Histamine H1 receptor

Details

Name
Histamine H1 receptor
Kind
protein
Synonyms
  • H1-R
  • H1R
  • HH1R
Gene Name
HRH1
UniProtKB Entry
P35367Swiss-Prot
Organism
Humans
NCBI Taxonomy ID
9606
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 serotonin receptor activity / neurotransmitter receptor activity
Processes
chemical synaptic transmission / G protein-coupled receptor signaling pathway / G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger / phospholipase C-activating G protein-coupled receptor signaling pathway
Components
cytosol / dendrite / synapse
General Function
G-protein-coupled receptor for histamine, a biogenic amine that functions as an immune modulator and a neurotransmitter (PubMed:33828102, PubMed:8280179). Through the H1 receptor, histamine mediates the contraction of smooth muscles and increases capillary permeability due to contraction of terminal venules. Also mediates neurotransmission in the central nervous system and thereby regulates circadian rhythms, emotional and locomotor activities as well as cognitive functions (By similarity)
Specific Function
G protein-coupled serotonin receptor activity
Pfam Domain Function
Signal Regions
Not Available
Transmembrane Regions
30-50 65-89 98-123 145-164 189-211 417-440 447-469
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
3p25.3
External Identifiers
ResourceLink
UniProtKB IDP35367
UniProtKB Entry NameHRH1_HUMAN
GenBank Protein ID510296
GenBank Gene IDZ34897
GeneCard IDHRH1
GenAtlas IDHRH1
HGNC IDHGNC:5182
PDB ID(s)3RZE, 7DFL
KEGG IDhsa:3269
IUPHAR/Guide To Pharmacology ID262
NCBI Gene ID3269
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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]

