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整体动物测定阿片类药物的身体依赖性耗药多、费时,因此有必要建立体外模型用于药物初筛。我们在豚鼠回肠上建立一个快速简便地测定阿片类药物依赖性的体外模型,并且应用此模型研究阿片受体亚型选择性配体的交叉依赖性。豚鼠回肠和阿片类药物在37℃孵育1-6 h后,拮抗剂纳洛酮可引起戒断性收缩。戒断性收缩的高度随孵育时间的延长而迅速增加,并且直接依赖于培养液中阿片类药物的浓度和催促的纳洛酮浓度。成瘾性较弱的药物如烯内吗啡、度冷丁和羟甲芬太尼的戒断性收缩明显弱于吗啡、芬太尼和υ50488H的戒断性收缩。
It is time-consuming to determine the body-dependence of opioids in whole animals. Therefore, it is necessary to establish an in vitro model for drug screening. We established an in vitro model of opioid dependence in guinea pig ileum that was quick and easy to determine and used this model to study the cross-dependence of opioid receptor-selective ligands. After the guinea pig ileum and opioids were incubated for 1-6 h at 37 ° C, the antagonist naloxone caused abstinence contractions. The height of abstinence contractions increases rapidly with increasing incubation time and is directly dependent on the concentration of opioid in the culture and the urinary naloxone concentration. Addictive weaker drugs such as enamelimine, meperidine and oxymetazidine abstinence contraction was significantly weaker than morphine, fentanyl and υ 50488H withdrawal withdrawal.