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Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation.

Abstract：

:In HEK293 cells stably expressing alpha4beta2 nAChRs, naltrexone, but not naloxone, blocked alpha4beta2 nAChRs via an open-channel blocking mechanism. In primary hippocampal cultures, naltrexone inhibited alpha7 nAChRs up-regulated by nicotine, and in organotypic hippocampal cultures naltrexone caused a time-dependent up-regulation of functional alpha7 nAChRs that was detected after removal of the drug. These results indicate that naltrexone could be used as a smoking cessation aid.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Almeida LE,Pereira EF,Camara AL,Maelicke A,Albuquerque EX

doi

10.1016/j.bmcl.2004.01.004

subject

Has Abstract

pub_date

2004-04-19 00:00:00

pages

1879-87

issue

8

eissn

0960-894X

issn

1464-3405

pii

S0960894X04000290

journal_volume

14

pub_type

杂志文章

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