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==References==
==References==
{{reflist}}
{{reflist}}

==External link==
* {{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2337 | title = 5-HT<sub>7</sub> | accessdate = | author = | authorlink = | coauthors = | date = | format = | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | pages = | language = | archiveurl = | archivedate = | quote = }}


==Further reading==
==Further reading==

Revision as of 11:15, 25 November 2008

The correct title of this article is 5-HT7 receptor. It appears incorrectly here due to technical restrictions.

Template:PBB 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]

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 - 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-naphthalenyl)-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]
  • EGIS-12233 - mixed 5-HT6 / 5-HT7 antagonist

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.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  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.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  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. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)
  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.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  7. ^ Forbes IT, Douglas S, Gribble AD; 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. {{cite journal}}: Explicit use of et al. in: |author= (help); Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  8. ^ Volk B, Barkóczy J, Hegedus E; et al. (2008). "(Phenylpiperazinyl-butyl)oxindoles as selective 5-HT7 receptor antagonists". J. Med. Chem. 51 (8): 2522–32. doi:10.1021/jm070279v. PMID 18361484. {{cite journal}}: Explicit use of et al. in: |author= (help); Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  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.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  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. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)
  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.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  12. ^ Forbes IT, Dabbs S, Duckworth DM; et al. (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. {{cite journal}}: Explicit use of et al. in: |author= (help); Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  • "5-HT7". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. {{cite web}}: Cite has empty unknown parameter: |coauthors= (help)

Further reading

Template:PBB Further reading

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

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