5-HT4 receptor

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5-hidroksitriptaminski (serotoninski) receptor 4

Identifikatori

HTR4; 5-HT4; 5-HT4R

Vanjski ID

OMIM: 602164 MGI: 109246 HomoloGene: 20243 IUPHAR: 5-HT₄ GeneCards: HTR4 Gene

Ontologija gena
Molekularna funkcija	• aktivnost rodopsinu-sličnog receptora • receptorska aktivnost • adrenoceptorska aktivnost • serotoninska receptorska aktivnost
Celularna komponenta	• membranska frakcija • integralno sa ćelijskom membranom • membrana • integralno sa membranom
Biološki proces	• prenos signala • signalni put G-protein spregnutog receptora • G-proteinska signalizacija, spregnuta sa cikličnim nukleotidnim sekundarnim glasnikom

Pregled RNK izražavanja

podaci

Ortolozi

Vrsta

Čovek

Miš

Entrez

3360

15562

Ensembl

ENSG00000164270

ENSMUSG00000026322

UniProt

Q13639

Q3URB5

RefSeq (mRNA)

NM_000870

NM_008313

RefSeq (protein)

NP_000861

NP_032339

Lokacija (UCSC)

Chr 5:
147.81 - 148.01 Mb

Chr 18:
62.45 - 62.59 Mb

PubMed pretraga

[1]

[2]

5-HT4 receptor (5-hidroksitriptaminski receptor 4) je protein koji je kod ljudi kodiran HTR4 genom.^[1]^[2]

Ovaj gen je član familije serotoninskih receptora, koji su G protein spregnuti receptori koji stimulišu cAMP produkciju u responsu na vezivanje serotonina (5-hidroksitriptamina). To je glikolizirani transmembranski protein koji funkcioniše u perifernom i centralnom nervnom sistemu gde modulara otpuštanje raznih neurotransmitera. Postoji više transkriptnih varijanti koje kodiraju proteine sa distinktnim C-terminalnim sekvencama.^[3]

Lokacija

Receptor je lociran u alimentarnom traktu, mokraćnoj bešiki, srcu i nadbubrežnoj žlezdi, kao i u centralnom nervnom sistemu (CNS).^[4] On nije nađen u cerebelumu.^[5]

Izoforme

Internalizacija je specifična za pojedine izoforme.^[6]

Ligandi

Postoji nekoliko lekova kaji deluju na 5-HT₄ kao selektivni agonisti. Oni se koriste u naučnim istraživanjima i kliničkoj medicini. Neki od lekova koji deluju kao 5-HT₄ agonisti su isto tako aktivni kao 5-HT₃ antagonisti, npr, mosaprid, metoclopramid, renzaprid i zacoprid.^[7] SB-207,145 radio obeležen sa ugljenikom-11 se koristi kao radioligand za 5-HT₄ ispitivanja pozitronskom emisionom tomografijom na životinjama^[8] i u humanim ispitivanjima.^[9].

Vidi još

5-HT receptor

Reference

↑ Claeysen S, Faye P, Sebben M, Lemaire S, Bockaert J, Dumuis A, Taviaux S (December 1997). „Assignment of 5-hydroxytryptamine receptor (HTR4) to human chromosome 5 bands q31→q33 by in situ hybridization.”. Cytogenet Cell Genet 78 (2): 133–4. DOI:10.1159/000134646. PMID 9371406.
↑ , Blondel O, Vandecasteele G, Gastineau M, Leclerc S, Dahmoune Y, Langlois M, Fischmeister R (September 1997). „Molecular and functional characterization of a 5-HT4 receptor cloned from human atrium.”. FEBS Lett 412 (3): 465–74. DOI:10.1016/S0014-5793(97)00820-X. PMID 9276448.
↑ „Entrez Gene: HTR4 5-hydroxytryptamine (serotonin) receptor 4”.
↑ S. S. Hegde, R. M. Eglen (1996-01-10). „Peripheral 5-HT4 receptors”. The FASEB journal 10 (12): 1398–1407. PMID 8903510.
↑ Katarina Varnäs, Christer Halldin, Victor W. Pike, Håkan Hall (2003). „Distribution of 5-HT₄ receptors in the postmortem human brain–an autoradiographic study using [¹²⁵]SB 207710”. European Neuropsychopharmacology 13: 228–234. DOI:10.1016/S0924-977X(03)00009-9.
↑ PMID 19922792
↑ Pellissier LP, Sallander J, Campillo M, Gaven F, Queffeulou E, Pillot M, Dumuis A, Claeysen S, Bockaert J, Pardo L (April 2009). „Conformational toggle switches implicated in basal constitutive and agonist-induced activated states of 5-hydroxytryptamine-4 receptors”. Molecular Pharmacology 75 (4): 982–90. DOI:10.1124/mol.108.053686. PMID 19168624.
↑ B. R. Kornum, N. M. Lind, N. Gillings, Lisbeth Marner, F. Andersen, Gitte Moos Knudsen (September 2008). „Evaluation of the novel 5-HT(4) receptor PET ligand [(11)C]SB207145 in the Gottingen minipig”. Journal of Cerebral Blood Flow and Metabolism 29 (1): 186. DOI:10.1038/jcbfm.2008.110. PMID 18797470.
↑ Lisbeth Marner, Nic Gillings, Roger Gunn, Robert Comley, William Baaré, Steen Hasselbalch and Gitte Knudsen (2008-01-05). „Quantification of 11C-SB207145-PET for 5-HT4 receptors in the human brain: Preliminary results”. Journal of Nuclear Medicine 48 (Supplement 2) (Supplement 2): 159P. Arhivirano iz originala na datum 2016-03-03. Pristupljeno 2014-05-02.
↑ Gale JD, Grossman CJ, Whitehead, JW Oxford AW, Bunce KT, Humphrey PP (1994). „GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor.”. British journal of pharmacology 111 (1): 332–8. PMC 1910004. PMID 8012715.
↑ Xu R, Hong J, Morse CL, Pike VW (2010-10-14). „Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography”. J Med Chem 53 (19): 7035-47. PMID 20812727.

