5-HT receptor

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Serotonin

The serotonin receptors also known as 5-hydroxytryptamine receptors or 5-HT receptors are a group of G protein-coupled receptors (GPCRs) and ligand-gated ion channels (LGICs) found in the central and peripheral nervous systems.[1][2] They mediate both excitatory and inhibitory neurotransmission. The serotonin receptors are activated by the neurotransmitter serotonin, which acts as their natural ligand.

The serotonin receptors modulate the release of many neurotransmitters, including glutamate, GABA, dopamine, epinephrine / norepinephrine, and acetylcholine, as well as many hormones, including oxytocin, prolactin, vasopressin, cortisol, corticotropin, and substance P, among others. The serotonin receptors influence various biological and neurological processes such as aggression, anxiety, appetite, cognition, learning, memory, mood, nausea, sleep, and thermoregulation. The serotonin receptors are the target of a variety of pharmaceutical and illicit drugs, including many antidepressants, antipsychotics, anorectics, antiemetics, gastroprokinetic agents, antimigraine agents, hallucinogens, and entactogens.[3]

Classification

With the exception of the 5-HT3 receptor, a ligand-gated ion channel, all other serotonin receptors are G protein-coupled receptors that activate an intracellular second messenger cascade to produce an excitatory or inhibitory response.

Families

Family Type Mechanism Potential
5-HT1 Gi/Go-protein coupled. Decreasing cellular levels of cAMP. Inhibitory
5-HT2 Gq/G11-protein coupled. Increasing cellular levels of IP3 and DAG. Excitatory
5-HT3 Ligand-gated Na+ and K+ cation channel. Depolarizing plasma membrane. Excitatory
5-HT4 Gs-protein coupled. Increasing cellular levels of cAMP. Excitatory
5-HT5 Gi/Go-protein coupled.[4] Decreasing cellular levels of cAMP. Inhibitory
5-HT6 Gs-protein coupled. Increasing cellular levels of cAMP. Excitatory
5-HT7 Gs-protein coupled. Increasing cellular levels of cAMP. Excitatory

Subtypes

Within these general classes of serotonin receptors, a number of specific types have been characterized:[5][6][7]

Overview of Serotonin Receptors
Receptor Gene(s) Distribution Function Agonists Antagonists
5-HT1A
  • Blood Vessels
  • CNS
5-HT1B
  • Blood Vessels
  • CNS
5-HT1D
  • Blood Vessels
  • CNS
5-HT1E
  • Blood Vessels
  • CNS
5-HT1F
  • Blood Vessels
  • CNS
  • Vasoconstriction
5-HT2A
  • Blood Vessels
  • CNS
  • GI Tract
  • Platelets
  • PNS
  • Smooth Muscle
  • Addiction (potentially modulating) [40]
  • Anxiety[41]
  • Appetite
  • Cognition
  • Imagination
  • Learning
  • Memory
  • Mood
  • Perception
  • Sexual Behavior[42]
  • Sleep[43]
  • Thermoregulation[44]
  • Vasoconstriction[45]
5-HT2B
  • Blood Vessels
  • CNS
  • GI Tract
  • Platelets
  • PNS
  • Smooth Muscle
5-HT2C
  • Blood Vessels
  • CNS
  • GI Tract
  • Platelets
  • PNS
  • Smooth Muscle
5-HT3
  • CNS
  • GI Tract
  • PNS
  • Addiction
  • Anxiety
  • Emesis
  • GI Motility
  • Learning[59]
  • Memory[59]
  • Nausea
5-HT4
  • CNS
  • GI Tract
  • PNS
5-HT5A
  • CNS
5-HT6
  • CNS
5-HT7
  • Blood Vessels
  • CNS
  • GI Tract

Note that there is no 5-HT1C receptor since, after the receptor was cloned and further characterized, it was found to have more in common with the 5-HT2 family of receptors and was redesignated as the 5-HT2C receptor. Note that there is also no 5-HT5B receptor, as it exists only in mice and rats and not in humans or monkeys.

