5-HT receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on 5-HT receptors [65] and subsequently revised [59]) are, with the exception of the ionotropic 5-HT₃ class, GPCRs where the endogenous agonist is 5-hydroxytryptamine. The diversity of metabotropic 5-HT receptors is increased by alternative splicing that produces isoforms of the 5-HT_2A (non-functional), 5-HT_2C (non-functional), 5-HT₄, 5-HT₆ (non-functional) and 5-HT₇ receptors. Unique amongst the GPCRs, RNA editing produces 5-HT_2C receptor isoforms that differ in function, such as efficiency and specificity of coupling to G_q/11 and also pharmacology [14,159]. Most 5-HT receptors (except 5-ht_1e and 5-ht_5b) play specific roles mediating functional responses in different tissues (reviewed by [125,150]).

Tabulated pK_i and K_D values refer to binding to human 5-HT receptors unless indicated otherwise. The nomenclature of 5-HT_1B/5-HT_1D receptors has been revised [59]. Only the non-rodent form of the receptor was previously called 5-HT_1D: the human 5-HT_1B receptor (tabulated) displays a different pharmacology to the rodent forms of the receptor due to Thr335 of the human sequence being replaced by Asn in rodent receptors [57]. Wang et al. (2013) report X-ray structures which reveal the binding modality of ergotamine and dihydroergotamine (DHE) to the 5-HT_1B receptor in comparison with the structure of the 5-HT_2B receptor [156]; some of these drugs adopt rather different conformations depending on the target receptor [123]. Various 5-HT receptors have multiple partners in addition to G proteins, which may affect function and pharmacology [95]. NAS181 is a selective antagonist of the rodent 5-HT_1B receptor. Fananserin (LSD) and ketanserin bind with high affinity to dopamine D4 and histamine H₁ receptors respectively, and ketanserin is a potent α1 adrenoceptor antagonist, in addition to blocking 5-HT_2A receptors. Lysergic acid (LSD) and ergotamine show a strong preference for arrestin recruitment over G protein coupling at the 5-HT_2B receptor, with no such preference evident at 5-HT_1B receptors, and they also antagonise 5-HT_7A receptors [151]. DHE (dihydroergocryptine), pergolide and cabergoline also show significant preference for arrestin recruitment over G protein coupling at 5-HT_2B receptors [151]. The 5-HT_2B (and other 5-HT) receptors interact with immunocompetent cells [118]. The serotonin antagonist mesulergine was key to the discovery of the 5-HT_2C receptor [122], initially known as 5-HT_1C [4]. The human 5-HT_5A receptor may couple to several signal transduction pathways when stably expressed in C6 glioma cells [116] and rodent prefrontal cortex (layer V pyramidal neurons) [51]. The human orthologue of the mouse 5-ht_5b receptor is non-functional (stop codons); the 5-ht_1e receptor has not been cloned from mouse, or rat, impeding definition of its function [57]. In addition to accepted receptors, an 'orphan' receptor, unofficially termed 5-HT_1P, has been described [47].

* Key recommended reading is highlighted with an asterisk

Aloyo VJ, Berg KA, Spampinato U, Clarke WP, Harvey JA. (2009) Current status of inverse agonism at serotonin2A (5-HT2A) and 5-HT2C receptors. Pharmacol Ther, 121 (2): 160-73. [PMID:19109993]

Barnes NM, Sharp T. (1999) A review of central 5-HT receptors and their function. Neuropharmacology, 38 (8): 1083-152. [PMID:10462127]

Berger M, Gray JA, Roth BL. (2009) The expanded biology of serotonin. Annu Rev Med, 60: 355-66. [PMID:19630576]

Bockaert J, Claeysen S, Bécamel C, Dumuis A, Marin P. (2006) Neuronal 5-HT metabotropic receptors: fine-tuning of their structure, signaling, and roles in synaptic modulation. Cell Tissue Res, 326 (2): 553-72. [PMID:16896947]

Bockaert J, Claeysen S, Compan V, Dumuis A. (2008) 5-HT(4) receptors: history, molecular pharmacology and brain functions. Neuropharmacology, 55 (6): 922-31. [PMID:18603269]

* Bockaert J, Claeysen S, Compan V, Dumuis A. (2011) 5-HT(4) receptors, a place in the sun: act two. Curr Opin Pharmacol, 11 (1): 87-93. [PMID:21342787]

Bojarski AJ. (2006) Pharmacophore models for metabotropic 5-HT receptor ligands. Curr Top Med Chem, 6 (18): 2005-26. [PMID:17017971]

Bonasera SJ, Tecott LH. (2000) Mouse models of serotonin receptor function: toward a genetic dissection of serotonin systems. Pharmacol Ther, 88 (2): 133-42. [PMID:11150593]

Bureau R, Boulouard M, Dauphin F, Lezoualc'h F, Rault S. (2010) Review of 5-HT4R ligands: state of art and clinical applications. Curr Top Med Chem, 10 (5): 527-53. [PMID:20166943]

Caliendo G, Santagada V, Perissutti E, Fiorino F. (2005) Derivatives as 5HT1A receptor ligands--past and present. Curr Med Chem, 12 (15): 1721-53. [PMID:16029144]

Codony X, Vela JM, Ramírez MJ. (2011) 5-HT(6) receptor and cognition. Curr Opin Pharmacol, 11 (1): 94-100. [PMID:21330210]

Fink KB, Göthert M. (2007) 5-HT receptor regulation of neurotransmitter release. Pharmacol Rev, 59 (4): 360-417. [PMID:18160701]

Gershon MD. (1999) Review article: roles played by 5-hydroxytryptamine in the physiology of the bowel. Aliment Pharmacol Ther, 13 Suppl 2: 15-30. [PMID:10429737]

Glennon RA, Siripurapu U, Roth BL, Kolanos R, Bondarev ML, Sikazwe D, Lee M, Dukat M. (2010) The medicinal chemistry of 5-HT6 receptor ligands with a focus on arylsulfonyltryptamine analogs. Curr Top Med Chem, 10 (5): 579-95. [PMID:20166945]

Gumpper RH, Fay JF, Roth BL. (2022) Molecular insights into the regulation of constitutive activity by RNA editing of 5HT_2C serotonin receptors. Cell Rep, 40 (7): 111211. [PMID:35977511]

Gupta S, Villalón CM. (2010) The relevance of preclinical research models for the development of antimigraine drugs: focus on 5-HT(1B/1D) and CGRP receptors. Pharmacol Ther, 128 (1): 170-90. [PMID:20655327]

Hartig PR, Hoyer D, Humphrey PP, Martin GR. (1996) Alignment of receptor nomenclature with the human genome: classification of 5-HT1B and 5-HT1D receptor subtypes. Trends Pharmacol Sci, 17 (3): 103-5. [PMID:8936345]

* Hayes DJ, Greenshaw AJ. (2011) 5-HT receptors and reward-related behaviour: a review. Neurosci Biobehav Rev, 35 (6): 1419-49. [PMID:21402098]

Heal DJ, Smith SL, Fisas A, Codony X, Buschmann H. (2008) Selective 5-HT6 receptor ligands: progress in the development of a novel pharmacological approach to the treatment of obesity and related metabolic disorders. Pharmacol Ther, 117 (2): 207-31. [PMID:18068807]

* 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]

Hoyer D, Hannon JP, Martin GR. (2002) Molecular, pharmacological and functional diversity of 5-HT receptors. Pharmacol Biochem Behav, 71 (4): 533-54. [PMID:11888546]

Jensen NH, Cremers TI, Sotty F. (2010) Therapeutic potential of 5-HT2C receptor ligands. ScientificWorldJournal, 10: 1870-85. [PMID:20852829]

King MV, Marsden CA, Fone KC. (2008) A role for the 5-HT(1A), 5-HT4 and 5-HT6 receptors in learning and memory. Trends Pharmacol Sci, 29 (9): 482-92. [PMID:19086256]

Kitson SL. (2007) 5-hydroxytryptamine (5-HT) receptor ligands. Curr Pharm Des, 13 (25): 2621-37. [PMID:17897004]