Literatura

Cecilie Löe Licht, Changes in the 5-HT₄ receptor in animal models of depression and antidepressant treatment, PhD thesis, Faculty of Health Sciences, University of Copenhagen. Submitted 2008 October.
Ullmer C, Schmuck K, Kalkman HO, Lübbert H (1995). „Expression of serotonin receptor mRNAs in blood vessels.”. FEBS Lett. 370 (3): 215–21. DOI:10.1016/0014-5793(95)00828-W. PMID 7656980.
Blondel O, Vandecasteele G, Gastineau M, et al. (1997). „Molecular and functional characterization of a 5-HT4 receptor cloned from human atrium.”. FEBS Lett. 412 (3): 465–74. DOI:10.1016/S0014-5793(97)00820-X. PMID 9276448.
Van den Wyngaert I, Gommeren W, Verhasselt P, et al. (1997). „Cloning and expression of a human serotonin 5-HT4 receptor cDNA.”. J. Neurochem. 69 (5): 1810–9. DOI:10.1046/j.1471-4159.1997.69051810.x. PMID 9349523.
Claeysen S, Faye P, Sebben M, et al. (1997). „Cloning and expression of human 5-HT4S receptors. Effect of receptor density on their coupling to adenylyl cyclase.”. Neuroreport 8 (15): 3189–96. DOI:10.1097/00001756-199710200-00002. PMID 9351641.
Blondel O, Gastineau M, Dahmoune Y, et al. (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. DOI:10.1046/j.1471-4159.1998.70062252.x. PMID 9603189.
Cichon S, Kesper K, Propping P, Nöthen MM (1998). „Assignment of the human serotonin 4 receptor gene (HTR4) to the long arm of chromosome 5 (5q31-q33).”. Mol. Membr. Biol. 15 (2): 75–8. DOI:10.3109/09687689809027521. PMID 9724925.
Claeysen S, Sebben M, Becamel C, et al. (1999). „Novel brain-specific 5-HT4 receptor splice variants show marked constitutive activity: role of the C-terminal intracellular domain.”. Mol. Pharmacol. 55 (5): 910–20. PMID 10220570.
Bender E, Pindon A, van Oers I, et al. (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. DOI:10.1046/j.1471-4159.2000.740478.x. PMID 10646498.
Mialet J, Berque-Bestel I, Eftekhari P, 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. DOI:10.1038/sj.bjp.0703101. PMC 1571890. PMID 10683202.
Bach T, Syversveen T, Kvingedal AM, et al. (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. DOI:10.1007/s002100000299. PMID 11218067.
Medhurst AD, Lezoualc'h F, Fischmeister R, et al. (2001). „Quantitative mRNA analysis of five C-terminal splice variants of the human 5-HT4 receptor in the central nervous system by TaqMan real time RT-PCR.”. Brain Res. Mol. Brain Res. 90 (2): 125–34. DOI:10.1016/S0169-328X(01)00095-X. PMID 11406291.
Hiroi T, Hayashi-Kobayashi N, Nagumo S, et al. (2002). „Identification and characterization of the human serotonin-4 receptor gene promoter.”. Biochem. Biophys. Res. Commun. 289 (2): 337–44. DOI:10.1006/bbrc.2001.5979. PMID 11716477.
Vilaró MT, Doménech T, Palacios JM, Mengod G (2002). „Cloning and characterization of a novel human 5-HT4 receptor variant that lacks the alternatively spliced carboxy terminal exon. RT-PCR distribution in human brain and periphery of multiple 5-HT4 receptor variants.”. Neuropharmacology 42 (1): 60–73. DOI:10.1016/S0028-3908(01)00154-X. PMID 11750916.
López-Rodríguez ML, Murcia M, Benhamú B, et al. (2002). „Computational model of the complex between GR113808 and the 5-HT4 receptor guided by site-directed mutagenesis and the crystal structure of rhodopsin.”. J. Comput. Aided Mol. Des. 15 (11): 1025–33. DOI:10.1023/A:1014895611874. PMID 11989623.
Ohtsuki T, Ishiguro H, Detera-Wadleigh SD, et al. (2003). „Association between serotonin 4 receptor gene polymorphisms and bipolar disorder in Japanese case-control samples and the NIMH Genetics Initiative Bipolar Pedigrees.”. Mol. Psychiatry 7 (9): 954–61. DOI:10.1038/sj.mp.4001133. PMID 12399948.
Norum JH, Hart K, Levy FO (2003). „Ras-dependent ERK activation by the human G(s)-coupled serotonin receptors 5-HT4(b) and 5-HT7(a).”. J. Biol. Chem. 278 (5): 3098–104. DOI:10.1074/jbc.M206237200. PMID 12446729.
Strausberg RL, Feingold EA, Grouse LH, et al. (2003). „Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.”. Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. DOI:10.1073/pnas.242603899. PMC 139241. PMID 12477932.
Cartier D, Lihrmann I, Parmentier F, et al. (2003). „Overexpression of serotonin4 receptors in cisapride-responsive adrenocorticotropin-independent bilateral macronodular adrenal hyperplasia causing Cushing's syndrome.”. J. Clin. Endocrinol. Metab. 88 (1): 248–54. DOI:10.1210/jc.2002-021107. PMID 12519861.
Manzke T, Guenther U, Ponimaskin EG, et al. (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.