Very nonselective agonists of 5-HT receptor subtypes include ergotamine (an antimigraine), which activates 5-HT1A, 5-HT1D, 5-HT1B, D2 and norepinephrine receptors.[31] LSD (a psychedelic) is a 5-HT1A, 5-HT2A, 5-HT2C, 5-HT5A, 5-HT5, 5-HT6 agonist.[31]

References

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External links


Class A: Rhodopsin like
α1 (A, B, D) · α2 (A, B, C) · β1 · β2 · β3
Adenosine (A1, A2A, A2B, A3) · P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
Serotonin
(all but 5-HT3) 5-HT1 (A, B, D, E, F) · 5-HT2 (A, B, C) · 5-HT (4, 5A, 6, 7)
Other
Acetylcholine (M1, M2, M3, M4, M5) · Dopamine (D1, D2, D3, D4, D5) · Histamine (H1, H2, H3, H4) · Melatonin (1A, 1B, 1C) · TAAR (1, 2, 3, 5, 6, 8, 9)
Metabolites and
signaling molecules
CysLT (1, 2) · LTB4 (1, 2) · FPRL1 · OXE · Prostaglandin (DP (1, 2), EP (1, 2, 3, 4), FP) · Prostacyclin · Thromboxane
Other
Bile acid · Cannabinoid (CB1, CB2, GPR (18, 55, 119)) · EBI2 · Estrogen · Free fatty acid (1, 2, 3, 4) · Lactate  · Lysophosphatidic acid (1, 2, 3, 4, 5, 6)  · Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) · Niacin (1, 2) · Oxoglutarate · PAF · Sphingosine-1-phosphate (1, 2, 3, 4, 5) · Succinate
Peptide
B/W (1, 2) · FF (1, 2) · S · Y (1, 2, 4, 5) · Neuromedin (B, U (1, 2)) · Neurotensin (1, 2)
Other
Miscellaneous
GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 81, 82, 83, 84, 85, 87, 88, 92, 101, 103, 109A, 109B, 119, 120, 132, 135, 137B, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 173, 174, 176, 177, 182, 183)
Other
Class B: Secretin like
GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 155, 157)
Other
Class C: Metabotropic
glutamate / pheromone
TAS1R (1, 2, 3) · TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 19, 20, 30, 31, 38, 39, 40, 41, 42, 43, 45, 46, 50)
Other
Class F:
Frizzled / Smoothened
Frizzled
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10)
Smoothened
Cys-loop receptors
5-HT/serotonin
5-HT3 (A, B, C, D, E)
GABAA (α1, α2, α3, α4, α5, α6, β1, β2, β3, γ1, γ2, γ3, δ, ε, π, θ) · GABAA-ρ (ρ1, ρ2, ρ3)
α1 · α2 · α3 · α4 · β
monomers: α1 · α2 · α3 · α4 · α5 · α6 · α7 · α9 · α10 · β1 · β2 · β3 · β4 · δ · ε
pentamers: (α3)2(β4)3 · (α4)2(β2)3 · (α7)5 · (α1)2(β4)3 - Ganglion type · (α1)2β1δε - Muscle type
Zinc
Ionotropic glutamates
Ligand-gated only
AMPA (1, 2, 3, 4) · Kainate (1, 2, 3, 4, 5)
Voltage- and ligand-gated
NMDA (1, 2A, 2B, 2C, 2D, 3A, 3B, L1A, L1B)
‘Orphan’
GluD (δ1, δ2)
ATP-gated channels
P2X (1, 2, 3, 4, 5, 6, 7)
de:5-HT-Rezeptor

es:Receptor de 5-HT it:Recettori serotoninergici ja:セロトニン受容体 pl:Receptory serotoninowe pt:Receptor 5-HT

