5-hydroxytryptamine receptor 3A

Details

Name
5-hydroxytryptamine receptor 3A
Synonyms
  • 5-HT-3
  • 5-HT3-A
  • 5-HT3R
  • 5-hydroxytryptamine receptor 3
  • 5HT3R
  • HTR3
  • Serotonin receptor 3A
  • Serotonin-gated ion channel receptor
Gene Name
HTR3A
Organism
Humans
Amino acid sequence
>lcl|BSEQ0000619|5-hydroxytryptamine receptor 3A
MLLWVQQALLALLLPTLLAQGEARRSRNTTRPALLRLSDYLLTNYRKGVRPVRDWRKPTT
VSIDVIVYAILNVDEKNQVLTTYIWYRQYWTDEFLQWNPEDFDNITKLSIPTDSIWVPDI
LINEFVDVGKSPNIPYVYIRHQGEVQNYKPLQVVTACSLDIYNFPFDVQNCSLTFTSWLH
TIQDINISLWRLPEKVKSDRSVFMNQGEWELLGVLPYFREFSMESSNYYAEMKFYVVIRR
RPLFYVVSLLLPSIFLMVMDIVGFYLPPNSGERVSFKITLLLGYSVFLIIVSDTLPATAI
GTPLIGVYFVVCMALLVISLAETIFIVRLVHKQDLQQPVPAWLRHLVLERIAWLLCLREQ
STSQRPPATSQATKTDDCSAMGNHCSHMGGPQDFEKSPRDRCSPPPPPREASLAVCGLLQ
ELSSIRQFLEKRDEIREVARDWLRVGSVLDKLLFHIYLLAVLAYSITLVMLWSIWQYA
Number of residues
478
Molecular Weight
55279.835
Theoretical pI
7.43
GO Classification
Functions
receptor activity / serotonin binding / serotonin receptor activity / serotonin-activated cation-selective channel activity / voltage-gated potassium channel activity
Processes
cation transmembrane transport / cellular response to growth factor stimulus / digestion / ion transmembrane transport / neurological system process / regulation of membrane potential / response to cocaine / response to ethanol / serotonin receptor signaling pathway / synaptic transmission / transmembrane transport / transport
Components
axon / cell junction / cytoplasm / integral component of plasma membrane / neuron projection / neuronal cell body / plasma membrane / postsynaptic membrane / synapse
General Function
Voltage-gated potassium channel activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses in neurons. It is a cation-specific, but otherwise relatively nonselective, ion channel.
Pfam Domain Function
Transmembrane Regions
242-268 274-292 303-321 456-475
Cellular Location
Cell junction
Gene sequence
>lcl|BSEQ0010242|5-hydroxytryptamine receptor 3A (HTR3A)
ATGCTTGGAAAGCTCGCTATGCTGCTGTGGGTCCAGCAGGCGCTGCTCGCCTTGCTCCTC
CCCACACTCCTGGCACAGGGAGAAGCCAGGAGGAGCCGAAACACCACCAGGCCCGCTCTG
CTGAGGCTGTCGGATTACCTTTTGACCAACTACAGGAAGGGTGTGCGCCCCGTGAGGGAC
TGGAGGAAGCCAACCACCGTATCCATTGACGTCATTGTCTATGCCATCCTCAACGTGGAT
GAGAAGAATCAGGTGCTGACCACCTACATCTGGTACCGGCAGTACTGGACTGATGAGTTT
CTCCAGTGGAACCCTGAGGACTTTGACAACATCACCAAGTTGTCCATCCCCACGGACAGC
ATCTGGGTCCCGGACATTCTCATCAATGAGTTCGTGGATGTGGGGAAGTCTCCAAATATC
CCGTACGTGTATATTCGGCATCAAGGCGAAGTTCAGAACTACAAGCCCCTTCAGGTGGTG
ACTGCCTGTAGCCTCGACATCTACAACTTCCCCTTCGATGTCCAGAACTGCTCGCTGACC
TTCACCAGTTGGCTGCACACCATCCAGGACATCAACATCTCTTTGTGGCGCTTGCCAGAA
AAGGTGAAATCCGACAGGAGTGTCTTCATGAACCAGGGAGAGTGGGAGTTGCTGGGGGTG
CTGCCCTACTTTCGGGAGTTCAGCATGGAAAGCAGTAACTACTATGCAGAAATGAAGTTC
TATGTGGTCATCCGCCGGCGGCCCCTCTTCTATGTGGTCAGCCTGCTACTGCCCAGCATC
TTCCTCATGGTCATGGACATCGTGGGCTTCTACCTGCCCCCCAACAGTGGCGAGAGGGTC
TCTTTCAAGATTACACTCCTCCTGGGCTACTCGGTCTTCCTGATCATCGTTTCTGACACG
CTGCCGGCCACTGCCATCGGCACTCCTCTCATTGGTGTCTACTTTGTGGTGTGCATGGCT
CTGCTGGTGATAAGTTTGGCCGAGACCATCTTCATTGTGCGGCTGGTGCACAAGCAAGAC
CTGCAGCAGCCCGTGCCTGCTTGGCTGCGTCACCTGGTTCTGGAGAGAATCGCCTGGCTA
CTTTGCCTGAGGGAGCAGTCAACTTCCCAGAGGCCCCCAGCCACCTCCCAAGCCACCAAG
ACTGATGACTGCTCAGCCATGGGAAACCACTGCAGCCACATGGGAGGACCCCAGGACTTC