Spoljašnje veze

„5-HT₄”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Arhivirano iz originala na datum 2016-06-05.

Transmembranski receptor: G protein spregnuti receptori

Klasa A: Rodopsinu slični

Neurotransmiter

Adrenergički	α1 (A, B, D) • α2 (A, B, C) • β1 • β2 • β3
Purinski	Adenozinski (A1, A2A, A2B, A3) • P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
Serotoninski	(svi osim 5-HT3) 5-HT1 (A, B, D, E, F) • 5-HT2 (A, B, C) • 5-HT (4, 5A, 6, 7)
Drugi	Acetilholin (M1, M2, M3, M4, M5) • Dopamin (D1, D2, D3, D4, D5) • Histamin (H1, H2, H3, H4) • Melatonin (1A, 1B, 1C) • TAAR (1, 2, 3, 5, 6, 8, 9)

Metaboliti i
signalni molekuli

Eikozanoidni	CysLT (1, 2) • LTB4 (1, 2) • FPRL1 • OXE • Prostaglandin (DP (1, 2), EP (1, 2, 3, 4), FP) • Prostaciklin • Tromboksan
Drugi	Žučna kiselina • Kanabinoidni (CB1, CB2, GPR (18, 55, 119)) • EBI2 • Estrogen • Slobodna masna kiselina (1, 2, 3, 4) • Laktat • Lizofosfatidna kiselina (1, 2, 3, 4, 5, 6) • Lizofosfolipid (1, 2, 3, 4, 5, 6, 7, 8) • Niacin (1, 2) • Oksoglutarat • PAF • Sfingozin-1-fosfat (1, 2, 3, 4, 5) • Sukcinat

Peptid

Neuropeptidni

B/W (1, 2) • FF (1, 2) • S • Y (1, 2, 4, 5) • Neuromedin (B, U (1, 2)) • Neurotenzin (1, 2)

