Histamine H1 receptor

Details

Name
Histamine H1 receptor
Synonyms
  • H1R
Gene Name
HRH1
Organism
Humans
Amino acid sequence
>lcl|BSEQ0016092|Histamine H1 receptor
MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHT
VGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFI
LCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKC
ETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLR
PENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKL
YCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSR
TDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFI
MAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFK
RILHIRS
Number of residues
487
Molecular Weight
55783.61
Theoretical pI
9.58
GO Classification
Functions
G-protein coupled receptor activity / histamine binding / histamine receptor activity
Processes
cellular response to histamine / eosinophil chemotaxis / G-protein coupled receptor signaling pathway / inflammatory response / inositol phosphate-mediated signaling / memory / modulation of synaptic transmission / phospholipase C-activating G-protein coupled receptor signaling pathway / positive regulation of inositol trisphosphate biosynthetic process / positive regulation of vasoconstriction / regulation of synaptic plasticity / regulation of vascular permeability / regulation of vasoconstriction / sensory perception of chemical stimulus / visual learning
Components
cytoplasm / integral component of plasma membrane / nucleoplasm / plasma membrane
General Function
Histamine receptor activity
Specific Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Pfam Domain Function
Transmembrane Regions
30-52 63-83 102-123 144-164 190-210 417-438 451-470
Cellular Location
Cell membrane
Gene sequence
>lcl|BSEQ0016093|Histamine H1 receptor (HRH1)
ATGAGCCTCCCCAATTCCTCCTGCCTCTTAGAAGACAAGATGTGTGAGGGCAACAAGACC
ACTATGGCCAGCCCCCAGCTGATGCCCCTGGTGGTGGTCCTGAGCACTATCTGCTTGGTC
ACAGTAGGGCTCAACCTGCTGGTGCTGTATGCCGTACGGAGTGAGCGGAAGCTCCACACT
GTGGGGAACCTGTACATCGTCAGCCTCTCGGTGGCGGACTTGATCGTGGGTGCCGTCGTC
ATGCCTATGAACATCCTCTACCTGCTCATGTCCAAGTGGTCACTGGGCCGTCCTCTCTGC
CTCTTTTGGCTTTCCATGGACTATGTGGCCAGCACAGCGTCCATTTTCAGTGTCTTCATC
CTGTGCATTGATCGCTACCGCTCTGTCCAGCAGCCCCTCAGGTACCTTAAGTATCGTACC
AAGACCCGAGCCTCGGCCACCATTCTGGGGGCCTGGTTTCTCTCTTTTCTGTGGGTTATT
CCCATTCTAGGCTGGAATCACTTCATGCAGCAGACCTCGGTGCGCCGAGAGGACAAGTGT
GAGACAGACTTCTATGATGTCACCTGGTTCAAGGTCATGACTGCCATCATCAACTTCTAC
CTGCCCACCTTGCTCATGCTCTGGTTCTATGCCAAGATCTACAAGGCCGTACGACAACAC
TGCCAGCACCGGGAGCTCATCAATAGGTCCCTCCCTTCCTTCTCAGAAATTAAGCTGAGG
CCAGAGAACCCCAAGGGGGATGCCAAGAAACCAGGGAAGGAGTCTCCCTGGGAGGTTCTG
AAAAGGAAGCCAAAAGATGCTGGTGGTGGATCTGTCTTGAAGTCACCATCCCAAACCCCC
AAGGAGATGAAATCCCCAGTTGTCTTCAGCCAAGAGGATGATAGAGAAGTAGACAAACTC
TACTGCTTTCCACTTGATATTGTGCACATGCAGGCTGCGGCAGAGGGGAGTAGCAGGGAC
TATGTAGCCGTCAACCGGAGCCATGGCCAGCTCAAGACAGATGAGCAGGGCCTGAACACA
CATGGGGCCAGCGAGATATCAGAGGATCAGATGTTAGGTGATAGCCAATCCTTCTCTCGA
ACGGACTCAGATACCACCACAGAGACAGCACCAGGCAAAGGCAAATTGAGGAGTGGGTCT
AACACAGGCCTGGATTACATCAAGTTTACTTGGAAGAGGCTCCGCTCGCATTCAAGACAG
TATGTATCTGGGTTGCACATGAACCGCGAAAGGAAGGCCGCCAAACAGTTGGGTTTTATC
