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

編輯

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

編輯

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

編輯
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]

參考資料

編輯
  1. ^ Hoyer D, Clarke DE, Fozard JR, Hartig PR, Martin GR, Mylecharane EJ, Saxena PR, Humphrey PP. International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin). Pharmacol. Rev. 1994, 46 (2): 157–203 [2016-04-25]. PMID 7938165. （原始內容存檔於2009-04-10）. 
  2. ^ Frazer A, Hensler JG. Chapter 13: Serotonin Receptors. Siegel GJ, Agranoff BW, Albers RW, Fisher SK, Uhler MD, editors (編). Basic Neurochemistry: Molecular, Cellular, and Medical Aspects. Philadelphia: Lippincott-Raven. 1999: 263–292 [2008-04-11]. ISBN 0-397-51820-X. （原始內容存檔於2008-12-01）. 
  3. ^ Qi YX, Xia RY, Wu YS, Stanley D, Huang J, Ye GY. Larvae of the small white butterfly, Pieris rapae, express a novel serotonin receptor. J. Neurochem. 2014, 131: 767–77. PMID 25187179. doi:10.1111/jnc.12940. 
  4. ^ Francken BJ, Jurzak M, Vanhauwe JF, Luyten WH, Leysen JE. The human 5-ht5A receptor couples to Gi/Go proteins and inhibits adenylate cyclase in HEK 293 cells.. Eur J Pharmacol. 1998, 361 (2–3): 299–309. PMID 9865521. doi:10.1016/S0014-2999(98)00744-4. 
  5. ^ Tomkins DM, Higgins GA, Sellers EM. Low doses of the 5-HT1A agonist 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH DPAT) increase ethanol intake. Psychopharmacology (Berl). 1994, 115 (1–2): 173–9. PMID 7862892. doi:10.1007/BF02244769. 
  6. ^ Müller CP, Carey RJ, Huston JP, De Souza Silva MA. Serotonin and psychostimulant addiction: focus on 5-HT1A-receptors. Prog Neurobiol. 2007, 81 (3): 133–78. PMID 17316955. doi:10.1016/j.pneurobio.2007.01.001. 
  7. ^ Carey RJ, DePalma G, Damianopoulos E, Shanahan A, Müller CP, Huston JP. Evidence that the 5-HT1A autoreceptor is an important pharmacological target for the modulation of cocaine behavioral stimulant effects. Brain Res. 2005, 1034 (1–2): 162–71. PMID 15713268. doi:10.1016/j.brainres.2004.12.012. 
  8. ^ 8.0 8.1 de Boer SF, Koolhaas JM. 5-HT1A and 5-HT1B receptor agonists and aggression: a pharmacological challenge of the serotonin deficiency hypothesis. Eur J Pharmacol. 2005, 526 (1–3): 125–39. PMID 16310183. doi:10.1016/j.ejphar.2005.09.065. 
  9. ^ Parks CL, Robinson PS, Sibille E, Shenk T, Toth M. Increased anxiety of mice lacking the serotonin1A receptor. Proceedings of the National Academy of Sciences of the United States of America. 1998, 195 (18): 10734–9. PMC 27964  . PMID 9724773. doi:10.1073/pnas.95.18.10734. 
  10. ^ Ebenezer IS, Arkle MJ, Tite RM. 8-Hydroxy-2-(di-n-propylamino)-tetralin inhibits food intake in fasted rats by an action at 5-HT1A receptors. Methods Find Exp Clin Pharmacol. 1998, 29 (4): 269–72. PMID 17609739. doi:10.1358/mf.2007.29.4.1075362. 
  11. ^ 11.0 11.1 Wouters W, Tulp MT, Bevan P. Flesinoxan lowers blood pressure and heart rate in cats via 5-HT1A receptors. Eur J Pharmacol. 1998, 149 (3): 213–23. PMID 2842163. doi:10.1016/0014-2999(88)90651-6. 
  12. ^ 12.0 12.1 Horiuchi J, McDowall LM, Dampney RA. Role of 5-HT(1A) receptors in the lower brainstem on the cardiovascular response to dorsomedial hypothalamus activation. Auton Neurosci. 2008, 142 (1–2): 71–6. PMID 18667366. doi:10.1016/j.autneu.2008.06.004. 
