5-HT7

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The correct title of this article is 5-HT7 receptor. It appears incorrectly here because of technical restrictions.
 Please help improve this article or section by expanding it. Further information might be found on the talk page or at requests for expansion. (May 2008)
5-hydroxytryptamine (serotonin) receptor 7 (adenylate cyclase-coupled)
Identifiers
Symbols HTR7; 5-HT7
External IDs OMIM: 182137 MGI: 99841 HomoloGene: 20244
RNA expression pattern

More reference expression data
Orthologs
Human Mouse
Entrez 3363 15566
Ensembl ENSG00000148680 ENSMUSG00000024798
Uniprot P34969 Q14A50
Refseq NM_000872 (mRNA)
NP_000863 (protein)		 NM_008315 (mRNA)
NP_032341 (protein)
Location Chr 10: 92.49 - 92.61 Mb Chr 19: 36.03 - 36.12 Mb
Pubmed search [1] [2]

5-hydroxytryptamine (serotonin) receptor 7 (adenylate cyclase-coupled), also known as HTR7, is a human gene.[1]

The neurotransmitter, serotonin, is thought to play a role in various cognitive and behavioral functions. The serotonin receptor encoded by this gene belongs to the superfamily of G protein-coupled receptors and the gene is a candidate locus for involvement in autistic disorder and other neuropsychiatric disorders. Three splice variants have been identified which encode proteins that differ in the length of their carboxy terminal ends.[1]

Contents

Ligands

Numerous ligands bind to the 5-HT7 receptor:[2][3]

  • N-(1,2,3,4-Tetrahydronaphthalen-1-yl)-4-aryl- 1-piperazinehexanamides[4][5] (can be either agonists or antagonists depending on side chain substitution)

Agonists

  • AS-19 ((2S)-(+)-5-(1,3,5-Trimethylpyrazol-4-yl)-2-(dimethylamino)tetralin) - potent agonist, IC50 0.83nM
  • LP-12 (4-(2-Diphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1- piperazinehexanamide)
  • LP-44 (4-[2-(Methylthio)phenyl]-N-(1,2,3,4-tetrahydro-1-naphth alenyl)-1-piperazinehexanamide)
  • 8-OH-DPAT (mixed 5-HT1A / 5-HT7 agonist)[6]

Antagonists

  • SB-656,104-A[7]
  • 3-{4-[4-(4-chlorophenyl)-piperazin-1-yl]-butyl}-3-ethyl-6-fluoro- 1,3-dihydro-2 H-indol-2-one[8]

Inverse Agonists

  • SB-269,970: quasi-full inverse agonist[9][10]
  • SB-691,673: full inverse agonist[11]
  • SB-258,741: partial inverse agonist[9]
  • SB-258,719: partial inverse agonist[11][12] or silent antagonist?[9]

See also

References

  1. ^ a b "Entrez Gene: HTR7 5-hydroxytryptamine (serotonin) receptor 7 (adenylate cyclase-coupled)".
  2. ^ Pittalà V, Salerno L, Modica M, Siracusa MA, Romeo G (2007). "5-HT7 receptor ligands: recent developments and potential therapeutic applications". Mini Rev Med Chem 7 (9): 945–60. PMID 17897083. 
  3. ^ Leopoldo M (2004). "Serotonin(7) receptors (5-HT(7)Rs) and their ligands". Curr. Med. Chem. 11 (5): 629–61. PMID 15032609. 
  4. ^ 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. doi:10.1021/jm070487n. PMID 17649988. 
  5. ^ Leopoldo M, Berardi F, Colabufo NA, et al (2004). "Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents". J. Med. Chem. 47 (26): 6616–24. doi:10.1021/jm049702f. PMID 15588097. 
  6. ^ Sprouse J, Reynolds L, Li X, Braselton J, Schmidt A (2004). "8-OH-DPAT as a 5-HT7 agonist: phase shifts of the circadian biological clock through increases in cAMP production". Neuropharmacology 46 (1): 52–62. doi:10.1016/j.neuropharm.2003.08.007. PMID 14654097. 
  7. ^ Forbes IT, Douglas S, Gribble AD, et al (November 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. 
  8. ^ Volk B, Barkóczy J, Hegedus E, et al (April 2008). "(Phenylpiperazinyl-butyl)oxindoles as selective 5-HT7 receptor antagonists". J. Med. Chem. 51 (8): 2522–32. doi:10.1021/jm070279v. PMID 18361484. 
  9. ^ a b c Mahé C, Loetscher E, Feuerbach D, Müller W, Seiler MP, Schoeffter P (2004). "Differential inverse agonist efficacies of SB-258719, SB-258741 and SB-269970 at human recombinant serotonin 5-HT7 receptors". Eur. J. Pharmacol. 495 (2-3): 97–102. doi:10.1016/j.ejphar.2004.05.033. PMID 15249157. 
  10. ^ Lovell PJ, Bromidge SM, Dabbs S, et al (2000). "A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB-269970)". J. Med. Chem. 43 (3): 342–5. PMID 10669560. 
  11. ^ a b Romero G, Pujol M, Pauwels PJ (2006). "Reanalysis of constitutively active rat and human 5-HT7(a) receptors in HEK-293F cells demonstrates lack of silent properties for reported neutral antagonists". Naunyn Schmiedebergs Arch. Pharmacol. 374 (1): 31–9. doi:10.1007/s00210-006-0093-y. PMID 16967291. 
  12. ^ Forbes IT, Dabbs S, Duckworth DM, et al (February 1998). "(R)-3,N-dimethyl-N-[1-methyl-3-(4-methyl-piperidin-1-yl) propyl]benzenesulfonamide: the first selective 5-HT7 receptor antagonist". J. Med. Chem. 41 (5): 655–7. doi:10.1021/jm970519e. PMID 9513592. 