Lanfumey L, Hamon M. (2004) 5-HT1 receptors. Curr Drug Targets CNS Neurol Disord, 3 (1): 1-10. [PMID:14965240]

* Leopoldo M, Lacivita E, Berardi F, Perrone R, Hedlund PB. (2011) Serotonin 5-HT7 receptor agents: Structure-activity relationships and potential therapeutic applications in central nervous system disorders. Pharmacol Ther, 129 (2): 120-48. [PMID:20923682]

Leysen JE. (2004) 5-HT2 receptors. Curr Drug Targets CNS Neurol Disord, 3 (1): 11-26. [PMID:14965241]

Lezoualc'h F, Jockers R, Berque-Bestel I. (2009) Multivalent-based drug design applied to serotonin 5-HT(4) receptor oligomers. Curr Pharm Des, 15 (6): 719-29. [PMID:19199991]

* Meltzer HY, Massey BW. (2011) The role of serotonin receptors in the action of atypical antipsychotic drugs. Curr Opin Pharmacol, 11 (1): 59-67. [PMID:21420906]

Nelson DL. (2004) 5-HT5 receptors. Curr Drug Targets CNS Neurol Disord, 3 (1): 53-8. [PMID:14965244]

Pauwels PJ. (2000) Diverse signalling by 5-hydroxytryptamine (5-HT) receptors. Biochem Pharmacol, 60 (12): 1743-50. [PMID:11108789]

Ramage AG, Villalón CM. (2008) 5-hydroxytryptamine and cardiovascular regulation. Trends Pharmacol Sci, 29 (9): 472-81. [PMID:19086344]

* Roberts AJ, Hedlund PB. (2012) The 5-HT(7) receptor in learning and memory. Hippocampus, 22 (4): 762-71. [PMID:21484935]

Sanger GJ. (2008) 5-hydroxytryptamine and the gastrointestinal tract: where next?. Trends Pharmacol Sci, 29 (9): 465-71. [PMID:19086255]

Saxena PR, De Vries P, Villalón CM. (1998) 5-HT1-like receptors: a time to bid goodbye. Trends Pharmacol Sci, 19 (8): 311-6. [PMID:9745358]

Thomas DR. (2006) 5-ht5A receptors as a therapeutic target. Pharmacol Ther, 111 (3): 707-14. [PMID:16516972]

Thomas DR, Hagan JJ. (2004) 5-HT7 receptors. Curr Drug Targets CNS Neurol Disord, 3 (1): 81-90. [PMID:14965246]

Villalón CM, Centurión D. (2007) Cardiovascular responses produced by 5-hydroxytriptamine:a pharmacological update on the receptors/mechanisms involved and therapeutic implications. Naunyn Schmiedebergs Arch Pharmacol, 376 (1-2): 45-63. [PMID:17703282]

Volk B, Nagy BJ, Vas S, Kostyalik D, Simig G, Bagdy G. (2010) Medicinal chemistry of 5-HT5A receptor ligands: a receptor subtype with unique therapeutical potential. Curr Top Med Chem, 10 (5): 554-78. [PMID:20166946]

Ward SE, Watson JM. (2010) Recent advances in the discovery of selective and non-selective 5-HT(1D) receptor ligands. Curr Top Med Chem, 10 (5): 479-92. [PMID:20166947]

Werry TD, Loiacono R, Sexton PM, Christopoulos A. (2008) RNA editing of the serotonin 5HT2C receptor and its effects on cell signalling, pharmacology and brain function. Pharmacol Ther, 119 (1): 7-23. [PMID:18554725]

Woolley ML, Marsden CA, Fone KC. (2004) 5-ht6 receptors. Curr Drug Targets CNS Neurol Disord, 3 (1): 59-79. [PMID:14965245]

1. Adham N, Bard JA, Zgombick JM, Durkin MM, Kucharewicz S, Weinshank RL, Branchek TA. (1997) Cloning and characterization of the guinea pig 5-HT1F receptor subtype: a comparison of the pharmacological profile to the human species homolog. Neuropharmacology, 36 (4-5): 569-76. [PMID:9225282]

2. Adham N, Kao HT, Schecter LE, Bard J, Olsen M, Urquhart D, Durkin M, Hartig PR, Weinshank RL, Branchek TA. (1993) Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase. Proc Natl Acad Sci USA, 90 (2): 408-12. [PMID:8380639]

3. Amlaiky N, Ramboz S, Boschert U, Plassat JL, Hen R. (1992) Isolation of a mouse "5HT1E-like" serotonin receptor expressed predominantly in hippocampus. J Biol Chem, 267 (28): 19761-4. [PMID:1328180]

4. Ayme-Dietrich E, Lawson R, Côté F, de Tapia C, Da Silva S, Ebel C, Hechler B, Gachet C, Guyonnet J, Rouillard H et al.. (2017) The role of 5-HT_2B receptors in mitral valvulopathy: bone marrow mobilization of endothelial progenitors. Br J Pharmacol, 174 (22): 4123-4139. [PMID:28806488]

5. Bach T, Syversveen T, Kvingedal AM, Krobert KA, Brattelid T, Kaumann AJ, Levy FO. (2001) 5HT4(a) and 5-HT4(b) receptors have nearly identical pharmacology and are both expressed in human atrium and ventricle. Naunyn Schmiedebergs Arch Pharmacol, 363 (2): 146-60. [PMID:11218067]

6. Bang-Andersen B, Ruhland T, Jørgensen M, Smith G, Frederiksen K, Jensen KG, Zhong H, Nielsen SM, Hogg S, Mørk A et al.. (2011) Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder. J Med Chem, 54 (9): 3206-21. [PMID:21486038]

7. Bard JA, Zgombick J, Adham N, Vaysse P, Branchek TA, Weinshank RL. (1993) Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase. J Biol Chem, 268 (31): 23422-6. [PMID:8226867]

8. Beattie DT, Smith JA, Marquess D, Vickery RG, Armstrong SR, Pulido-Rios T, McCullough JL, Sandlund C, Richardson C, Mai N et al.. (2004) The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo. Br J Pharmacol, 143 (5): 549-60. [PMID:15466450]

9. Bender E, Pindon A, van Oers I, Zhang YB, Gommeren W, Verhasselt P, Jurzak M, Leysen J, Luyten W. (2000) Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant. J Neurochem, 74 (2): 478-89. [PMID:10646498]

10. Bernotas RC, Lenicek S, Antane S, Cole DC, Harrison BL, Robichaud AJ, Zhang GM, Smith D, Platt B, Lin Q et al.. (2009) Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists. Bioorg Med Chem, 17 (14): 5153-63. [PMID:19523834]

11. Berque-Bestel I, Soulier JL, Giner M, Rivail L, Langlois M, Sicsic S. (2003) Synthesis and characterization of the first fluorescent antagonists for human 5-HT4 receptors. J Med Chem, 46 (13): 2606-20. [PMID:12801225]

12. Blair JB, Kurrasch-Orbaugh D, Marona-Lewicka D, Cumbay MG, Watts VJ, Barker EL, Nichols DE. (2000) Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines. J Med Chem, 43 (24): 4701-10. [PMID:11101361]

13. Blondel O, Gastineau M, Dahmoune Y, Langlois M, Fischmeister R. (1998) Cloning, expression, and pharmacology of four human 5-hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus. J Neurochem, 70 (6): 2252-61. [PMID:9603189]

14. Bockaert J, Claeysen S, Bécamel C, Dumuis A, Marin P. (2006) Neuronal 5-HT metabotropic receptors: fine-tuning of their structure, signaling, and roles in synaptic modulation. Cell Tissue Res, 326 (2): 553-72. [PMID:16896947]

15. Boess FG, Monsma FJ, Meyer V, Zwingelstein C, Sleight AJ. (1997) Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor. Mol Pharmacol, 52: 515-523. [PMID:9284367]

16. Boess FG, Riemer C, Bos M, Bentley J, Bourson A, Sleight AJ. (1998) The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum. Mol Pharmacol, 54: 577-583. [PMID:9730917]

