fbpx
维基百科

5-羟色胺受体

十二月 02, 2023

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。

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（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受體亚家族包括5-HT2A、5-HT2B，和5-HT2C三種受體蛋白。
  • 5-HT3受體
  • 5-HT4受體
  • 5-HT5受體亚家族包括5-HT5A、5-HT5B两種受體蛋白。（其中5B受体在人类中为假基因，无受体表达）
  • 5-HT6受體
  • 5-HT7受體

總共有十四種受體亞型。

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 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IP3和DAG（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
  • HTR1A
 是 是 否 否 否 否

選擇性

  • Vilazodone（英语：Vilazodone） (Viibryd)
  • F-15,599（英语：F-15,599） (research compound, highly potent and selective for 5-HT1A)
  • Flesinoxan（英语：Flesinoxan） (potent, EC50 = 24 nM)
  • Gepirone（英语：Gepirone） (部分激动剂, Ki = 70 nM)
  • 氟哌啶醇
  • Ipsapirone（英语：Ipsapirone） (部分激动剂, Ki = 12.1 nM)
  • 喹硫平
  • Trazodone (SARI（英语：Serotonin antagonist and reuptake inhibitor）, selective in the sense that on all other 5-HT receptors it acts as either an antagonist or has no action. Kd = 78nM)
  • 育亨宾 (unselective 部分激动剂)
  • 坦度螺酮 (potent and selective 部分激动剂)

