5-羟色胺受体

求闻百科，共笔求闻
5-HT1B 受体]] 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。

分类

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蛋白偶联受体和配体门控离子通道(G protein-coupled receptor and a ligand-gated ion channe)。

  • 5-HT1受体是5-HT受体家族中最庞大的一科，目前有A、B、D、E、F5种亚型, 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受体次家族有A、B、C, 3种亚型, 5-HT2A、5-HT2B，和5-HT2C三种受体蛋白。
  • 5-HT3受体
  • 5-HT4受体
  • 5-HT5受体次家族有A、B、2种亚型, 5-HT5A、5-HT5B二种受体蛋白。
  • 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

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|5-HT1]] [[:Gi/Go|Gi/Go]]-蛋白偶联受体 减少cAMP在细胞内的水平 抑制性
5-HT2 [[:Gq/G11|Gq/G11]]-蛋白偶联受体 增加细胞内IP3和DAG的水平 兴奋性
[[:5-HT3|5-HT3]] 配体门控Na+，K+离子通道 使质膜去极化 兴奋性
5-HT4 [[:Gs|Gs]]蛋白偶联受体 增加细胞内cAMP的水平 兴奋性
[[:5-HT5|5-HT5]] [[:Gi/Go|Gi/Go]]-蛋白偶联受体[4] 减少cAMP在细胞内的水平 抑制性
[[:5-HT6|5-HT6]] [[:Gs|Gs]]-蛋白偶联受体 增加细胞内cAMP的水平 兴奋性
[[:5-HT7|5-HT7]] [[:Gs|Gs]]-蛋白偶联受体 增加细胞内cAMP的水平 兴奋性

亚型

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|5-HT1A]] 1987 是 是 否 否 否 否

选择性

非选择性

[[:5-HT1B|5-HT1B]] 1992 是 是 否 否 否 否
[[:5-HT1D|5-HT1D]] 1991 是 是 否 否 否 否
[[:5-HT1E|5-HT1E]] 1992 是 是 否 否 否 否
  • None known
[[:5-HT1F|5-HT1F]] 1993 否 是 否 否 否 否
  • Migraine
  • None known
[[:5-HT2A|5-HT2A]] 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|5-HT2C]] 1988 是 是 是 是 是 是
[[:5-HT3|5-HT3]] 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|5-HT5A]] 1994 否 是 否 否 否 否
  • None thus far
[[:5-HT5B|5-HT5B]] 1993 否 否 否 否 否 否

Functions in rodents,
pseudogene in humans

  • None thus far
[[:5-HT6|5-HT6]] 1993 否 是 否 否 否 否
[[:5-HT7|5-HT7]] 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，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