ATGGCAGCCTTCATCCTCTGCTGGATCCCTTATTTCATCTTCTTCATGGTCATTGCCTTC
TGCAAGAACTGTTGCAATGAACATTTGCACATGTTCACCATCTGGCTGGGCTACATCAAC
TCCACACTGAACCCCCTCATCTACCCCTTGTGCAATGAGAACTTCAAGAAGACATTCAAG
AGAATTCTGCATATTCGCTCCTAA
Chromosome Location
3
Locus
3p25
External Identifiers
ResourceLink
UniProtKB IDP35367
UniProtKB Entry NameHRH1_HUMAN
GenBank Protein ID510296
GenBank Gene IDZ34897
GenAtlas IDHRH1
HGNC IDHGNC:5182
General References
  1. De Backer MD, Gommeren W, Moereels H, Nobels G, Van Gompel P, Leysen JE, Luyten WH: Genomic cloning, heterologous expression and pharmacological characterization of a human histamine H1 receptor. Biochem Biophys Res Commun. 1993 Dec 30;197(3):1601-8. [PubMed:8280179]
  2. Fukui H, Fujimoto K, Mizuguchi H, Sakamoto K, Horio Y, Takai S, Yamada K, Ito S: Molecular cloning of the human histamine H1 receptor gene. Biochem Biophys Res Commun. 1994 Jun 15;201(2):894-901. [PubMed:8003029]
  3. Moguilevsky N, Varsalona F, Noyer M, Gillard M, Guillaume JP, Garcia L, Szpirer C, Szpirer J, Bollen A: Stable expression of human H1-histamine-receptor cDNA in Chinese hamster ovary cells. Pharmacological characterisation of the protein, tissue distribution of messenger RNA and chromosomal localisation of the gene. Eur J Biochem. 1994 Sep 1;224(2):489-95. [PubMed:7925364]
  4. Kitano T, Liu YH, Ueda S, Saitou N: Human-specific amino acid changes found in 103 protein-coding genes. Mol Biol Evol. 2004 May;21(5):936-44. Epub 2004 Mar 10. [PubMed:15014171]
  5. 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]
  6. 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]
  7. Horio S, Kato T, Ogawa M, Fujimoto K, Fukui H: Two threonine residues and two serine residues in the second and third intracellular loops are both involved in histamine H1 receptor downregulation. FEBS Lett. 2004 Aug 27;573(1-3):226-30. [PubMed:15328002]
  8. Daub H, Olsen JV, Bairlein M, Gnad F, Oppermann FS, Korner R, Greff Z, Keri G, Stemmann O, Mann M: Kinase-selective enrichment enables quantitative phosphoproteomics of the kinome across the cell cycle. Mol Cell. 2008 Aug 8;31(3):438-48. doi: 10.1016/j.molcel.2008.07.007. [PubMed:18691976]
  9. Dephoure N, Zhou C, Villen J, Beausoleil SA, Bakalarski CE, Elledge SJ, Gygi SP: A quantitative atlas of mitotic phosphorylation. Proc Natl Acad Sci U S A. 2008 Aug 5;105(31):10762-7. doi: 10.1073/pnas.0805139105. Epub 2008 Jul 31. [PubMed:18669648]
  10. Shimamura T, Shiroishi M, Weyand S, Tsujimoto H, Winter G, Katritch V, Abagyan R, Cherezov V, Liu W, Han GW, Kobayashi T, Stevens RC, Iwata S: Structure of the human histamine H1 receptor complex with doxepin. Nature. 2011 Jun 22;475(7354):65-70. doi: 10.1038/nature10236. [PubMed:21697825]
  11. Sjoblom T, Jones S, Wood LD, Parsons DW, Lin J, Barber TD, Mandelker D, Leary RJ, Ptak J, Silliman N, Szabo S, Buckhaults P, Farrell C, Meeh P, Markowitz SD, Willis J, Dawson D, Willson JK, Gazdar AF, Hartigan J, Wu L, Liu C, Parmigiani G, Park BH, Bachman KE, Papadopoulos N, Vogelstein B, Kinzler KW, Velculescu VE: The consensus coding sequences of human breast and colorectal cancers. Science. 2006 Oct 13;314(5797):268-74. Epub 2006 Sep 7. [PubMed:16959974]