非選擇性

  • BMY 7378（英语：BMY 7378）
  • Cyanopindolol（英语：Cyanopindolol）
  • Iodocyanopindolol（英语：Iodocyanopindolol）
  • Lecozotan（英语：Lecozotan）
  • Methiothepin（英语：Methiothepin）
  • Methysergide（英语：Methysergide）[30]
  • NAN-190（英语：NAN-190）
  • Nebivolol（英语：Nebivolol）
  • Nefazodone（英语：Nefazodone）
  • WAY-100,135（英语：WAY-100,135）
  • WAY-100,635（英语：WAY-100,635）
  • Mefway（英语：Mefway）
  • 镇痛药 (agonists)
  • 抗抑郁药 (post-synaptic receptor agonists and pre-synaptic autoreceptor（英语：autoreceptor） antagonists serve as antidepressants)
  • Anxiolytics（英语：Anxiolytics）[31] (antagonist)
5-HT1B（英语：5-HT1B receptor） 1992
  • HTR1B
 是 是 否 否 否 否
  • 5-CT（英语：5-Carboxamidotryptamine）
  • CGS-12066A（英语：CGS-12066A）
  • CP-93,129（英语：CP-93,129）
  • CP-94,253（英语：CP-94,253）
  • Dihydroergotamine（英语：Dihydroergotamine）
  • Eltoprazine（英语：Eltoprazine）
  • Ergotamine
  • Methysergide（英语：Methysergide）
  • RU 24969（英语：RU 24969）
  • TFMPP（英语：TFMPP）
  • Triptans（英语：Triptans）[28] (antimigraine（英语：antimigraine）[28])
  • Vortioxetine (部分激动剂, Ki = 33 nM)[29]
  • Alprenolol
  • AR-A000002（英语：AR-A000002）
  • Asenapine（英语：Asenapine）
  • Cyanopindolol（英语：Cyanopindolol）
  • GR-127,935（英语：GR-127,935）
  • Iodocyanopindolol（英语：Iodocyanopindolol）
  • Isamoltane（英语：Isamoltane）
  • Metergoline（英语：Metergoline）
  • Methiothepin（英语：Methiothepin）
  • Oxprenolol（英语：Oxprenolol）
  • Pindolol（英语：Pindolol）
  • 普萘洛尔
  • SB-216,641（英语：SB-216,641）
  • 育亨宾
  • 偏頭痛 (e.g. triptans（英语：triptans）)
5-HT1D（英语：5-HT1D receptor） 1991
  • HTR1D
 是 是 否 否 否 否
  • 5-CT（英语：5-Carboxamidotryptamine）
  • CP-135,807（英语：CP-135,807）
  • Dihydroergotamine（英语：Dihydroergotamine）
  • Ergotamine
  • Methysergide（英语：Methysergide）
  • Triptans（英语：Triptans）[28] (antimigraine（英语：antimigraine）[28])
  • 育亨宾
  • BRL-15572（英语：BRL-15572）
  • GR-127,935（英语：GR-127,935）
  • Ketanserin（英语：Ketanserin）
  • Metergoline（英语：Metergoline）
  • Methiothepin（英语：Methiothepin）
  • Rauwolscine（英语：Rauwolscine）
  • Ritanserin（英语：Ritanserin）
  • Vortioxetine (Ki = 54 nM)[29]
  • Ziprasidone
  • 偏頭痛 (e.g. triptans（英语：triptans）)
5-HT1E（英语：5-HT1E） 1992
  • HTR1E
 是 是 否 否 否 否
  • BRL-54443（英语：BRL-54443）
  • None known
5-HT1F（英语：5-HT1F） 1993
  • HTR1F
 否 是 否 否 否 否
  • Migraine
  • BRL-54443（英语：BRL-54443）
  • Lasmiditan（英语：Lasmiditan）
  • LY-334,370（英语：LY-334,370）
  • Naratriptan（英语：Naratriptan）
  • None known
5-HT2A（英语：5-HT2A receptor） 1988
  • HTR2A
 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
  • HTR2B
 是 是 是 是 是 是
  • 阿戈美拉汀
  • Asenapine（英语：Asenapine）
  • BZP（英语：Benzylpiperazine）
  • Ketanserin（英语：Ketanserin）
  • Methysergide（英语：Methysergide）
  • Ritanserin（英语：Ritanserin）
  • RS-127,445（英语：RS-127,445）
  • Tegaserod（英语：Tegaserod）
  • 育亨宾
5-HT2C（英语：5-HT2C receptor） 1988
  • HTR2C
 是 是 是 是 是 是
  • A-372,159（英语：A-372,159）
  • AL-38022A（英语：AL-38022A）
  • 阿立哌唑
  • Ergonovine
  • Lorcaserin（英语：Lorcaserin）
  • PNU-22394（英语：PNU-22394） (Full agonist)[46][47][48]
  • Ro60-0175（英语：Ro60-0175）
  • TFMPP（英语：TFMPP）
  • Trazodone[28] (安眠药[28])
  • YM-348（英语：YM-348）
5-HT3（英语：5-HT3 receptor） 1993
  • HTR3A
  • HTR3B
  • HTR3C
  • HTR3D
  • HTR3E
 否 是 是 否 是 否
  • 成瘾
  • 焦虑
  • Emesis
  • GI Motility[62]
  • Learning[63]
  • 记忆[63]
  • Nausea
  • 2-Methyl-5-HT
  • BZP（英语：Benzylpiperazine）
  • Quipazine（英语：Quipazine）
  • RS-56812（英语：RS-56812）
5-HT4 1995
  • HTR4
 否 是 是 否 是 否
  • 5-MT
  • BIMU-8（英语：BIMU-8）
  • Cinitapride（英语：Cinitapride）
  • Cisapride（英语：Cisapride）[28] (gastroprokinetic（英语：prokinetic agent）)
  • Dazopride（英语：Dazopride）
  • Metoclopramide
  • Mosapride
  • Prucalopride（英语：Prucalopride）
  • RS-67333（英语：RS-67333）
  • Renzapride（英语：Renzapride）
  • Tegaserod（英语：Tegaserod）
  • Zacopride
5-HT5A（英语：5-HT5A receptor） 1994
  • HTR5A
 否 是 否 否 否 否
  • Asenapine（英语：Asenapine）
  • Dimebolin（英语：Dimebolin）
  • Methiothepin（英语：Methiothepin）
  • Ritanserin（英语：Ritanserin）
  • SB-699,551（英语：SB-699,551）
  • SB-699,551-A（英语：SB-699,551-A）
  • None thus far
5-HT5B（英语：5-HT5B receptor） 1993
  • HTR5BP
 否 否 否 否 否 否