GAGAAGAGCCCGAGGGACAGATGTAGCCCTCCCCCACCACCTCGGGAGGCCTCGCTGGCG
GTGTGTGGGCTGCTGCAGGAGCTGTCCTCCATCCGGCAATTCCTGGAAAAGCGGGATGAG
ATCCGAGAGGTGGCCCGAGACTGGCTGCGCGTGGGCTCCGTGCTGGACAAGCTGCTATTC
CACATTTACCTGCTAGCGGTGCTGGCCTACAGCATCACCCTGGTTATGCTCTGGTCCATC
TGGCAGTACGCTTGA
Chromosome Location
11
Locus
11q23.1
External Identifiers
ResourceLink
UniProtKB IDP46098
UniProtKB Entry Name5HT3A_HUMAN
GenBank Protein ID681914
GenBank Gene IDD49394
GenAtlas IDHTR3A
HGNC IDHGNC:5297
General References
  1. Miyake A, Mochizuki S, Takemoto Y, Akuzawa S: Molecular cloning of human 5-hydroxytryptamine3 receptor: heterogeneity in distribution and function among species. Mol Pharmacol. 1995 Sep;48(3):407-16. [PubMed:7565620]
  2. Belelli D, Balcarek JM, Hope AG, Peters JA, Lambert JJ, Blackburn TP: Cloning and functional expression of a human 5-hydroxytryptamine type 3AS receptor subunit. Mol Pharmacol. 1995 Dec;48(6):1054-62. [PubMed:8848005]
  3. Bruss M, Gothert M, Hayer M, Bonisch H: Molecular cloning of alternatively spliced human 5-HT3 receptor cDNAs. Ann N Y Acad Sci. 1998 Dec 15;861:234-5. [PubMed:9928262]
  4. Bruss M, Eucker T, Gothert M, Bonisch H: Exon-intron organization of the human 5-HT3A receptor gene. Neuropharmacology. 2000 Jan 4;39(2):308-15. [PubMed:10670426]
  5. Jin P, Fu GK, Wilson AD, Yang J, Chien D, Hawkins PR, Au-Young J, Stuve LL: PCR isolation and cloning of novel splice variant mRNAs from known drug target genes. Genomics. 2004 Apr;83(4):566-71. [PubMed:15028279]
  6. Ota T, Suzuki Y, Nishikawa T, Otsuki T, Sugiyama T, Irie R, Wakamatsu A, Hayashi K, Sato H, Nagai K, Kimura K, Makita H, Sekine M, Obayashi M, Nishi T, Shibahara T, Tanaka T, Ishii S, Yamamoto J, Saito K, Kawai Y, Isono Y, Nakamura Y, Nagahari K, Murakami K, Yasuda T, Iwayanagi T, Wagatsuma M, Shiratori A, Sudo H, Hosoiri T, Kaku Y, Kodaira H, Kondo H, Sugawara M, Takahashi M, Kanda K, Yokoi T, Furuya T, Kikkawa E, Omura Y, Abe K, Kamihara K, Katsuta N, Sato K, Tanikawa M, Yamazaki M, Ninomiya K, Ishibashi T, Yamashita H, Murakawa K, Fujimori K, Tanai H, Kimata M, Watanabe M, Hiraoka S, Chiba Y, Ishida S, Ono Y, Takiguchi S, Watanabe S, Yosida M, Hotuta T, Kusano J, Kanehori K, Takahashi-Fujii A, Hara H, Tanase TO, Nomura Y, Togiya S, Komai F, Hara R, Takeuchi K, Arita M, Imose N, Musashino K, Yuuki H, Oshima A, Sasaki N, Aotsuka S, Yoshikawa Y, Matsunawa H, Ichihara T, Shiohata N, Sano S, Moriya S, Momiyama H, Satoh N, Takami S, Terashima Y, Suzuki O, Nakagawa S, Senoh A, Mizoguchi H, Goto Y, Shimizu F, Wakebe H, Hishigaki H, Watanabe T, Sugiyama A, Takemoto M, Kawakami B, Yamazaki M, Watanabe K, Kumagai A, Itakura S, Fukuzumi Y, Fujimori Y, Komiyama M, Tashiro H, Tanigami A, Fujiwara T, Ono T, Yamada K, Fujii Y, Ozaki K, Hirao M, Ohmori Y, Kawabata A, Hikiji T, Kobatake N, Inagaki H, Ikema Y, Okamoto S, Okitani R, Kawakami T, Noguchi S, Itoh T, Shigeta K, Senba T, Matsumura K, Nakajima Y, Mizuno T, Morinaga M, Sasaki M, Togashi T, Oyama M, Hata H, Watanabe M, Komatsu T, Mizushima-Sugano J, Satoh T, Shirai Y, Takahashi Y, Nakagawa K, Okumura K, Nagase T, Nomura N, Kikuchi H, Masuho Y, Yamashita R, Nakai K, Yada T, Nakamura Y, Ohara O, Isogai T, Sugano S: Complete sequencing and characterization of 21,243 full-length human cDNAs. Nat Genet. 2004 Jan;36(1):40-5. Epub 2003 Dec 21. [PubMed:14702039]
