Motilin receptor in GtoPdb v.2023.1

Anthony P. Davenport, Takio Kitazawa, Gareth Sanger
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Abstract

Motilin receptors (provisional nomenclature) are activated by motilin, a 22 amino-acid peptide derived from a precursor (MLN, P12872), which may also generate a motilin-associated peptide. There are significant species differences in the structure of motilin and its receptor, and in the functions of motilin. In humans and large mammals such as dog, activation of these receptors by motilin released from endocrine cells in the duodenal mucosa during fasting, induces propulsive phase III movements. This activity is associated with promoting hunger in humans. In humans and other mammals drugs and other non-peptide compounds which activate the motilin receptor may generate a more long-lasting ability to increase cholinergic activity within the upper gut, to promote upper gastrointestinal motility; this activity is suggested to be responsible for the gastrointestinal prokinetic effects of certain macrolide antibacterials (often called motilides; e.g. erythromycin, azithromycin), although for many of these molecules the evidence is sparse. Relatively high doses may induce vomiting and in humans, nausea.
GtoPdb v.2023.1中的胃动素受体
动素受体(临时命名)被动素激活,动素是一种从前体(MLN, P12872)衍生的22个氨基酸的肽,也可能产生动素相关肽。在胃动素及其受体的结构和功能上存在着明显的物种差异。在人类和大型哺乳动物(如狗)中,禁食期间十二指肠黏膜内分泌细胞释放的胃动素激活这些受体,诱导推进性III期运动。这种活动与促进人类饥饿有关。在人类和其他哺乳动物中,激活胃动素受体的药物和其他非肽化合物可能产生更持久的能力,以增加上肠内的胆碱能活性,促进上消化道运动;这种活性被认为是某些大环内酯类抗菌药(通常称为motilides;例如红霉素,阿奇霉素),尽管这些分子的证据很少。相对高的剂量可能会引起呕吐,对人类来说,会引起恶心。
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