17. Bonaventure P, Dugovic C, Kramer M, De Boer P, Singh J, Wilson S, Bertelsen K, Di J, Shelton J, Aluisio L et al.. (2012) Translational evaluation of JNJ-18038683, a 5-hydroxytryptamine type 7 receptor antagonist, on rapid eye movement sleep and in major depressive disorder. J Pharmacol Exp Ther, 342 (2): 429-40. [PMID:22570363]

18. Bonhaus DW, Berger J, Adham N, Branchek TA, Hsu SA, Loury DN, Leung E, Wong EH, Clark RD, Eglen RM. (1997) [3H]RS 57639, a high affinity, selective 5-HT4 receptor partial agonist, specifically labels guinea-pig striatal and rat cloned (5-HT4S and 5-HT4L) receptors. Neuropharmacology, 36 (4-5): 671-9. [PMID:9225293]

19. Bonhaus DW, Flippin LA, Greenhouse RJ, Jaime S, Rocha C, Dawson M, Van Natta K, Chang LK, Pulido-Rios T, Webber A et al.. (1999) RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Br J Pharmacol, 127 (5): 1075-82. [PMID:10455251]

20. Bonhaus DW, Weinhardt KK, Taylor M, DeSouza A, McNeeley PM, Szczepanski K, Fontana DJ, Trinh J, Rocha CL, Dawson MW et al.. (1997) RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist. Neuropharmacology, 36 (4-5): 621-9. [PMID:9225287]

21. Boulenguez P, Segu L, Chauveau J, Morel A, Lanoir J, Delaage M. (1992) Biochemical and pharmacological characterization of serotonin-O-carboxymethylglycyl[125I]iodotyrosinamide, a new radioiodinated probe for 5-HT1B and 5-HT1D binding sites. J Neurochem, 58 (3): 951-9. [PMID:1738002]

22. Branchek T, Adham N, Macchi M, Kao HT, Hartig PR. (1990) [3H]-DOB(4-bromo-2,5-dimethoxyphenylisopropylamine) and [3H] ketanserin label two affinity states of the cloned human 5-hydroxytryptamine2 receptor. Mol Pharmacol, 38 (5): 604-9. [PMID:2233697]

23. Brenchat A, Romero L, García M, Pujol M, Burgueño J, Torrens A, Hamon M, Baeyens JM, Buschmann H, Zamanillo D et al.. (2009) 5-HT7 receptor activation inhibits mechanical hypersensitivity secondary to capsaicin sensitization in mice. Pain, 141 (3): 239-47. [PMID:19118950]

24. Bromidge SM, Brown AM, Clarke SE, Dodgson K, Gager T, Grassam HL, Jeffrey PM, Joiner GF, King FD, Middlemiss DN et al.. (1999) 5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist. J Med Chem, 42 (2): 202-5. [PMID:9925723]

25. Bromidge SM, Clarke SE, Gager T, Griffith K, Jeffrey P, Jennings AJ, Joiner GF, King FD, Lovell PJ, Moss SF et al.. (2001) Phenyl benzenesulfonamides are novel and selective 5-HT6 antagonists: identification of N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134). Bioorg Med Chem Lett, 11 (1): 55-8. [PMID:11140733]

26. Brown AM, Avenell K, Young TJ, Ho M, Porter RA, Vimal M, Middlemiss DN. (1998) BRL 54443, a potent agonist with selectivity for human cloned 5-HT1E and 5-HT1F receptors. Br J Pharmacol, 123 (1): 233.

27. Brown AM, Young TJ, Patch TL, Cheung CW, Kaumann AJ, Gaster L, King FD. (1993) [¹²⁵I]-SB 207710, A potent, slective radioligand for 5-HT₄ receptors. Br J Pharmacol, 110: 10.

28. Bruinvels AT, Palacios JM, Hoyer D. (1993) Autoradiographic characterisation and localisation of 5-HT1D compared to 5-HT1B binding sites in rat brain. Naunyn Schmiedebergs Arch Pharmacol, 347 (6): 569-82. [PMID:8361548]

29. Bryant HU, Nelson DL, Button D, Cole HW, Baez MB, Lucaites VL, Wainscott DB, Whitesitt C, Reel J, Simon R et al.. (1996) A novel class of 5-HT2A receptor antagonists: aryl aminoguanidines. Life Sci, 59 (15): 1259-68. [PMID:8845011]

30. Claeysen S, Faye P, Sebben M, Lemaire S, Bockaert J, Dumuis A. (1997) Cloning and expression of human 5-HT4S receptors. Effect of receptor density on their coupling to adenylyl cyclase. Neuroreport, 8 (15): 3189-96. [PMID:9351641]

31. Commery TA. (2010) SAM-531, N,N-dimethyl-3-{[3-(1-naphthylsulfonyl)-1H-indazol-5-yl]oxy} propan-1-amine, a novel serotonin-6 receptor antagonist with preclinical pro-cognitive efficacy. Alzheimers Dement, 6 (4): S548-S549.

32. Corbett DF, Heightman TD, Moss SF, Bromidge SM, Coggon SA, Longley MJ, Roa AM, Williams JA, Thomas DR. (2005) Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry. Bioorg Med Chem Lett, 15 (18): 4014-8. [PMID:16002289]

33. Costes N, Merlet I, Ostrowsky K, Faillenot I, Lavenne F, Zimmer L, Ryvlin P, Le Bars D. (2005) A 18F-MPPF PET normative database of 5-HT1A receptor binding in men and women over aging. J Nucl Med, 46 (12): 1980-9. [PMID:16330560]

34. Dawson LA, Watson JM. (2009) Vilazodone: a 5-HT1A receptor agonist/serotonin transporter inhibitor for the treatment of affective disorders. CNS Neurosci Ther, 15 (2): 107-17. [PMID:19499624]

35. De Vry J, Schohe-Loop R, Heine HG, Greuel JM, Mauler F, Schmidt B, Sommermeyer H, Glaser T. (1998) Characterization of the aminomethylchroman derivative BAY x 3702 as a highly potent 5-hydroxytryptamine1A receptor agonist. J Pharmacol Exp Ther, 284 (3): 1082-94. [PMID:9495870]

36. Doménech T, Beleta J, Palacios JM. (1997) Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist. Naunyn Schmiedebergs Arch Pharmacol, 356 (3): 328-34. [PMID:9303569]

37. Dunlop J, Sabb AL, Mazandarani H, Zhang J, Kalgaonker S, Shukhina E, Sukoff S, Vogel RL, Stack G, Schechter L et al.. (2005) WAY-163909 [(7bR, 10aR)-1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta-[b][1,4]diazepino[6,7,1hi]indole], a novel 5-hydroxytryptamine 2C receptor-selective agonist with anorectic activity. J Pharmacol Exp Ther, 313 (2): 862-9. [PMID:15705738]

38. Egan C, Grinde E, Dupre A, Roth BL, Hake M, Teitler M, Herrick-Davis K. (2000) Agonist high and low affinity state ratios predict drug intrinsic activity and a revised ternary complex mechanism at serotonin 5-HT(2A) and 5-HT(2C) receptors. Synapse, 35: 144-150. [PMID:10611640]

39. Ennis MD, Ghazal NB, Hoffman RL, Smith MW, Schlachter SK, Lawson CF, Im WB, Pregenzer JF, Svensson KA, Lewis RA et al.. (1998) Isochroman-6-carboxamides as highly selective 5-HT1D agonists: potential new treatment for migraine without cardiovascular side effects. J Med Chem, 41 (13): 2180-3. [PMID:9632349]

40. Erlander MG, Lovenberg TW, Baron BM, de Lecea L, Danielson PE, Racke M, Slone AL, Siegel BW, Foye PE, Cannon K et al.. (1993) Two members of a distinct subfamily of 5-hydroxytryptamine receptors differentially expressed in rat brain. Proc Natl Acad Sci USA, 90 (8): 3452-6. [PMID:7682702]

41. Fiorino F, Magli E, Kędzierska E, Ciano A, Corvino A, Severino B, Perissutti E, Frecentese F, Di Vaio P, Saccone I et al.. (2017) New 5-HT_1A, 5HT_2Aand 5HT_2Creceptor ligands containing a picolinic nucleus: Synthesis, in vitro and in vivo pharmacological evaluation. Bioorg Med Chem, 25 (20): 5820-5837. [PMID:28943244]

