維基百科

5-羥色胺受體

跨膜蛋白

5-羥色胺受體，也被稱為血清素受體或5-HT受體，是一羣於中樞神經系統中央處和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。

以5-HT1B 受體（英語：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。

分類

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（G protein-coupled receptor）和配體門控離子通道(ligand-gated ion channel)。

  • 5-HT1受體是5-HT受體家族中最龐大的一科，包括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受體亞家族包括5-HT2A、5-HT2B，和5-HT2C三種受體蛋白。
  • 5-HT3受體
  • 5-HT4受體
  • 5-HT5受體亞家族包括5-HT5A、5-HT5B兩種受體蛋白。（其中5B受體在人類中為假基因，無受體表達）
  • 5-HT6受體
  • 5-HT7受體

總共有十四種受體亞型。

除了5-HT3受體是配體門控離子通道以外，其它的所有血清素受體都是G蛋白偶聯受體，激活細胞內的第二信使來產生效應。在2014年，在菜粉蝶基因組中發現了一種新的5-HT受體，被命名為pr5-HT8。它與已知的各類5-HT受體相似度很低，在哺乳動物中沒有類似基因。[3]

家族

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（英語：5-HT1） Gi/Go（英語：Gi alpha subunit）-蛋白偶聯受體 減少cAMP在細胞內的水平 抑制性
5-HT2 Gq/G11（英語：Gq protein）-蛋白偶聯受體 增加細胞內IP3和DAG（英語：diglyceride）的水平 興奮性
5-HT3（英語：5-HT3） 配體門控Na+，K+離子通道 使質膜去極化 興奮性
5-HT4 Gs（英語：G(s)alpha）蛋白偶聯受體 增加細胞內cAMP的水平 興奮性
5-HT5（英語：5-HT5A） Gi/Go（英語：Gi alpha subunit）-蛋白偶聯受體[4] 減少cAMP在細胞內的水平 抑制性
5-HT6（英語：5-HT6） Gs（英語：G(s)alpha）-蛋白偶聯受體 增加細胞內cAMP的水平 興奮性
5-HT7（英語：5-HT7） Gs（英語：G(s)alpha）-蛋白偶聯受體 增加細胞內cAMP的水平 興奮性

亞型

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（英語：5-HT1A receptor） 1987 是 是 否 否 否 否

選擇性

非選擇性

5-HT1B（英語：5-HT1B receptor） 1992 是 是 否 否 否 否
5-HT1D（英語：5-HT1D receptor） 1991 是 是 否 否 否 否
5-HT1E（英語：5-HT1E） 1992 是 是 否 否 否 否
  • None known
5-HT1F（英語：5-HT1F） 1993 否 是 否 否 否 否
  • Migraine
  • None known
5-HT2A（英語：5-HT2A receptor） 1988 是 是 是 是 是 是
  • 成癮 (potentially modulating) [40]
  • 焦慮[41]
  • 食慾
  • Cognition
  • Imagination
  • Learning
  • 記憶
  • 情緒
  • Perception
  • 性行為[42]
  • 睡眠[43]
  • 體溫調節[44]
  • 血管收縮[45]
5-HT2B 1992 是 是 是 是 是 是
5-HT2C（英語：5-HT2C receptor） 1988 是 是 是 是 是 是
5-HT3（英語：5-HT3 receptor） 1993 否 是 是 否 是 否
  • 成癮
  • 焦慮
  • Emesis
  • GI Motility[62]
  • Learning[63]
  • 記憶[63]
  • Nausea
5-HT4 1995 否 是 是 否 是 否
5-HT5A（英語：5-HT5A receptor） 1994 否 是 否 否 否 否
  • None thus far
5-HT5B（英語：5-HT5B receptor） 1993 否 否 否 否 否 否

Functions in rodents,
pseudogene in humans

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

注意沒有5-HT1C受體。這是因為在克隆這個受體並進一步分類之後，發現它和5-HT2家族共同點更多，於是就改名成了5-HT2C受體。

對各5-HT受體亞型選擇性極弱的激動劑有麥角胺（一種antimigraine（英語：antimigraine），激活5-HT1A、5-HT1D、5-HT1B、D2、去甲腎上腺素受體[28]）、LSD（一種合成迷幻藥物，可以激活5-HT1A、5-HT2A、5-HT2C、5-HT5A、5-HT6）。[28]

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