Discriminative stimulus effects of narcotics: evidence for multiple receptor-mediated actions.
Discriminative stimulus effects of narcotics: evidence for multiple receptor-mediated actions.
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DOI：
10.1016/0024-3205(81)90311-8
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发表时间：
1981-04
期刊：
影响因子：
6.1
通讯作者：
S. Herling;J. Woods
中科院分区：
文献类型：
--
作者：
S. Herling;J. Woods
麻醉剂的区别性刺激效应的研究结果与多个受体介导这些化合物的作用的假设是一致的。在大鼠中，至少存在三个子集的区分效应，尽管有些药物似乎具有超越一个以上子集的效应。例如，吗啡样麻醉剂（μ激动剂）的辨别作用通常与κ激动剂（如酮唑辛）产生的辨别作用以及苯环己哌啶样激动剂（如SKF-10，047和环唑辛）产生的辨别作用明显不同。然而，据报道，环佐辛与吗啡（45）和芬太尼（17）一样具有辨别作用，并且除了苯环己哌啶样辨别作用外，似乎还具有κ样辨别作用。纯麻醉剂拮抗剂阻断这些化合物的区分作用的相对能力也为这些药物的不同药理作用提供了证据。在大鼠中，吗啡的辨别作用被纳洛酮的剂量阻断，纳洛酮的剂量比阻断环唑辛的辨别作用所需的剂量小得多（44）。苯环利定的辨别作用完全不受纳洛酮的影响（63）。
Results of studies on the discriminative stimulus effects of narcotics are consistent with the hypothesis that multiple receptors mediate the effects of these compounds. In the rat, at least three subsets of discriminative effects exist, although some drugs appear to have effects that transcend more than one subset. The discriminative effects of morphine-like narcotics (μ agonists), for example, are often clearly distinguishable from the discriminative effects produced by κ agonists, such as ketazocine, and from those produced by phencyclidine-like agonists, such as SKF-10,047 and cyclazocine. Cyclazocine, however, has been reported to have discriminative effects in common with morphine (45) and fentanyl (17) and appears to have κ-like, in addition to phencyclidine-like, discriminative effects. The relative ability of pure narcotic antagonists to block the discriminative effects of these compounds also provides evidence for distinct pharmacologic actions of these drugs. In the rat, the discriminative effects of morphine are blocked by doses of naloxone that are considerably smaller than those that are needed to block the discriminative effects of cyclazocine (44). The discriminative effects of phencyclidine are not altered at all by naltrexone (63).