine (Mor) in guinea pig ileum longitudinal muscle (GPILM).
METHODS
The experiment was performed in electric field stimulation (EFS) test in vitro.
RESULTS
Mor inhibited twitch contractions of GPILM induced by EFS [IC50 = 140 (107-182) nmol.L-1]. Incubation of GPILM with Mor 270 nmol.L-1 for 8 h evoked a 37-fold increase in IC50 of Mor (tolerance) and a contractile response to naloxone (Nal, substance dependence). When the preparations were coincubated with Mor + Nal and Mor + Agm, Mor lost the ability to induce tolerance and inhibited the contractile responses of the preparations to Nal by 90% and 75%, respectively. These effects of Agm could be almost completely antagonized by idazoxan.
CONCLUSION
Agm prevented the development of tolerance to and substance dependence on Mor in GPILM in vitro by activation of imidazoline receptors.
目的
观察胍丁胺（Agm）对豚鼠回肠纵肌（GPILM）对吗啡（Mor）耐受性及物质依赖性的影响。
方法
实验在体外电场刺激（EFS）试验中进行。
结果
Mor抑制EFS诱导的GPILM抽搐收缩[IC50 = 140（107 - 182）nmol·L-1]。将GPILM与270 nmol·L-1的Mor孵育8小时，可使Mor的IC50增加37倍（耐受性），并引发对纳洛酮（Nal，物质依赖性）的收缩反应。当制剂与Mor + Nal和Mor + Agm共同孵育时，Mor失去诱导耐受性的能力，并分别抑制制剂对Nal的收缩反应90%和75%。Agm的这些作用几乎可被咪唑克生完全拮抗。
结论
Agm通过激活咪唑啉受体，在体外阻止了GPILM对Mor耐受性及物质依赖性的形成。
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