ru:Серотониновый рецептор
  1. ↑ Hoyer D, Clarke DE, Fozard JR, Hartig PR, Martin GR, Mylecharane EJ, Saxena PR, Humphrey PP (1994). "International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin)". Pharmacol. Rev. 46 (2): 157–203. PMID 7938165. 
  2. ↑ Frazer A, Hensler JG (1999). "Chapter 13: Serotonin Receptors". In Siegel GJ, Agranoff BW, Albers RW, Fisher SK, Uhler MD, editors. Basic Neurochemistry: Molecular, Cellular, and Medical Aspects. Philadelphia: Lippincott-Raven. pp. 263–292. ISBN 0-397-51820-X. Retrieved 2008-04-11. 
  3. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  4. ↑ Francken BJ, Jurzak M, Vanhauwe JF, Luyten WH, Leysen JE. (1998). "The human 5-ht5A receptor couples to Gi/Go proteins and inhibits adenylate cyclase in HEK 293 cells". Eur J Pharmacol. 361 (2-3): 299–309. doi:10.1016/S0014-2999(98)00744-4. PMID 9865521. 
  5. ↑ Glennon RA, Dukat M, Westkaemper RB (2000-01-01). "Serotonin Receptor Subtypes and Ligands". American College of Neurophyscopharmacology. Retrieved 2008-04-11. 
  6. ↑ "5-Hydroxytryptamine Receptors". IUPHAR Receptor Database. International Union of Basic and Clinical Pharmacology. Retrieved 2008-04-11. 
  7. ↑ Wesolowska A (2002). "In the search for selective ligands of 5-HT5, 5-HT6 and 5-HT7 serotonin receptors" (PDF). Polish Journal of Pharmacology. 54 (4): 327–41. PMID 12523486. 
  8. ↑ Tomkins DM, Higgins GA, Sellers EM (1994). "Low doses of the 5-HT1A agonist 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH DPAT) increase ethanol intake". Psychopharmacology (Berl). 115 (1-2): 173–9. doi:10.1007/BF02244769. PMID 7862892. 
  9. ↑ Müller CP, Carey RJ, Huston JP, De Souza Silva MA (2007). "Serotonin and psychostimulant addiction: focus on 5-HT1A-receptors". Prog Neurobiol. 81 (3): 133–78. doi:10.1016/j.pneurobio.2007.01.001. PMID 17316955. 
  10. ↑ Carey RJ, DePalma G, Damianopoulos E, Shanahan A, Müller CP, Huston JP (2005). "Evidence that the 5-HT1A autoreceptor is an important pharmacological target for the modulation of cocaine behavioral stimulant effects". Brain Res. 1034 (1-2): 162–71. doi:10.1016/j.brainres.2004.12.012. PMID 15713268. 
  11. ↑ 11.0 11.1 de Boer SF, Koolhaas JM (2005). "5-HT1A and 5-HT1B receptor agonists and aggression: a pharmacological challenge of the serotonin deficiency hypothesis". Eur J Pharmacol. 526 (1-3): 125–39. doi:10.1016/j.ejphar.2005.09.065. PMID 18853336. 
  12. ↑ Parks CL, Robinson PS, Sibille E, Shenk T, Toth M (1998). "Increased anxiety of mice lacking the serotonin1A receptor". Proc Natl Acad Sci U S A. 195 (18): 10734–9. PMC 27964 Freely accessible. PMID 9724773. 
  13. ↑ Ebenezer IS, Arkle MJ, Tite RM (1998). "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. 29 (4): 269–72. doi:10.1358/mf.2007.29.4.1075362. PMID 17609739. 
  14. ↑ 14.0 14.1 Wouters W, Tulp MT, Bevan P (1998). "Flesinoxan lowers blood pressure and heart rate in cats via 5-HT1A receptors". Eur J Pharmacol. 149 (3): 213–23. doi:10.1016/0014-2999(88)90651-6. PMID 2842163. 
  15. ↑ 15.0 15.1 Horiuchi J, McDowall LM, Dampney RA (2008). "Role of 5-HT(1A) receptors in the lower brainstem on the cardiovascular response to dorsomedial hypothalamus activation". Auton Neurosci. 142 (1-2): 71–6. doi:10.1016/j.autneu.2008.06.004. PMID 18667366. 