42. Fitzgerald LW, Conklin DS, Krause CM, Marshall AP, Patterson JP, Tran DP, Iyer G, Kostich WA, Largent BL, Hartig PR. (1999) High-affinity agonist binding correlates with efficacy (intrinsic activity) at the human serotonin 5-HT2A and 5-HT2C receptors: evidence favoring the ternary complex and two-state models of agonist action. J Neurochem, 72 (5): 2127-34. [PMID:10217294]

43. Forbes IT, Douglas S, Gribble AD, Ife RJ, Lightfoot AP, Garner AE, Riley GJ, Jeffrey P, Stevens AJ, Stean TO et al.. (2002) SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties. Bioorg Med Chem Lett, 12 (22): 3341-4. [PMID:12392747]

44. Gardell LR, Vanover KE, Pounds L, Johnson RW, Barido R, Anderson GT, Veinbergs I, Dyssegaard A, Brunmark P, Tabatabaei A et al.. (2007) ACP-103, a 5-hydroxytryptamine 2A receptor inverse agonist, improves the antipsychotic efficacy and side-effect profile of haloperidol and risperidone in experimental models. J Pharmacol Exp Ther, 322 (2): 862-70. [PMID:17519387]

45. Gaster LM, Blaney FE, Davies S, Duckworth DM, Ham P, Jenkins S, Jennings AJ, Joiner GF, King FD, Mulholland KR et al.. (1998) The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo. J Med Chem, 41 (8): 1218-35. [PMID:9548813]

46. Gerald C, Adham N, Kao HT, Olsen MA, Laz TM, Schechter LE, Bard JA, Vaysse PJ, Hartig PR, Branchek TA et al.. (1995) The 5-HT4 receptor: molecular cloning and pharmacological characterization of two splice variants. EMBO J, 14 (12): 2806-15. [PMID:7796807]

47. Gershon MD. (1999) Review article: roles played by 5-hydroxytryptamine in the physiology of the bowel. Aliment Pharmacol Ther, 13 Suppl 2: 15-30. [PMID:10429737]

48. Gilet M, Eutamene H, Han H, Kim HW, Bueno L. (2014) Influence of a new 5-HT4 receptor partial agonist, YKP10811, on visceral hypersensitivity in rats triggered by stress and inflammation. Neurogastroenterol Motil, 26 (12): 1761-70. [PMID:25316608]

49. Glennon RA. (2003) Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). J Med Chem, 46 (14): 2795-812. [PMID:12825922]

50. Glennon RA, Lee M, Rangisetty JB, Dukat M, Roth BL, Savage JE, McBride A, Rauser L, Hufeisen S, Lee DK. (2000) 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem, 43 (5): 1011-8. [PMID:10715164]

51. Goodfellow NM, Bailey CD, Lambe EK. (2012) The native serotonin 5-HT(5A) receptor: electrophysiological characterization in rodent cortex and 5-HT(1A)-mediated compensatory plasticity in the knock-out mouse. J Neurosci, 32 (17): 5804-9. [PMID:22539842]

52. Grailhe R, Grabtree GW, Hen R. (2001) Human 5-HT(5) receptors: the 5-HT(5A) receptor is functional but the 5-HT(5B) receptor was lost during mammalian evolution. Eur J Pharmacol, 418 (3): 157-67. [PMID:11343685]

53. Grånäs C, Larhammar D. (1999) Identification of an amino acid residue important for binding of methiothepin and sumatriptan to the human 5-HT(1B) receptor. Eur J Pharmacol, 380 (2-3): 171-81. [PMID:10513577]

54. Hall H, Farde L, Halldin C, Lundkvist C, Sedvall G. (2000) Autoradiographic localization of 5-HT(2A) receptors in the human brain using [(3)H]M100907 and [(11)C]M100907. Synapse, 38 (4): 421-31. [PMID:11044889]

55. Hamblin MW, Metcalf MA. (1991) Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor. Mol Pharmacol, 40 (2): 143-8. [PMID:1652050]

56. Hameg A, Bayle F, Nuss P, Dupuis P, Garay RP, Dib M. (2003) Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes. Biochem Pharmacol, 65 (3): 435-40. [PMID:12527336]

57. Hannon J, Hoyer D. (2008) Molecular biology of 5-HT receptors. Behav Brain Res, 195 (1): 198-213. [PMID:18571247]

58. Harada K, Aota M, Inoue T, Matsuda R, Mihara T, Yamaji T, Ishibashi K, Matsuoka N. (2006) Anxiolytic activity of a novel potent serotonin 5-HT2C receptor antagonist FR260010: a comparison with diazepam and buspirone. Eur J Pharmacol, 553 (1-3): 171-84. [PMID:17074317]

59. Hartig PR, Hoyer D, Humphrey PP, Martin GR. (1996) Alignment of receptor nomenclature with the human genome: classification of 5-HT1B and 5-HT1D receptor subtypes. Trends Pharmacol Sci, 17 (3): 103-5. [PMID:8936345]

60. Hegde SS, Eglen RM. (1996) Peripheral 5-HT4 receptors. FASEB J, 10 (12): 1398-407. [PMID:8903510]

61. Herrick-Davis K, Grinde E, Teitler M. (2000) Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors. J Pharmacol Exp Ther, 295 (1): 226-32. [PMID:10991983]

62. Heusler P, Palmier C, Tardif S, Bernois S, Colpaert FC, Cussac D. (2010) [(3)H]-F13640, a novel, selective and high-efficacy serotonin 5-HT(1A) receptor agonist radioligand. Naunyn Schmiedebergs Arch Pharmacol, 382 (4): 321-30. [PMID:20799027]

63. Hirst WD, Stean TO, Rogers DC, Sunter D, Pugh P, Moss SF, Bromidge SM, Riley G, Smith DR, Bartlett S et al.. (2006) SB-399885 is a potent, selective 5-HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition models. Eur J Pharmacol, 553 (1-3): 109-19. [PMID:17069795]

64. Holenz J, Mercè R, Díaz JL, Guitart X, Codony X, Dordal A, Romero G, Torrens A, Mas J, Andaluz B et al.. (2005) Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands. J Med Chem, 48 (6): 1781-95. [PMID:15771424]

65. 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]

66. Hoyer D, Hannon JP, Martin GR. (2002) Molecular, pharmacological and functional diversity of 5-HT receptors. Pharmacol Biochem Behav, 71 (4): 533-54. [PMID:11888546]

67. Ishibashi T, Horisawa T, Tokuda K, Ishiyama T, Ogasa M, Tagashira R, Matsumoto K, Nishikawa H, Ueda Y, Toma S et al.. (2010) Pharmacological profile of lurasidone, a novel antipsychotic agent with potent 5-hydroxytryptamine 7 (5-HT7) and 5-HT1A receptor activity. J Pharmacol Exp Ther, 334 (1): 171-81. [PMID:20404009]

68. Jerning E, Svantesson GT, Mohell N. (1998) Receptor binding characteristics of [3H]NAD-299, a new selective 5-HT1A receptor antagonist. Eur J Pharmacol, 360 (2-3): 219-25. [PMID:9851589]

69. Johansson L, Sohn D, Thorberg SO, Jackson DM, Kelder D, Larsson LG, Rényi L, Ross SB, Wallsten C, Eriksson H et al.. (1997) The pharmacological characterization of a novel selective 5-hydroxytryptamine1A receptor antagonist, NAD-299. J Pharmacol Exp Ther, 283 (1): 216-25. [PMID:9336327]

70. Kalipatnapu S, Pucadyil TJ, Harikumar KG, Chattopadhyay A. (2004) Ligand binding characteristics of the human serotonin1A receptor heterologously expressed in CHO cells. Biosci Rep, 24 (2): 101-15. [PMID:15628665]

71. Kennett GA, Wood MD, Bright F, Trail B, Riley G, Holland V, Avenell KY, Stean T, Upton N, Bromidge S et al.. (1997) SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology, 36 (4-5): 609-20. [PMID:9225286]

