Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation.
Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation.
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神经元烟碱乙酰胆碱受体对阿片拮抗剂纳曲酮和纳洛酮的敏感性：受体阻断和上调。
DOI：
10.1016/j.bmcl.2004.01.004
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发表时间：
2004
期刊：
影响因子：
--
通讯作者：
Albuquerque,EdsonX
中科院分区：
文献类型：
--
作者：
Almeida,LuisEF;Pereira,EdnaFR;Camara,AdrianaL;Maelicke,Alfred;Albuquerque,EdsonX
在稳定表达α4β2 nAChR的HEK 293细胞中，纳曲酮（而不是纳洛酮）通过开放通道阻断机制阻断α4β2 nAChR。在原代海马培养物中，纳洛酮抑制尼古丁上调的α7 nAChR，在器官型海马培养物中，纳洛酮引起功能性α7 nAChR的时间依赖性上调，在去除药物后检测到。这些结果表明，纳洛酮可用作戒烟辅助剂。
In HEK293 cells stably expressing α4β2 nAChRs, naltrexone, but not naloxone, blocked α4β2 nAChRs via an open-channel blocking mechanism. In primary hippocampal cultures, naltrexone inhibited α7 nAChRs up-regulated by nicotine, and in organotypic hippocampal cultures naltrexone caused a time-dependent up-regulation of functional α7 nAChRs that was detected after removal of the drug. These results indicate that naltrexone could be used as a smoking cessation aid.