Functions in rodents,
pseudogene in humans

  • None thus far
5-HT6（英语：5-HT6 receptor） 1993
  • HTR6
 否 是 否 否 否 否
  • EMD-386,088（英语：EMD-386,088）
  • EMDT（英语：2-Ethyl-5-methoxy-N,N-dimethyltryptamine）
  • Amitriptyline
  • Aripiprazole
  • Asenapine（英语：Asenapine）
  • Clomipramine
  • Clozapine
  • Dimebolin（英语：Dimebolin）
  • EGIS-12233（英语：EGIS-12233）
  • Haloperidol
  • Iloperidone（英语：Iloperidone）
  • MS-245（英语：MS-245）
  • Olanzapine
  • Ro04-6790（英语：Ro04-6790）
  • SB-258,585（英语：SB-258,585）
  • SB-271,046（英语：SB-271,046）[82]
  • SB-357,134（英语：SB-357,134）
  • SB-399,885（英语：SB-399,885）
5-HT7（英语：5-HT7 receptor） 1993
  • HTR7
 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（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 编辑

  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. （原始内容于2009-04-10）. 
  2. ^ Frazer A, Hensler JG. Chapter 13: Serotonin Receptors. Siegel GJ, Agranoff BW, Albers RW, Fisher SK, Uhler MD, editors (编). Basic Neurochemistry: Molecular, Cellular, and Medical Aspects. Philadelphia: Lippincott-Raven. 1999: 263–292 [2008-04-11]. ISBN 0-397-51820-X. （原始内容于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 （页面存档备份，存于互联网档案馆） 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] （页面存档备份，存于互联网档案馆）
  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] （页面存档备份，存于互联网档案馆） 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]. （原始内容于2014-11-04）.  |conference=被忽略 (帮助)
  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]. （原始内容于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. （原始内容于2022-10-06） （英语）. 
  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. ^ . The Association of the British Pharmaceutical Industry. [2008-04-11]. （原始内容存档于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 （页面存档备份，存于互联网档案馆）

外部链接 编辑

  • 醫學主題詞表（MeSH）：Serotonin+Receptors
  • 5-Hydroxytryptamine Receptors. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. （原始内容于2016-06-01）. 
  • Rubenstein, LA, Lanzara RG. Activation of G protein-coupled receptors entails cysteine modulation of agonist binding. Cogprints. 2005-02-16 [2008-04-11]. （原始内容于2011-05-16）. 