Associated Data

Drug Relations
DrugDrug groupPharmacological action?TypeActionsDetails
Clemastineapproved, investigationalyestargetantagonistDetails
CetirizineapprovedyestargetantagonistDetails
Terfenadineapproved, withdrawnyestargetantagonistDetails
BuclizineapprovedyestargetantagonistDetails
Doxylamineapproved, vet_approvedyestargetantagonistDetails
DexbrompheniramineapprovedyestargetantagonistDetails
TriprolidineapprovedyestargetantagonistDetails
Loratadineapproved, investigationalyestargetantagonistDetails
Hydroxyzineapprovedyestargetinverse agonistDetails
Cinnarizineapproved, investigationalyestargetantagonistDetails
Astemizoleapproved, withdrawnyestargetantagonistDetails
Histamineapproved, investigationalyestargetagonistDetails
AzatadineapprovedyestargetantagonistDetails
MeclizineapprovedyestargetantagonistDetails
CarbinoxamineapprovedyestargetantagonistDetails
OlopatadineapprovedyestargetantagonistDetails
Tripelennamineapproved, vet_approvedyestargetantagonistDetails
BrompheniramineapprovedyestargetantagonistDetails
MethdilazineapprovedyestargetantagonistDetails
Maprotilineapproved, investigationalnotargetantagonistDetails
Fexofenadineapproved, investigationalyestargetantagonistDetails
Desloratadineapproved, investigationalyestargetantagonistDetails
AzelastineapprovedyestargetantagonistDetails
DimenhydrinateapprovedyestargetantagonistDetails
MequitazineexperimentalyestargetantagonistDetails
Diphenhydramineapproved, investigationalyestargetantagonistDetails
EmedastineapprovedyestargetantagonistDetails
ChlorpheniramineapprovedyestargetantagonistDetails
Diphenylpyralineapproved, investigationalyestargetantagonistDetails
CyclizineapprovedyestargetantagonistDetails
BromodiphenhydramineapprovedyestargetantagonistDetails
Alimemazineapproved, vet_approvedyestargetantagonistDetails
ZiprasidoneapprovedunknowntargetantagonistDetails
Olanzapineapproved, investigationalunknowntargetantagonistDetails
ClozapineapprovedunknowntargetantagonistDetails
Promazineapproved, vet_approvedunknowntargetantagonistDetails
Trazodoneapproved, investigationalunknowntargetantagonistDetails
BenzquinamidewithdrawnyestargetantagonistDetails
PropiomazineapprovedyestargetantagonistDetails
KetotifenapprovedyestargetantagonistDetails
Promethazineapproved, investigationalyestargetantagonistDetails
Levocabastineapproved, investigationalyestargetantagonistDetails
Doxepinapproved, investigationalyestargetantagonistDetails
Desipramineapproved, investigationalnotargetantagonistDetails
OrphenadrineapprovedyestargetantagonistDetails
Methotrimeprazineapproved, investigationalunknowntargetantagonistDetails
PhenindamineapprovedyestargetantagonistDetails
Pheniramineapprovedyestargetinverse agonistDetails
Clofedanolapproved, withdrawnyestargetantagonistDetails
FlunarizineapprovedunknowntargetantagonistDetails
AceprometazineexperimentalyestargetantagonistDetails
Chlorprothixeneapproved, experimental, investigational, withdrawnyestargetantagonistDetails
MirtazapineapprovednotargetantagonistDetails
QuetiapineapprovedunknowntargetantagonistDetails
CyproheptadineapprovedyestargetantagonistDetails
BepotastineapprovedyestargetantagonistDetails
Epinastineapproved, investigationalyestargetantagonistDetails
Mianserinapproved, investigationalunknowntargetantagonistDetails
TesmilifeneinvestigationalunknowntargetantagonistDetails
HY10275investigationalunknowntargetDetails
SO-101investigationalunknowntargetDetails
OBE101investigationalunknowntargetDetails
Epicept NP-1investigationalunknowntargetDetails
AsenapineapprovedunknowntargetantagonistDetails
OcaperidoneinvestigationalunknowntargetDetails
BenzatropineapprovedunknowntargetantagonistDetails
PaliperidoneapprovedunknowntargetantagonistDetails
Aripiprazoleapproved, investigationalnotargetantagonistDetails
AmitriptylineapprovednotargetantagonistDetails
ImipramineapprovednotargetantagonistDetails
NortriptylineapprovednotargetantagonistDetails
EscitalopramapprovedunknowntargetinhibitorDetails
TrimipramineapprovedunknowntargetantagonistDetails
Tolazolineapproved, vet_approvedunknowntargetagonistDetails
AlcaftadineapprovedyestargetantagonistDetails
AntazolineapprovedyestargetantagonistDetails
ChloropyramineexperimentalyestargetantagonistDetails
Dimetindeneapproved, investigationalyestargetantagonistDetails
IsothipendylexperimentalyestargetantagonistDetails
Betahistineapproved, investigationalyestargetagonistDetails
Mepyramineapproved, vet_approvedyestargetantagonistDetails
Chlorpromazineapproved, investigational, vet_approvedyestargetantagonistDetails
IloperidoneapprovedunknowntargetantagonistDetails
CitalopramapprovednotargetbinderDetails
Zuclopenthixolapproved, investigationalunknowntargetantagonistDetails
ChlorcyclizineapprovedyestargetantagonistDetails
LoxapineapprovedunknowntargetbinderDetails
AmoxapineapprovedunknowntargetantagonistDetails
Butriptylineapproved, withdrawnyestargetantagonistDetails
Esmirtazapineinvestigationalunknowntargetinverse agonistDetails
LevocetirizineapprovedyestargetantagonistinhibitorDetails
Bilastineapproved, investigationalyestargetantagonistDetails
AcrivastineapprovedyestargetantagonistDetails
Dexchlorpheniramine maleateapprovedyestargetantagonistDetails
Perospironeexperimentalunknowntargetinverse agonistDetails
DosulepinapprovedyestargetantagonistDetails
RupatadineapprovedyestargetantagonistDetails
LorpiprazoleapprovedyestargetantagonistDetails
Lamotrigineapproved, investigationalunknowntargetantagonistDetails
PizotifenapprovedunknowntargetantagonistDetails
ThonzylamineapprovedyestargetantagonistDetails
Aripiprazole lauroxilapproved, investigationalnotargetantagonistDetails
Prochlorperazineapproved, vet_approvedunknowntargetantagonistDetails
HaloperidolapprovedunknowntargetDetails
Paroxetineapproved, investigationalunknowntargetinhibitorDetails
Risperidoneapproved, investigationalunknowntargetantagonistDetails
Cariprazineapproved, investigationalunknowntargetantagonistDetails
Repaglinideapproved, investigationalyestargetantagonistDetails
Viloxazineapproved, investigational, withdrawnunknowntargetantagonistDetails
Brexpiprazoleapproved, investigationalunknowntargetantagonistDetails
ClorotepineexperimentalyestargetinhibitorDetails
AZACYCLONOLwithdrawnyestargetinhibitorDetails
LatrepirdineinvestigationalyestargetinhibitorDetails
GSK-1004723investigationalyestargetantagonistDetails
VapitadineinvestigationalyestargetantagonistDetails
LY-2624803investigationalyestargetmodulatorDetails
TranilastinvestigationalyestargetantagonistDetails
Pemirolastapproved, investigationalyestargetantagonistDetails
Mizolastineapproved, investigationalyestargetantagonistDetails
Oxatomideapproved, investigationalyestargetantagonistDetails
ProfenamineapprovedyestargetmodulatorDetails
TecastemizoleinvestigationalyestargetmodulatorDetails