维基百科

5-羟色胺受体

跨膜蛋白
（重定向自血清素受體）

5-羟色胺受体，也被称为血清素受体或5-HT受体，是一群于中枢神经系统中央处和末梢神经系统周边出现的G蛋白偶联受体及配体门控离子通道。[1][2]它们同时调节兴奋性和抑制性神经传导物质的传递。

以5-HT1B 受体（英语：5-HT1B receptor） 作为代谢型血清素受体的一个例子。其呈现出缎带状的晶体结构。

分类

编辑

血清素受体可分为七个亚科 5-HT1, 5-HT2, 5-HT3, 5-HT4, 5-HT5, 5-HT6, 5-HT7。至少有十四种受体亚型已被发现，包含G蛋白偶联受体（G protein-coupled receptor）和配体门控离子通道(ligand-gated ion channel)。

  • 5-HT1受体是5-HT受体家族中最庞大的一科，包括5-HT1A、5-HT1B、5-HT1D、5-HT1E、5-HT1F五种受体蛋白。没有5-HT1C受体，因为它被重新分类为5-HT2C受体。
  • 5-HT2受体亚家族包括5-HT2A、5-HT2B，和5-HT2C三种受体蛋白。
  • 5-HT3受体
  • 5-HT4受体
  • 5-HT5受体亚家族包括5-HT5A、5-HT5B两种受体蛋白。（其中5B受体在人类中为假基因，无受体表达）
  • 5-HT6受体
  • 5-HT7受体

总共有十四种受体亚型。

除了5-HT3受体是配体门控离子通道以外，其它的所有血清素受体都是G蛋白偶联受体，激活细胞内的第二信使来产生效应。在2014年，在菜粉蝶基因组中发现了一种新的5-HT受体，被命名为pr5-HT8。它与已知的各类5-HT受体相似度很低，在哺乳动物中没有类似基因。[3]

家族

编辑

七个亚科 5-HT1, 5-HT2, 5-HT3, 5-HT4, 5-HT5, 5-HT6, 5-HT7。

家族 类型 作用机制 类别
5-HT1（英语：5-HT1） Gi/Go（英语：Gi alpha subunit）-蛋白偶联受体 减少cAMP在细胞内的水平 抑制性
5-HT2 Gq/G11（英语：Gq protein）-蛋白偶联受体 增加细胞内IP3和DAG（英语：diglyceride）的水平 兴奋性
5-HT3（英语：5-HT3） 配体门控Na+，K+离子通道 使质膜去极化 兴奋性
5-HT4 Gs（英语：G(s)alpha）蛋白偶联受体 增加细胞内cAMP的水平 兴奋性
5-HT5（英语：5-HT5A） Gi/Go（英语：Gi alpha subunit）-蛋白偶联受体[4] 减少cAMP在细胞内的水平 抑制性
5-HT6（英语：5-HT6） Gs（英语：G(s)alpha）-蛋白偶联受体 增加细胞内cAMP的水平 兴奋性
5-HT7（英语：5-HT7） Gs（英语：G(s)alpha）-蛋白偶联受体 增加细胞内cAMP的水平 兴奋性

亚型

编辑
血清素受体功能概述
受体 首次克隆 基因 分布 作用 激动剂 拮抗剂 用途
血管 中枢神经系统 胃肠道 血小板 外周神经系统 平滑肌
5-HT1A（英语：5-HT1A receptor） 1987 是 是 否 否 否 否

选择性

非选择性

5-HT1B（英语：5-HT1B receptor） 1992 是 是 否 否 否 否
5-HT1D（英语：5-HT1D receptor） 1991 是 是 否 否 否 否
5-HT1E（英语：5-HT1E） 1992 是 是 否 否 否 否
  • None known
5-HT1F（英语：5-HT1F） 1993 否 是 否 否 否 否
  • Migraine
  • None known
5-HT2A（英语：5-HT2A receptor） 1988 是 是 是 是 是 是
  • 成瘾 (potentially modulating) [40]
  • 焦虑[41]
  • 食欲
  • Cognition
  • Imagination
  • Learning
  • 记忆
  • 情绪
  • Perception
  • 性行为[42]
  • 睡眠[43]
  • 体温调节[44]
  • 血管收缩[45]
5-HT2B 1992 是 是 是 是 是 是
5-HT2C（英语：5-HT2C receptor） 1988 是 是 是 是 是 是
5-HT3（英语：5-HT3 receptor） 1993 否 是 是 否 是 否
  • 成瘾
  • 焦虑
  • Emesis
  • GI Motility[62]
  • Learning[63]
  • 记忆[63]
  • Nausea
5-HT4 1995 否 是 是 否 是 否
5-HT5A（英语：5-HT5A receptor） 1994 否 是 否 否 否 否
  • None thus far
5-HT5B（英语：5-HT5B receptor） 1993 否 否 否 否 否 否

Functions in rodents,
pseudogene in humans

  • None thus far
5-HT6（英语：5-HT6 receptor） 1993 否 是 否 否 否 否
5-HT7（英语：5-HT7 receptor） 1993 是 是 是 否 否 否

注意没有5-HT1C受体。这是因为在克隆这个受体并进一步分类之后，发现它和5-HT2家族共同点更多，于是就改名成了5-HT2C受体。

对各5-HT受体亚型选择性极弱的激动剂有麦角胺（一种antimigraine（英语：antimigraine），激活5-HT1A、5-HT1D、5-HT1B、D2、去甲肾上腺素受体[28]）、LSD（一种合成迷幻药物，可以激活5-HT1A、5-HT2A、5-HT2C、5-HT5A、5-HT6）。[28]

参考资料

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