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5-羟色胺受体

维基百科,自由的百科全书
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。

5-羟色胺受体,也被称为血清素受体5-HT受体,是一群于中枢神经系统中央处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。

分类

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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-HT2A5-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

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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IP3DAG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

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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

选择性

非选择性

5-HT1B英语5-HT1B receptor 1992
5-HT1D英语5-HT1D receptor 1991
5-HT1E英语5-HT1E 1992
  • None known
5-HT1F英语5-HT1F 1993
  • Migraine
  • None known
5-HT2A英语5-HT2A receptor 1988
  • 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
5-HT2C英语5-HT2C receptor 1988
5-HT3英语5-HT3 receptor 1993
  • 成瘾
  • 焦虑
  • Emesis
  • GI Motility[62]
  • Learning[63]
  • 记忆[63]
  • Nausea
5-HT4 1995
5-HT5A英语5-HT5A receptor 1994
  • None thus far
5-HT5B英语5-HT5B receptor 1993

Functions in rodents,
pseudogene in humans

  • None thus far
5-HT6英语5-HT6 receptor 1993
5-HT7英语5-HT7 receptor 1993

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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