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  62. ↑ Michel K, Zeller F, Langer R, Nekarda H, Kruger D, Dover TJ, Brady CA, Barnes NM, Schemann M. Serotonin excites neurons in the human submucous plexus via 5-HT3 receptors.. National Center for Biotechnology Information. 2005-05 [2014-10-10]. 
  63. ↑ 63.0 63.1 Pitsikas N, Brambilla A, Borsini F. Effect of DAU 6215, a novel 5-HT3 receptor antagonist, on scopolamine-induced amnesia in the rat in a spatial learning task. Pharmacol Biochem Behav. 1994, 47 (1): 95–99. PMID 8115433. doi:10.1016/0091-3057(94)90116-3. 
  64. ↑ 64.0 64.1 Smriga M, Torii K. L-Lysine acts like a partial serotonin receptor 4 antagonist and inhibits serotonin-mediated intestinal pathologies and anxiety in rats. Proceedings of the National Academy of Sciences of the United States of America. 2003, 100 (26): 15370–5. PMC 307574 可免费查阅. PMID 14676321. doi:10.1073/pnas.2436556100. 
  65. ↑ Kennett GA, Bright F, Trail B, Blackburn TP, Sanger GJ. Anxiolytic-like actions of the selective 5-HT4 receptor antagonists SB 204070A and SB 207266A in rats. Neuropharmacology. 1997, 36 (4–5): 707–12. PMID 9225297. doi:10.1016/S0028-3908(97)00037-3. 
  66. ↑ Jean A, Conductier G, Manrique C, Bouras C, Berta P, Hen R, Charnay Y, Bockaert J, Compan V. Anorexia induced by activation of serotonin 5-HT4 receptors is mediated by increases in CART in the nucleus accumbens. Proceedings of the National Academy of Sciences of the United States of America. 2007, 104 (41): 16335–40. PMC 2042207 可免费查阅. PMID 17913892. doi:10.1073/pnas.0701471104. 
  67. ↑ J Soc Biol.; Charnay, Y; Dusticier, N; Daszuta, A; Hen, R; Bockaert, J. Compan V, Charnay Y, Dusticier N, Daszuta A, Hen R, Bockaert J. J Soc Biol. 2004, 198 (1): 37–49. PMID 15146954. 
  68. ↑ 68.0 68.1 Meneses A, Hong E. Effects of 5-HT4 receptor agonists and antagonists in learning. Pharmacol Biochem Behav. 1997, 56 (3): 347–51. PMID 9077568. doi:10.1016/S0091-3057(96)00224-9. 
  69. ↑ 69.0 69.1 Fontana DJ, Daniels SE, Wong EH, Clark RD, Eglen RM. The effects of novel, selective 5-hydroxytryptamine (5-HT)4 receptor ligands in rat spatial navigation. Neuropharmacology. 1997, 36 (4–5): 689–96. PMID 9225295. doi:10.1016/S0028-3908(97)00055-5. 
  70. ↑ Fontana DJ, Daniels SE, Wong EH, Clark RD, Eglen RM. Role of 5-HT4 receptors in the mouse passive avoidance test. J Pharmacol Exp Ther. 1998, 286 (3): 1115–21. PMID 9732367. 
  71. ↑ Lucas, G.; Rymar, V. V.; Du, J.; Mnie-Filali, O.; Bisgaard, C.; Manta, S.; Lambas-Senas, L.; Wiborg, O.; Haddjeri, N.; Piñeyro, G.; Sadikot, A. F.; Debonnel, G. Serotonin4 (5-HT4) Receptor Agonists Are Putative Antidepressants with a Rapid Onset of Action. Neuron. 2007, 55 (5): 712–725. PMID 17785179. doi:10.1016/j.neuron.2007.07.041. 
  72. ↑ Duman, R. S. A Silver Bullet for the Treatment of Depression?. Neuron. 2007, 55 (5): 679–681. PMID 17785173. doi:10.1016/j.neuron.2007.08.011. 
  73. ↑ Manzke, T. 5-HT4(a) Receptors Avert Opioid-Induced Breathing Depression Without Loss of Analgesia. Science. 2003, 301 (5630): 226–229. ISSN 0036-8075. PMID 12855812. doi:10.1126/science.1084674. 
  74. ↑ Nelson DL. 5-HT5 receptors. Curr Drug Targets CNS Neurol Disord. 2004, 3 (1): 53–8. PMID 14965244. doi:10.2174/1568007043482606. 
  75. ↑ 75.0 75.1 Dietz BM, Mahady GB, Pauli GF, Farnsworth NR. Valerian extract and valerenic acid are partial agonist of the 5-HT5a receptor in vitro. Brain Res Mol Brain Res. 2005, 138 (2): 191–7. PMID 15921820. doi:10.1016/j.molbrainres.2005.04.009. 
  76. ↑ Wesolowska A. The anxiolytic-like effect of the selective 5-HT6 receptor antagonist SB-399885: the impact of benzodiazepine receptors. European Journal of Pharmacology. 2008-02, 580 (3): 355–60. PMID 18096153. doi:10.1016/j.ejphar.2007.11.022. 
  77. ↑ 77.0 77.1 Wesolowska A, Nikiforuk A. Effects of the brain-penetrant and selective 5-HT6 receptor antagonist SB-399885 in animal models of anxiety and depression. Neuropharmacology. 2007-04, 52 (5): 1274–83. PMID 17320917. doi:10.1016/j.neuropharm.2007.01.007. 
  78. ↑ Hirst WD, Stean TO, Rogers DC, Sunter D, Pugh P, Moss SF, Bromidge SM, Riley G, Smith DR, Bartlett S, Heidbreder CA, Atkins AR, Lacroix LP, Dawson LA, Foley AG, Regan CM, Upton N. SB-399885 is a potent, selective 5-HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition models. European Journal of Pharmacology. 2006-12, 553 (1–3): 109–19. PMID 17069795. doi:10.1016/j.ejphar.2006.09.049. 
  79. ↑ 79.0 79.1 Perez-García G, Meneses A. Oral administration of the 5-HT6 receptor antagonists SB-357134 and SB-399885 improves memory formation in an autoshaping learning task. Pharmacology, Biochemistry, and Behavior. 2005-07, 81 (3): 673–82. PMID 15964617. doi:10.1016/j.pbb.2005.05.005. 
  80. ↑ Wesolowska A, Nikiforuk A. The selective 5-HT(6) receptor antagonist SB-399885 enhances anti-immobility action of antidepressants in rats. European Journal of Pharmacology. 2008-03, 582 (1–3): 88–93. PMID 18234190. doi:10.1016/j.ejphar.2007.12.013. 
  81. ↑ Target Schizophrenia - Possible future developments. The Association of the British Pharmaceutical Industry. [2008-04-11]. 
  82. ↑ 82.0 82.1 82.2 Hedlund PB, Huitron-Resendiz S, Henriksen SJ, Sutcliffe JG. 5-HT7 receptor inhibition and inactivation induce antidepressantlike behavior and sleep pattern. Biological Psychiatry. 2005-11, 58 (10): 831–7. PMID 16018977. doi:10.1016/j.biopsych.2005.05.012. 
  83. ↑ 83.0 83.1 Wesolowska A, Nikiforuk A, Stachowicz K, Tatarczynska E. Effect of the selective 5-HT7 receptor antagonist SB 269970 in animal models of anxiety and depression. Neuropharmacology. 2006-09, 51 (3): 578–86. PMID 16828124. doi:10.1016/j.neuropharm.2006.04.017. 
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外部链接