Drugi

Anafilatoksin (C3a, C5a) • Angiotenzin (1, 2) • Apelin • Bombezin (BRS3, GRPR, NMBR) • Bradikinin (B1, B2) • Hemokin • Holecistokinin (A, B) • Endotelin (A, B) • Formil peptid (1, 2, 3) • FSH • Galanin (1, 2, 3) • GHB receptor • Gonadotropin-oslobađajući hormon (1, 2) • Grelin • Kispeptin • Luteinizirajući hormon/horiogonadotropin • MAS (1, 1L, D, E, F, G, X1, X2, X3, X4) • Melanokortin (1, 2, 3, 4, 5) • MCHR (1, 2) • Motilin • Opioidni (δ, κ, μ, Nociceptin & ζ, ali ne σ) • Oreksin (1, 2) • Oksitocin • Prokineticin (1, 2) • Prolaktin-oslobađajući peptid • Relaksin (1, 2, 3, 4) • Somatostatin (1, 2, 3, 4, 5) • Tahikinin (1, 2, 3) • Tirotropin • Tirotropin-oslobađajući hormon • Urotenzin-II • Vazopresin (1A, 1B, 2)

Razno

Orfan	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)
Drugi	Adrenomedulin • Mirisni • Opsin (3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) • Proteazom-aktivirani (1, 2, 3, 4) • SREB (1, 2, 3)

Klasa B: Sekretinu slični

Orfan	GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 155, 157)
Drugi	Moždano specifični angiogenezni inhibitor (1, 2, 3) • Cadherin (1, 2, 3) • Kalcitonin • CALCRL • CD97 • Kortikotropin-oslobađajući hormon (1, 2) • EMR (1, 2, 3) • Glukagon (GR, GIPR, GLP1R, GLP2R) • Hormon rasta oslobađajući hormon • PACAPR1 • GPR • Latrofilin (1, 2, 3, ELTD1) • Metuselah-slični proteini • Paratiroidni hormon (1, 2) • Sekretin • Vazoaktivni intestinalni peptid (1, 2)

Orfan

GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 155, 157)

Drugi

Moždano specifični angiogenezni inhibitor (1, 2, 3) • Cadherin (1, 2, 3) • Kalcitonin • CALCRL • CD97 • Kortikotropin-oslobađajući hormon (1, 2) • EMR (1, 2, 3) • Glukagon (GR, GIPR, GLP1R, GLP2R) • Hormon rasta oslobađajući hormon • PACAPR1 • GPR • Latrofilin (1, 2, 3, ELTD1) • Metuselah-slični proteini • Paratiroidni hormon (1, 2) • Sekretin • Vazoaktivni intestinalni peptid (1, 2)

Klasa C: Metabotropni
glutamat / feromon

Ukus	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)
Drugi	Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A • GPR (156, 158, 179) • RAIG (1, 2, 3, 4)

Klasa F:
Frizzled / Zaglađeni

Uvojiti	Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10)
Zaglađeni	Zaglađeni

B trdu: peptidi (nrpl/grfl/cytl/horl), receptori (lgic, enzr, gprc, igsr, intg, nrpr/grfr/cytr), itra (adap, gbpr, mapk), calc, lipd, signalni putevi (hedp, wntp, tgfp+mapp, notp, jakp, fsap, hipp, tlrp)

