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An odorant derivative as an antagonist for an olfactory receptor

机译：气味衍生物作为嗅觉受体的拮抗剂

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Different odorants are recognized by different combinations of G protein-coupled olfactory receptors, and thereby, odor identity is determined by a combinatorial receptor code for each odorant. We recently demonstrated that odorants appeared to compete for receptor sites to act as an agonist or an antagonist. Therefore, in natural circumstances where we always perceive a mixture of various odorants, olfactory receptor antagonism between odorants may result in a receptor code for the mixture that cannot be predicted from the codes for its individual components. Here we show that stored isoeugenol has an antagonistic effect on a mouse olfactory receptor, mOR-EG. However, freshly purified isoeugenol did not have an inhibitory effect. Instead, an isoeugenol derivative produced during storage turned out to be a potent competitive antagonist of mOR-EG. Structural analysis revealed that this derivative is an oxidatively dimerized isoeugenol that naturally occurs by oxidative reaction. The current study indicates that as odorants age, they decompose or react with other odorants, which in turn affects responsiveness of an olfactory receptor(s).
机译：G蛋白偶联的嗅觉受体的不同组合可以识别出不同的气味，因此，气味的识别性取决于每种气味的组合受体代码。我们最近证明，加味剂似乎竞争受体位点以充当激动剂或拮抗剂。因此，在我们总是感觉到各种加味剂的混合物的自然环境中，加味剂之间的嗅觉受体拮抗作用可能会导致无法从混合物的单个成分代码中预测出该混合物的受体代码。在这里，我们显示存储的异丁香酚对小鼠嗅觉受体mOR-EG具有拮抗作用。但是，新鲜纯化的异丁香酚没有抑制作用。相反，在储存期间产生的异丁香酚衍生物被证明是mOR-EG的有效竞争性拮抗剂。结构分析表明，该衍生物是氧化二聚异丁香酚，其自然通过氧化反应发生。当前的研究表明，随着加味剂的老化，它们会分解或与其他加味剂反应，进而影响嗅觉受体的响应能力。

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