A CLASSIFICATION OF OPIATE RECEPTORS THAT MEDIATE ANTINOCICEPTION IN ANIMALS
A CLASSIFICATION OF OPIATE RECEPTORS THAT MEDIATE ANTINOCICEPTION IN ANIMALS
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DOI：
10.1111/j.1476-5381.1980.tb07041.x
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发表时间：
1980-07
影响因子：
7.3
通讯作者：
M. Tyers
中科院分区：
文献类型：
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作者：
M. Tyers
为了研究介导抗痛觉的阿片受体，在小鼠和大鼠中测定了阿片镇痛药物在不同痛觉刺激下的活性谱。在使用热作为伤害性刺激的试验中，μ -阿片受体激动剂，如吗啡、哌替啶和右丙氧芬，具有陡峭的平行剂量反应曲线，能够达到最大的效果。此外，在热试验中，这些药物的抗痛觉效力比与人类镇痛药相似。κ‐激动剂，如乙基氯他嗪、纳洛啡、Mr2034和戊唑嗪，除引起镇静和运动失能的剂量外，基本上对热伤害性无活性。在扭动和爪压试验中，μ‐和κ‐激动剂均产生陡峭且平行的剂量-反应曲线。由此可见，μ‐和κ‐阿片受体均介导动物的抗痛觉作用，镇痛药物与这些受体的相互作用可根据它们对不同性质的痛觉刺激的抗痛觉活性进行分类。
1 To investigate the opiate receptors that mediate antinociception, the activity profiles of opioid analgesic drugs have been determined against different nociceptive stimuli in the mouse and rat. 2 In tests that employ heat as the nociceptive stimulus, μ‐opiate receptor agonists, such as morphine, pethidine and dextropropoxyphene, had steep and parallel dose‐response curves and were capable of achieving maximum effects. In addition, the antinociceptive potency ratios of these drugs in heat tests were similar to those for analgesia in man. 3 The κ‐agonists, such as ethylketazocine, nalorphine, Mr2034 and pentazocine, were essentially inactive against heat nociception except at doses that caused sedation and motor incapacitation. 4 In the writhing and paw pressure tests both μ‐ and κ‐agonists produced steep and parallel dose‐response curves. 5 It is concluded that both μ‐ and κ‐opiate receptors mediate antinociception in animals and that the interactions of analgesic drugs with these receptors may be classified in terms of their antinociceptive activities against qualitatively different nociceptive stimuli.