72. Khawaja X, Ennis C, Minchin MC. (1997) Pharmacological characterization of recombinant human 5-hydroxytryptamine1A receptors using a novel antagonist radioligand, [3H]WAY-100635. Life Sci, 60 (9): 653-65. [PMID:9048968]

73. Kikuchi C, Nagaso H, Hiranuma T, Koyama M. (1999) Tetrahydrobenzindoles: selective antagonists of the 5-HT7 receptor. J Med Chem, 42 (4): 533-5. [PMID:10052959]

74. Kim Y, Kim J, Tae J, Roth BL, Rhim H, Keum G, Nam G, Choo H. (2013) Discovery of aryl-biphenyl-2-ylmethylpiperazines as novel scaffolds for 5-HT(7) ligands and role of the aromatic substituents in binding to the target receptor. Bioorg Med Chem, 21 (9): 2568-76. [PMID:23541835]

75. Kimura Y, Hatanaka K, Naitou Y, Maeno K, Shimada I, Koakutsu A, Wanibuchi F, Yamaguchi T. (2004) Pharmacological profile of YM348, a novel, potent and orally active 5-HT2C receptor agonist. Eur J Pharmacol, 483 (1): 37-43. [PMID:14709324]

76. Klein MT, Dukat M, Glennon RA, Teitler M. (2011) Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships. J Pharmacol Exp Ther, 337 (3): 860-7. [PMID:21422162]

77. Knight AR, Misra A, Quirk K, Benwell K, Revell D, Kennett G, Bickerdike M. (2004) Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol, 370 (2): 114-23. [PMID:15322733]

78. Koe BK, Nielsen JA, Macor JE, Heym J. (1992) Biochemical and behavioural studies of the 5-HT_1B receptor agonist, CP-94,253. Drug Dev Res, 26: 241-250.

79. Kongsamut S, Kang J, Chen XL, Roehr J, Rampe D. (2002) A comparison of the receptor binding and HERG channel affinities for a series of antipsychotic drugs. Eur J Pharmacol, 450 (1): 37-41. [PMID:12176106]

80. Kovács A, Gacsályi I, Wellmann J, Schmidt E, Szücs Z, Dubreuil V, Nicolas JP, Boutin J, Bózsing D, Egyed A et al.. (2003) Effects of EGIS-7625, a selective and competitive 5-HT2B receptor antagonist. Cardiovasc Drugs Ther, 17 (5-6): 427-34. [PMID:15107597]

81. Kroeze WK, Hufeisen SJ, Popadak BA, Renock SM, Steinberg S, Ernsberger P, Jayathilake K, Meltzer HY, Roth BL. (2003) H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology, 28 (3): 519-26. [PMID:12629531]

82. Kursar JD, Nelson DL, Wainscott DB, Baez M. (1994) Molecular cloning, functional expression, and mRNA tissue distribution of the human 5-hydroxytryptamine2B receptor. Mol Pharmacol, 46 (2): 227-34. [PMID:8078486]

83. Kursar JD, Nelson DL, Wainscott DB, Cohen ML, Baez M. (1992) Molecular cloning, functional expression, and pharmacological characterization of a novel serotonin receptor (5-hydroxytryptamine2F) from rat stomach fundus. Mol Pharmacol, 42 (4): 549-57. [PMID:1331748]

84. Lejeune F, Newman-Tancredi A, Audinot V, Millan MJ. (1997) Interactions of (+)- and (-)-8- and 7-hydroxy-2-(di-n-propylamino)tetralin at human (h)D3, hD2 and h serotonin1A receptors and their modulation of the activity of serotoninergic and dopaminergic neurones in rats. J Pharmacol Exp Ther, 280 (3): 1241-9. [PMID:9067310]

85. Leopoldo M, Lacivita E, Contino M, Colabufo NA, Berardi F, Perrone R. (2007) Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2. J Med Chem, 50 (17): 4214-21. [PMID:17649988]

86. Leopoldo M, Lacivita E, De Giorgio P, Fracasso C, Guzzetti S, Caccia S, Contino M, Colabufo NA, Berardi F, Perrone R. (2008) Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III. J Med Chem, 51 (18): 5813-22. [PMID:18800769]

87. Lesage AS, Wouters R, Van Gompel P, Heylen L, Vanhoenacker P, Haegeman G, Luyten WH, Leysen JE. (1998) Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines. Br J Pharmacol, 123 (8): 1655-65. [PMID:9605573]

88. Leysen JE, Gommeren W, Heylen L, Luyten WH, Van de Weyer I, Vanhoenacker P, Haegeman G, Schotte A, Van Gompel P, Wouters R et al.. (1996) Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan. Mol Pharmacol, 50 (6): 1567-80. [PMID:8967979]

89. Long DD, Armstrong SR, Beattie DT, Choi SK, Fatheree PR, Gendron RA, Genov D, Goldblum AA, Humphrey PP, Jiang L et al.. (2012) Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT(4) receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation. Bioorg Med Chem Lett, 22 (19): 6048-52. [PMID:22959244]

90. Lopez-Gimenez JF, Villazon M, Brea J, Loza MI, Palacios JM, Mengod G, Vilaro MT. (2001) Multiple conformations of native and recombinant human 5-hydroxytryptamine(2a) receptors are labeled by agonists and discriminated by antagonists. Mol Pharmacol, 60: 690-699. [PMID:11562430]

91. Lovenberg TW, Erlander MG, Baron BM, Racke M, Slone AL, Siegel BW, Craft CM, Burns JE, Danielson PE, Sutcliffe JG. (1993) Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes. Proc Natl Acad Sci USA, 90 (6): 2184-8. [PMID:8384716]

92. Madsen K, Marner L, Haahr M, Gillings N, Knudsen GM. (2011) Mass dose effects and in vivo affinity in brain PET receptor studies--a study of cerebral 5-HT4 receptor binding with [11C]SB207145. Nucl Med Biol, 38 (8): 1085-91. [PMID:21831646]

93. Maier DL, Sobotka-Briner C, Ding M, Powell ME, Jiang Q, Hill G, Heys JR, Elmore CS, Pierson ME, Mrzljak L. (2009) [N-methyl-3H3]AZ10419369 binding to the 5-HT1B receptor: in vitro characterization and in vivo receptor occupancy. J Pharmacol Exp Ther, 330 (1): 342-51. [PMID:19401496]

94. Malgouris C, Flamand F, Doble A. (1993) Autoradiographic studies of RP 62203, a potent 5-HT2 receptor antagonist. Pharmacological characterization of [3H]RP 62203 binding in the rat brain. Eur J Pharmacol, 233 (1): 37-45. [PMID:8472747]

95. Marin P, Becamel C, Dumuis A, Bockaert J. (2012) 5-HT receptor-associated protein networks: new targets for drug discovery in psychiatric disorders?. Curr Drug Targets, 13 (1): 28-52. [PMID:21777185]

96. Matthes H, Boschert U, Amlaiky N, Grailhe R, Plassat JL, Muscatelli F, Mattei MG, Hen R. (1993) Mouse 5-hydroxytryptamine5A and 5-hydroxytryptamine5B receptors define a new family of serotonin receptors: cloning, functional expression, and chromosomal localization. Mol Pharmacol, 43 (3): 313-9. [PMID:8450829]

97. Mattsson C, Sonesson C, Sandahl A, Greiner HE, Gassen M, Plaschke J, Leibrock J, Böttcher H. (2005) 2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. Bioorg Med Chem Lett, 15 (19): 4230-4. [PMID:16055331]

98. McAllister G, Charlesworth A, Snodin C, Beer MS, Noble AJ, Middlemiss DN, Iversen LL, Whiting P. (1992) Molecular cloning of a serotonin receptor from human brain (5HT1E): a fifth 5HT1-like subtype. Proc Natl Acad Sci USA, 89 (12): 5517-21. [PMID:1608964]

99. McCall RB, Romero AG, Bienkowski MJ, Harris DW, McGuire JC, Piercey MF, Shuck ME, Smith MW, Svensson KA, Schreur PJ et al.. (1994) Characterization of U-92016A as a selective, orally active, high intrinsic activity 5-hydroxytryptamine1A agonist. J Pharmacol Exp Ther, 271 (2): 875-83. [PMID:7965808]

