抗伤害感受测试对阿片类激动剂和部分激动剂的差异敏感性。
Differential sensitivity of antinociceptive tests to opioid agonists and partial agonists.
作者信息
Shaw J S, Rourke J D, Burns K M
机构信息
Bioscience Department, ICI Pharmaceuticals Division, Macclesfield, Cheshire.
出版信息
Br J Pharmacol. 1988 Oct;95(2):578-84. doi: 10.1111/j.1476-5381.1988.tb11679.x.
Abstract
- The antinociceptive activity of a range of opioid agonists and agonist-antagonist analgesics was determined in mice by use of the 55 degrees C hot plate and abdominal constriction assays. 2. Opioid agonists were approximately 10 times more effective in the abdominal constriction assay. 3. The agonist-antagonists produced analgesia only in the abdominal constriction assay, and antagonized the antinociceptive action of opioid agonists in the 55 degrees C hot plate test. 4. These differences were shown to be attributable to the different levels of stimulus employed in the two tests. 5. By comparing the antagonist potencies of the agonist-antagonists in the 55 degrees C hot plate test with their antinociceptive ED50 values in the abdominal constriction assay, an index of intrinsic activity was calculated.
摘要
- 通过使用55摄氏度热板法和腹部收缩试验，测定了一系列阿片类激动剂和激动-拮抗剂镇痛药在小鼠体内的抗伤害感受活性。2. 阿片类激动剂在腹部收缩试验中的效果约为热板法的10倍。3. 激动-拮抗剂仅在腹部收缩试验中产生镇痛作用，并在55摄氏度热板试验中拮抗阿片类激动剂的抗伤害感受作用。4. 这些差异表明是由于两种试验中所采用的刺激水平不同所致。5. 通过比较激动-拮抗剂在55摄氏度热板试验中的拮抗效力与其在腹部收缩试验中的抗伤害感受ED50值，计算出内在活性指数。
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