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研究了阿片类药物在豚鼠离体回肠中的交互依赖性和交互耐受性.豚鼠回肠分别与羟甲芬太尼(OMF1nmol·L-1),D-Ala2,D-Leu5-脑啡肽(DADLE,0.3μmol·L-1)或U50488H(50nmol·L-1)在37℃温育4h,它们相互及自身均能抑制纳洛酮(0.1μmol·L-1)或Mr2266(0.1μmol·L-1)引起的戒断性收缩.它们也能自身预先阻断戒断性收缩的产生.U50488H能预先阻断OMF,DADLE温育后纳洛酮所产生的戒断性收缩,但后两者不能预先阻断U50488H温育后由Mr2266所产生的戒断性收缩,并且OMF和DADLE之间也不能相互阻断.豚鼠回肠分别与OMF(1nmol·L-1),DADLE(0.3μmol·L-1)在37℃温育2h后,对去甲吗啡(NM),OMF,DADLE的敏感性明显下降,浓度反应曲线右移,但对U50488H不产生耐受.在U50488H(10nmol·L-1)中温育1h的回肠,对U50488H的敏感性下降,浓度反应曲线右移,但对OMF,NM,DADLE的敏感性不变.这些结果表明豚鼠回肠中μ,κ阿片受体是分离的.
The interactive dependence and interactive tolerance of opioids in isolated ileum of guinea pigs were studied. The ileum of guinea pigs were significantly inhibited by OMF1nmol·L-1, D-Ala2, D-Leu5-enkephalin (0.3μmol·L-1) or U50488H (50nmol·L- ℃ incubated for 4h, they can inhibit each other and their own naloxone (0.1μmol·L-1) or Mr2266 (0.1μmol·L-1) induced withdrawal contractility. They can also block the withdrawal of withdrawal in advance. U50488H can pre-block the abstinence produced by naloxone after OMF and DADLE incubation, but the latter two can not pre-block withdrawal-induced contractions caused by Mr2266 after U50488H incubation and the difference between OMF and DADLE Neither can we block each other. The sensitivities of NMD, OMF and DADLE to guinea pig ileum were significantly decreased with OMF (1nmol·L-1) and DADLE (0.3μmol·L-1) respectively at 37 ℃ for 2h, The curve moves to the right, but no tolerance to U50488H. In U50488H (10nmol·L-1) incubated for 1h in the ileum, the sensitivity of U50488H decreased, the concentration response curve shifted to the right, but the sensitivity of OMF, NM, DADLE remained unchanged. These results indicate that the μ, κ opioid receptors are isolated in the ileum of guinea pigs.