Drug Relations

Drug Relations
DrugBank IDNameDrug groupPharmacological action?ActionsDetails
DB00283Clemastineapproved, investigationalyesantagonistDetails
DB00341CetirizineapprovedyesantagonistDetails
DB00342Terfenadineapproved, withdrawnyesantagonistDetails
DB00354BuclizineapprovedyesantagonistDetails
DB00366Doxylamineapproved, vet_approvedyesantagonistDetails
DB00405DexbrompheniramineapprovedyesantagonistDetails
DB00427TriprolidineapprovedyesantagonistDetails
DB00455Loratadineapproved, investigationalyesantagonistDetails
DB00557HydroxyzineapprovedyesantagonistDetails
DB00568Cinnarizineapproved, investigationalyesantagonistDetails
DB00637Astemizoleapproved, withdrawnyesantagonistDetails
DB05381Histamineapproved, investigationalyesagonistDetails
DB00719AzatadineapprovedyesantagonistDetails
DB00734Risperidoneapproved, investigationalunknownantagonistDetails
DB00737MeclizineapprovedyesantagonistDetails
DB00748CarbinoxamineapprovedyesantagonistDetails
DB00768OlopatadineapprovedyesantagonistDetails
DB00792Tripelennamineapproved, vet_approvedyesantagonistDetails
DB00835BrompheniramineapprovedyesantagonistDetails
DB00902MethdilazineapprovedyesantagonistDetails
DB00934Maprotilineapproved, investigationalnoantagonistDetails
DB00950Fexofenadineapproved, investigationalyesantagonistDetails
DB00967Desloratadineapproved, investigationalyesantagonistDetails
DB00972AzelastineapprovedyesantagonistDetails
DB00985DimenhydrinateapprovedyesantagonistDetails
DB01071MequitazineexperimentalyesantagonistDetails
DB01075Diphenhydramineapproved, investigationalyesantagonistDetails
DB01084EmedastineapprovedyesantagonistDetails
DB01114ChlorphenamineapprovedyesantagonistDetails
DB01146Diphenylpyralineapproved, investigationalyesantagonistDetails
DB01176CyclizineapprovedyesantagonistDetails
DB01237BromodiphenhydramineapprovedyesantagonistDetails
DB01246Alimemazineapproved, vet_approvedyesantagonistDetails
DB00246ZiprasidoneapprovednoantagonistDetails
DB00334Olanzapineapproved, investigationalunknownantagonistDetails
DB00363ClozapineapprovednoantagonistDetails
DB00420Promazineapproved, vet_approvedunknownantagonistDetails
DB00656Trazodoneapproved, investigationalunknownantagonistDetails
DB00767BenzquinamidewithdrawnyesantagonistDetails
DB00777PropiomazineapprovedyesantagonistDetails
DB00920KetotifenapprovedyesantagonistDetails
DB01069Promethazineapproved, investigationalyesantagonistDetails
DB01106Levocabastineapproved, investigationalyesantagonistDetails
DB01142Doxepinapproved, investigationalyesantagonistDetails
DB01151Desipramineapproved, investigationalnoantagonistDetails
DB01173OrphenadrineapprovedyesantagonistDetails
DB01403Methotrimeprazineapproved, investigationalunknownantagonistDetails
DB01619PhenindamineapprovedyesantagonistDetails
DB01620PheniramineapprovedyesantagonistDetails
DB04837Clofedanolapproved, withdrawnyesantagonistDetails
