Quantification of the analgesic activity of narcotic antagonists by a modified hot-plate procedure.
Quantification of the analgesic activity of narcotic antagonists by a modified hot-plate procedure.
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发表时间：
1975-03
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通讯作者：
J. O'Callaghan;S. Holtzman
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作者：
J. O'Callaghan;S. Holtzman
吗啡及其麻醉拮抗剂pentazocine， cyclazocine， leallorphan和nalorphine的镇痛活性，在大鼠中使用两个热板进行评估：一个保持在49.5℃，另一个保持在“标准”54.5℃。对于吗啡耐受和不耐受受试者，使用49.5℃热板的吗啡镇痛效果明显大于使用54.5℃热板的吗啡镇痛效果。使用49.5℃热板测试的所有麻醉拮抗剂均观察到剂量相关效应；只有最高剂量的戊唑嗪在54.5℃的热板上表现出活性。纳洛酮（3.0 mg/kg）可拮抗吗啡和所有麻醉拮抗剂的镇痛作用，但在49.5℃高温实验中，当剂量高达30 mg/kg时，纳洛酮本身没有活性。在49.5摄氏度的实验板中，阿司匹林也没有作用，而毒豆碱只有在产生严重运动缺陷的剂量下才会增加潜伏期。建议用低温热板评价麻醉拮抗剂在大鼠体内的镇痛活性。这个简单的程序提供的结果与剂量相关，可量化，可重复，大幅度和特异性。
The analgesic activity of morphine and the narcotic antagonists, pentazocine, cyclazocine, levallorphan and nalorphine, was assessed in the rat using two hot plates: one maintained at 49.5 degrees C and the other at the "standard" 54.5 degrees C. The analgesic effects of morphine using the 49.5 degrees C hot plate were of a significantly greater magnitude than its effects using the 54.5 degrees C hot plate for both nontolerant and morphine-tolerant subjects. Dose-related effects were observed with all of the narcotic antagonists tested using the 49.5 degrees C hot plate; only the highest dose of pentazocine exhibited activity using the 54.5 degrees C hot plate. Naloxone (3.0 mg/kg) antagonized the analgesic effects of morphine and all of the narcotic antagonists, but was without activity itself when tested using the 49.5 degrees C hot plate at doses as high as 30 mg/kg. Aspirin was also inactive using the 49.5 degrees C plate, whereas physostigmine increased latencies only at a dose that produced severe motor deficit. A low temperature hot plate is recommended for evaluating the analgesic activity of narcotic antagonists in the rat. This simple procedure provides results which are dose-related, quantifiable, reproducible, of a large magnitude and specific.