{{Navbox | name = G蛋白偶联受体 | title = 细胞表面受体: G蛋白偶联受体 | titlestyle = background:#e7dcc3 | groupstyle = background-color: AntiqueWhite |groupwidth = 6em; | group1 = 类型A: 视紫质类 | list1 =

{{Navbox subgroup

| group1 = 神经递质 | list1 =

肾上腺素
α1 (A, B, D) · α2 (A, B, C) · β1 · β2 · β3
嘌呤
腺苷受体(A1, A2A, A2B, A3) · P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
血清素
除5-HT3之外：5-HT1 (A, B, D, E, F) · 5-HT2 (A, B, C) · 5-HT (4, 5A, 6, 7)
其它
乙酰胆碱 (M1, M2, M3, M4, M5) · 多巴胺 (D1, D2, D3, D4, D5) · 组织胺 (H1, H2, H3, H4) · 褪黑素 (1A, 1B, 1C) · 痕量胺相关受体 (1, 2, 3, 5, 6, 8, 9)

| group2 = 代谢物及
信号分子 | list2 = {{Navbox subgroup 

 | oddstyle = background-color: AntiqueWhite;

| group1 = 花生酸 | list1 = 半胱氨酰白三烯素 (1, 2) · LTB4 (1, 2) · FPRL1 · 酮基花生酸 · 前列腺素 (D型 (1, 2

离子通道，细胞表面受体：配体门控离子通道
半胱氨酸环受体
5-HT/血清素
  • [[:5-HT3受体|5-HT3受体]]
GABA受体
  • GABAA
    • [[:α1|α1]]
    • [[:α2|α2]]
    • [[:α3|α3]]
    • [[:α4|α4]]
    • [[:α5|α5]]
    • [[:α6|α6]]
    • [[:β1|β1]]
    • [[:β2|β2]]
    • [[:β3|β3]]
    • [[:γ1|γ1]]
    • [[:γ2|γ2]]
    • [[:γ3|γ3]]
    • δ
    • ε
    • π
    • θ
  • [[:GABAA-ρ|GABAA-ρ]]
    • [[:ρ1|ρ1]]
    • [[:ρ2|ρ2]]
    • [[:ρ3|ρ3]]
甘氨酸受体
  • [[:α1|α1]]
  • [[:α2|α2]]
  • [[:α3|α3]]
  • [[:α4|α4]]
  • β
烟碱型乙酰胆碱受体
  • 五聚体：[[:(α3)2(β4)3|(α3)2(β4)3]]
  • [[:(α4)2(β2)3|(α4)2(β2)3]]
  • [[:(α7)5|(α7)5]]
  • [[:(α1)2(β4)3 - Ganglion type|(α1)2(β4)3 - Ganglion type]]
  • [[:(α1)2β1δε - Muscle type|(α1)2β1δε - Muscle type]]
锌激活
谷氨酸 门控离子型受体
仅能配体门控
电压和配体门控
孤儿受体
  • GluD
    • [[:δ1|δ1]]
    • [[:δ2|δ2]]
ATP门控
嘌呤受体
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