  13. ^ Nalivaiko E, Ootsuka Y, Blessing WW. Activation of 5-HT1A receptors in the medullary raphe reduces cardiovascular changes elicited by acute psychological and inflammatory stresses in rabbits. Am J Physiol Regul Integr Comp Physiol. 2005, 289 (2): R596–R604. PMID 15802554. doi:10.1152/ajpregu.00845.2004. 
  14. ^ 14.0 14.1 Lucot JB. Antiemetic effects of flesinoxan in cats: comparisons with 8-hydroxy-2-(di-n-propylamino)tetralin. Eur J Pharmacol. 1994, 253 (1–2): 53–60. PMID 8013549. doi:10.1016/0014-2999(94)90756-0. 
  15. ^ Winstanley CA, Theobald DE, Dalley JW, Robbins TW. Interactions between serotonin and dopamine in the control of impulsive choice in rats: therapeutic implications for impulse control disorders. Neuropsychopharmacology. 2005, 30 (4): 669–682. PMID 15688093. doi:10.1038/sj.npp.1300610. 
  16. ^ Ogren SO, Eriksson TM, Elvander-Tottie E, D'Addario C, Ekström JC, Svenningsson P, Meister B, Kehr J, Stiedl O. The role of 5-HT(1A) receptors in learning and memory. Behav. Brain Res. 2008, 195 (1): 54–77. PMID 18394726. doi:10.1016/j.bbr.2008.02.023. 
  17. ^ Yasuno F, Suhara T, Nakayama T, Ichimiya T, Okubo Y, Takano A, Ando T, Inoue M, Maeda J, Suzuki K. Inhibitory effect of hippocampal 5-HT1A receptors on human explicit memory. Am J Psychiatry. 2003, 160 (2): 334–40. PMID 12562581. doi:10.1176/appi.ajp.160.2.334. 
  18. ^ Kennett GA, Dourish CT, Curzon G. Antidepressant-like action of 5-HT1A agonists and conventional antidepressants in an animal model of depression. Eur J Pharmacol. 1987, 134 (3): 265–74. PMID 2883013. doi:10.1016/0014-2999(87)90357-8. 
  19. ^ Bardin L, Tarayre JP, Malfetes N, Koek W, Colpaert FC. Profound, non-opioid analgesia produced by the high-efficacy 5-HT(1A) agonist F 13640 in the formalin model of tonic nociceptive pain. Pharmacology. 2003, 67 (4): 182–194. PMID 12595749. doi:10.1159/000068404. 
  20. ^ 20.0 20.1 Millan MJ, Perrin-Monneyron S. Potentiation of fluoxetine-induced penile erections by combined blockade of 5-HT1A and 5-HT1B receptors. Eur J Pharmacol. 1997, 321 (3): 11–3. PMID 9085055. doi:10.1016/S0014-2999(97)00050-2. 
  21. ^ Prow MR, Martin KF, Heal DJ. 8-OH-DPAT-induced mydriasis in mice: a pharmacological characterisation. Eur J Pharmacol. 1996, 317 (1): 21–8. PMID 8982715. doi:10.1016/S0014-2999(96)00693-0. 
  22. ^ 22.0 22.1 Meyer LC, Fuller A, Mitchell D. Zacopride and 8-OH-DPAT reverse opioid-induced respiratory depression and hypoxia but not catatonic immobilization in goats. American Journal of Physiology. Regulatory, Integrative and Comparative Physiology. February 2006, 290 (2): R405–13. PMID 16166206. doi:10.1152/ajpregu.00440.2005. 
  23. ^ 23.0 23.1 Popova NK, Amstislavskaya TG. Involvement of the 5-HT(1A) and 5-HT(1B) serotonergic receptor subtypes in sexual arousal in male mice. Psychoneuroendocrinology. 2002, 27 (5): 609–18. PMID 11965359. doi:10.1016/S0306-4530(01)00097-X. 
  24. ^ Monti JM, Jantos H. Dose-dependent effects of the 5-HT1A receptor agonist 8-OH-DPAT on sleep and wakefulness in the rat. J Sleep Res. 1992, 1 (3): 169–175. PMID 10607047. doi:10.1111/j.1365-2869.1992.tb00033.x. 
  25. ^ Thompson MR, Callaghan PD, Hunt GE, Cornish JL, McGregor IS. A role for oxytocin and 5-HT(1A) receptors in the prosocial effects of 3,4 methylenedioxymethamphetamine ("ecstasy"). Neuroscience. 2007, 146 (2): 509–14. PMID 17383105. doi:10.1016/j.neuroscience.2007.02.032. 
