5-HT6

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The correct title of this article is 5-HT6 receptor. It appears incorrectly here because of technical restrictions.
5-hydroxytryptamine (serotonin) receptor 6
Identifiers
Symbols HTR6; 5-HT6; 5-HT6R
External IDs OMIM: 601109 MGI: 1196627 HomoloGene: 673
RNA expression pattern

More reference expression data
Orthologs
Human Mouse
Entrez 3362 15565
Ensembl ENSG00000158748 ENSMUSG00000028747
Uniprot P50406 Q14AW8
Refseq NM_000871 (mRNA)
NP_000862 (protein)		 NM_021358 (mRNA)
NP_067333 (protein)
Location Chr 1: 19.86 - 19.88 Mb Chr 4: 138.33 - 138.35 Mb
Pubmed search [1] [2]

The 5-HT6 receptor, also known as the 5-hydroxytryptamine (serotonin) receptor 6 (HTR6), is a human gene.[1][2] The 5-HT6 receptor is primarily expressed in the brain and is involved in glutamatergic and cholinergic neuronal activity.[3] It is a potential target for drugs treating cognitive diseases, schizophrenia, anxiety and obesity.[4]

Contents

Ligands

Full agonists

Agonists for the 5-HT6 receptor include:

  • 2-ethyl-5-methoxy-N,N-dimethyltryptamine (EMDT)[5]
  • arylsulfonyl-tryptamines[6]
  • arylsulfonyl-heterocycles.[7]
  • EMD-386,088 (5-Chloro-2-methyl-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H -indole) - potent and selective 5HT6 agonist (EC50 1nM)[8]
  • WAY-181,187
  • WAY-208,466

Antagonists

  • SB-258,585 (4-Iodo-N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]benzenesulfonamide)
  • SB-399,885

Genetics

The receptor is coded by the HTR6 gene. As the protein is a neuroreceptor it is possible that genetic variations in the gene would have an effect on brain, and research studies have investigated whether polymorphisms is associated with brain-related variables, such as neuropsychiatric disorders. For example, in 2004 one Chinese study reported an association between the C267T (rs1805054) polymorphism and Alzheimer's disease.[9] Others have studied the polymorphism in relation to Parkinson's disease.[10]

See also

References

  1. ^ "Entrez Gene: HTR6 5-hydroxytryptamine (serotonin) receptor 6".
  2. ^ Kohen R, Metcalf MA, Khan N, Druck T, Huebner K, Lachowicz JE, Meltzer HY, Sibley DR, Roth BL, Hamblin MW (1996). "Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor". J. Neurochem. 66 (1): 47–56. doi:10.1046/j.1471-4159.1996.66010047.x. PMID 8522988. 
  3. ^ Woolley ML, Marsden CA, Fone KC (2004). "5-HT6 receptors". Curr Drug Targets CNS Neurol Disord 3 (1): 59–79. PMID 14965245. 
  4. ^ Holenz J, Pauwels PJ, Díaz JL, Mercè R, Codony X, Buschmann H (2006). "Medicinal chemistry strategies to 5-HT6 receptor ligands as potential cognitive enhancers and antiobesity agents". Drug Discov. Today 11 (7-8): 283–99. doi:10.1016/j.drudis.2006.02.004. PMID 16580970. 
  5. ^ 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-HT6 serotonin receptors". J. Med. Chem. 43 (5): 1011–8. doi:10.1021/jm990550b. PMID 10715164. 
  6. ^ Cole DC, Stock JR, Lennox WJ, Bernotas RC, Ellingboe JW, Boikess S, Coupet J, Smith DL, Leung L, Zhang GM, Feng X, Kelly MF, Galante R, Huang P, Dawson LA, Marquis K, Rosenzweig-Lipson S, Beyer CE, Schechter LE (2007). "Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT6 receptor agonist". J. Med. Chem. 50 (23): 5535–8. doi:10.1021/jm070521y. PMID 17948978. 
  7. ^ Elokdah H, Li D, McFarlane G, Bernotas RC, Robichaud AJ, Magolda RL, Zhang GM, Smith D, Schechter LE (2007). "Novel 1-(azacyclyl)-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines as 5-HT6 agonists and antagonists". Bioorg. Med. Chem. 15 (18): 6208–26. doi:10.1016/j.bmc.2007.06.024. PMID 17624788. 
  8. ^ Mattsson C, Sonesson C, Sandahl A, Greiner HE, Gassen M, Plaschke J, Leibrock J, Böttcher H (October 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. doi:10.1016/j.bmcl.2005.06.067. PMID 16055331. 
  9. ^ Kan R, Wang B, Zhang C, Yang Z, Ji S, Lu Z, Zheng C, Jin F, Wang L (November 2004). "Association of the HTR6 polymorphism C267T with late-onset Alzheimer's disease in Chinese". Neurosci. Lett. 372 (1-2): 27–9. doi:10.1016/j.neulet.2004.09.007. PMID 15531082. 
  10. ^ Messina D, Annesi G, Serra P, Nicoletti G, Pasqua A, Annesi F, Tomaino C, Cirò-Candiano IC, Carrideo S, Caracciolo M, Spadafora P, Zappia M, Savettieri G, Quattrone A (March 2002). "Association of the 5-HT6 receptor gene polymorphism C267T with Parkinson's disease". Neurology 58 (5): 828–9. PMID 11889255. 