  16. ↑ Nalivaiko E, Ootsuka Y, Blessing WW. (2005). "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. 289 (2): R596–R604. doi:10.1152/ajpregu.00845.2004. PMID 15802554. 
  17. ↑ 17.0 17.1 Lucot JB. (1994). "Antiemetic effects of flesinoxan in cats: comparisons with 8-hydroxy-2-(di-n-propylamino)tetralin". Eur J Pharmacol. 253 (1-2): 53–60. doi:10.1016/0014-2999(94)90756-0. PMID 8013549. 
  18. ↑ Winstanley CA, Theobald DE, Dalley JW, Robbins TW. (2005). "Interactions between serotonin and dopamine in the control of impulsive choice in rats: therapeutic implications for impulse control disorders". Neuropsychopharmacology. 30 (4): 669–682. doi:10.1038/sj.npp.1300610. PMID 15688093. 
  19. ↑ Ogren SO, Eriksson TM, Elvander-Tottie E, D'Addario C, Ekström JC, Svenningsson P, Meister B, Kehr J, Stiedl O (2008). "The role of 5-HT(1A) receptors in learning and memory". Behav Brain Res. 195 (1): 54–77. doi:10.1016/j.bbr.2008.02.023. PMID 18394726. 
  20. ↑ Yasuno F, Suhara T, Nakayama T, Ichimiya T, Okubo Y, Takano A, Ando T, Inoue M, Maeda J, Suzuki K (2003). "Inhibitory effect of hippocampal 5-HT1A receptors on human explicit memory". Am J Psychiatry. 160 (2): 334–40. doi:10.1176/appi.ajp.160.2.334. PMID 12562581. 
  21. ↑ Kennett GA, Dourish CT, Curzon G (1987). "Antidepressant-like action of 5-HT1A agonists and conventional antidepressants in an animal model of depression". Eur J Pharmacol. 134 (3): 265–74. doi:10.1016/0014-2999(87)90357-8. PMID 2883013. 
  22. ↑ Bardin L, Tarayre JP, Malfetes N, Koek W, Colpaert FC. (2003). "Profound, non-opioid analgesia produced by the high-efficacy 5-HT(1A) agonist F 13640 in the formalin model of tonic nociceptive pain". Pharmacology. 67 (4): 182–194. doi:10.1159/000068404. PMID 12595749. 
  23. ↑ 23.0 23.1 Millan MJ, Perrin-Monneyron S (1997). "Potentiation of fluoxetine-induced penile erections by combined blockade of 5-HT1A and 5-HT1B receptors". Eur J Pharmacol. 321 (3): 11–3. PMID 9085055. 
  24. ↑ Prow MR, Martin KF, Heal DJ (1996). "8-OH-DPAT-induced mydriasis in mice: a pharmacological characterisation". Eur J Pharmacol. 317 (1): 21–8. doi:10.1016/S0014-2999(96)00693-0. PMID 8982715. 
  25. ↑ 25.0 25.1 25.2 Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  26. ↑ 26.0 26.1 Popova NK, Amstislavskaya TG (2002). "Involvement of the 5-HT(1A) and 5-HT(1B) serotonergic receptor subtypes in sexual arousal in male mice". Psychoneuroendocrinology. 27 (5): 609–18. doi:10.1016/S0306-4530(01)00097-X. PMID 11965359. 
  27. ↑ Monti JM, Jantos H (1992). "Dose-dependent effects of the 5-HT1A receptor agonist 8-OH-DPAT on sleep and wakefulness in the rat". J Sleep Res. 1 (3): 169–175. doi:10.1111/j.1365-2869.1992.tb00033.x. PMID 10607047. 
  28. ↑ Thompson MR, Callaghan PD, Hunt GE, Cornish JL, McGregor IS (2007). "A role for oxytocin and 5-HT(1A) receptors in the prosocial effects of 3,4 methylenedioxymethamphetamine ("ecstasy")". Neuroscience. 146 (2): 509–14. doi:10.1016/j.neuroscience.2007.02.032. PMID 17383105. 
  29. ↑ Gudelsky GA, Koenig JI, Meltzer HY (1986). "Thermoregulatory responses to serotonin (5-HT) receptor stimulation in the rat. Evidence for opposing roles of 5-HT2 and 5-HT1A receptors". Neuropharmacology. 25 (12): 1307–13. doi:10.1016/0028-3908(86)90101-2. PMID 2951611. 