  26. ^ Gudelsky GA, Koenig JI, Meltzer HY. Thermoregulatory responses to serotonin (5-HT) receptor stimulation in the rat. Evidence for opposing roles of 5-HT2 and 5-HT1A receptors. Neuropharmacology. 1986, 25 (12): 1307–13. PMID 2951611. doi:10.1016/0028-3908(86)90101-2. 
  27. ^ Ootsuka Y, Blessing WW. Activation of 5-HT1A receptors in rostral medullary raphé inhibits cutaneous vasoconstriction elicited by cold exposure in rabbits. Brain Res. 2006,. 1073-1074: 252–61. PMID 16455061. doi:10.1016/j.brainres.2005.12.031. 
  28. ^ 28.00 28.01 28.02 28.03 28.04 28.05 28.06 28.07 28.08 28.09 28.10 28.11 28.12 28.13 28.14 28.15 28.16 28.17 28.18 28.19 28.20 Pharmacology Corner > Serotonin (5-HT): receptors, agonists and antagonists （頁面存檔備份，存於互聯網檔案館） By Flavio Guzmán, M.D. on 9/08/09
  29. ^ 29.0 29.1 29.2 29.3 29.4 "BRINTELLIX™ (vortioxetine) tablets for oral use. Full Prescribing Information, Section 12.2 (Pharmacodynamics)." Takeda Pharmaceuticals America Inc. and Lundbeck, 2013. Revised September 2013. [1] （頁面存檔備份，存於互聯網檔案館）
  30. ^ Saxena, PR; Lawang, A. A comparison of cardiovascular and smooth muscle effects of 5-hydroxytryptamine and 5-carboxamidotryptamine, a selective agonist of 5-HT1 receptors.. Archives Internationales de Pharmacodynamie et de Thérapie. Oct 1985, 277 (2): 235–52. PMID 2933009. 
  31. ^ Cao BJ, Rodgers RJ. Comparative effects of novel 5-HT1A receptor ligands, LY293284, LY315712 and LY297996, on plus-maze anxiety in mice. Psychopharmacology. October 1998, 139 (3): 185–94. PMID 9784072. doi:10.1007/s002130050703. 
  32. ^ Harrison AA, Parsons LH, Koob GF, Markou A. RU 24969, a 5-HT1A/1B agonist, elevates brain stimulation reward thresholds: an effect reversed by GR 127935, a 5-HT1B/1D antagonist. Psychopharmacology (Berl). 1999, 141 (3): 242–50. PMID 10027505. doi:10.1007/s002130050831. 
  33. ^ Chojnacka-Wójcik E, Klodzinska A, Tatarczynska E. The anxiolytic-like effect of 5-HT1B receptor ligands in rats: a possible mechanism of action. J Pharm Pharmacol. 2005, 57 (2): 253–7. PMID 15720791. doi:10.1211/0022357055399. 
  34. ^ Lin D, Parsons LH. Anxiogenic-like effect of serotonin(1B) receptor stimulation in the rat elevated plus-maze. Pharmacol Biochem Behav. 2002, 71 (4): 581–7. PMID 11888549. doi:10.1016/S0091-3057(01)00712-2. 
  35. ^ 35.0 35.1 Tatarczynska E, Klodzinska A, Stachowicz K, Chojnacka-Wójcik E. Effects of a selective 5-HT1B receptor agonist and antagonists in animal models of anxiety and depression. Behav Pharmacol. 2004, 15 (8): 523–34. PMID 15577451. doi:10.1097/00008877-200412000-00001. 
  36. ^ 36.0 36.1 Eriksson TM, Madjid N, Elvander-Tottie E, Stiedl O, Svenningsson P, Ogren SO. Blockade of 5-HT 1B receptors facilitates contextual aversive learning in mice by disinhibition of cholinergic and glutamatergic neurotransmission. Neuropharmacology. 2008, 54 (7): 1041–50. PMID 18394658. doi:10.1016/j.neuropharm.2008.02.007. 
  37. ^ 37.0 37.1 McCreary AC, Bankson MG, Cunningham KA. Pharmacological studies of the acute and chronic effects of (+)-3, 4-methylenedioxymethamphetamine on locomotor activity: role of 5-hydroxytryptamine(1A) and 5-hydroxytryptamine(1B/1D) receptors. J Pharmacol Exp Ther. 1999, 290 (3): 965–73. PMID 10454466. 