Further reading

  • 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. 
  • Raymond JR, Mukhin YV, Gelasco A, et al. (2002). "Multiplicity of mechanisms of serotonin receptor signal transduction.". Pharmacol. Ther. 92 (2-3): 179–212. PMID 11916537. 
  • Van Oekelen D, Luyten WH, Leysen JE (2003). "5-HT2A and 5-HT2C receptors and their atypical regulation properties.". Life Sci. 72 (22): 2429–49. PMID 12650852. 
  • Dubertret C, Hanoun N, Adès J, et al. (2004). "Family-based association study of the serotonin-6 receptor gene (C267T polymorphism) in schizophrenia.". Am. J. Med. Genet. B Neuropsychiatr. Genet. 126 (1): 10–5. doi:10.1002/ajmg.b.20120. PMID 15048641. 
  • Ullmer C, Schmuck K, Kalkman HO, Lübbert H (1995). "Expression of serotonin receptor mRNAs in blood vessels.". FEBS Lett. 370 (3): 215–21. PMID 7656980. 
  • Kohen R, Metcalf MA, Khan N, et al. (1996). "Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.". J. Neurochem. 66 (1): 47–56. PMID 8522988. 
  • Orlacchio A, Kawarai T, Paciotti E, et al. (2002). "Association study of the 5-hydroxytryptamine(6) receptor gene in Alzheimer's disease.". Neurosci. Lett. 325 (1): 13–6. PMID 12023056. 
  • 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. PMID 12477932. 
  • Ham BJ, Kim YH, Choi MJ, et al. (2004). "Serotonergic genes and personality traits in the Korean population.". Neurosci. Lett. 354 (1): 2–5. PMID 14698468. 
  • Bernotas R, Lenicek S, Antane S, et al. (2005). "1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-indoles as novel 5-HT6 receptor ligands.". Bioorg. Med. Chem. Lett. 14 (22): 5499–502. doi:10.1016/j.bmcl.2004.09.003. PMID 15482912. 
  • Gerhard DS, Wagner L, Feingold EA, et al. (2004). "The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).". Genome Res. 14 (10B): 2121–7. doi:10.1101/gr.2596504. PMID 15489334. 
  • Kang H, Lee WK, Choi YH, et al. (2005). "Molecular analysis of the interaction between the intracellular loops of the human serotonin receptor type 6 (5-HT6) and the alpha subunit of GS protein.". Biochem. Biophys. Res. Commun. 329 (2): 684–92. doi:10.1016/j.bbrc.2005.02.040. PMID 15737640. 
  • Tao WA, Wollscheid B, O'Brien R, et al. (2005). "Quantitative phosphoproteome analysis using a dendrimer conjugation chemistry and tandem mass spectrometry.". Nat. Methods 2 (8): 591–8. doi:10.1038/nmeth776. PMID 16094384. 
  • Lorke DE, Lu G, Cho E, Yew DT (2006). "Serotonin 5-HT2A and 5-HT6 receptors in the prefrontal cortex of Alzheimer and normal aging patients.". BMC neuroscience 7: 36. doi:10.1186/1471-2202-7-36. PMID 16640790. 
  • Yun HM, Kim S, Kim HJ, et al. (2007). "The novel cellular mechanism of human 5-HT6 receptor through an interaction with Fyn.". J. Biol. Chem. 282 (8): 5496–505. doi:10.1074/jbc.M606215200. PMID 17189269. 

