Density of α4β2* nAChR on the surface of neurons is modulated by chronic antagonist exposure

Pharmacology Research & Perspectives
C A ZambranoMichael J Marks

Abstract

The expression of high-affinity α4β2* nicotinic acetylcholine receptors (nAChR) increases following chronic exposure to nicotinic agonists. While, nAChR antagonists can also produce upregulation, these changes are often less pronounced than achieved with agonists. It is unknown if nAChR agonists and antagonists induce receptor upregulation by the same mechanisms. In this study, primary neuronal cultures prepared from cerebral cortex, hippocampus, diencephalon, and midbrain/hindbrain of C57BL/6J mouse embryos were treated chronically with nicotine (agonist), mecamylamine (noncompetitive antagonist) or dihydro-β-erythroidine (competitive antagonist) or the combination of nicotine with each antagonist. The distribution of intracellular and surface [(125)I]epibatidine-binding sites were subsequently measured. Treatment with 1 μmol/L nicotine upregulated intracellular and cell surface [(125)I]epibatidine binding after 96 h. Chronic dihydro-β-erythroidine (10 μmol/L) treatment also increased [(125)I]epibatidine binding on the cell surface; however, mecamylamine was ineffective in upregulating receptors by itself. The combination of 1 μmol/L nicotine plus 10 μmol/L mecamylamine elicited a significantly higher upregulation than that ac...Continue Reading

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Citations

Aug 4, 2015·Chemical Biology & Drug Design·Pattaporn JaikhanOpa Vajragupta

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