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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Opioid antagonist profile of SC nor-binaltorphimine in the formalin paw assay.
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Opioid antagonist profile of SC nor-binaltorphimine in the formalin paw assay.

机译：福尔马林爪测定法中，SC去甲双甲托非明的阿片类拮抗剂概况。

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The antinociceptive effects of mu and kappa agonists were examined after the systemic administration of the opioid antagonists nor-binaltorphimine (nor-BNI) and naloxone in the late response or tonic nociceptive phase of the mouse formalin assay. Initially, SC morphine (ED50, 0.97 mg/kg), racemic U-50488H (ED50, 0.79 mg/kg), (-)U-50488 (ED50, 0.41 mg/kg), and another agonist PD 117,302 (ED50, 0.28 mg/kg) were found to produce graded increases in the level of antinociception as measured by this procedure; naloxone, administered immediately before morphine and U-50488H, antagonized their antinociceptive actions. The effects of morphine and U-50488H then were evaluated 10 min to 96 h after the administration of nor-BNI. Subcutaneous nor-BNI at 30.0 mg/kg, but not at 3.0 or 10.0 mg/kg, attenuated the antinociceptive effects of morphine and U-50488H when the interval separating nor-BNI and the agonists was kept constant at 1 h. Time-course analysis of the effects of combinations of nor-BNI with morphine ledto irregular findings: 10.0 mg/kg of nor-BNI lessened the effects of morphine (2.0 mg/kg) if the dosing interval was 10 min, whereas 30.0 mg/kg of nor-BNI attenuated the effects of morphine (2.0 mg/kg) if the dosing interval was 1 or 4 h; 10.0 mg/kg of nor-BNI also diminished the antinociceptive effects of U-50488H (1.7 mg/kg) only if the interval spacing the two drugs was 24 h. In comparison, a threefold higher dose of nor-BNI (30.0 mg/kg) reduced the effects of U-50488H (1.7 mg/kg) if the interval was 1 h or more. In these latter experiments, the antagonist effects of SC nor-BNI (30.0 mg/kg) were evident up to 96 h posttreatment. These results show that the mu opioid antagonist activity of nor-BNI is variable and that the kappa opioid antagonist selectivity of nor-BNI is a function of dose and treatment interval and is long-lasting even after systemic administration.
机译：在小鼠福尔马林试验的晚期反应或强直伤害感受阶段中，系统性给予阿片样物质拮抗剂去甲双萘酚胺（nor-BNI）和纳洛酮后，检查了mu和kappa激动剂的抗伤害作用。最初使用SC吗啡（ED50，0.97 mg / kg），外消旋U-50488H（ED50，0.79 mg / kg），（-）U-50488（ED50，0.41 mg / kg）和另一种激动剂PD 117,302（ED50，0.28）如按此程序测量，发现mg / kg的抗伤害性水平会逐步增加;在吗啡和U-50488H之前立即使用的纳洛酮拮抗其抗伤害感受作用。然后在给予nor-BNI后10分钟至96小时内评估吗啡和U-50488H的作用。当将nor-BNI和激动剂分开的间隔保持恒定在1 h时，皮下的nor-BNI浓度为30.0 mg / kg，而不是3.0或10.0 mg / kg时，减弱了吗啡和U-50488H的抗伤害感受。 nor-BNI与吗啡组合的时程分析导致结果不规则：如果给药间隔为10分钟，则10.0 mg / kg的nor-BNI会降低吗啡（2.0 mg / kg）的作用，而30.0 mg / kg如果给药间隔为1或4小时，则kg的nor-BNI会减弱吗啡（2.0 mg / kg）的作用;仅当两种药物的间隔时间为24 h时，10.0 mg / kg的nor-BNI才能减弱U-50488H（1.7 mg / kg）的镇痛作用。相比之下，如果间隔为1小时或更长时间，则nor-BNI（30.0 mg / kg）的三倍高剂量会降低U-50488H（1.7 mg / kg）的作用。在这些后面的实验中，SC nor-BNI（30.0 mg / kg）的拮抗作用在治疗后长达96 h时都是明显的。这些结果表明，nor-BNI的μ阿片样物质拮抗剂活性是可变的，并且nor-BNI的κ阿片样物质拮抗剂选择性是剂量和治疗间隔的函数，并且即使在全身给药后也持久。

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