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
- FunctionsG-protein coupled receptor activity / histamine binding / histamine receptor activityProcessescellular 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 learningComponentscytoplasm / 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
- 7tm_1 (PF00001)
- 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
Resource Link UniProtKB ID P35367 UniProtKB Entry Name HRH1_HUMAN GenBank Protein ID 510296 GenBank Gene ID Z34897 GenAtlas ID HRH1 HGNC ID HGNC:5182 - General References
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
Drug Relations
- Drug Relations
DrugBank ID Name Drug group Pharmacological action? Actions Details DB00283 Clemastine approved, investigational yes antagonist Details DB00341 Cetirizine approved yes antagonist Details DB00342 Terfenadine approved, withdrawn yes antagonist Details DB00354 Buclizine approved yes antagonist Details DB00366 Doxylamine approved, vet_approved yes antagonist Details DB00405 Dexbrompheniramine approved yes antagonist Details DB00427 Triprolidine approved yes antagonist Details DB00455 Loratadine approved, investigational yes antagonist Details DB00557 Hydroxyzine approved yes inverse agonist Details DB00568 Cinnarizine approved, investigational yes antagonist Details DB00637 Astemizole approved, withdrawn yes antagonist Details DB05381 Histamine approved, investigational yes agonist Details DB00719 Azatadine approved yes antagonist Details DB00737 Meclizine approved yes antagonist Details DB00748 Carbinoxamine approved yes antagonist Details DB00768 Olopatadine approved yes antagonist Details DB00792 Tripelennamine approved, vet_approved yes antagonist Details DB00835 Brompheniramine approved yes antagonist Details DB00902 Methdilazine approved yes antagonist Details DB00934 Maprotiline approved, investigational no antagonist Details DB00950 Fexofenadine approved, investigational yes antagonist Details DB00967 Desloratadine approved, investigational yes antagonist Details DB00972 Azelastine approved yes antagonist Details DB00985 Dimenhydrinate approved yes antagonist Details DB01071 Mequitazine experimental yes antagonist Details DB01075 Diphenhydramine approved, investigational yes antagonist Details DB01084 Emedastine approved yes antagonist Details DB01114 Chlorpheniramine approved yes antagonist Details DB01146 Diphenylpyraline approved, investigational yes antagonist Details DB01176 Cyclizine approved yes antagonist Details DB01237 Bromodiphenhydramine approved yes antagonist Details DB01246 Alimemazine approved, vet_approved yes antagonist Details DB00246 Ziprasidone approved unknown antagonist Details DB00334 Olanzapine approved, investigational unknown antagonist Details DB00363 Clozapine approved unknown antagonist Details DB00420 Promazine approved, vet_approved unknown antagonist Details DB00656 Trazodone approved, investigational unknown antagonist Details DB00767 Benzquinamide withdrawn yes antagonist Details DB00777 Propiomazine approved yes antagonist Details DB00920 Ketotifen approved yes antagonist Details DB01069 Promethazine approved, investigational yes antagonist Details DB01106 Levocabastine approved, investigational yes antagonist Details DB01142 Doxepin approved, investigational yes antagonist Details DB01151 Desipramine approved, investigational no antagonist Details DB01173 Orphenadrine approved yes antagonist Details DB01403 Methotrimeprazine approved, investigational unknown antagonist Details DB01619 Phenindamine approved yes antagonist Details DB01620 Pheniramine approved yes inverse agonist Details DB04837 Clofedanol approved, withdrawn yes antagonist Details DB04841 Flunarizine approved unknown antagonist Details DB01615 Aceprometazine experimental yes antagonist Details DB01239 Chlorprothixene approved, experimental, investigational, withdrawn yes antagonist Details DB00370 Mirtazapine approved no antagonist Details DB01224 Quetiapine approved unknown antagonist Details DB00434 Cyproheptadine approved yes antagonist Details DB04890 Bepotastine approved yes antagonist Details DB00751 Epinastine approved, investigational yes antagonist Details DB06148 Mianserin approved, investigational unknown antagonist Details DB04905 Tesmilifene investigational unknown antagonist Details DB05079 HY10275 investigational unknown Details DB05345 SO-101 investigational unknown Details DB05080 OBE101 investigational unknown Details DB05492 Epicept NP-1 investigational unknown Details DB06216 Asenapine approved unknown antagonist Details DB06229 Ocaperidone investigational unknown Details DB00245 Benzatropine approved unknown antagonist Details DB01267 Paliperidone approved unknown antagonist Details DB01238 Aripiprazole approved, investigational no antagonist Details DB00321 Amitriptyline approved no antagonist Details DB00458 Imipramine approved no antagonist Details DB00540 Nortriptyline approved no antagonist Details DB01175 Escitalopram approved unknown inhibitor Details DB00726 Trimipramine approved unknown antagonist Details DB00797 Tolazoline approved, vet_approved unknown agonist Details DB06766 Alcaftadine approved unknown antagonist Details DB08799 Antazoline approved yes antagonist Details DB08800 Chloropyramine experimental yes antagonist Details DB08801 Dimetindene approved, investigational yes antagonist Details DB08802 Isothipendyl experimental yes antagonist Details DB06698 Betahistine approved, investigational yes agonist Details DB06691 Mepyramine approved, vet_approved yes antagonist Details DB00477 Chlorpromazine approved, investigational, vet_approved yes antagonist Details DB04946 Iloperidone approved unknown antagonist Details DB00215 Citalopram approved no binder Details DB01624 Zuclopenthixol approved, investigational unknown antagonist Details DB08936 Chlorcyclizine approved yes antagonist Details DB00408 Loxapine approved unknown binder Details DB00543 Amoxapine approved unknown antagonist Details DB09016 Butriptyline approved, withdrawn yes antagonist Details DB06678 Esmirtazapine investigational unknown inverse agonist Details DB06282 Levocetirizine approved yes antagonistinhibitor Details DB11591 Bilastine approved, investigational yes antagonist Details DB09488 Acrivastine approved yes antagonist Details DB09555 Dexchlorpheniramine maleate approved yes antagonist Details DB08922 Perospirone experimental unknown inverse agonist Details DB09167 Dosulepin approved yes antagonist Details DB11614 Rupatadine approved yes antagonist Details DB09195 Lorpiprazole approved yes antagonist Details DB00555 Lamotrigine approved, investigational unknown antagonist Details DB06153 Pizotifen approved unknown antagonist Details DB11235 Thonzylamine approved yes antagonist Details DB14185 Aripiprazole lauroxil approved, investigational no antagonist Details DB00433 Prochlorperazine approved, vet_approved unknown antagonist Details DB00502 Haloperidol approved unknown Details DB00715 Paroxetine approved, investigational unknown inhibitor Details DB00734 Risperidone approved, investigational unknown antagonist Details DB06016 Cariprazine approved, investigational unknown antagonist Details DB00912 Repaglinide approved, investigational yes antagonist Details DB09185 Viloxazine approved, investigational, withdrawn unknown antagonist Details DB09128 Brexpiprazole approved, investigational unknown antagonist Details