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碱基腺嘌呤作为肾脏中的信号分子。

The nucleobase adenine as a signalling molecule in the kidney.

机构信息

PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, Bonn, Germany.

出版信息

Acta Physiol (Oxf). 2015 Apr;213(4):808-18. doi: 10.1111/apha.12452. Epub 2015 Jan 28.

Abstract

In 2002, the first receptor activated by the nucleobase adenine was discovered in rats. In the past years, two adenine receptors (AdeRs) in mice and one in Chinese hamsters, all of which belong to the family of G protein-coupled receptors (GPCRs), were cloned and pharmacologically characterized. Based on the nomenclature for other purinergic receptor families (P1 for adenosine receptors and P2 for nucleotide, e.g. ATP, receptors), AdeRs were designated P0 receptors. Pharmacological data indicate the existence of G protein-coupled AdeRs in pigs and humans as well; however, those have not been cloned so far. Current data suggest a role for adenine and AdeRs in renal proximal tubules. Furthermore, AdeRs are suggested to be functional counterplayers of vasopressin in the collecting duct system, thus exerting diuretic effects. We are only at the beginning of understanding the significance of this new class of purinergic receptors, which might become future drug targets.

摘要

2002 年,在大鼠中发现了第一个被碱基腺嘌呤激活的受体。在过去的几年中,已经在小鼠中克隆并药理学鉴定了两种腺嘌呤受体(AdeRs)和一种中国仓鼠中的腺嘌呤受体,它们均属于 G 蛋白偶联受体(GPCR)家族。根据其他嘌呤能受体家族(例如腺苷受体 P1 和核苷酸受体 P2,如 ATP 受体)的命名法,AdeRs 被指定为 P0 受体。药理学数据表明,在猪和人中也存在 G 蛋白偶联的 AdeRs;然而,到目前为止尚未对其进行克隆。目前的数据表明,腺嘌呤和 AdeRs 在肾脏近曲小管中发挥作用。此外,AdeRs 被认为是集合管系统中血管加压素的功能性拮抗物,从而发挥利尿作用。我们才刚刚开始了解这一类新的嘌呤能受体的重要性,它们可能成为未来的药物靶点。

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