Serotonergici

Ligandi 5-HT₁ receptora

5-HT_1A	Agonisti: Azapironi: Alnespiron • Binospiron • Buspiron • Enilospiron • Eptapiron • Gepiron • Ipsapiron • Perospiron • Revospiron • Tandospiron • Tiospiron • Umespiron • Zalospiron; Antidepresivi: Etoperidon • Nefazodon • Trazodon; Antipsihotici: Aripiprazol • Asenapin • Klozapin • Kvetiapin • Ziprasidon; Ergolini: Dihidroergotamin • Ergotamin • Lisurid • Metisergid • LSD; Triptamini: 5-CT • 5-MeO-DMT • 5-MT • Bufotenin • DMT • Indorenat • Psilocin • Psilocibin; Drugi: 8-OH-DPAT • Adatanserin • Bay R 1531 • Befiradol • BMY-14802 • Kanabidiol • Dimemebfe • Ebalzotan • Eltoprazin • F-11,461 • F-12,826 • F-13,714 • F-14,679 • F-15,063 • F-15,599 • Flesinoksan • Flibanserin • Lesopitron • Lu AA21004 • LY-293,284 • LY-301,317 • MKC-242 • NBUMP • Osemozotan • Oksaflozan • Pardoprunoks • Piklozotan • Rauvolscin • Repinotan • Roksindol • RU-24,969 • S 14,506 • S-14,671 • S-15,535 • Sarizotan • SSR-181,507 • Sunepitron • U-92,016-A • Urapidil • Vilazodon • Ksaliproden • Johimbin Antagonisti: Antipsihotici: Iloperidon • Risperidon • Sertindol; Beta blokatori: Alprenolol • Cianopindolol • Jodocianopindolol • Oksprenolol • Pindobind • Pindolol • Propranolol • Tertatolol; Drugi: AV965 • BMY-7,378 • CSP-2503 • Dotarizin • Flopropion • GR-46611 • Isamoltan • Lekozotan • Metitepin/Metiotepin • MPPF • NAN-190 • PRX-00023 • Robalzotan • S-15535 • SB-649,915 • SDZ 216-525 • Spiperon • Spiramid • Spiroksatrin • UH-301 • WAY-100,135 • WAY-100,635 • Ksilamidin
5-HT_1B	Agonisti: Lisergamidi: Dihidroergotamin • Ergotamin • Metisergid; Piperazini: Eltoprazin • TFMPP; Triptani: Avitriptan • Eletriptan • Sumatriptan • Zolmitriptan; Triptamini: 5-CT • 5-MT; Drugi: CGS-12066A • CP-93,129 • CP-94,253 • CP-135,807 • RU-24,969 Antagonisti: Lisergamidi: Metergolin; Drugi: AR-A000002 • Elzasonan • GR-127,935 • Isamoltan • Metitepin/Metiotepin • SB-216,641 • SB-224,289 • SB-236,057 • Johimbin
5-HT_1D	Agonisti: Lisergamidi: Dihidroergotamin • Metisergid; Triptani: Almotriptan • Avitriptan • Eletriptan • Frovatriptan • Naratriptan • Rizatriptan • Sumatriptan • Zolmitriptan; Triptamini: 5-CT • 5-Etil-DMT • 5-MT • 5-(Noniloksi)triptamin; Drugi: CP-135,807 • CP-286,601 • GR-46611 • L-694,247 • L-772,405 • PNU-109,291 • PNU-142,633 Antagonisti: Lisergamidi: Metergolin; Drugi: Alniditan • BRL-15,572 • Elzasonan • GR-127,935 • Ketanserin • LY-310,762 • LY-367,642 • LY-456,219 • LY-456,220 • Metitepin/Metiotepin • Ritanserin • Johimbin • Ziprasidon
5-HT_1E	Agonisti: Lisergamidi: Metisergid; Triptani: Eletriptan; Triptamini: BRL-54443 • Triptamin Antagonisti: Metitepin/Metiotepin
5-HT_1F	Agonisti: Triptani: Eletriptan • Naratriptan • Sumatriptan; Triptamini: 5-MT; Drugi: BRL-54443 • Lasmiditan • LY-334,370 Antagonisti: Metitepin/Metiotepin

