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在小鼠中,异丁嗪存在时吗啡的镇痛增强作用及分布

Analgesic potentiation and the distribution of morphine in the presence of triplennamine in mice.

作者信息

Bluhm R E, Evans M A, Zsigmond E K

出版信息

Life Sci. 1983;33 Suppl 1:673-6. doi: 10.1016/0024-3205(83)90592-1.

Abstract

Interest in the interaction of opioids and histamine antagonists arose from the observation that abusers of pentazocine and triplennamine experience a heroin-like euphoria that neither drug alone produces. The present study was conducted to evaluate the analgesic properties of the combination of the histamine antagonist, triplennamine (TRP), and morphine (MS). Analgesia was assessed using the hot plate at 55 degrees C and all drugs were administered intravenously. TRP had no analgesic effect. When a suboptimal dose of MS (3.5 mg/kg) was combined with TRP in a dosage range of 2.5-5 mg/kg, the latency in response to pain 10 minutes after drug administration was significantly increased and this potentiation was still evident 30 minutes after drug administration. Naloxone completely reversed the analgesia of MS and the MS-TRP combination. The distribution of 3H morphine in representative brain areas and plasma was not different in the presence or absence of triplennamine.

摘要

对阿片类药物与组胺拮抗剂相互作用的兴趣源于以下观察结果

喷他佐辛和曲吡那敏的滥用者会体验到一种海洛因样的欣快感,而这两种药物单独使用时均不会产生这种效果。本研究旨在评估组胺拮抗剂曲吡那敏(TRP)与吗啡(MS)联合使用的镇痛特性。使用55摄氏度的热板评估镇痛效果,所有药物均通过静脉注射给药。TRP没有镇痛作用。当次优剂量的MS(3.5毫克/千克)与2.5 - 5毫克/千克剂量范围内的TRP联合使用时,给药后10分钟对疼痛反应的潜伏期显著延长,并且在给药后30分钟这种增强作用仍然明显。纳洛酮完全逆转了MS和MS - TRP联合用药的镇痛作用。在有或没有曲吡那敏的情况下,3H吗啡在代表性脑区和血浆中的分布没有差异。

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