100. McKinnell RM, Armstrong SR, Beattie DT, Fatheree PR, Long DD, Marquess DG, Shaw JP, Vickery RG. (2013) Discovery of TD-8954, a clinical stage 5-HT(4) receptor agonist with gastrointestinal prokinetic properties. Bioorg Med Chem Lett, 23 (14): 4210-5. [PMID:23756062]

101. Mialet J, Berque-Bestel I, Eftekhari P, Gastineau M, Giner M, Dahmoune Y, Donzeau-Gouge P, Hoebeke J, Langlois M, Sicsic S et al.. (2000) Isolation of the serotoninergic 5-HT4(e) receptor from human heart and comparative analysis of its pharmacological profile in C6-glial and CHO cell lines. Br J Pharmacol, 129 (4): 771-81. [PMID:10683202]

102. Mialet J, Berque-Bestel I, Sicsic S, Langlois M, Fischmeister R, Lezoualc'h F. (2000) Pharmacological characterization of the human 5-HT(4(d)) receptor splice variant stably expressed in Chinese hamster ovary cells. Br J Pharmacol, 131 (4): 827-35. [PMID:11030734]

103. Mialet J, Dahmoune Y, Lezoualc'h F, Berque-Bestel I, Eftekhari P, Hoebeke J, Sicsic S, Langlois M, Fischmeister R. (2000) Exploration of the ligand binding site of the human 5-HT(4) receptor by site-directed mutagenesis and molecular modeling. Br J Pharmacol, 130 (3): 527-38. [PMID:10821780]

104. Middlemiss DN, Göthert M, Schlicker E, Scott CM, Selkirk JV, Watson J, Gaster LM, Wyman P, Riley G, Price GW. (1999) SB-236057, a selective 5-HT1B receptor inverse agonist, blocks the 5-HT human terminal autoreceptor. Eur J Pharmacol, 375 (1-3): 359-65. [PMID:10443589]

105. Millan MJ, Gobert A, Newman-Tancredi A, Audinot V, Lejeune F, Rivet JM, Cussac D, Nicolas JP, Muller O, Lavielle G. (1998) S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison with clozapine and haloperidol. J Pharmacol Exp Ther, 286 (3): 1341-55. [PMID:9732398]

106. Millan MJ, Newman-Tancredi A, Audinot V, Cussac D, Lejeune F, Nicolas JP, Cogé F, Galizzi JP, Boutin JA, Rivet JM et al.. (2000) Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states. Synapse, 35 (2): 79-95. [PMID:10611634]

107. Napier C, Stewart M, Melrose H, Hopkins B, McHarg A, Wallis R. (1999) Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. Eur J Pharmacol, 368 (2-3): 259-68. [PMID:10193663]

108. Nelson DL, Lucaites VL, Wainscott DB, Glennon RA. (1999) Comparisons of hallucinogenic phenylisopropylamine binding affinities at cloned human 5-HT2A, -HT(2B) and 5-HT2C receptors. Naunyn Schmiedebergs Arch Pharmacol, 359 (1): 1-6. [PMID:9933142]

109. Nelson DL, Phebus LA, Johnson KW, Wainscott DB, Cohen ML, Calligaro DO, Xu YC. (2010) Preclinical pharmacological profile of the selective 5-HT1F receptor agonist lasmiditan. Cephalalgia, 30 (10): 1159-69. [PMID:20855361]

110. Newman-Tancredi A, Audinot V, Moreira C, Verrièle L, Millan MJ. (2000) Inverse agonism and constitutive activity as functional correlates of serotonin h5-HT(1B) receptor/G-protein stoichiometry. Mol Pharmacol, 58 (5): 1042-9. [PMID:11040052]

111. Newman-Tancredi A, Cussac D, Audinot V, Millan MJ. (1999) Actions of roxindole at recombinant human dopamine D2, D3 and D4 and serotonin 5-HT1A, 5-HT1B and 5-HT1D receptors. Naunyn Schmiedebergs Arch Pharmacol, 359 (6): 447-53. [PMID:10431754]

112. Newman-Tancredi A, Gavaudan S, Conte C, Chaput C, Touzard M, Verrièle L, Audinot V, Millan MJ. (1998) Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study. Eur J Pharmacol, 355 (2-3): 245-56. [PMID:9760039]

113. Newman-Tancredi A, Martel JC, Assié MB, Buritova J, Lauressergues E, Cosi C, Heusler P, Bruins Slot L, Colpaert FC, Vacher B et al.. (2009) Signal transduction and functional selectivity of F15599, a preferential post-synaptic 5-HT1A receptor agonist. Br J Pharmacol, 156 (2): 338-53. [PMID:19154445]

114. Newman-Tancredi A, Verrièle L, Chaput C, Millan MJ. (1998) Labelling of recombinant human and native rat serotonin 5-HT1A receptors by a novel, selective radioligand, [3H]-S 15535: definition of its binding profile using agonists, antagonists and inverse agonists. Naunyn Schmiedebergs Arch Pharmacol, 357 (3): 205-17. [PMID:9550290]

115. Newman-Tancredi A, Wootton R, Strange PG. (1992) High-level stable expression of recombinant 5-HT1A 5-hydroxytryptamine receptors in Chinese hamster ovary cells. Biochem J, 285 ( Pt 3): 933-8. [PMID:1386736]

116. Noda M, Yasuda S, Okada M, Higashida H, Shimada A, Iwata N, Ozaki N, Nishikawa K, Shirasawa S, Uchida M et al.. (2003) Recombinant human serotonin 5A receptors stably expressed in C6 glioma cells couple to multiple signal transduction pathways. J Neurochem, 84 (2): 222-32. [PMID:12558985]

117. Ochi T, Sakamoto M, Minamida A, Suzuki K, Ueda T, Une T, Toda H, Matsumoto K, Terauchi Y. (2005) Syntheses and properties of the major hydroxy metabolites in humans of blonanserin AD-5423, a novel antipsychotic agent. Bioorg Med Chem Lett, 15 (4): 1055-9. [PMID:15686911]

118. Palacios JM, Pazos A, Hoyer D. (2017) A short history of the 5-HT_2C receptor: from the choroid plexus to depression, obesity and addiction treatment. Psychopharmacology (Berl.), 234 (9-10): 1395-1418. [PMID:28265714]

119. Parker CA, Gunn RN, Rabiner EA, Slifstein M, Comley R, Salinas C, Johnson CN, Jakobsen S, Houle S, Laruelle M et al.. (2012) Radiosynthesis and characterization of 11C-GSK215083 as a PET radioligand for the 5-HT6 receptor. J Nucl Med, 53 (2): 295-303. [PMID:22223878]

120. Parker EM, Izzarelli DG, Lewis-Higgins L, Palmer D, Shapiro RA. (1996) Two amino acid differences in the sixth transmembrane domain are partially responsible for the pharmacological differences between the 5-HT1D beta and 5-HT1E 5-hydroxytryptamine receptors. J Neurochem, 67 (5): 2096-103. [PMID:8863519]

121. Pauwels PJ, Wurch T, Amoureux MC, Palmier C, Colpaert FC. (1996) Stimulation of cloned human serotonin 5-HT1D beta receptor sites in stably transfected C6 glial cells promotes cell growth. J Neurochem, 66 (1): 65-73. [PMID:8522991]

122. Pazos A, Hoyer D, Palacios JM. (1984) The binding of serotonergic ligands to the porcine choroid plexus: characterization of a new type of serotonin recognition site. Eur J Pharmacol, 106 (3): 539-46. [PMID:6519175]

123. Peng Y, McCorvy JD, Harpsøe K, Lansu K, Yuan S, Popov P, Qu L, Pu M, Che T, Nikolajsen LF et al.. (2018) 5-HT_2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology. Cell, 172 (4): 719-730.e14. [PMID:29398112]

124. Phebus LA, Johnson KW, Zgombick JM, Gilbert PJ, Van Belle K, Mancuso V, Nelson DL, Calligaro DO, Kiefer Jr AD, Branchek TA et al.. (1997) Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine. Life Sci, 61 (21): 2117-26. [PMID:9395253]