#invoke:navbox

十二月 02, 2023
羟色胺受体, 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, 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, 英语, 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, 目录, 分類, 家族, 亞型, 参考资料, 外部链接分類, 编辑血清素受體可分為七個亞科, 至少有十四種受體亞型已被發現, 包含g蛋白偶聯受體, protein, coupled, rece. 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 目录 1 分類 1 1 家族 1 2 亞型 2 参考资料 3 外部链接分類 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 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受體亚家族包括5 HT2A 5 HT2B 和5 HT2C三種受體蛋白 5 HT3受體5 HT4受體5 HT5受體亚家族包括5 HT5A 5 HT5B两種受體蛋白 其中5B受体在人类中为假基因 无受体表达 5 HT6受體5 HT7受體總共有十四種受體亞型 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 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IP3和DAG 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 HTR1A 是 是 否 否 否 否 成癮 5 6 7 侵略性 8 焦慮 9 食慾 10 自身受體 血壓 11 12 心血管功能 13 嘔吐 14 心率 11 12 Impulsivity 15 記憶 16 17 情緒 18 噁心 14 痛覺 19 陰莖勃起 20 散瞳 21 呼吸 22 性方面的舉動 23 睡覺 24 社交能力 25 體溫調節 26 血管收縮 27 選擇性 Vilazodone 英语 Vilazodone Viibryd F 15 599 英语 F 15 599 research compound highly potent and selective for 5 HT1A Flesinoxan 英语 Flesinoxan potent EC50 24 nM Gepirone 英语 Gepirone 部分激动剂 Ki 70 nM 氟哌啶醇 Ipsapirone 英语 Ipsapirone 部分激动剂 Ki 12 1 nM 喹硫平 Trazodone SARI 英语 Serotonin antagonist and reuptake inhibitor selective in the sense that on all other 5 HT receptors it acts as either an antagonist or has no action Kd 78nM 育亨宾 unselective 部分激动剂 坦度螺酮 potent and selective 部分激动剂 非選擇性 5 CT 英语 5 Carboxamidotryptamine potent Ki 250 50 pM 8 OH DPAT potent 阿立哌唑 atypical antipsychotic Asenapine 英语 Asenapine atypical antipsychotic 丁螺環酮 28 部分激动剂 Vortioxetine high efficacy 部分激动剂 29 Ziprasidone 部分激动剂 Ki 3 4 nM BMY 7378 英语 BMY 7378 Cyanopindolol 英语 Cyanopindolol Iodocyanopindolol 英语 Iodocyanopindolol Lecozotan 英语 Lecozotan Methiothepin 英语 Methiothepin Methysergide 英语 Methysergide 30 NAN 190 英语 NAN 190 Nebivolol 英语 Nebivolol Nefazodone 英语 Nefazodone WAY 100 135 英语 WAY 100 135 WAY 100 635 英语 WAY 100 635 Mefway 英语 Mefway 镇痛药 agonists 抗抑郁药 post synaptic receptor agonists and pre synaptic autoreceptor 英语 autoreceptor antagonists serve as antidepressants Anxiolytics 英语 Anxiolytics 31 antagonist 5 HT1B 英语 5 HT1B receptor 1992 HTR1B 是 是 否 否 否 否 成瘾 32 Aggression 8 焦虑 33 34 35 Autoreceptor Learning 36 Locomotion 37 记忆 36 情绪 35 陰莖勃起 20 性行为 23 血管收缩 5 CT 英语 5 Carboxamidotryptamine CGS 12066A 英语 CGS 12066A CP 93 129 英语 CP 93 129 CP 94 253 英语 CP 94 253 Dihydroergotamine 英语 Dihydroergotamine Eltoprazine 英语 Eltoprazine Ergotamine Methysergide 英语 Methysergide RU 24969 英语 RU 24969 TFMPP 英语 TFMPP Triptans 英语 Triptans 28 antimigraine 英语 antimigraine 28 佐米曲普坦 Eletriptan 英语 Eletriptan 舒马曲坦 Vortioxetine 部分激动剂 Ki 33 nM 29 Alprenolol AR A000002 英语 AR A000002 Asenapine 英语 Asenapine Cyanopindolol 英语 Cyanopindolol GR 127 935 英语 GR 127 935 Iodocyanopindolol 英语 Iodocyanopindolol Isamoltane 英语 Isamoltane Metergoline 英语 Metergoline Methiothepin 英语 Methiothepin Oxprenolol 英语 Oxprenolol Pindolol 英语 Pindolol 普萘洛尔 SB 216 641 英语 SB 216 641 育亨宾 偏頭痛 e g triptans 英语 triptans 5 HT1D 英语 5 HT1D receptor 1991 HTR1D 是 是 否 否 否 否 焦虑 38 39 Autoreceptor Locomotion 37 血管收缩 5 CT 英语 5 Carboxamidotryptamine CP 135 807 英语 CP 135 807 Dihydroergotamine 英语 Dihydroergotamine Ergotamine Methysergide 英语 Methysergide Triptans 英语 Triptans 28 antimigraine 英语 antimigraine 28 Almotriptan 英语 Almotriptan Eletriptan 英语 Eletriptan Frovatriptan 英语 Frovatriptan Naratriptan 英语 Naratriptan 利扎曲坦 舒马曲坦 佐米曲普坦 育亨宾 BRL 15572 英语 BRL 15572 GR 127 935 英语 GR 127 935 Ketanserin 英语 Ketanserin Metergoline 英语 Metergoline Methiothepin 英语 Methiothepin Rauwolscine 英语 Rauwolscine Ritanserin 英语 Ritanserin Vortioxetine Ki 54 nM 29 Ziprasidone 偏頭痛 e g triptans 英语 triptans 5 HT1E 英语 5 HT1E 1992 HTR1E 是 是 否 否 否 否 BRL 54443 英语 BRL 54443 None known5 HT1F 英语 5 HT1F 1993 HTR1F 否 是 否 否 否 否 Migraine BRL 54443 英语 BRL 54443 Lasmiditan 英语 Lasmiditan LY 334 370 英语 LY 334 370 Naratriptan 英语 Naratriptan None known5 HT2A 英语 5 HT2A receptor 1988 HTR2A 