Ligandi 5-HT₂ receptora

5-HT_2A	Agonisti: Lisergamidi: ALD-52 • Ergometrin • Lisurid • LA-SS-Az • LSD • LSD-Pip • 2-butil amid liserginske kiseline • 3-pentil amid liserginske kiseline • Metisergid; Fenetilamini: 25I-NBF • 25I-NBMD • 25I-NBOH • 25I-NBOMe • 2C-B • 2C-B-FLY • 2CB-Ind • 2C-C-NBOMe • 2C-E • 2C-I • 2C-TFM-NBOMe • 2C-T-2 • 2C-T-7 • 2C-T-21 • 2CBCB-NBOMe • 2CBFly-NBOMe • Bromo-DragonFLY • DOB • DOC • DOI • DOM • MDA • MDMA • Meskalin • TCB-2 • TFMFly; Piperazini: BZP • Hipazin • TFMPP; Triptamini: 5-CT • 5-MeO-α-ET • 5-MeO-α-MT • 5-MeO-DET • 5-MeO-DiPT • 5-MeO-DMT • 5-MeO-DPT • 5-MT • α-ET • α-Metil-5-HT • α-MT • Bufotenin • DET • DiPT • DMT • DPT • Psilocin • Psilocibin; Drugi: AL-34662 • AL-37350A • Dimemebfe • Medifoksamin • Oksaflozan • PNU-22394 • RH-34 Antagonisti: Atipični antipsihotici: Amperozid • Aripiprazol • Karpipramin • Klokapramin • Klozapin • Gevotrolin • Iloperidon • Melperon • Mosapramin • Olanzapin • Paliperidon • Pimozid • Hetiapin • Risperidon • Sertindol • Ziprasidon • Zotepin; Tipični antipsihotici: Loksapin • Pipamperon; Antidepresivi: Amitriptilin • Amoksapin • Aptazapin • Etoperidon • Mianserin • Mirtazapin • Nefazodon • Trazodon; Drugi: 5-I-R91150 • AC-90179 • Adatanserin • Altanserin • AMDA • APD-215 • Blonanserin • Cinanserin • CSP-2503 • Ciproheptadin • Deramciklan • Dotarizin • Eplivanserin • Esmirtazapin • Fananserin • Flibanserin • Ketanserin • KML-010 • Lubazodon • Mepiprazol • Metitepin/Metiotepin • Nantenin • Pimavanserin • Pizotifen • Pruvanserin • Rauvolscin • Ritanserin • S-14,671 • Sarpogrelat • Setoperon • Spiperon • Spiramid • SR-46349B • Volinanserin • Ksilamidin • Johimbin
5-HT_2B	Agonisti: Oksazolini: 4-Metilaminoreks • Aminoreks; Fenetilamini: Hlorfentermin • Kloforeks • DOB • DOC • DOI • DOM • Fenfluramin • MDA • MDMA • Norfenfluramin; Triptamini: 5-CT • 5-MT • α-Metil-5-HT; Drugi: BW-723C86 • Kabergolin • mCPP • Pergolid • PNU-22394 • Ro60-0175 Antagonisti: Agomelatin • Asenapin • EGIS-7625 • Ketanserin • Lisurid • LY-272,015 • Metitepin/Metiotepin • PRX-08066 • Rauvolscin • Ritanserin • RS-127,445 • Sarpogrelat • SB-200,646 • SB-204,741 • SB-206,553 • SB-215,505 • SB-221,284 • SB-228,357 • SDZ SER-082 • Tegaserod • Johimbin
5-HT_2C	Agonisti: Fenetilamini: 2C-B • 2C-E • 2C-I • 2C-T-2 • 2C-T-7 • 2C-T-21 • DOB • DOC • DOI • DOM • MDA • MDMA • Meskalin; Piperazini: Aripiprazol • mCPP • TFMPP; Triptamini: 5-CT • 5-MeO-α-ET • 5-MeO-α-MT • 5-MeO-DET • 5-MeO-DiPT • 5-MeO-DMT • 5-MeO-DPT • 5-MT • α-ET • α-Metil-5-HT • α-MT • Bufotenin • DET • DiPT • DMT • DPT • Psilocin • Psilocibin; Drugi: A-372,159 • AL-38022A • CP-809,101 • Dimemebfe • Lorkaserin• Medifoksamin • MK-212 • Org 12,962 • ORG-37,684 • Oksaflozan • PNU-22394 • Ro60-0175 • Ro60-0213 • Vabicaserin • WAY-629 • WAY-161,503 • YM-348 Antagonisti: Atipični antipsihotici: Klozapin • Iloperidon • Melperon • Olanzapin • Paliperidon • Pimozid • Hetiapin • Risperidon • Sertindol • Ziprasidon • Zotepin; Tipični antipsihotici: Hlorpromazin • Loksapin • Pipamperon; Antidepresivi: Agomelatin • Amitriptilin • Amoksapin • Aptazapin • Etoperidon • Fluoksetin • Mianserin • Mirtazapin • Nefazodon • Nortriptilin • Trazodon; Drugi: Adatanserin • Cinanserin • Ciproheptadin • Deramciklan • Dotarizin • Eltoprazin • Esmirtazapin • FR-260,010 • Ketanserin • Ketotifen • Latrepirdin • Lu AA24530 • Metitepin/Metiotepin • Metisergid • Pizotifen • Ritanserin • RS-102,221 • S-14,671 • SB-200,646 • SB-206,553 • SB-221,284 • SB-228,357 • SB-242,084 • SB-243,213 • SDZ SER-082 • Ksilamidin

