吗啡 - N - 氧化物的镇痛作用。
The analgesic action of morphine-n-oxide.
作者信息
Fennessy M R
出版信息
Br J Pharmacol. 1968 Oct;34(2):337-44. doi: 10.1111/j.1476-5381.1968.tb07055.x.
Abstract
- The analgesic activity of morphine-N-oxide in mice and rats has been investigated and compared with that of morphine.2. Both morphine and morphine-N-oxide were more active when given subcutaneously than when given intraperitoneally.3. Given subcutaneously, morphine was 11-22 times more potent than morphine-N-oxide and when given intraperitoneally it was 39-89 times more potent. The potencies depended on the test situation and the species of animal used.4. In animals pretreated with amiphenazole or tacrine, the analgesic activities of morphine and morphine-N-oxide were increased. The potencies of these analgesic drugs given intraperitoneally were increased to a greater extent than were the potencies obtained by subcutaneous administration.5. A possible explanation for the increase in analgesic potency of morphine-N-oxide produced by pretreatment with amiphenazole or tacrine may be that morphine-N-oxide is rapidly inactivated in the liver and this inactivation is impaired by amiphenazole and tacrine.
摘要
已对氧化吗啡在小鼠和大鼠中的镇痛活性进行了研究，并与吗啡的镇痛活性作了比较。
吗啡和氧化吗啡皮下给药时均比腹腔给药时活性更强。
皮下给药时，吗啡的效力比氧化吗啡强11至22倍，腹腔给药时则强39至89倍。效力取决于试验情况及所用动物的种类。
在预先用安米苯唑或他克林处理过的动物中，吗啡和氧化吗啡的镇痛活性增强。这些镇痛药腹腔给药时效力的增强程度比皮下给药时更大。
用安米苯唑或他克林预处理使氧化吗啡镇痛效力增强的一个可能解释是，氧化吗啡在肝脏中迅速失活，而安米苯唑和他克林会损害这种失活过程。
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Proc Soc Exp Biol Med. 1950 Jul;74(3):589-91. doi: 10.3181/00379727-74-17983.
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The effect of the liver on the metabolism of d,1-methadone in vitro and in vivo.肝脏在体外和体内对消旋美沙酮代谢的影响。
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