DB04841FlunarizineapprovedunknownantagonistDetails
DB01615AceprometazineexperimentalyesantagonistDetails
DB01239Chlorprothixeneapproved, experimental, investigational, withdrawnunknownantagonistDetails
DB00370MirtazapineapprovednoantagonistDetails
DB01224QuetiapineapprovedunknownantagonistDetails
DB00434CyproheptadineapprovedyesantagonistDetails
DB04890BepotastineapprovedyesantagonistDetails
DB00751Epinastineapproved, investigationalyesantagonistDetails
DB06148Mianserinapproved, investigationalunknownantagonistDetails
DB04905TesmilifeneinvestigationalunknownantagonistDetails
DB05079HY10275investigationalunknownDetails
DB05345SO-101investigationalunknownDetails
DB05080OBE101investigationalunknownDetails
DB05492Epicept NP-1investigationalunknownDetails
DB06216AsenapineapprovedunknownantagonistDetails
DB06229OcaperidoneinvestigationalunknownDetails
DB00245BenzatropineapprovedunknownantagonistDetails
DB01267PaliperidoneapprovedunknownantagonistDetails
DB01238Aripiprazoleapproved, investigationalnoantagonistDetails
DB00321AmitriptylineapprovednoantagonistDetails
DB00458ImipramineapprovednoantagonistDetails
DB00540NortriptylineapprovednoantagonistDetails
DB01175Escitalopramapproved, investigationalunknownantagonistDetails
DB00726TrimipramineapprovedunknownantagonistDetails
DB00797Tolazolineapproved, vet_approvedunknownagonistDetails
DB06766AlcaftadineapprovedunknownantagonistDetails
DB08799AntazolineapprovedyesantagonistDetails
DB08800ChloropyramineexperimentalyesantagonistDetails
DB08801Dimetindeneapproved, investigationalyesantagonistDetails
DB08802IsothipendylexperimentalyesantagonistDetails
DB06698Betahistineapproved, investigationalyesagonistDetails
DB06691Mepyramineapproved, vet_approvedyesantagonistDetails
DB00477Chlorpromazineapproved, investigational, vet_approvedyesantagonistDetails
DB04946IloperidoneapprovedunknownantagonistDetails
DB00215CitalopramapprovednobinderDetails
DB01624Zuclopenthixolapproved, investigationalunknownantagonistDetails
DB08936ChlorcyclizineapprovedyesantagonistDetails
DB00408LoxapineapprovedunknownbinderDetails
DB00543AmoxapineapprovedunknownantagonistDetails
DB09016ButriptylineapprovedyesantagonistDetails
DB06678Esmirtazapineinvestigationalunknowninverse agonistDetails
DB06282LevocetirizineapprovedyesantagonistinhibitorDetails
DB06016Cariprazineapproved, investigationalyesantagonistDetails
DB11591Bilastineapproved, investigationalyesantagonistDetails
DB09488AcrivastineapprovedyesantagonistDetails
DB09555Dexchlorpheniramine maleateapprovedyesantagonistDetails
DB08922Perospironeexperimentalunknowninverse agonistDetails
DB09167DosulepinapprovedyesantagonistDetails
DB11614RupatadineapprovedyesantagonistDetails
DB09195LorpiprazoleapprovedyesantagonistDetails
DB00555Lamotrigineapproved, investigationalunknowninhibitorDetails
DB06153PizotifenapprovedunknownantagonistDetails
DB11235ThonzylamineapprovedyesantagonistDetails
DB14185Aripiprazole lauroxilapproved, investigationalnoantagonistDetails
DB00433Prochlorperazineapproved, vet_approvedunknownantagonistDetails