  7. Taylor TD, Noguchi H, Totoki Y, Toyoda A, Kuroki Y, Dewar K, Lloyd C, Itoh T, Takeda T, Kim DW, She X, Barlow KF, Bloom T, Bruford E, Chang JL, Cuomo CA, Eichler E, FitzGerald MG, Jaffe DB, LaButti K, Nicol R, Park HS, Seaman C, Sougnez C, Yang X, Zimmer AR, Zody MC, Birren BW, Nusbaum C, Fujiyama A, Hattori M, Rogers J, Lander ES, Sakaki Y: Human chromosome 11 DNA sequence and analysis including novel gene identification. Nature. 2006 Mar 23;440(7083):497-500. [PubMed:16554811]
  8. Gerhard DS, Wagner L, Feingold EA, Shenmen CM, Grouse LH, Schuler G, Klein SL, Old S, Rasooly R, Good P, Guyer M, Peck AM, Derge JG, Lipman D, Collins FS, Jang W, Sherry S, Feolo M, Misquitta L, Lee E, Rotmistrovsky K, Greenhut SF, Schaefer CF, Buetow K, Bonner TI, Haussler D, Kent J, Kiekhaus M, Furey T, Brent M, Prange C, Schreiber K, Shapiro N, Bhat NK, Hopkins RF, Hsie F, Driscoll T, Soares MB, Casavant TL, Scheetz TE, Brown-stein MJ, Usdin TB, Toshiyuki S, Carninci P, Piao Y, Dudekula DB, Ko MS, Kawakami K, Suzuki Y, Sugano S, Gruber CE, Smith MR, Simmons B, Moore T, Waterman R, Johnson SL, Ruan Y, Wei CL, Mathavan S, Gunaratne PH, Wu J, Garcia AM, Hulyk SW, Fuh E, Yuan Y, Sneed A, Kowis C, Hodgson A, Muzny DM, McPherson J, Gibbs RA, Fahey J, Helton E, Ketteman M, Madan A, Rodrigues S, Sanchez A, Whiting M, Madari A, Young AC, Wetherby KD, Granite SJ, Kwong PN, Brinkley CP, Pearson RL, Bouffard GG, Blakesly RW, Green ED, Dickson MC, Rodriguez AC, Grimwood J, Schmutz J, Myers RM, Butterfield YS, Griffith M, Griffith OL, Krzywinski MI, Liao N, Morin R, Palmquist D, Petrescu AS, Skalska U, Smailus DE, Stott JM, Schnerch A, Schein JE, Jones SJ, Holt RA, Baross A, Marra MA, Clifton S, Makowski KA, Bosak S, Malek J: The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. 2004 Oct;14(10B):2121-7. [PubMed:15489334]
  9. Davies PA, Pistis M, Hanna MC, Peters JA, Lambert JJ, Hales TG, Kirkness EF: The 5-HT3B subunit is a major determinant of serotonin-receptor function. Nature. 1999 Jan 28;397(6717):359-63. [PubMed:9950429]
  10. Dubin AE, Huvar R, D'Andrea MR, Pyati J, Zhu JY, Joy KC, Wilson SJ, Galindo JE, Glass CA, Luo L, Jackson MR, Lovenberg TW, Erlander MG: The pharmacological and functional characteristics of the serotonin 5-HT(3A) receptor are specifically modified by a 5-HT(3B) receptor subunit. J Biol Chem. 1999 Oct 22;274(43):30799-810. [PubMed:10521471]
  11. Kelley SP, Dunlop JI, Kirkness EF, Lambert JJ, Peters JA: A cytoplasmic region determines single-channel conductance in 5-HT3 receptors. Nature. 2003 Jul 17;424(6946):321-4. [PubMed:12867984]
  12. Cheng A, McDonald NA, Connolly CN: Cell surface expression of 5-hydroxytryptamine type 3 receptors is promoted by RIC-3. J Biol Chem. 2005 Jun 10;280(23):22502-7. Epub 2005 Apr 4. [PubMed:15809299]
  13. Niesler B, Walstab J, Combrink S, Moller D, Kapeller J, Rietdorf J, Bonisch H, Gothert M, Rappold G, Bruss M: Characterization of the novel human serotonin receptor subunits 5-HT3C,5-HT3D, and 5-HT3E. Mol Pharmacol. 2007 Jul;72(1):8-17. Epub 2007 Mar 28. [PubMed:17392525]
