5-HT7 receptor

5-hydroxytryptamine (serotonin) receptor 7 (adenylate cyclase-coupled), also known as HTR7, is a human gene.cite web | title = Entrez Gene: HTR7 5-hydroxytryptamine (serotonin) receptor 7 (adenylate cyclase-coupled)| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=3363| accessdate = ]

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.cite web | title = Entrez Gene: HTR7 5-hydroxytryptamine (serotonin) receptor 7 (adenylate cyclase-coupled)| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=3363| accessdate = ]

Ligands

Numerous ligands bind to the 5-HT₇ receptor:cite journal |author=Pittalà V, Salerno L, Modica M, Siracusa MA, Romeo G |title=5-HT7 receptor ligands: recent developments and potential therapeutic applications |journal=Mini Rev Med Chem |volume=7 |issue=9 |pages=945–60 |year=2007 |pmid=17897083 |doi= |url=http://www.bentham-direct.org/pages/content.php?MRMC/2007/00000007/00000009/0006N.SGM] cite journal |author=Leopoldo M |title=Serotonin(7) receptors (5-HT(7)Rs) and their ligands |journal=Curr. Med. Chem. |volume=11 |issue=5 |pages=629–61 |year=2004 |pmid=15032609 |doi= |url=http://www.bentham-direct.org/pages/content.php?CMC/2004/00000011/00000005/0010C.SGM]
* "N"-(1,2,3,4-Tetrahydronaphthalen-1-yl)-4-aryl- 1-piperazinehexanamidescite journal | author = Leopoldo M, Lacivita E, Contino M, Colabufo NA, Berardi F, Perrone R | title = 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 | journal = J. Med. Chem. | volume = 50 | issue = 17 | pages = 4214–21 | year = 2007 | pmid = 17649988 | doi = 10.1021/jm070487n | issn = ] cite journal |author=Leopoldo M, Berardi F, Colabufo NA, "et al" |title=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 |journal=J. Med. Chem. |volume=47 |issue=26 |pages=6616–24 |year=2004 |pmid=15588097 |doi=10.1021/jm049702f |url=] (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-HT_1A / 5-HT₇ agonist)cite journal | author = Sprouse J, Reynolds L, Li X, Braselton J, Schmidt A | title = 8-OH-DPAT as a 5-HT₇ agonist: phase shifts of the circadian biological clock through increases in cAMP production | journal = Neuropharmacology | volume = 46 | issue = 1 | pages = 52–62 | year = 2004 | pmid = 14654097 | doi = 10.1016/j.neuropharm.2003.08.007 | issn = ]

Antagonists

*SB-656,104-Acite journal |author=Forbes IT, Douglas S, Gribble AD, "et al" |title=SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties |journal=Bioorg. Med. Chem. Lett. |volume=12 |issue=22 |pages=3341–4 |year=2002 |month=November |pmid=12392747 |doi= |url=http://linkinghub.elsevier.com/retrieve/pii/S0960894X0200690X]
*3-{4- [4-(4-chlorophenyl)-piperazin-1-yl] -butyl}-3-ethyl-6-fluoro- 1,3-dihydro-2 H-indol-2-onecite journal |author=Volk B, Barkóczy J, Hegedus E, "et al" |title=(Phenylpiperazinyl-butyl)oxindoles as selective 5-HT7 receptor antagonists |journal=J. Med. Chem. |volume=51 |issue=8 |pages=2522–32 |year=2008 |month=April |pmid=18361484 |doi=10.1021/jm070279v |url=]