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 25I NBOMe 英语 25I NBOMe Full agonist 2C B 5 MeO DMT BZP 英语 Benzylpiperazine 蟾毒色胺 DMT DOM 英语 2 5 Dimethoxy 4 methylamphetamine Ergonovine Lisuride 英语 Lisuride LSD 麦司卡林 Myristicin PNU 22394 英语 PNU 22394 部分激动剂 46 47 48 脱磷酸裸盖菇素 裸盖菇素 TFMPP 英语 TFMPP 部分激动剂 or antagonist Atypical antipsychotics Clozapine 28 奥氮平 喹硫平 維思通 Ziprasidone 阿立哌唑 Asenapine 英语 Asenapine 阿米替林 Clomipramine Cyproheptadine Eplivanserin 英语 Eplivanserin Etoperidone 英语 Etoperidone 氟哌啶醇 羟嗪 Iloperidone 英语 Iloperidone Ketanserin 英语 Ketanserin 28 抗高血压药 28 Methysergide 英语 Methysergide 米塞林 米氮平 Nefazodone 英语 Nefazodone Pimavanserin 英语 Pimavanserin Pizotifen 英语 Pizotifen Ritanserin 英语 Ritanserin Trazodone 育亨宾 Atypical antipsychotics antagonist 迷幻药物 部分激动剂 去甲肾上腺素和特异性5 羟色胺能抗抑郁药s antidepressants and anxiolytics they serve as antagonists at this site Treating serotonin syndrome 英语 serotonin syndrome antagonists e g cyproheptadine 睡眠ing aid antagonists e g trazodone 5 HT2B 1992 HTR2B 是 是 是 是 是 是 焦虑 49 50 51 食欲 52 心血管功能 GI Motility 53 睡眠 43 血管收缩 BW 723C86 氟苯丙胺 MDMA Norfenfluramine 英语 Norfenfluramine PNU 22394 英语 PNU 22394 部分激动剂 46 47 48 Ro60 0175 英语 Ro60 0175 阿戈美拉汀 Asenapine 英语 Asenapine BZP 英语 Benzylpiperazine Ketanserin 英语 Ketanserin Methysergide 英语 Methysergide Ritanserin 英语 Ritanserin RS 127 445 英语 RS 127 445 Tegaserod 英语 Tegaserod 育亨宾 偏頭痛 拮抗剂 5 HT2C 英语 5 HT2C receptor 1988 HTR2C 是 是 是 是 是 是 成瘾 potentially modulating 40 焦虑 54 55 56 食欲 GI Motility 57 Heteroreceptor 英语 Heteroreceptor for 去甲肾上腺素 and 多巴胺 Locomotion 情绪 55 56 陰莖勃起 58 59 性行为 42 睡眠 60 体温调节 44 血管收缩 A 372 159 英语 A 372 159 AL 38022A 英语 AL 38022A 阿立哌唑 Ergonovine Lorcaserin 英语 Lorcaserin PNU 22394 英语 PNU 22394 Full agonist 46 47 48 Ro60 0175 英语 Ro60 0175 TFMPP 英语 TFMPP Trazodone 28 安眠药 28 YM 348 英语 YM 348 阿戈美拉汀 28 抗抑郁药 28 阿米替林 Asenapine 英语 Asenapine Clomipramine Clozapine 28 抗精神病药 28 Cyproheptadine Dimebolin 英语 Dimebolin Eltoprazine 英语 Eltoprazine Etoperidone 英语 Etoperidone 氟西汀 氟哌啶醇 Iloperidone 英语 Iloperidone Ketanserin 英语 Ketanserin 28 抗高血压药 28 Lisuride 英语 Lisuride Methysergide 英语 Methysergide 61 米塞林 米氮平 Nefazodone 英语 Nefazodone 奥氮平 帕罗西汀 喹硫平 維思通 Ritanserin 英语 Ritanserin 曲马多 Trazodone Ziprasidone 抗抑郁药 e g 阿戈美拉汀 氟西汀 米氮平 Orexigenic 英语 Orexigenic e g mirtazapine clozapine and olanzapine antagonists Anorectic 英语 Anorectic Lorcaserin 抗精神病药 Vabicaserin agonists 5 HT3 英语 5 HT3 receptor 1993 HTR3A HTR3B HTR3C HTR3D HTR3E 否 是 是 否 是 否 成瘾 焦虑 Emesis GI Motility 62 Learning 63 记忆 63 Nausea 2 Methyl 5 HT BZP 英语 Benzylpiperazine Quipazine 英语 Quipazine RS 56812 英语 RS 56812 Alosetron 英语 Alosetron Several antiemetics 28 Dolasetron 英语 Dolasetron Ondansetron 28 Granisetron 英语 Granisetron Tropisetron 英语 Tropisetron Clozapine Memantine Metoclopramide Mianserin Mirtazapine Olanzapine Quetiapine Vortioxetine Ki 3 7 nM 29 Antiemetic5 HT4 1995 HTR4 否 是 是 否 是 否 焦虑 64 65 食欲 66 67 GI Motility Learning 68 69 记忆 68 69 70 情绪 71 72 呼吸 73 5 MT BIMU 8 英语 BIMU 8 Cinitapride 英语 Cinitapride Cisapride 英语 Cisapride 28 gastroprokinetic 英语 prokinetic agent Dazopride 英语 Dazopride Metoclopramide Mosapride Prucalopride 英语 Prucalopride RS 67333 英语 RS 67333 Renzapride 英语 Renzapride Tegaserod 英语 Tegaserod Zacopride L Lysine 64 Piboserod 英语 Piboserod Gastroprokinetics e g Tegaserod 5 HT5A 英语 5 HT5A receptor 1994 HTR5A 否 是 否 否 否 否 Autoreceptor Locomotion 74 睡眠 75 5 CT 英语 5 Carboxamidotryptamine Ergotamine Lisuride 部分激动剂 76 Valerenic Acid 部分激动剂 75 Asenapine 英语 Asenapine Dimebolin 英语 Dimebolin Methiothepin 英语 Methiothepin Ritanserin 英语 Ritanserin SB 699 551 英语 SB 699 551 SB 699 551 A 英语 SB 699 551 A None thus far5 HT5B 英语 5 HT5B receptor 1993 HTR5BP 否 否 否 否 否 否 Functions in rodents pseudogene in humans None thus far5 HT6 英语 5 HT6 receptor 1993 HTR6 否 是 否 否 否 否 焦虑 77 78 Cognition 79 Learning 80 记忆 80 情绪 78 81 EMD 386 088 英语 EMD 386 088 EMDT 英语 2 Ethyl 5 methoxy N N dimethyltryptamine Amitriptyline Aripiprazole Asenapine 英语 Asenapine Clomipramine Clozapine Dimebolin 英语 Dimebolin EGIS 12233 英语 