  30. ↑ Ootsuka Y, Blessing WW. (2006). "Activation of 5-HT1A receptors in rostral medullary raphé inhibits cutaneous vasoconstriction elicited by cold exposure in rabbits". Brain Res. 1073-1074: 252–61. doi:10.1016/j.brainres.2005.12.031. PMID 16455061. 
  31. ↑ 31.00 31.01 31.02 31.03 31.04 31.05 31.06 31.07 31.08 31.09 31.10 31.11 31.12 31.13 31.14 31.15 31.16 31.17 31.18 31.19 31.20 31.21 pharmamotion.com > Serotonin (5-HT): receptors, agonists and antagonists By Flavio Guzmán, M.D. on 9/08/09
  32. ↑ Harrison AA, Parsons LH, Koob GF, Markou A (1999). "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). 141 (3): 242–50. doi:10.1007/s002130050831. PMID 10027505. 
  33. ↑ Chojnacka-Wójcik E, Klodzinska A, Tatarczynska E (2005). "The anxiolytic-like effect of 5-HT1B receptor ligands in rats: a possible mechanism of action". J Pharm Pharmacol. 57 (2): 253–7. doi:10.1211/0022357055399. PMID 15720791. 
  34. ↑ Lin D, Parsons LH (2002). "Anxiogenic-like effect of serotonin(1B) receptor stimulation in the rat elevated plus-maze". Pharmacol Biochem Behav. 71 (4): 581–7. doi:10.1016/S0091-3057(01)00712-2. PMID 11888549. 
  35. ↑ 35.0 35.1 Tatarczynska E, Klodzinska A, Stachowicz K, Chojnacka-Wójcik E (2004). "Effects of a selective 5-HT1B receptor agonist and antagonists in animal models of anxiety and depression". Behav Pharmacol. 15 (8): 523–34. doi:10.1097/00008877-200412000-00001. PMID 15577451. 
  36. ↑ 36.0 36.1 Eriksson TM, Madjid N, Elvander-Tottie E, Stiedl O, Svenningsson P, Ogren SO (2008). "Blockade of 5-HT 1B receptors facilitates contextual aversive learning in mice by disinhibition of cholinergic and glutamatergic neurotransmission". Neuropharmacology. 54 (7): 1041–50. doi:10.1016/j.neuropharm.2008.02.007. PMID 18394658. 
  37. ↑ 37.0 37.1 McCreary AC, Bankson MG, Cunningham KA (1999). "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. 290 (3): 965–73. PMID 10454466. 
  38. ↑ Amital D, Fostick L, Sasson Y, Kindler S, Amital H, Zohar J (2005). "Anxiogenic effects of Sumatriptan in panic disorder: a double-blind, placebo-controlled study". Eur Neuropsychopharmacol. 15 (3): 279–82. doi:10.1016/j.euroneuro.2004.12.002. PMID 15820416. 
  39. ↑ Feuerstein TJ, Hüring H, van Velthoven V, Lücking CH, Landwehrmeyer GB (1996). "5-HT1D-like receptors inhibit the release of endogenously formed [3H]GABA in human, but not in rabbit, neocortex". Neurosci Lett. 209 (3): 210–4. doi:10.1016/0304-3940(96)12637-9. PMID 8736648. 
  40. ↑ 40.0 40.1 [1] 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 (1998). "The role of 5-HT receptor subtypes in the anxiolytic effects of selective serotonin reuptake inhibitors in the rat ultrasonic vocalization test". Psychopharmacology (Berl). 135 (4): 383–91. doi:10.1007/s002130050526. PMID 9539263. 
  42. ↑ 42.0 42.1 Popova NK, Amstislavskaya TG (2002). "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. 76 (1): 28–34. doi:10.1159/000063681. PMID 12097814. 
  43. ↑ 43.0 43.1 Popa D, Léna C, Fabre V, Prenat C, Gingrich J, Escourrou P, Hamon M, Adrien J (2005). "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. 25 (49): 11231–8. doi:10.1523/JNEUROSCI.1724-05.2005. PMID 16339018. 
