The pharmacology of butorphanol, a 3,14-dihydroxymorphinan narcotic antagonist analgesic.
The pharmacology of butorphanol, a 3,14-dihydroxymorphinan narcotic antagonist analgesic.
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布托啡诺的药理学，一种 3,14-二羟基吗啡喃麻醉拮抗剂镇痛药。
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发表时间：
1976
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通讯作者：
Bierwagen Me
中科院分区：
文献类型：
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作者：
A. Pircio;Gylys Ja;Cavanagh Rl;J. Buyniski;Bierwagen Me
布托啡诺是一种新的全合成吗啡喃，与纳洛酮在化学上相关，已被证明具有镇痛和麻醉拮抗剂性质。在啮齿动物的扭体镇痛试验中，布托啡诺的效力分别是吗啡和dl-喷他佐辛的4 - 30倍。作为拮抗剂，布托啡诺与纳洛啡相当，效力是dl-喷他佐辛的30倍。根据纳洛酮诱导的小鼠跳跃试验和戒断吗啡依赖小鼠中缺乏替代，估计布托啡诺的身体依赖性潜力小于dl-喷他佐辛，但大于纳洛啡和dl-环唑辛。动物数据还表明，布托啡诺的激动作用（如呼吸抑制和瞳孔缩小）达到上限效应，其低于剂量增加时吗啡的作用。因此，布托啡诺与吗啡不同，吗啡表现出剂量相关的激动剂作用。布托啡诺在显著高于（大于100 X）产生镇痛作用的剂量下显示出弱至中度的中枢镇痛作用。在清醒犬中观察到布托啡诺对心血管和呼吸系统的影响极小。
Butorphanol, a new, totally synthetic morphinan, which is chemically related to naloxone, has been demonstrated to have both analgesic and narcotic antagonist properties. In rodent antiwrithing analgesic tests, butorphanol was 4 to 30 times more potent than morphine and dl-pentazocine, respectively. As an antagonist, butorphanol was about equivalent to nalorphine and 30 times more potent than dl-pentazocine. On the basis of the naloxone-induced mouse jumping test and the lack of substitution in withdrawn morphine-dependent mice, it is estimated that the potential for physical dependence of butorphanol will be less than that of dl-pentazocine but greater than that of nalorphine and dl-cyclazocine. Animal data also show that agonistic actions of butorphanol, such as respiratory depression and miosis, reach ceiling effects which are lower than those seen with morphine with an increase in dosage. Thus, butorphanol differed from morphine which exhibited agonist effects in a dose-related manner. Butorphanol showed weak to moderate central depressant properties at doses which were considerably higher (greater than 100 X) than those producing analgesia. Minimal cardiovascular and respiratory effects were seen with butorphanol in conscious dogs.