EGIS 12233 Haloperidol Iloperidone 英语 Iloperidone MS 245 英语 MS 245 Olanzapine Ro04 6790 英语 Ro04 6790 SB 258 585 英语 SB 258 585 SB 271 046 英语 SB 271 046 82 SB 357 134 英语 SB 357 134 SB 399 885 英语 SB 399 885 Antidepressant antagonists and agonists Anxiolytic antagonists and agonist Nootropic antagonists Anorectic 英语 Anorectic antagonists 5 HT7 英语 5 HT7 receptor 1993 HTR7 是 是 是 否 否 否 焦虑 83 84 自身受體 记忆 85 86 情绪 83 84 呼吸 22 87 睡眠 83 87 88 体温调节 血管收缩 5 CT 英语 5 Carboxamidotryptamine 8 OH DPAT 阿立哌唑 部分激动剂 89 AS 19 英语 AS 19 drug E 55888 英语 E 55888 RA 7 阿米替林 Asenapine 英语 Asenapine Clomipramine Clozapine EGIS 12233 英语 EGIS 12233 氟哌啶醇 Iloperidone 英语 Iloperidone Imipramine 英语 Imipramine Ketanserin 英语 Ketanserin 米氮平 奥氮平 Ritanserin 英语 Ritanserin 維思通 SB 269 970 英语 SB 269 970 Vortioxetine Ki 19 nM 29 抗抑郁药 antagonists Anxiolytics 英语 Anxiolytics antagonists 益智药 antagonists 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 编辑 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 原始内容存档于2009 04 10 Frazer A Hensler JG Chapter 13 Serotonin Receptors Siegel GJ Agranoff BW Albers RW Fisher SK Uhler MD editors 编 Basic Neurochemistry Molecular Cellular and Medical Aspects Philadelphia Lippincott Raven 1999 263 292 2008 04 11 ISBN 0 397 51820 X 原始内容存档于2008 12 01 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 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 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 Muller 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 Carey RJ DePalma G Damianopoulos E Shanahan A Muller 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 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 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 nbsp PMID 9724773 doi 10 1073 pnas 95 18 10734 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 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 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 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 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 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 Ogren SO Eriksson TM Elvander Tottie E D Addario C Ekstrom 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 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 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 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 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 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 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 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 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 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 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 Ootsuka Y Blessing WW Activation of 5 HT1A receptors in rostral medullary raphe 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 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 gt Serotonin 5 HT receptors agonists and antagonists 页面存档备份 存于互联网档案馆 By Flavio Guzman M D on 9 08 09 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 页面存档备份 存于互联网档案馆 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 Therapie Oct 1985 277 2 235 52 PMID 2933009 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 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 Chojnacka Wojcik 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 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 0 35 1 Tatarczynska E Klodzinska A Stachowicz K Chojnacka Wojcik 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 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 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 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 Feuerstein TJ Huring H van Velthoven V Lucking 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 0 40 1 2 页面存档备份 存于互联网档案馆 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 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 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 