Inverse Agonists

*SB-269,970: quasi-full inverse agonistcite journal |author=Mahé C, Loetscher E, Feuerbach D, Müller W, Seiler MP, Schoeffter P |title=Differential inverse agonist efficacies of SB-258719, SB-258741 and SB-269970 at human recombinant serotonin 5-HT7 receptors |journal=Eur. J. Pharmacol. |volume=495 |issue=2-3 |pages=97–102 |year=2004 |pmid=15249157 |doi=10.1016/j.ejphar.2004.05.033 |url=] cite journal |author=Lovell PJ, Bromidge SM, Dabbs S, "et al" |title=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) |journal=J. Med. Chem. |volume=43 |issue=3 |pages=342–5 |year=2000 |pmid=10669560 |doi= |url=]
*SB-691,673: full inverse agonistcite journal |author=Romero G, Pujol M, Pauwels PJ |title=Reanalysis of constitutively active rat and human 5-HT7(a) receptors in HEK-293F cells demonstrates lack of silent properties for reported neutral antagonists |journal=Naunyn Schmiedebergs Arch. Pharmacol. |volume=374 |issue=1 |pages=31–9 |year=2006 |pmid=16967291 |doi=10.1007/s00210-006-0093-y |url=]
* SB-258,741: partial inverse agonistcite journal |author=Mahé C, Loetscher E, Feuerbach D, Müller W, Seiler MP, Schoeffter P |title=Differential inverse agonist efficacies of SB-258719, SB-258741 and SB-269970 at human recombinant serotonin 5-HT7 receptors |journal=Eur. J. Pharmacol. |volume=495 |issue=2-3 |pages=97–102 |year=2004 |pmid=15249157 |doi=10.1016/j.ejphar.2004.05.033 |url=]
*SB-258,719: partial inverse agonistcite journal |author=Forbes IT, Dabbs S, Duckworth DM, "et al" |title=(R)-3,N-dimethyl-N- [1-methyl-3-(4-methyl-piperidin-1-yl) propyl] benzenesulfonamide: the first selective 5-HT7 receptor antagonist |journal=J. Med. Chem. |volume=41 |issue=5 |pages=655–7 |year=1998 |month=February |pmid=9513592 |doi=10.1021/jm970519e |url=] or silent antagonist?