  44. ↑ 44.0 44.1 Mazzola-Pomietto P, Aulakh CS, Tolliver T, Murphy DL (1997). "Functional subsensitivity of 5-HT2A and 5-HT2C receptors mediating hyperthermia following acute and chronic treatment with 5-HT2A/2C receptor antagonists". Psychopharmacology (Berl). 130 (2): 144–51. doi:10.1007/s002130050222. PMID 9106912. 
  45. ↑ Blessing WW, Seaman B. (2003). "5-hydroxytryptamine(2A) receptors regulate sympathetic nerves constricting the cutaneous vascular bed in rabbits and rats". Neuroscience. 117 (4): 939–948. doi:10.1016/S0306-4522(02)00810-2. PMID 12654345. 
  46. ↑ Kennett GA, Bright F, Trail B, Baxter GS, Blackburn TP (1996). "Effects of the 5-HT2B receptor agonist, BW 723C86, on three rat models of anxiety". Br J Pharmacol. 117 (7): 1443–8. PMC 1909458 Freely accessible. PMID 8730737. 
  47. ↑ Duxon MS, Kennett GA, Lightowler S, Blackburn TP, Fone KC (1997). "Activation of 5-HT2B receptors in the medial amygdala causes anxiolysis in the social interaction test in the rat". Neuropharmacology. 36 (4-5): 601–8. doi:10.1016/S0028-3908(97)00042-7. PMID 9225285. 
  48. ↑ Kennett GA, Trail B, Bright F (1998). "Anxiolytic-like actions of BW 723C86 in the rat Vogel conflict test are 5-HT2B receptor mediated". Neuropharmacology. 37 (12): 1603–10. doi:10.1016/S0028-3908(98)00115-4. PMID 9886683. 
  49. ↑ Kennett GA, Ainsworth K, Trail B, Blackburn TP (1997). "BW 723C86, a 5-HT2B receptor agonist, causes hyperphagia and reduced grooming in rats". Neuropharmacology. 36 (2): 233–9. doi:10.1016/S0028-3908(96)00171-2. PMID 9144661. 
  50. ↑ Borman RA, Tilford NS, Harmer DW, Day N, Ellis ES, Sheldrick RL, Carey J, Coleman RA, Baxter GS. (2002). "5-HT(2B) receptors play a key role in mediating the excitatory effects of 5-HT in human colon in vitro". Br J Pharmacol. 135 (5): 1144–1151. doi:10.1038/sj.bjp.0704571. PMC 1573235 Freely accessible. PMID 11877320. 
  51. ↑ 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 (1997). "SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist". Neuropharmacology. 36 (4-5): 609–20. doi:10.1016/S0028-3908(97)00038-5. PMID 9225286. 
  52. ↑ 52.0 52.1 Millan MJ, Brocco M, Gobert A, Dekeyne A (2005). "Anxiolytic properties of agomelatine, an antidepressant with melatoninergic and serotonergic properties: role of 5-HT2C receptor blockade". Psychopharmacology (Berl). 177 (4): 448–58. doi:10.1007/s00213-004-1962-z. PMID 15289999. 
  53. ↑ 53.0 53.1 Millan MJ, Brocco M, Gobert A, Dekeyne A (2008). "S32006, a novel 5-HT2C receptor antagonist displaying broad-based antidepressant and anxiolytic properties in rodent models". Psychopharmacology (Berl). 199 (4): 549–68. doi:10.1007/s00213-008-1177-9. PMID 18523738. 
  54. ↑ Fujitsuka N, Asakawa A, Hayashi M, Sameshima M, Amitani H, Kojima S, Fujimiya M, Inui A. (2009). "Selective serotonin reuptake inhibitors modify physiological gastrointestinal motor activities via 5-HT2c receptor and acyl ghrelin". Biol Psychiatry. 65 (9): 748–759. doi:10.1016/j.biopsych.2008.10.031. PMID 19058784. 
  55. ↑ Millan MJ, Peglion JL, Lavielle G, Perrin-Monneyron S (1997). "5-HT2C receptors mediate penile erections in rats: actions of novel and selective agonists and antagonists". Eur J Pharmacol. 325 (1): 9–12. doi:10.1016/S0014-2999(97)89962-1. PMID 9151932. 