0 43 1 Popa D Lena 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 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 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 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 原始内容存档于2014 11 04 conference 被忽略 帮助 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 nbsp PMID 19029184 doi 10 1113 jphysiol 2008 164152 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 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 nbsp PMID 8730737 doi 10 1111 j 1476 5381 1996 tb15304 x 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 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 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 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 nbsp PMID 11877320 doi 10 1038 sj bjp 0704571 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 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 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 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 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 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 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 nbsp PMID 12431861 doi 10 1016 S0893 133X 02 00353 6 Rang H P Pharmacology Edinburgh Churchill Livingstone 2003 ISBN 0 443 07145 4 Page 187 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 原始内容存档于2016 09 23 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 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 nbsp PMID 14676321 doi 10 1073 pnas 2436556100 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 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 nbsp PMID 17913892 doi 10 1073 pnas 0701471104 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 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 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 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 Lucas G Rymar V V Du J Mnie Filali O Bisgaard C Manta S Lambas Senas L Wiborg O Haddjeri N Pineyro 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 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 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 Nelson DL 5 HT5 receptors Curr Drug Targets CNS Neurol Disord 2004 3 1 53 8 PMID 14965244 doi 10 2174 1568007043482606 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 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 amp Molecular Biology 2022 07 29 7 2022 10 02 ISSN 1545 9993 PMC 9299520 nbsp PMID 35835867 doi 10 1038 s41594 022 00796 6 原始内容存档于2022 10 06 英语 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 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 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 0 80 1 Perez Garcia 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 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 Target Schizophrenia Possible future developments The Association of the British Pharmaceutical Industry 2008 04 11 原始内容存档于2008 06 12 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 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 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 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 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 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 nbsp PMID 12812993 doi 10 1038 sj bjp 0705290 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 页面存档备份 存于互联网档案馆 外部链接 编辑醫學主題詞表 MeSH Serotonin Receptors 5 Hydroxytryptamine Receptors IUPHAR Database of Receptors and Ion Channels International Union of Basic and Clinical Pharmacology 原始内容存档于2016 06 01 Rubenstein LA Lanzara RG Activation of G protein coupled receptors entails cysteine modulation of agonist binding Cogprints 2005 02 16 2008 04 11 原始内容存档于2011 05 16 invoke navbox 取自 https zh wikipedia org w index php title 5 羟色胺受体 amp oldid 79616975, 维基百科，wiki，书籍，书籍，图书馆，

文章

，阅读，下载，免费，免费下载，mp3，视频，mp4，3gp， jpg，jpeg，gif，png，图片，音乐，歌曲，电影，书籍，游戏，游戏。