125. Ramage AG, Villalón CM. (2008) 5-hydroxytryptamine and cardiovascular regulation. Trends Pharmacol Sci, 29 (9): 472-81. [PMID:19086344]

126. Rashid M, Manivet P, Nishio H, Pratuangdejkul J, Rajab M, Ishiguro M, Launay JM, Nagatomo T. (2003) Identification of the binding sites and selectivity of sarpogrelate, a novel 5-HT2 antagonist, to human 5-HT2A, 5-HT2B and 5-HT2C receptor subtypes by molecular modeling. Life Sci, 73 (2): 193-207. [PMID:12738034]

127. Reavill C, Kettle A, Holland V, Riley G, Blackburn TP. (1999) Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist. Br J Pharmacol, 126 (3): 572-4. [PMID:10188965]

128. Reynolds GP, Mason SL, Meldrum A, De Keczer S, Parnes H, Eglen RM, Wong EH. (1995) 5-Hydroxytryptamine (5-HT)4 receptors in post mortem human brain tissue: distribution, pharmacology and effects of neurodegenerative diseases. Br J Pharmacol, 114 (5): 993-8. [PMID:7780656]

129. Rivail L, Giner M, Gastineau M, Berthouze M, Soulier JL, Fischmeister R, Lezoualc'h F, Maigret B, Sicsic S, Berque-Bestel I. (2004) New insights into the human 5-HT4 receptor binding site: exploration of a hydrophobic pocket. Br J Pharmacol, 143 (3): 361-70. [PMID:15351779]

130. Rosier A, Dupont P, Peuskens J, Bormans G, Vandenberghe R, Maes M, de Groot T, Schiepers C, Verbruggen A, Mortelmans L. (1996) Visualisation of loss of 5-HT2A receptors with age in healthy volunteers using [18F]altanserin and positron emission tomographic imaging. Psychiatry Res, 68 (1): 11-22. [PMID:9027929]

131. Roth BL, Craigo SC, Choudhary MS, Uluer A, Monsma Jr FJ, Shen Y, Meltzer HY, Sibley DR. (1994) Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. J Pharmacol Exp Ther, 268 (3): 1403-10. [PMID:7908055]

132. Rothman RB, Baumann MH, Savage JE, Rauser L, McBride A, Hufeisen SJ, Roth BL. (2000) Evidence for possible involvement of 5-HT(2B) receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications. Circulation, 102 (23): 2836-41. [PMID:11104741]

133. Schaerlinger B, Hickel P, Etienne N, Guesnier L, Maroteaux L. (2003) Agonist actions of dihydroergotamine at 5-HT2B and 5-HT2C receptors and their possible relevance to antimigraine efficacy. Br J Pharmacol, 140 (2): 277-84. [PMID:12970106]

134. Schechter LE, Lin Q, Smith DL, Zhang G, Shan Q, Platt B, Brandt MR, Dawson LA, Cole D, Bernotas R et al.. (2008) Neuropharmacological profile of novel and selective 5-HT6 receptor agonists: WAY-181187 and WAY-208466. Neuropsychopharmacology, 33 (6): 1323-35. [PMID:17625499]

135. Schmitz B, Ullmer C, Segelcke D, Gwarek M, Zhu XR, Lübbert H. (2015) BF-1--a novel selective 5-HT2B receptor antagonist blocking neurogenic dural plasma protein extravasation in guinea pigs. Eur J Pharmacol, 751: 73-80. [PMID:25666387]

136. Schotte A, Janssen PF, Gommeren W, Luyten WH, Van Gompel P, Lesage AS, De Loore K, Leysen JE. (1996) Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl.), 124 (1-2): 57-73. [PMID:8935801]

137. Selkirk JV, Scott C, Ho M, Burton MJ, Watson J, Gaster LM, Collin L, Jones BJ, Middlemiss DN, Price GW. (1998) SB-224289--a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity. Br J Pharmacol, 125 (1): 202-8. [PMID:9776361]

138. Shahid M, Walker GB, Zorn SH, Wong EH. (2009) Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol (Oxford), 23 (1): 65-73. [PMID:18308814]

139. Sleight AJ, Boess FG, Bös M, Levet-Trafit B, Riemer C, Bourson A. (1998) Characterization of Ro 04-6790 and Ro 63-0563: potent and selective antagonists at human and rat 5-HT6 receptors. Br J Pharmacol, 124 (3): 556-62. [PMID:9647481]

140. Sleight AJ, Stam NJ, Mutel V, Vanderheyden PM. (1996) Radiolabelling of the human 5-HT2A receptor with an agonist, a partial agonist and an antagonist: effects on apparent agonist affinities. Biochem Pharmacol, 51 (1): 71-6. [PMID:8534270]

141. Smith JA, Beattie DT, Marquess D, Shaw JP, Vickery RG, Humphrey PP. (2008) The in vitro pharmacological profile of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity. Naunyn Schmiedebergs Arch Pharmacol, 378 (1): 125-37. [PMID:18415081]

142. Stam NJ, Roesink C, Dijcks F, Garritsen A, van Herpen A, Olijve W. (1997) Human serotonin 5-HT7 receptor: cloning and pharmacological characterisation of two receptor variants. FEBS Lett, 413 (3): 489-94. [PMID:9303561]

143. Thomas DR, Atkinson PJ, Ho M, Bromidge SM, Lovell PJ, Villani AJ, Hagan JJ, Middlemiss DN, Price GW. (2000) [(3)H]-SB-269970--A selective antagonist radioligand for 5-HT(7) receptors. Br J Pharmacol, 130 (2): 409-17. [PMID:10807680]

144. Thomas DR, Gittins SA, Collin LL, Middlemiss DN, Riley G, Hagan J, Gloger I, Ellis CE, Forbes IT, Brown AM. (1998) Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719. Br J Pharmacol, 124 (6): 1300-6. [PMID:9720804]

145. Thomsen WJ, Grottick AJ, Menzaghi F, Reyes-Saldana H, Espitia S, Yuskin D, Whelan K, Martin M, Morgan M, Chen W et al.. (2008) Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization. J Pharmacol Exp Ther, 325 (2): 577-87. [PMID:18252809]

146. Turner MR, Rabiner EA, Hammers A, Al-Chalabi A, Grasby PM, Shaw CE, Brooks DJ, Leigh PN. (2005) [11C]-WAY100635 PET demonstrates marked 5-HT1A receptor changes in sporadic ALS. Brain, 128 (Pt 4): 896-905. [PMID:15689356]

147. Van den Wyngaert I, Gommeren W, Verhasselt P, Jurzak M, Leysen J, Luyten W, Bender E. (1997) Cloning and expression of a human serotonin 5-HT4 receptor cDNA. J Neurochem, 69 (5): 1810-9. [PMID:9349523]

148. Vanover KE, Harvey SC, Son T, Bradley SR, Kold H, Makhay M, Veinbergs I, Spalding TA, Weiner DM, Andersson CM et al.. (2004) Pharmacological characterization of AC-90179 [2-(4-methoxyphenyl)-N-(4-methyl-benzyl)-N-(1-methyl-piperidin-4-yl)-acetamide hydrochloride]: a selective serotonin 2A receptor inverse agonist. J Pharmacol Exp Ther, 310 (3): 943-51. [PMID:15102927]

149. Varnäs K, Nyberg S, Halldin C, Varrone A, Takano A, Karlsson P, Andersson J, McCarthy D, Smith M, Pierson ME et al.. (2011) Quantitative analysis of [11C]AZ10419369 binding to 5-HT1B receptors in human brain. J Cereb Blood Flow Metab, 31 (1): 113-23. [PMID:20424633]

150. Villalón CM, Centurión D. (2007) Cardiovascular responses produced by 5-hydroxytriptamine:a pharmacological update on the receptors/mechanisms involved and therapeutic implications. Naunyn Schmiedebergs Arch Pharmacol, 376 (1-2): 45-63. [PMID:17703282]

151. Wacker D, Wang C, Katritch V, Han GW, Huang XP, Vardy E, McCorvy JD, Jiang Y, Chu M, Siu FY et al.. (2013) Structural features for functional selectivity at serotonin receptors. Science, 340 (6132): 615-9. [PMID:23519215]

