5-羟色胺受体

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5-HT1B 受體英语5-HT1B receptor 作為代謝型血清素受體的一個例子。其呈現出緞帶狀的晶體結構。

5-羥色胺受體,也被稱為血清素受體5-HT受體,是一羣於中樞神經系統中央處末梢神經系統周邊出現的G蛋白偶聯受體及配體門控離子通道。[1][2]它們同時調節興奮性和抑制性神經傳導物質的傳遞。

分類[编辑]

血清素受體可分為七個亞科 5-HT1, 5-HT2, 5-HT3, 5-HT4, 5-HT5, 5-HT6, 5-HT7。至少有十四種受體亞型已被發現,包含G蛋白偶聯受體和配體門控離子通道(G protein-coupled receptor and a ligand-gated ion channe)。

  • 5-HT1受體是5-HT受體家族中最龐大的一科,目前有A、B、D、E、F5種亞型, 5-HT1A、5-HT1B、5-HT1D、5-HT1E、5-HT1F五種受體蛋白。沒有5-HT1C受體,因為它被重新分類為5-HT2C受體。
  • 5-HT2受體次家族有A、B、C, 3種亞型, 5-HT2A5-HT2B,和5-HT2C三種受體蛋白。
  • 5-HT3受體
  • 5-HT4受體
  • 5-HT5受體次家族有A、B、2種亞型, 5-HT5A、5-HT5B二種受體蛋白。
  • 5-HT6受體
  • 5-HT7受體

總共有十四種受體亞型。

除了5-HT3受体配体门控离子通道英语ligand gated ion channel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[编辑]

七個亞科 5-HT1, 5-HT2, 5-HT3, 5-HT4, 5-HT5, 5-HT6, 5-HT7

家族 類型 作用機制 類別
5-HT1英语5-HT1 Gi/Go英语Gi alpha subunit-蛋白偶聯受体 減少cAMP在細胞內的水平 抑制性
5-HT2 Gq/G11英语Gq protein-蛋白偶聯受体 增加細胞內IP3DAG英语diglyceride的水平 興奮性
5-HT3英语5-HT3 配體門控Na+K+离子通道 使質膜去極化 興奮性
5-HT4 Gs英语G(s)alpha蛋白偶聯受体 增加細胞內cAMP的水平 興奮性
5-HT5英语5-HT5A Gi/Go英语Gi alpha subunit-蛋白偶聯受体[4] 減少cAMP在細胞內的水平 抑制性
5-HT6英语5-HT6 Gs英语G(s)alpha-蛋白偶聯受体 增加細胞內cAMP的水平 興奮性
5-HT7英语5-HT7 Gs英语G(s)alpha-蛋白偶聯受体 增加細胞內cAMP的水平 興奮性

亞型[编辑]

血清素受體功能概述
受體 首次克隆 基因 分佈 作用 激動劑 拮抗劑 用途
血管 中樞神經系統 胃腸道 血小板 外周神經系統 平滑肌
5-HT1A英语5-HT1A receptor 1987

選擇性

非選擇性

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(一种迷幻药物,激活5-HT1A、5-HT2A、5-HT2C、5-HT5A、5-HT5、5-HT6)。[28]

参考资料[编辑]

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