  38. ^ Amital D, Fostick L, Sasson Y, Kindler S, Amital H, Zohar J. Anxiogenic effects of Sumatriptan in panic disorder: a double-blind, placebo-controlled study. Eur Neuropsychopharmacol. 2005, 15 (3): 279–82. PMID 15820416. doi:10.1016/j.euroneuro.2004.12.002. 
  39. ^ Feuerstein TJ, Hüring H, van Velthoven V, Lücking CH, Landwehrmeyer GB. 5-HT1D-like receptors inhibit the release of endogenously formed [3H]GABA in human, but not in rabbit, neocortex. Neurosci Lett. 1996, 209 (3): 210–4. PMID 8736648. doi:10.1016/0304-3940(96)12637-9. 
  40. ^ 40.0 40.1 [2] （頁面存檔備份，存於互聯網檔案館） Bubar MJ, Cunningham KA. Serotonin 5-HT2A and 5-HT2C receptors as potential targets for modulation of psychostimulant use and dependence. Curr Top Med Chem. 2006;6(18):1971-85.
  41. ^ Schreiber R, Melon C, De Vry J. The role of 5-HT receptor subtypes in the anxiolytic effects of selective serotonin reuptake inhibitors in the rat ultrasonic vocalization test. Psychopharmacology (Berl). 1998, 135 (4): 383–91. PMID 9539263. doi:10.1007/s002130050526. 
  42. ^ 42.0 42.1 Popova NK, Amstislavskaya TG. 5-HT2A and 5-HT2C serotonin receptors differentially modulate mouse sexual arousal and the hypothalamo-pituitary-testicular response to the presence of a female. Neuroendocrinology. 2002, 76 (1): 28–34. PMID 12097814. doi:10.1159/000063681. 
  43. ^ 43.0 43.1 Popa D, Léna C, Fabre V, Prenat C, Gingrich J, Escourrou P, Hamon M, Adrien J. Contribution of 5-HT2 receptor subtypes to sleep-wakefulness and respiratory control, and functional adaptations in knock-out mice lacking 5-HT2A receptors. J Neurosci. 2005, 25 (49): 11231–8. PMID 16339018. doi:10.1523/JNEUROSCI.1724-05.2005. 
  44. ^ 44.0 44.1 Mazzola-Pomietto P, Aulakh CS, Tolliver T, Murphy DL. Functional subsensitivity of 5-HT2A and 5-HT2C receptors mediating hyperthermia following acute and chronic treatment with 5-HT2A/2C receptor antagonists. Psychopharmacology (Berl). 1997, 130 (2): 144–51. PMID 9106912. doi:10.1007/s002130050222. 
  45. ^ Blessing WW, Seaman B. 5-hydroxytryptamine(2A) receptors regulate sympathetic nerves constricting the cutaneous vascular bed in rabbits and rats. Neuroscience. 2003, 117 (4): 939–948. PMID 12654345. doi:10.1016/S0306-4522(02)00810-2. 
  46. ^ 46.0 46.1 46.2 McCall, R. B.; Franklin, S. R.; Hyslop, D. K.; Knauer, C. S.; Chio, C. L.; Haber, C. L.; Fitzgerald, L. W. PNU-22394, a 5-HT2C receptor agonist, reduced feeding in rodents and produces weight loss in humans (Online) 27 (309.2). Presentation Number 309.2. Convention Center Exhibit Hall, Poster Board TT-45, San Diego, CA: Society for Neuroscience Abstracts. 2001 [18 July 2014]. （原始內容存檔於2014-11-04）.  |conference=被忽略 (幫助)
  47. ^ 47.0 47.1 47.2 Garfield AS, Heisler LK. Pharmacological targeting of the serotonergic system for the treatment of obesity. The Journal of Physiology. 2009, 587 (1): 49–60. PMC 2670022  . PMID 19029184. doi:10.1113/jphysiol.2008.164152. 
  48. ^ 48.0 48.1 48.2 Jensen, Anders A.; Plath, Niels; Pedersen, Martin Holst Friborg; Isberg, Vignir; et al. Design, Synthesis, and Pharmacological Characterization of N- and O-Substituted 5,6,7,8-Tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol Analogues: Novel 5-HT2A/5-HT2C Receptor Agonists with Pro-Cognitive Properties. Journal of Medicinal Chemistry. 2013, 56 (3): 1211–1227. ISSN 0022-2623. doi:10.1021/jm301656h. 