152. Waeber C, Grailhe R, Yu XJ, Hen R, Moskowitz MA. (1998) Putative 5-ht5 receptors: localization in the mouse CNS and lack of effect in the inhibition of dural protein extravasation. Ann N Y Acad Sci, 861: 85-90. [PMID:9928243]

153. Wainscott DB, Cohen ML, Schenck KW, Audia JE, Nissen JS, Baez M, Kursar JD, Lucaites VL, Nelson DL. (1993) Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor. Mol Pharmacol, 43 (3): 419-26. [PMID:8450835]

154. Wainscott DB, Krushinski Jr JH, Audia JE, Schaus JM, Zgombick JM, Lucaites VL, Nelson DL. (2005) [3H]LY334370, a novel radioligand for the 5-HT1F receptor. I. In vitro characterization of binding properties. Naunyn Schmiedebergs Arch Pharmacol, 371 (3): 169-77. [PMID:15900510]

155. Wainscott DB, Sasso DA, Kursar JD, Baez M, Lucaites VL, Nelson DL. (1998) [3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor. Naunyn Schmiedebergs Arch Pharmacol, 357 (1): 17-24. [PMID:9459568]

156. Wang C, Jiang Y, Ma J, Wu H, Wacker D, Katritch V, Han GW, Liu W, Huang XP, Vardy E et al.. (2013) Structural basis for molecular recognition at serotonin receptors. Science, 340 (6132): 610-4. [PMID:23519210]

157. Ward SE, Harrington FP, Gordon LJ, Hopley SC, Scott CM, Watson JM. (2005) Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist. J Med Chem, 48 (10): 3478-80. [PMID:15887956]

158. Weinshank RL, Zgombick JM, Macchi MJ, Branchek TA, Hartig PR. (1992) Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta. Proc Natl Acad Sci USA, 89 (8): 3630-4. [PMID:1565658]

159. Werry TD, Loiacono R, Sexton PM, Christopoulos A. (2008) RNA editing of the serotonin 5HT2C receptor and its effects on cell signalling, pharmacology and brain function. Pharmacol Ther, 119 (1): 7-23. [PMID:18554725]

160. Wurch T, Colpaert FC, Pauwels PJ. (1998) Chimeric receptor analysis of the ketanserin binding site in the human 5-Hydroxytryptamine1D receptor: importance of the second extracellular loop and fifth transmembrane domain in antagonist binding. Mol Pharmacol, 54 (6): 1088-96. [PMID:9855638]

161. Xie Z, Lee SP, O'Dowd BF, George SR. (1999) Serotonin 5-HT1B and 5-HT1D receptors form homodimers when expressed alone and heterodimers when co-expressed. FEBS Lett, 456 (1): 63-7. [PMID:10452531]

162. Xu X, Wei Y, Guo Q, Zhao S, Liu Z, Xiao T, Liu Y, Qiu Y, Hou Y, Zhang G et al.. (2018) Pharmacological Characterization of H05, a Novel Serotonin and Noradrenaline Reuptake Inhibitor with Moderate 5-HT_2A Antagonist Activity for the Treatment of Depression. J Pharmacol Exp Ther, 365 (3): 624-635. [PMID:29615471]

163. Xu YC, Schaus JM, Walker C, Krushinski J, Adham N, Zgombick JM, Liang SX, Kohlman DT, Audia JE. (1999) N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist. J Med Chem, 42 (3): 526-31. [PMID:9986723]

Subcommittee members: Nicholas M. Barnes (Chairperson) Neuropharmacology Research Group College of Medical and Dental Sciences University of Birmingham Edgbaston Birmingham B15 2TT UK Daniel Hoyer (Co-chairperson) Faculty of Medicine, Dentistry and Health Sciences School of Biomedical Sciences Department of Biochemistry and Pharmacology The University of Melbourne Parkville, Victoria 3010 Australia Rodrigo Andrade Department of Pharmacology Wayne State University School of Medicine 540 East Canfield Detroit MI 48201 USA Joel Bockaert LaboratoDepartment of Pharmacology Wayne State University School of Medicine 540 East Canfield Detroit MI 48201 USA Amy Butler Cellular and Molecular Neuropharmacology Research Group Clinical and Experimental Medicine The Medical School, University of Birmingham Birmingham B15 2TT UK Michel Hamon UMR-677 INSERM/UPMC Faculté de Médecine Pierre et Marie Curie Site Pitié-Salpêtrière 91 Boulevard de l’hôpital 75634 Paris Cedex 13 France Julie Hensler Department of Pharmacology University of Texas Health Science Center 7703 Floyd Curl Drive San Antonia Texas 78229-3900 USA Katharine Herrick-Davis Department of Pharmacology and Neuroscience A-136, Albany Medical College Center for Neuropharmacology and Neuroscience Albany NY 12208 USA Luc Maroteaux Developmental Neurobiology Hôpital Salpêtrière 47 Blvd de l'Hôpital Paris 75651 France Graeme R. Martin Discovery-Insight 37 Erin Lane Half Moon Bay CA 94019-1770 USA John Neumaier (Past chairperson) Department of Psychiatry and Behavioral Sciences Harborview Medical Center University of Washington Seattle WA 98104 USA John A. Peters Room CB 08 Carnelley Building School of Life Sciences The University of Dundee Dundee DD1 5EH Scotland UK Bryan Roth Department of Pharmacology School of Medicine University of North Carolina Chapel Hill NC 27599 USA Trevor Sharp University Department of Pharmacology Oxford University Mansfield Road Oxford OX1 3QT UK Carlos M. Villalon Seccion de Terapeutica Experimental Departmento de Farmacologia y Toxicologia CINVESTAV IPN Adpo Postal 22026 Mexico DF 14000 Mexico

Other contributors: Gordon Baxter Pharmagene Laboratories 2A Orchard Road Royston SG8 5HD UK Theresa Branchek Synaptic Pharmaceutical Corporation 215 College Road Paramus NJ 07652-1410 USA Marlene L. Cohen Cardiovascular Pharmacology 0821 Lilly Research Laboratories MC304 Indianapolis IN 46285-0001 USA Aline Dumuis Directeur de Recherche CNRS Institut de Génomique Fonctionnelle - Dépt. de Neurobiologie UMR 5203 CNRS - U 661 INSERM - Univ. Montpellier I & II 141, rue de la Cardonille Montpellier 34094 France Richard M. Eglen PerkinElmer William Street Wellesley Hills MA 02481 USA Manfred Göthert Institut für Pharmakologie und Toxikologie Universität Bonn Reuterstrasse 2b Bonn 5300 Germany Mark Hamblin Department of Psychiatry and Behavioural Sciences Geriatric Research Education and Clinical Center (182B) Seattle Veterans Affairs Medical Center 1660 South Columbian Way Seattle WA 98108 USA Paul R. Hartig DuPont-Merck Pharmaceutical Company Experimental Station PO Box 80400 Wilmington DE 19880-0400 USA René Hen Columbia University College of Physicians and Surgeons Center for Neurobiology and Behavior 722 West 168th Street New York NY 10032 USA Rebecca Hills (Past curator) Patrick P. A. Humphrey Glaxo Institute of Applied Pharmacology Department of Pharmacology University of Cambridge Tennis Court Road Cambridge CB2 1QJ UK Klaus Peter Latté axxonis Pharma AG Schöneberger Strasse 15 (2.OG) Berlin D-10963 Germany Derek N. Middlemiss Psychiatry Research Department Smith-Kline-Beecham Pharmaceuticals New Frontiers Science Park Third Avenue Harlow CM19 5AD UK Ewan Mylecharane Department of Pharmacology University of Sydney Sydney NSW 2006 Australia Stephen J. Peroutka 1025 Tournament Drive Hillsborough CA 94010 USA Pramod R. Saxena Department of Pharmacology Erasmus Universiteit Rotterdam Postbus 1738 Rotterdam 3000 DR The Netherlands Andrew Sleight Department of Neuropharmacology Hoffman-La Roche Postfach 4002 Basel CH-4050 Switzerland Frank Yocca Preclinical CNS Research Bristol-Myers Squibb PO Box 5100 5 Research Park Wallingford CT 06492-7660 USA