Ligandi 5-HT₃, 5-HT₄, 5-HT₅, 5-HT₆, i 5-HT₇ receptora

5-HT₃	Agonisti: Piperazini: BZP • Hipazin; Triptamini: 2-Metil-5-HT • 5-CT; Drugi: Hlorofenilbiguanid • Butanol • Etanol • Halotan • Izofluran • RS-56812 • SR-57,227 • SR-57,227-A • Toluen • Trihloroetan • Trihloroetanol • Trihloroetilen • YM-31636 Antagonisti: Antiemetici: AS-8112 • Alosetron • Azasetron • Batanoprid • Bemesetron • Cilansetron • Dazoprid • Dolasetron • Granisetron • Lerisetron • Ondansetron • Palonosetron • Ramosetron • Renzaprid • Tropisetron • Zacoprid • Zatosetron; Atipični antipsihotici: Klozapin • Olanzapin • Hetiapin; Tetraciklični antidepresivi: Amoksapin • Mianserin • Mirtazapin; Drugi: CSP-2503 • ICS-205,930 • Lu AA21004 • Lu AA24530 • MDL-72,222 • Memantin • Azot-monoksid • Ricasetron • Sevofluran • Tujon • Ksenon
5-HT₄	Agonisti: Gastroprokinetički agensi: Cinitaprid • Cisaprid • Dazoprid • Metoklopramid • Mosaprid • Prukaloprid • Renzaprid • Tegaserod • Zakoprid; Drugi: 5-MT • BIMU8 • CJ-033,466 • PRX-03140 • RS-67333 • RS-67506 • SL65.0155 • TD-5108 Antagonisti: GR-113,808 • GR-125,487 • L-Lizin • Piboserod • RS-39604 • RS-67532 • SB-203,186
5-HT_5A	Agonisti: Lisergamidi: Ergotamin • LSD; Triptamini: 5-CT; Drugi: Valerenska kiselina Antagonisti: Asenapin • Latrepirdin • Metitepin/Metiotepin • Ritanserin • SB-699,551 * 5-HT_5B receptor nije funkcionalan kod ljudi.
5-HT₆	Agonisti: Lisergamidi: Dihidroergotamin • Ergotamin • Lisurid • LSD • Mesulergin • Metergolin • Metisergid; Triptamini: 2-Metil-5-HT • 5-BT • 5-CT • 5-MT • Bufotenin • E-6801 • E-6837 • EMD-386,088 • EMDT • LY-586,713 • N-Metil-5-HT • Triptamin; Drugi: WAY-181,187 • WAY-208,466 Antagonisti: Antidepresanti: Amitriptilin • Amoksapin • Klomipramin • Doksepin • Mianserin • Nortriptilin; Atipični antipsihotici: Aripiprazol • Asenapin • Klozapin • Fluperlapin • Iloperidon • Olanzapin • Tiospiron; Tipični antipsihotici: Hlorpromazin • Loksapin; Drugi: BGC20-760 • BVT-5182 • BVT-74316 • EGIS-12,233 • GW-742,457 • Ketanserin • Latrepirdin • Lu AE58054 • Metitepin/Metiotepin • MS-245 • PRX-07034 • Ritanserin • Ro04-6790 • Ro 63-0563 • SB-258,585 • SB-271,046 • SB-357,134 • SB-399,885 • SB-742,457
5-HT₇	Agonisti: Lisergamidi: LSD; Triptamini: 5-CT • 5-MT • Bufotenin; Drugi: 8-OH-DPAT • AS-19 • Bifeprunoks • LP-12 • LP-44 • RU-24,969 • Sarizotan Antagonisti: Lisergamidi: 2-Bromo-LSD • Bromokriptin • Dihidroergotamin • Ergotamin • Mesulergin • Metergolin • Metisergid; Antidepresanti: Amitriptilin • Amoksapin • Klomipramin • Imipramin • Maprotilin • Mianserin; Atipični antipsihotici: Amisulprid • Aripiprazol • Klozapin • Olanzapin • Risperidon • Sertindol • Tiospiron • Ziprasidon • Zotepin; Tipični antipsihotici: Hlorpromazin • Loksapin; Drugi: Butaklamol • EGIS-12,233 • Ketanserin • LY-215,840 • Metitepin/Metiotepin • Pimozid • Ritanserin • SB-258,719 • SB-258,741 • SB-269,970 • SB-656,104 • SB-656,104-A • SB-691,673 • SLV-313 • SLV-314 • Spiperon • SSR-181,507