  56. ↑ Stancampiano R, Melis MR, Argiolas A (1994). "Penile erection and yawning induced by 5-HT1C receptor agonists in male rats: relationship with dopaminergic and oxytocinergic transmission". Eur J Pharmacol. 261 (1-2): 149–55. doi:10.1016/0014-2999(94)90313-1. PMID 8001637. 
  57. ↑ Frank MG, Stryker MP, Tecott LH (2002). "Sleep and sleep homeostasis in mice lacking the 5-HT2c receptor". Neuropsychopharmacology. 27 (5): 869–73. doi:10.1016/S0893-133X(02)00353-6. PMC 2452994 Freely accessible. PMID 12431861. 
  58. ↑ Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4.  Page 187
  59. ↑ 59.0 59.1 Pitsikas N, Brambilla A, Borsini F. (1994). "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. 47 (1): 95–99. doi:10.1016/0091-3057(94)90116-3. PMID 8115433. 
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  61. ↑ Kennett GA, Bright F, Trail B, Blackburn TP, Sanger GJ (1997). "Anxiolytic-like actions of the selective 5-HT4 receptor antagonists SB 204070A and SB 207266A in rats". Neuropharmacology. 36 (4-5): 707–12. doi:10.1016/S0028-3908(97)00037-3. PMID 9225297. 
  62. ↑ Jean A, Conductier G, Manrique C, Bouras C, Berta P, Hen R, Charnay Y, Bockaert J, Compan V (2007). "Anorexia induced by activation of serotonin 5-HT4 receptors is mediated by increases in CART in the nucleus accumbens". Proc Natl Acad Sci U S A. 104 (41): 16335–40. doi:10.1073/pnas.0701471104. PMC 2042207 Freely accessible. PMID 17913892. 
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  66. ↑ Meneses A, Hong E (1997). "Effects of 5-HT4 receptor agonists and antagonists in learning". Pharmacol Biochem Behav. 56 (3): 347–51. doi:10.1016/S0091-3057(96)00224-9. PMID 9077568. 
  67. ↑ Fontana DJ, Daniels SE, Wong EH, Clark RD, Eglen RM (1998). "Role of 5-HT4 receptors in the mouse passive avoidance test". J Pharmacol Exp Ther. 286 (3): 1115–21. PMID 9732367. 
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  69. ↑ Duman RS (2007). "A silver bullet for the treatment of depression?". Neuron. 55 (5): 712–25. doi:10.1016/j.neuron.2007.08.011. PMID 17785173. 
  70. ↑ Manzke T, Guenther U, Ponimaskin E, Haller M, Dutschmann M, Schwarzacher S, Richter D (2003). "5-HT4(a) receptors avert opioid-induced breathing depression without loss of analgesia". Science. 301 (5630): 226–9. doi:10.1126/science.1084674. PMID 12855812. 
  71. ↑ Nelson DL (2004). "5-HT5 receptors". Curr Drug Targets CNS Neurol Disord. 3 (1): 53–8. doi:10.2174/1568007043482606. PMID 14965244. 
  72. ↑ 72.0 72.1 Dietz BM, Mahady GB, Pauli GF, Farnsworth NR (2005). "Valerian extract and valerenic acid are partial agonists of the 5-HT5a receptor in vitro". Brain Res Mol Brain Res. 138 (2): 191–7. doi:10.1016/j.molbrainres.2005.04.009. PMID 15921820. 
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  84. ↑ 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 (2003). "SB-656104-A, a novel selective 5-HT7 receptor antagonist, modulates REM sleep in rats". Br J Pharmacol. 139 (4): 705–14. doi:10.1038/sj.bjp.0705290. PMC 1573887 Freely accessible. PMID 12812993. 
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