  49. ^ Kennett GA, Bright F, Trail B, Baxter GS, Blackburn TP. Effects of the 5-HT2B receptor agonist, BW 723C86, on three rat models of anxiety. Br J Pharmacol. 1996, 117 (7): 1443–8. PMC 1909458  . PMID 8730737. doi:10.1111/j.1476-5381.1996.tb15304.x. 
  50. ^ Duxon MS, Kennett GA, Lightowler S, Blackburn TP, Fone KC. Activation of 5-HT2B receptors in the medial amygdala causes anxiolysis in the social interaction test in the rat. Neuropharmacology. 1997, 36 (4–5): 601–8. PMID 9225285. doi:10.1016/S0028-3908(97)00042-7. 
  51. ^ Kennett GA, Trail B, Bright F. Anxiolytic-like actions of BW 723C86 in the rat Vogel conflict test are 5-HT2B receptor mediated. Neuropharmacology. 1998, 37 (12): 1603–10. PMID 9886683. doi:10.1016/S0028-3908(98)00115-4. 
  52. ^ Kennett GA, Ainsworth K, Trail B, Blackburn TP. BW 723C86, a 5-HT2B receptor agonist, causes hyperphagia and reduced grooming in rats. Neuropharmacology. 1997, 36 (2): 233–9. PMID 9144661. doi:10.1016/S0028-3908(96)00171-2. 
  53. ^ Borman RA, Tilford NS, Harmer DW, Day N, Ellis ES, Sheldrick RL, Carey J, Coleman RA, Baxter GS. 5-HT(2B) receptors play a key role in mediating the excitatory effects of 5-HT in human colon in vitro. Br J Pharmacol. 2002, 135 (5): 1144–1151. PMC 1573235  . PMID 11877320. doi:10.1038/sj.bjp.0704571. 
  54. ^ Kennett GA, Wood MD, Bright F, Trail B, Riley G, Holland V, Avenell KY, Stean T, Upton N, Bromidge S, Forbes IT, Brown AM, Middlemiss DN, Blackburn TP. SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology. 1997, 36 (4–5): 609–20. PMID 9225286. doi:10.1016/S0028-3908(97)00038-5. 
  55. ^ 55.0 55.1 Millan MJ, Brocco M, Gobert A, Dekeyne A. Anxiolytic properties of agomelatine, an antidepressant with melatoninergic and serotonergic properties: role of 5-HT2C receptor blockade. Psychopharmacology (Berl). 2005, 177 (4): 448–58. PMID 15289999. doi:10.1007/s00213-004-1962-z. 
  56. ^ 56.0 56.1 Millan MJ, Brocco M, Gobert A, Dekeyne A. S32006, a novel 5-HT2C receptor antagonist displaying broad-based antidepressant and anxiolytic properties in rodent models. Psychopharmacology (Berl). 2008, 199 (4): 549–68. PMID 18523738. doi:10.1007/s00213-008-1177-9. 
  57. ^ Fujitsuka N, Asakawa A, Hayashi M, Sameshima M, Amitani H, Kojima S, Fujimiya M, Inui A. Selective serotonin reuptake inhibitors modify physiological gastrointestinal motor activities via 5-HT2c receptor and acyl ghrelin. Biol Psychiatry. 2009, 65 (9): 748–759. PMID 19058784. doi:10.1016/j.biopsych.2008.10.031. 
  58. ^ Millan MJ, Peglion JL, Lavielle G, Perrin-Monneyron S. 5-HT2C receptors mediate penile erections in rats: actions of novel and selective agonists and antagonists. Eur J Pharmacol. 1997, 325 (1): 9–12. PMID 9151932. doi:10.1016/S0014-2999(97)89962-1. 
  59. ^ Stancampiano R, Melis MR, Argiolas A. Penile erection and yawning induced by 5-HT1C receptor agonists in male rats: relationship with dopaminergic and oxytocinergic transmission. Eur J Pharmacol. 1994, 261 (1–2): 149–55. PMID 8001637. doi:10.1016/0014-2999(94)90313-1. 
  60. ^ Frank MG, Stryker MP, Tecott LH. Sleep and sleep homeostasis in mice lacking the 5-HT2c receptor. Neuropsychopharmacology. 2002, 27 (5): 869–73. PMC 2452994  . PMID 12431861. doi:10.1016/S0893-133X(02)00353-6. 
  61. ^ Rang, H. P. Pharmacology. Edinburgh: Churchill Livingstone. 2003. ISBN 0-443-07145-4.  Page 187
  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. May 2005 [10 October 2014]. （原始內容存檔於2016-09-23）. 