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. 
  • Gelernter J, Rao PA, Pauls DL, et al. (1995). "Assignment of the 5HT7 receptor gene (HTR7) to chromosome 10q and exclusion of genetic linkage with Tourette syndrome.". Genomics 26 (2): 207–9. PMID 7601444. 
  • 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. 
  • Bard JA, Zgombick J, Adham N, et al. (1993). "Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.". J. Biol. Chem. 268 (31): 23422–6. PMID 8226867. 
  • Lovenberg TW, Baron BM, de Lecea L, et al. (1993). "A novel adenylyl cyclase-activating serotonin receptor (5-HT7) implicated in the regulation of mammalian circadian rhythms.". Neuron 11 (3): 449–58. PMID 8398139. 
  • Heidmann DE, Metcalf MA, Kohen R, Hamblin MW (1997). "Four 5-hydroxytryptamine7 (5-HT7) receptor isoforms in human and rat produced by alternative splicing: species differences due to altered intron-exon organization.". J. Neurochem. 68 (4): 1372–81. PMID 9084407. 
  • Erdmann J, Nöthen MM, Shimron-Abarbanell D, et al. (1997). "The human serotonin 7 (5-HT7) receptor gene: genomic organization and systematic mutation screening in schizophrenia and bipolar affective disorder.". Mol. Psychiatry 1 (5): 392–7. PMID 9154233. 
  • Jasper JR, Kosaka A, To ZP, et al. (1997). "Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).". Br. J. Pharmacol. 122 (1): 126–32. doi:10.1038/sj.bjp.0701336. PMID 9298538. 
  • Lassig JP, Vachirasomtoon K, Hartzell K, et al. (1999). "Physical mapping of the serotonin 5-HT(7) receptor gene (HTR7) to chromosome 10 and pseudogene (HTR7P) to chromosome 12, and testing of linkage disequilibrium between HTR7 and autistic disorder.". Am. J. Med. Genet. 88 (5): 472–5. PMID 10490701. 
  • Krobert KA, Levy FO (2002). "The human 5-HT7 serotonin receptor splice variants: constitutive activity and inverse agonist effects.". Br. J. Pharmacol. 135 (6): 1563–71. doi:10.1038/sj.bjp.0704588. PMID 11906971. 
  • 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. PMID 12477932. 
  • Slominski A, Pisarchik A, Zbytek B, et al. (2003). "Functional activity of serotoninergic and melatoninergic systems expressed in the skin.". J. Cell. Physiol. 196 (1): 144–53. doi:10.1002/jcp.10287. PMID 12767050. 
  • Simonin F, Karcher P, Boeuf JJ, et al. (2004). "Identification of a novel family of G protein-coupled receptor associated sorting proteins.". J. Neurochem. 89 (3): 766–75. doi:10.1111/j.1471-4159.2004.02411.x. PMID 15086532. 
  • 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. 
  • Brüss M, Kiel S, Bönisch H, et al. (2005). "Decreased agonist, but not antagonist, binding to the naturally occurring Thr92Lys variant of the h5-HT7(a) receptor.". Neurochem. Int. 47 (3): 196–203. doi:10.1016/j.neuint.2005.03.003. PMID 15896881. 
  • Ikeda M, Iwata N, Kitajima T, et al. (2006). "Positive association of the serotonin 5-HT7 receptor gene with schizophrenia in a Japanese population.". Neuropsychopharmacology 31 (4): 866–71. doi:10.1038/sj.npp.1300901. PMID 16192982. 

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

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
GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 157)
Other
Class C: Metabotropic
glutamate / pheromone
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)
Other
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)
Frizzled / Smoothened
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) • Smoothened

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