Farré A J, Colombo M, Gutiérrez B
Laboratorios Dr. Esteve, S.A., Department of Pharmacology, Barcelona, Spain.
Methods Find Exp Clin Pharmacol. 1989 May;11(5):303-7.
The methods most frequently employed for the study of analgesic activity of opiates are those based on thermal stimuli (hot-plate, tail-flick, TWR). These tests, however, are only sensitive for opiates which are pure agonists. In this work, we propose a modification of the TWR method capable of detecting analgesic activity in both agonist and agonist-antagonist opiates. In addition, non-opiate analgesics also show activity in this test. The ED50 (mg/kg, i.p.) of the substances studied, administered 30 min before commencement of the test, were as follows: buprenorphine: 0.02; methadone: 0.08; morphine: 1.9; pentazocine: 4.5; d-propoxyphene: 5.5; codeine: 7.6; pethidine: 9.2; zomepirac: 20.1; suprofen: 138.0; acetylsalicylic acid: 453.4. There was a statistically significant linear correlation between the results obtained by the proposed method (MTT) and those of some of the most frequently used methods for the study of analgesic agents (writhing induced by phenylbenzoquinone, acetic acid, acetylcholine bromide, hot-plate test and rat tail withdrawal test). The simplicity of the method makes it suitable for use in the battery of screening tests for analgesic activity of both narcotic and non-narcotic substances.
研究阿片类药物镇痛活性最常用的方法是基于热刺激的方法（热板法、甩尾法、扭体法）。然而，这些测试仅对纯激动剂阿片类药物敏感。在本研究中，我们提出了一种扭体法的改进方法，该方法能够检测激动剂和激动剂 - 拮抗剂阿片类药物的镇痛活性。此外，非阿片类镇痛药在该测试中也表现出活性。在测试开始前30分钟腹腔注射所研究物质的半数有效剂量（ED50，mg/kg）如下：丁丙诺啡：0.02；美沙酮：0.08；吗啡：1.9；喷他佐辛：4.5；右旋丙氧芬：5.5；可待因：7.6；哌替啶：9.2；佐美酸：20.1；舒洛芬：138.0；乙酰水杨酸：453.4。所提出的方法（MTT）得到的结果与一些研究镇痛药最常用方法（苯醌、乙酸、溴化乙酰胆碱诱导的扭体法、热板试验和大鼠甩尾试验）的结果之间存在统计学上显著的线性相关性。该方法的简单性使其适用于麻醉和非麻醉物质镇痛活性筛选试验组合。