ee also

* 5-HT receptor

References

Further reading

PBB_Further_reading
citations =
*cite journal | author=Hoyer D, Hannon JP, Martin GR |title=Molecular, pharmacological and functional diversity of 5-HT receptors. |journal=Pharmacol. Biochem. Behav. |volume=71 |issue= 4 |pages= 533–54 |year= 2002 |pmid= 11888546 |doi=
*cite journal | author=Raymond JR, Mukhin YV, Gelasco A, "et al." |title=Multiplicity of mechanisms of serotonin receptor signal transduction. |journal=Pharmacol. Ther. |volume=92 |issue= 2-3 |pages= 179–212 |year= 2002 |pmid= 11916537 |doi=
*cite journal | author=Gelernter J, Rao PA, Pauls DL, "et al." |title=Assignment of the 5HT7 receptor gene (HTR7) to chromosome 10q and exclusion of genetic linkage with Tourette syndrome. |journal=Genomics |volume=26 |issue= 2 |pages= 207–9 |year= 1995 |pmid= 7601444 |doi=
*cite journal | author=Ullmer C, Schmuck K, Kalkman HO, Lübbert H |title=Expression of serotonin receptor mRNAs in blood vessels. |journal=FEBS Lett. |volume=370 |issue= 3 |pages= 215–21 |year= 1995 |pmid= 7656980 |doi=
*cite journal | author=Bard JA, Zgombick J, Adham N, "et al." |title=Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase. |journal=J. Biol. Chem. |volume=268 |issue= 31 |pages= 23422–6 |year= 1993 |pmid= 8226867 |doi=
*cite journal | author=Lovenberg TW, Baron BM, de Lecea L, "et al." |title=A novel adenylyl cyclase-activating serotonin receptor (5-HT7) implicated in the regulation of mammalian circadian rhythms. |journal=Neuron |volume=11 |issue= 3 |pages= 449–58 |year= 1993 |pmid= 8398139 |doi=
*cite journal | author=Heidmann DE, Metcalf MA, Kohen R, Hamblin MW |title=Four 5-hydroxytryptamine7 (5-HT7) receptor isoforms in human and rat produced by alternative splicing: species differences due to altered intron-exon organization. |journal=J. Neurochem. |volume=68 |issue= 4 |pages= 1372–81 |year= 1997 |pmid= 9084407 |doi=
*cite journal | author=Erdmann J, Nöthen MM, Shimron-Abarbanell D, "et al." |title=The human serotonin 7 (5-HT7) receptor gene: genomic organization and systematic mutation screening in schizophrenia and bipolar affective disorder. |journal=Mol. Psychiatry |volume=1 |issue= 5 |pages= 392–7 |year= 1997 |pmid= 9154233 |doi=
*cite journal | author=Jasper JR, Kosaka A, To ZP, "et al." |title=Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b). |journal=Br. J. Pharmacol. |volume=122 |issue= 1 |pages= 126–32 |year= 1997 |pmid= 9298538 |doi= 10.1038/sj.bjp.0701336
*cite journal | author=Lassig JP, Vachirasomtoon K, Hartzell K, "et al." |title=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. |journal=Am. J. Med. Genet. |volume=88 |issue= 5 |pages= 472–5 |year= 1999 |pmid= 10490701 |doi=
*cite journal | author=Krobert KA, Levy FO |title=The human 5-HT7 serotonin receptor splice variants: constitutive activity and inverse agonist effects. |journal=Br. J. Pharmacol. |volume=135 |issue= 6 |pages= 1563–71 |year= 2002 |pmid= 11906971 |doi= 10.1038/sj.bjp.0704588
*cite journal | author=Norum JH, Hart K, Levy FO |title=Ras-dependent ERK activation by the human G(s)-coupled serotonin receptors 5-HT4(b) and 5-HT7(a). |journal=J. Biol. Chem. |volume=278 |issue= 5 |pages= 3098–104 |year= 2003 |pmid= 12446729 |doi= 10.1074/jbc.M206237200
*cite journal | author=Strausberg RL, Feingold EA, Grouse LH, "et al." |title=Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences. |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=99 |issue= 26 |pages= 16899–903 |year= 2003 |pmid= 12477932 |doi= 10.1073/pnas.242603899
*cite journal | author=Slominski A, Pisarchik A, Zbytek B, "et al." |title=Functional activity of serotoninergic and melatoninergic systems expressed in the skin. |journal=J. Cell. Physiol. |volume=196 |issue= 1 |pages= 144–53 |year= 2003 |pmid= 12767050 |doi= 10.1002/jcp.10287
*cite journal | author=Simonin F, Karcher P, Boeuf JJ, "et al." |title=Identification of a novel family of G protein-coupled receptor associated sorting proteins. |journal=J. Neurochem. |volume=89 |issue= 3 |pages= 766–75 |year= 2004 |pmid= 15086532 |doi= 10.1111/j.1471-4159.2004.02411.x
*cite journal | author=Gerhard DS, Wagner L, Feingold EA, "et al." |title=The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). |journal=Genome Res. |volume=14 |issue= 10B |pages= 2121–7 |year= 2004 |pmid= 15489334 |doi= 10.1101/gr.2596504
*cite journal | author=Brüss M, Kiel S, Bönisch H, "et al." |title=Decreased agonist, but not antagonist, binding to the naturally occurring Thr92Lys variant of the h5-HT7(a) receptor. |journal=Neurochem. Int. |volume=47 |issue= 3 |pages= 196–203 |year= 2005 |pmid= 15896881 |doi= 10.1016/j.neuint.2005.03.003
*cite journal | author=Ikeda M, Iwata N, Kitajima T, "et al." |title=Positive association of the serotonin 5-HT7 receptor gene with schizophrenia in a Japanese population. |journal=Neuropsychopharmacology |volume=31 |issue= 4 |pages= 866–71 |year= 2006 |pmid= 16192982 |doi= 10.1038/sj.npp.1300901

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