  14. Frank B, Niesler B, Bondy B, Spath M, Pongratz DE, Ackenheil M, Fischer C, Rappold G: Mutational analysis of serotonin receptor genes: HTR3A and HTR3B in fibromyalgia patients. Clin Rheumatol. 2004 Aug;23(4):338-44. Epub 2004 May 7. [PubMed:15293096]
  15. Yamada K, Hattori E, Iwayama Y, Ohnishi T, Ohba H, Toyota T, Takao H, Minabe Y, Nakatani N, Higuchi T, Detera-Wadleigh SD, Yoshikawa T: Distinguishable haplotype blocks in the HTR3A and HTR3B region in the Japanese reveal evidence of association of HTR3B with female major depression. Biol Psychiatry. 2006 Jul 15;60(2):192-201. Epub 2006 Feb 17. [PubMed:16487942]

Drug Relations

Drug Relations
DrugBank IDNameDrug groupPharmacological action?ActionsDetails
DB00377Palonosetronapproved, investigationalyesantagonistDetails
DB00757Dolasetronapproved, investigationalyesantagonistDetails
DB00889Granisetronapproved, investigationalyesantagonistDetails
DB00904OndansetronapprovedyesantagonistDetails
DB00969Alosetronapproved, withdrawnyesantagonistDetails
DB00721Procaineapproved, investigational, vet_approvedyesantagonistDetails
DB01161ChloroprocaineapprovedunknownantagonistDetails
DB00604Cisaprideapproved, investigational, withdrawnyesagonistDetails
DB01199TubocurarineapprovedyesantagonistDetails
DB04885CilansetroninvestigationalunknownDetails
DB04917RenzaprideinvestigationalunknownDetails
DB05049DDP733investigationalunknownDetails
DB05642DDP-225investigationalunknownDetails
DB06204TapentadolapprovedunknownDetails
DB06422TicaloprideinvestigationalunknownDetails
DB00246ZiprasidoneapprovedunknownantagonistDetails
DB00363ClozapineapprovedunknownantagonistDetails
DB01238Aripiprazoleapproved, investigationalunknownantagonistDetails
DB00334Olanzapineapproved, investigationalunknownantagonistDetails
DB01224QuetiapineapprovedunknownligandDetails
DB00728RocuroniumapprovedunknownantagonistDetails
DB01043Memantineapproved, investigationalunknownantagonistDetails
DB00408LoxapineapprovedunknownbinderDetails
DB00543AmoxapineapprovedunknownantagonistDetails
DB00726TrimipramineapprovedunknownbinderDetails
DB00333MethadoneapprovedunknownantagonistDetails
DB01233Metoclopramideapproved, investigationalyesagonistDetails
DB00898EthanolapprovedunknownDetails
DB09068Vortioxetineapproved, investigationalyesantagonistDetails
DB11699Tropisetronapproved, investigationalyesantagonistDetails
DB09290RamosetroninvestigationalunknownantagonistDetails
DB00988DopamineapprovedunknownDetails
DB08839Serotonininvestigational, nutraceuticalunknownDetails
DB00555Lamotrigineapproved, investigationalunknowninhibitorDetails
DB01221Ketamineapproved, vet_approvedyespotentiatorDetails
DB09061Cannabidiolapproved, investigationalunknownantagonistDetails
DB14185Aripiprazole lauroxilapproved, investigationalunknownDetails
DB01156Bupropionapprovedunknownnegative modulatorDetails
DB13025TiaprideinvestigationalyesantagonistDetails
DB09304SetiptilineexperimentalunknownantagonistDetails
DB13345Dihydroergocristineapproved, experimentalyesantagonistDetails
DB01049Ergoloid mesylateapprovedyesantagonistagonistDetails
DB11273DihydroergocornineapprovedyesantagonistagonistDetails
DB12141Gilteritinibapproved, investigationalnoinhibitorDetails
DB00715Paroxetineapproved, investigationalunknownDetails