  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  . 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  . 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. ^ Zhang, Shicheng; Chen, He; Zhang, Chengwei; Yang, Ying; Popov, Petr; Liu, Jing; Krumm, Brian E.; Cao, Can; Kim, Kuglae; Xiong, Yan; Katritch, Vsevolod. Inactive and active state structures template selective tools for the human 5-HT5A receptor. Nature Structural & Molecular Biology. 2022-07, 29 (7) [2022-10-02]. ISSN 1545-9993. PMC 9299520  . PMID 35835867. doi:10.1038/s41594-022-00796-6. （原始內容存檔於2022-10-06） （英語）. 
  77. ^ Wesolowska A. The anxiolytic-like effect of the selective 5-HT6 receptor antagonist SB-399885: the impact of benzodiazepine receptors. European Journal of Pharmacology. February 2008, 580 (3): 355–60. PMID 18096153. doi:10.1016/j.ejphar.2007.11.022. 
  78. ^ 78.0 78.1 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. April 2007, 52 (5): 1274–83. PMID 17320917. doi:10.1016/j.neuropharm.2007.01.007. 
  79. ^ 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. December 2006, 553 (1–3): 109–19. PMID 17069795. doi:10.1016/j.ejphar.2006.09.049. 
  80. ^ 80.0 80.1 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. July 2005, 81 (3): 673–82. PMID 15964617. doi:10.1016/j.pbb.2005.05.005. 
  81. ^ 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. March 2008, 582 (1–3): 88–93. PMID 18234190. doi:10.1016/j.ejphar.2007.12.013. 
  82. ^ Target Schizophrenia - Possible future developments. The Association of the British Pharmaceutical Industry. [2008-04-11]. （原始內容存檔於2008-06-12）. 
  83. ^ 83.0 83.1 83.2 Hedlund PB, Huitron-Resendiz S, Henriksen SJ, Sutcliffe JG. 5-HT7 receptor inhibition and inactivation induce antidepressantlike behavior and sleep pattern. Biological Psychiatry. November 2005, 58 (10): 831–7. PMID 16018977. doi:10.1016/j.biopsych.2005.05.012. 
  84. ^ 84.0 84.1 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. September 2006, 51 (3): 578–86. PMID 16828124. doi:10.1016/j.neuropharm.2006.04.017. 
  85. ^ Gasbarri A, Cifariello A, Pompili A, Meneses A. Effect of 5-HT(7) antagonist SB-269970 in the modulation of working and reference memory in the rat. Behavioural Brain Research. December 2008, 195 (1): 164–70. PMID 18308404. doi:10.1016/j.bbr.2007.12.020. 
  86. ^ Liy-Salmeron G, Meneses A. Effects of 5-HT drugs in prefrontal cortex during memory formation and the ketamine amnesia-model. Hippocampus. 2008, 18 (9): 965–74. PMID 18570192. doi:10.1002/hipo.20459. 
  87. ^ 87.0 87.1 Bonaventure P, Kelly L, Aluisio L, Shelton J, Lord B, Galici R, Miller K, Atack J, Lovenberg TW, Dugovic C. Selective blockade of 5-hydroxytryptamine (5-HT)7 receptors enhances 5-HT transmission, antidepressant-like behavior, and rapid eye movement sleep suppression induced by citalopram in rodents. J Pharmacol Exp Ther. 2007, 321 (2): 690–8. PMID 17314195. doi:10.1124/jpet.107.119404. 
  88. ^ Thomas DR, Melotto S, Massagrande M, Gribble AD, Jeffrey P, Stevens AJ, Deeks NJ, Eddershaw PJ, Fenwick SH, Riley G, Stean T, Scott CM, Hill MJ, Middlemiss DN, Hagan JJ, Price GW, Forbes IT. SB-656104-A, a novel selective 5-HT7 receptor antagonist, modulates REM sleep in rats. Br J Pharmacol. 2003, 139 (4): 705–14. PMC 1573887  . PMID 12812993. doi:10.1038/sj.bjp.0705290. 
  89. ^ Davies MA, Sheffler DJ, Roth BL. Aripiprazole: A Novel Atypical Antipsychotic Drug With a Uniquely Robust Pharmacology. CNS Drug Reviews [Internet]. 2004 [cited 2013 Aug 4];10(4):317–36. Available from: http://onlinelibrary.wiley.com/doi/10.1111/j.1527-3458.2004.tb00030.x/pdf （頁面存檔備份，存於互聯網檔案館）

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