Bitter perception plays a critical role for the detection of potentially harmful substances in food items for most vertebrates. The detection of bitter compounds is facilitated by specialized receptors located in taste buds of the oral cavity. This work focuses on the receptors, including their sensitivities, structure-function relationships, agonists and antagonists. Moreover, the existence of numerous bitter taste receptor variants in the human population and the fact that several of them affect individual bitter tasting profoundly, is discussed as well. The identification of bitter taste receptors in numerous tissues outside the oral cavity and their multiple proposed roles in these tissues is also described briefly. Although this work is mainly focused on human bitter taste receptors, it is imperative to compare human bitter taste with that of other animals to understand which evolutionary forces might have shaped bitter taste receptors and their functions and to distinguish apparent typical human from rather general features. For the readers who are not too familiar with the gustatory system short descriptions of taste anatomy, signal transduction and oral bitter taste receptor expression are included in the beginning of this article. Significance Statement Apart from their role as sensors for potentially harmful substances in the oral cavity, the numerous additional roles of bitter taste receptors in tissues outside the gustatory system have received much attention recently. For the careful assessment of functions inside and outside the taste system a solid knowledge about the specific and general pharmacological features of these receptors and the growing toolbox available for studying them is imperative and provided in this work.

中文翻译：

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国际基础与临床药理学联盟。 CXVII：味觉 2 受体：结构、功能、激活剂和阻断剂。


对于大多数脊椎动物来说，苦味感知对于检测食物中的潜在有害物质起着至关重要的作用。位于口腔味蕾的特殊受体有助于检测苦味化合物。这项工作的重点是受体，包括它们的敏感性、结构-功能关系、激动剂和拮抗剂。此外，还讨论了人类中存在的多种苦味受体变体，以及其中一些受体变体深刻影响个体苦味的事实。还简要描述了口腔外许多组织中苦味受体的识别及其在这些组织中的多种拟议作用。尽管这项工作主要集中在人类苦味受体上，但有必要将人类苦味与其他动物的苦味进行比较，以了解哪些进化力量可能塑造了苦味受体及其功能，并将明显的典型人类特征与相当普遍的特征区分开来。对于不太熟悉味觉系统的读者，本文开头包含了味觉解剖学、信号转导和口腔苦味受体表达的简短描述。意义陈述 除了作为口腔中潜在有害物质的传感器的作用之外，苦味受体在味觉系统以外的组织中的许多附加作用最近也受到了广泛的关注。为了仔细评估味觉系统内外的功能，对这些受体的具体和一般药理学特征的扎实了解以及可用于研究它们的不断增长的工具箱是必要的，并且在这项工作中提供。