Brain uptake and the analgesic effect of oxytocin - its usefulness as an analgesic agent

被引:52
作者
Kang, YS [1 ]
Park, JH [1 ]
机构
[1] Sookmyung Womens Univ, Coll Pharm, Seoul, South Korea
关键词
oxytocin; brain uptake; analgesic effect; naloxone;
D O I
10.1007/BF02975453
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
To establish the usefulness of oxytocin (OT) as an analgesic for women in delivery, the pharmacokinetic parameters and blood-brain barrier (BBB) permeability of [H-3]OT were obtained using an intravenous injection technique or the internal carotid artery perfusion/capillary depletion (ICAP/CDM) method. Brain uptake of OT was similar to that of sucrose, plasma space marker, indicating that OT has a poor BBB permeability. Moreover, the analgesic effects of OT injected through the jugular vein on nociception were evaluated by the tail-flick method. The antinociceptive effects of OT injected at a dose of 0.2 mg/kg or 2 mg/kg were dose-dependent. In addition, the analgesic effects of OT on the CNS were unaffected by naloxone, a m-receptor antagonist. In a similar manner to the opioid system, OT may play a modulatory role in antinociception.
引用
收藏
页码:391 / 395
页数:5
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