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This article incorporates text from the United States National Library of Medicine, which is in the public domain.

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v • d • e
Transmembrane receptor: G protein-coupled receptors
Class A: Rhodopsin like
α1 (A, B, D), α2 (A, B, C), β1, β2, β3
CysLT (1, 2), LTB4 (1, 2), FPRL1, OXE, Prostaglandin (DP, EP (1, 2, 3, 4), PGF), Prostacyclin, Thromboxane
B/W (1, 2), FF (1, 2), S, Y (1, 2, 4, 5)
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, 79, 82, 83, 84, 85, 87, 88, 92, 101, 103, 119, 120, 132, 135, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 172, 173, 174, 176, 177, 182)
Adenosine (A1, A2a, A2b, A3), P2Y, (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
(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) - Adrenomedullin - Anaphylatoxin (C3a, C5a) - Angiotensin (1, 2) - Apelin - Bile acid - Bombesin (BRS3, GRPR, NMBR) - Bradykinin (B1, B2) - Cannabinoid (CB1, CB2) - Chemokine - Cholecystokinin (A, B) - Dopamine (D1, D2, D3, D4, D5) - EBI2 - Endothelin (A, B) - Estrogen - Formyl peptide (1, L1, L2) - Free fatty acid (1, 2, 3, 4) - FSH - Galanin (1, 2, 3) - Gonadotropin-releasing hormone (1, 2) - Ghrelin - Histamine (H1, H2, H3, H4) - Kisspeptin - Luteinizing hormone/choriogonadotropin - Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) - MAS (1, 1L, D, E, F, G, X1, X2, X3, X4) - Melanocortin (1, 2, 3, 4, 5) - MCHR (1, 2) - Melatonin (1A, 1B)- Motilin - neuromedin (B, U (1, 2)) - Neurotensin (1, 2) - Opioid (Delta, Kappa, Mu, Nociceptin, but not Sigma) - Olfactory - Opsin (3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) - Orexin (1, 2) - Oxytocin - Oxoglutarate - PAF - Prokineticin (1, 2) - Prolactin-releasing peptide - Protease-activated (1, 2, 3, 4) - Relaxin (1, 2, 3, 4) - Somatostatin (1, 2, 3, 4, 5) - SREB - Succinate - TAAR (1, 2, 3, 5, 6, 8, 9) - Tachykinin (1, 2, 3) - Thyrotropin - Thyrotropin-releasing hormone - Urotensin-II - Vasopressin (1A, 1B, 2)
Class B: Secretin like
Class C: Metabotropic
glutamate / pheromone
Calcium-sensing receptor - GABA B (1, 2) - Glutamate receptor (Metabotropic glutamate (1, 2, 3, 4, 5, 6, 7, 8)) - GPRC6A - GPR (156, 158, 179) - RAIG (1, 2, 3, 4) - Taste receptors (TAS1R (1, 2, 3) TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50))
Frizzled / Smoothened
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) - Smoothened

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