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
- FunctionsG protein-coupled serotonin receptor activity / neurotransmitter receptor activityProcesseschemical 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 pathwayComponentscytosol / 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
- 7tm_1 (PF00001)
- 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
Resource Link UniProtKB ID P35367 UniProtKB Entry Name HRH1_HUMAN GenBank Protein ID 510296 GenBank Gene ID Z34897 GeneCard ID HRH1 GenAtlas ID HRH1 HGNC ID HGNC:5182 PDB ID(s) 3RZE, 7DFL KEGG ID hsa:3269 IUPHAR/Guide To Pharmacology ID 262 NCBI Gene ID 3269 - 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]
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Associated Data
- Drug Relations
Drug Drug group Pharmacological action? Type Actions Details Clemastine approved, investigational yes target antagonist Details Cetirizine approved yes target antagonist Details Terfenadine approved, withdrawn yes target antagonist Details Buclizine approved yes target antagonist Details Doxylamine approved, vet_approved yes target antagonist Details Dexbrompheniramine approved yes target antagonist Details Triprolidine approved yes target antagonist Details Loratadine approved, investigational yes target antagonist Details Hydroxyzine approved yes target inverse agonist Details Cinnarizine approved, investigational yes target antagonist Details Astemizole approved, withdrawn yes target antagonist Details Histamine approved, investigational yes target agonist Details Azatadine approved yes target antagonist Details Meclizine approved yes target antagonist Details Carbinoxamine approved yes target antagonist Details Olopatadine approved yes target antagonist Details Tripelennamine approved, vet_approved yes target antagonist Details Brompheniramine approved yes target antagonist Details Methdilazine approved yes target antagonist Details Maprotiline approved, investigational no target antagonist Details Fexofenadine approved, investigational yes target antagonist Details Desloratadine approved, investigational yes target antagonist Details Azelastine approved yes target antagonist Details Dimenhydrinate approved yes target antagonist Details Mequitazine experimental yes target antagonist Details Diphenhydramine approved, investigational yes target antagonist Details Emedastine approved yes target antagonist Details Chlorpheniramine approved yes target antagonist Details Diphenylpyraline approved, investigational yes target antagonist Details Cyclizine approved yes target antagonist Details Bromodiphenhydramine approved yes target antagonist Details Alimemazine approved, vet_approved yes target antagonist Details Ziprasidone approved unknown target antagonist Details Olanzapine approved, investigational unknown target antagonist Details Clozapine approved unknown target antagonist Details Promazine approved, vet_approved unknown target antagonist Details Trazodone approved, investigational unknown target antagonist Details Benzquinamide withdrawn yes target antagonist Details Propiomazine approved yes target antagonist Details Ketotifen approved yes target antagonist Details Promethazine approved, investigational yes target antagonist Details Levocabastine approved, investigational yes target antagonist Details Doxepin approved, investigational yes target antagonist Details Desipramine approved, investigational no target antagonist Details Orphenadrine approved yes target antagonist Details Methotrimeprazine approved, investigational unknown target antagonist Details Phenindamine approved yes target antagonist Details Pheniramine approved yes target inverse agonist Details Clofedanol approved, withdrawn yes target antagonist Details Flunarizine approved unknown target antagonist Details Aceprometazine experimental yes target antagonist Details Chlorprothixene approved, experimental, investigational, withdrawn yes target antagonist Details Mirtazapine approved no target antagonist Details Quetiapine approved unknown target antagonist Details Cyproheptadine approved yes target antagonist Details Bepotastine approved yes target antagonist Details Epinastine approved, investigational yes target antagonist Details Mianserin approved, investigational unknown target antagonist Details Tesmilifene investigational unknown target antagonist Details HY10275 investigational unknown target Details SO-101 investigational unknown target Details OBE101 investigational unknown target Details Epicept NP-1 investigational unknown target Details Asenapine approved unknown target antagonist Details Ocaperidone investigational unknown target Details Benzatropine approved unknown target antagonist Details Paliperidone approved unknown target antagonist Details Aripiprazole approved, investigational no target antagonist Details Amitriptyline approved no target antagonist Details Imipramine approved no target antagonist Details Nortriptyline approved no target antagonist Details Escitalopram approved unknown target inhibitor Details Trimipramine approved unknown target antagonist Details Tolazoline approved, vet_approved unknown target agonist Details Alcaftadine approved yes target antagonist Details Antazoline approved yes target antagonist Details Chloropyramine experimental yes target antagonist Details Dimetindene approved, investigational yes target antagonist Details Isothipendyl experimental yes target antagonist Details Betahistine approved, investigational yes target agonist Details Mepyramine approved, vet_approved yes target antagonist Details Chlorpromazine approved, investigational, vet_approved yes target antagonist Details Iloperidone approved unknown target antagonist Details Citalopram approved no target binder Details Zuclopenthixol approved, investigational unknown target antagonist Details Chlorcyclizine approved yes target antagonist Details Loxapine approved unknown target binder Details Amoxapine approved unknown target antagonist Details Butriptyline approved, withdrawn yes target antagonist Details Esmirtazapine investigational unknown target inverse agonist Details Levocetirizine approved yes target antagonistinhibitor Details Bilastine approved, investigational yes target antagonist Details Acrivastine approved yes target antagonist Details Dexchlorpheniramine maleate approved yes target antagonist Details Perospirone experimental unknown target inverse agonist Details Dosulepin approved yes target antagonist Details Rupatadine approved yes target antagonist Details Lorpiprazole approved yes target antagonist Details Lamotrigine approved, investigational unknown target antagonist Details Pizotifen approved unknown target antagonist Details Thonzylamine approved yes target antagonist Details Aripiprazole lauroxil approved, investigational no target antagonist Details Prochlorperazine approved, vet_approved unknown target antagonist Details Haloperidol approved unknown target Details Paroxetine approved, investigational unknown target inhibitor Details Risperidone approved, investigational unknown target antagonist Details Cariprazine approved, investigational unknown target antagonist Details Repaglinide approved, investigational yes target antagonist Details Viloxazine approved, investigational, withdrawn unknown target antagonist Details Brexpiprazole approved, investigational unknown target antagonist Details Clorotepine experimental yes target inhibitor Details AZACYCLONOL withdrawn yes target inhibitor Details Latrepirdine investigational yes target inhibitor Details GSK-1004723 investigational yes target antagonist Details Vapitadine investigational yes target antagonist Details LY-2624803 investigational yes target modulator Details Tranilast investigational yes target antagonist Details Pemirolast approved, investigational yes target antagonist Details Mizolastine approved, investigational yes target antagonist Details Oxatomide approved, investigational yes target antagonist Details Profenamine approved yes target modulator Details Tecastemizole investigational yes target modulator Details