| Title : Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation - Almeida_2004_Bioorg.Med.Chem.Lett_14_1879 |
| Author(s) : Almeida LE , Pereira EF , Camara AL , Maelicke A , Albuquerque EX |
| Ref : Bioorganic & Medicinal Chemistry Lett , 14 :1879 , 2004 |
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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. |
| PubMedSearch : Almeida_2004_Bioorg.Med.Chem.Lett_14_1879 |
| PubMedID: 15050620 |
Almeida LE, Pereira EF, Camara AL, Maelicke A, Albuquerque EX (2004)
Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation
Bioorganic & Medicinal Chemistry Lett
14 :1879
Almeida LE, Pereira EF, Camara AL, Maelicke A, Albuquerque EX (2004)
Bioorganic & Medicinal Chemistry Lett
14 :1879