Inhibitori preuzimanja

SERT

Selektivni inhibitori preuzimanja serotonina (SSRI): Alaproklat • Citalopram • Dapoksetin • Desmetilcitalopram • Desmetilsertralin • Escitalopram • Femoksetin • Fluoksetin • Fluvoksamin • Indalpin • Ifoksetin • Litoksetin • Lu AA21004 • Lubazodon • Panuramin • Paroksetin • Pirandamin • RTI-353 • Seproksetin • Sertralin • Vilazodon • Zimelidin; Inhibitori preuzimanja serotonin-norepinefrina (SNRI): Bicifadin • Desvenlafaksin • Duloksetin • Eklanamin • Levomilnacipran • Milnacipran • Sibutramin • Venlafaksin; Inhibitori preuzimanja serotonin-norepinefrin-dopamina (SNDRI): Brasofensin • Diklofensin • DOV-102,677 • DOV-21,947 • DOV-216,303 • NS-2359 • SEP-225289 • SEP-227,162 • Tesofensin; Triciklični antidepresivi (TCAs): Amitriptilin • Butriptilin • Cianopramin • Klomipramin • Desipramin • Dosulepin • Doksepin • Imipramin • Lofepramin • Nortriptilin • Pipofezin • Protriptilin • Trimipramin; Tetraciklični antidepresanti (TeCA): Amoksapin; Piperazini: Nefazodon • Trazodon; Antihistamini: Bromfeniramin • Hlorfenamin • Difenhidramin • Mepiramin/Pirilamin • Feniramin • Tripelenamin; Opioidi: Petidin • Metadon • Propoksifen; Drugi: Kokain • CP-39,332 • Ciklobenzaprin • Dekstrometorfan • Dekstrorfan • EXP-561 • Fezolamin • Mesembrin • Nefopam • PIM-35 • Pridefin • Roksindol • SB-649,915 • Ziprasidon

VMAT

Ibogain • Reserpin • Tetrabenazin

Agensi otpuštanja

Aminoindani: 5-IAI • AMMI • ETAI • MDAI • MDMAI • MMAI • TAI; Aminotetralini: 6-CAT • 8-OH-DPAT • MDAT • MDMAT; Oksazolini: 4-Metilaminoreks • Aminoreks • Klominoreks • Fluminoreks; Fenetilamini (takođe Amfetamini, Katinoni, Fentermini, itd): 2-Metil-MDA • 4-CAB • 4-FA • 4-FMA • 4-HA • 4-MTA • 5-APDB • 5-Metil-MDA • 6-APDB • 6-Metil-MDA • AEMMA • Amiflamin • BDB • BOH • Brefedron • Butilon • Hlorfentermin • Kloforeks • Amfepramon • Metamfepramon • DFMDA • DMA • DMMA • EBDB • EDMA • Etilon • Etoloreks • Fenfluramin (Deksfenfluramin) • Flefedron • IAP • IMP • Lofofin • MBDB • MDA • MDEA • MDHMA • MDMA • MDMPEA • MDOH • MDPEA • Mefedron • Metedron • Metilon • MMA • MMDA • MMDMA • MMMA • NAP • Norfenfluramin • 4-TFMA • pBA • pCA • pIA • PMA • PMEA • PMMA • TAP; Piperazini: 2C-B-BZP • 2-BZP • 3-MeOPP • BZP • DCPP • MBZP • mCPP • MDBZP • MeOPP • Mepiprazol • pCPP • pFPP • pTFMPP • TFMPP; Triptamini: 4-Metil-αET • 4-Metil-αMT • 5-CT • 5-MeO-αET • 5-MeO-αMT • 5-MT • αET • αMT • DMT • Triptamin (sam); Drugi: Indeloksazin • Tramadol • Viqualin

Inhibitori enzima

Anabolizam

TPH	AGN-2979 • Fenklonin
AAAD	Benserazid • Karbidopa • Genistein • Metildopa

Katabolizam

MAO

Neselektivni: Benmoksin • Karoksazon • Ehinopsidin • Furazolidon • Hidralazin • Indantadol • Iproklozid • Iproniazid • Izokarboksazid • Izoniazid • Linezolid • Mebanazin • Metfendrazin • Nialamid • Oktamoksin • Paraksazon • Fenelzin • Feniprazin • Fenoksipropazin • Pivalilbenzhidrazin • Prokarbazin • Safrazin • Tranilcipromin; MAO-A selektivni: Amiflamin • Bazinaprin • Befloksaton • Befol • Brofaromin • Cimoksaton • Klorgilin • Esupron • Harmala alkaloidi (Harmin, Harmalin, Tetrahidroharmin, Harman, Norharman, itd) • Metilensko plavo • Metralindol • Minaprin • Moklobemid • Pirlindol • Serkloremin • Tetrindol • Toloksaton • Tirima

Drugi

Prekursori	L-Triptofan → 5-HTP
Kofaktori	Fero gvožđe (Fe²⁺) • Magnezijum (Mg²⁺) • Tetrahidrobiopterin • Vitamin B₃ (Niacin, Nikotinamid → NADPH) • Vitamin B₆ (Piridoksin, Piridoksamin, Piridoksal → Piridoksal fosfat) • Vitamin B₉ (Folna kiselina → Tetrahidrofolna kiselina) • Vitamin C (Askorbinska kiselina) • Cink (Zn²⁺)
Drugi	Pojačivači aktivnosti: BPAP • PPAP; Pojačivači preuzimanja: Tianeptin