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Comparison of the antagonistic effects of 6β-naltrexol and naltrexone against morphine analgesia
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- Author:
- No author available
- Journal Title:
- ACTA PHARMACEUTICA SINICA
- Issue:
- 8
- DOI:
- 10.3321/j.issn:0513-4870.2003.08.005
- Key Word:
- 6β-纳曲醇;纳曲酮;吗啡;阿片受体
Abstract： 目的比较6β-纳曲醇(6β-naltrexol,6β-NOL)与纳曲酮(naltrexone,NTX)拮抗吗啡的镇痛作用.方法用小鼠热板法和小鼠热辐射甩尾法,sc和ig两种途径研究6β-NOL和NTX拮抗吗啡镇痛作用的强度和有效时间.用放射配体结合实验研究6β-NOL和NTX对阿片受体的亲和力.结果小鼠热板法和甩尾法显示,6β-NOL的抗吗啡镇痛作用强度和有效时间分别约为NTX的(6.1±1.7)%和3～4倍;po拮抗吗啡镇痛作用强度约为sc的30%,与NTX相近.在受体水平,6β-NOL对阿片-mu受体的亲和力约为NTX的12.5%,这与它们在整体水平拮抗吗啡镇痛作用的强度相近.结论 6β-NOL抗吗啡镇痛作用比NTX弱,但作用时间长.
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