鞘内注射吗啡-3-葡萄糖醛酸苷不会拮抗大鼠体内吗啡或吗啡-6-葡萄糖醛酸苷的脊髓镇痛作用。

Intrathecal morphine-3-glucuronide does not antagonize spinal antinociception by morphine or morphine-6-glucuronide in rats.

作者信息

Suzuki N, Kalso E, Rosenberg P H

机构信息

Department of Anaesthesia, Helsinki University Central Hospital, Finland.

出版信息

Eur J Pharmacol. 1993 Nov 9;249(2):247-50. doi: 10.1016/0014-2999(93)90441-j.

DOI:10.1016/0014-2999(93)90441-j

PMID:8287909

Abstract

Morphine or morphine-6-glucuronide either alone or in combination with morphine-3-glucuronide was administered intrathecally to rats. Antinociceptive effects were evaluated with the tail flick and the hot plate tests. Motor function was tested using the rotarod test. Estimated ED50 from the dose-response curves for morphine and morphine-6-glucuronide showed about a 30 times more potent antinociceptive effect of morphine-6-glucuronide compared with morphine. Morphine-3-glucuronide had no antinociceptive effect. Simultaneous administration of morphine-3-glucuronide 5.0 micrograms did not show any significant effect on antinociception induced by morphine 1.0 microgram or morphine-6-glucuronide 0.05 microgram.

摘要

将吗啡或吗啡 - 6 - 葡萄糖醛酸苷单独或与吗啡 - 3 - 葡萄糖醛酸苷联合鞘内注射给大鼠。通过甩尾试验和热板试验评估镇痛效果。使用转棒试验测试运动功能。从吗啡和吗啡 - 6 - 葡萄糖醛酸苷的剂量 - 反应曲线估计的ED50显示，与吗啡相比，吗啡 - 6 - 葡萄糖醛酸苷的镇痛作用强约30倍。吗啡 - 3 - 葡萄糖醛酸苷没有镇痛作用。同时给予5.0微克吗啡 - 3 - 葡萄糖醛酸苷对1.0微克吗啡或0.05微克吗啡 - 6 - 葡萄糖醛酸苷诱导的镇痛作用没有任何显著影响。