Histamine H1 receptor - wikipedia Histamine H receptor HRH1 Available structures PDB Ortholog search : PDBe RCSB show List of PDB id codes 3RZE Identifiers Aliases HRH1, H1 - R, H1R, HH1R, hisH1, histamine receptor H1 External IDs OMIM : 600167 MGI : 107619 HomoloGene : 668 GeneCards : HRH1 hide Gene location ( Human ) Chr. Chromosome 3 ( human ) Band 3p25. 3 Start 11,137,093 bp End 11,263,557 bp show Gene location ( Mouse ) Chr. Chromosome 6 ( mouse ) Band 6 E3 6 53.05 cM Start 114,397,936 bp End 114,483,296 bp hide RNA expression pattern More reference expression data show Gene ontology Molecular function histamine receptor activity signal transducer activity G - protein coupled receptor activity Cellular component integral component of membrane membrane integral component of plasma membrane plasma membrane cytosol Biological process eosinophil chemotaxis inositol phosphate - mediated signaling regulation of vasoconstriction positive regulation of inositol trisphosphate biosynthetic process cellular response to histamine regulation of vascular permeability phospholipase C - activating G - protein coupled receptor signaling pathway regulation of synaptic plasticity G - protein coupled receptor signaling pathway modulation of chemical synaptic transmission inflammatory response visual learning signal transduction memory positive regulation of vasoconstriction Sources : Amigo / QuickGO Orthologs Species Human Mouse Entrez 3269 15465 Ensembl ENSG00000196639 ENSMUSG00000053004 UniProt P35367 P70174 RefSeq ( mRNA ) NM_000861 NM_001098211 NM_001098212 NM_001098213 show NM_001252642 NM_001252643 NM_008285 NM_001317124 NM_001317125 NM_001317126 RefSeq ( protein ) NP_000852 NP_001091681 NP_001091682 NP_001091683 show NP_001239571 NP_001239572 NP_001304053 NP_001304054 NP_001304055 NP_032311 Location ( UCSC ) Chr 3 : 11.14 -- 11.26 Mb Chr 6 : 114.4 -- 114.48 Mb PubMed search Wikidata View / Edit Human View / Edit Mouse The H receptor is a histamine receptor belonging to the family of rhodopsin - like G - protein - coupled receptors. This receptor is activated by the biogenic amine histamine. It is expressed in smooth muscles, on vascular endothelial cells, in the heart, and in the central nervous system. The H receptor is linked to an intracellular G - protein ( G ) that activates phospholipase C and the inositol triphosphate ( IP3 ) signalling pathway. Antihistamines, which act on this receptor, are used as anti-allergy drugs. The crystal structure of the receptor has been determined ( shown on the right ) and used to discover new histamine H receptor ligands in structure - based virtual screening studies. Contents 1 Role in inflammation 2 Neurophysiology 3 See also 4 References 5 Further reading 6 External links Role in inflammation The expression of NF - κB, the transcription factor that regulates inflammatory processes, is promoted by the constitutive activity of the H receptor as well as by agonists that bind at the receptor. H - antihistamines have been shown to attenuate NF - κB expression and mitigate certain inflammatory processes in associated cells. Neurophysiology Histamine H receptors are activated by endogenous histamine, which is released by neurons that have their cell bodies in the tuberomammillary nucleus of the hypothalamus. The histaminergic neurons of the tuberomammillary nucleus become active during the ' wake ' cycle, firing at approximately 2 Hz ; during slow wave sleep, this firing rate drops to approximately 0.5 Hz. Finally, during REM sleep, histaminergic neurons stop firing altogether. It has been reported that histaminergic neurons have the most wake - selective firing pattern of all known neuronal types. The tuberomammillary nucleus is a histaminergic nucleus that strongly regulates the sleep - wake cycle. H - antihistamines that cross the blood - brain barrier inhibit H receptor activity on neurons that project from the tuberomammillary nucleus. This action is responsible for the drowsiness effect associated with these drugs. See also Antihistamine -- H - receptor antagonists References ^ Jump up to : GRCh38 : Ensembl release 89 : ENSG00000196639 - Ensembl, May 2017 ^ Jump up to : GRCm38 : Ensembl release 89 : ENSMUSG00000053004 - Ensembl, May 2017 Jump up ^ `` Human PubMed Reference : ''. Jump up ^ `` Mouse PubMed Reference : ''. Jump up ^ 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 ( Jul 2011 ). `` Structure of the human histamine H1 receptor complex with doxepin ''. Nature. 475 ( 7354 ) : 65 -- 70. doi : 10.1038 / nature10236. PMC 3131495. PMID 21697825. Jump up ^ de Graaf C, Kooistra AJ, Vischer HF, Katritch V, Kuijer M, Shiroishi M, Iwata S, Shimamura T, Stevens RC, de Esch IJ, Leurs R ( Dec 2011 ). `` Crystal structure - based virtual screening for fragment - like ligands of the human histamine H ( 1 ) receptor ''. Journal of Medicinal Chemistry. 54 ( 23 ) : 8195 -- 206. doi : 10.1021 / jm2011589. PMC 3228891. PMID 22007643. ^ Jump up to : Canonica GW, Blaiss M ( Feb 2011 ). `` Antihistaminic, anti-inflammatory, and antiallergic properties of the nonsedating second - generation antihistamine desloratadine : a review of the evidence ''. The World Allergy Organization Journal. 4 ( 2 ) : 47 -- 53. doi : 10.1097 / WOX. 0b013e3182093e19. PMC 3500039. PMID 23268457. The H1 - receptor is a transmembrane protein belonging to the G - protein coupled receptor family. Signal transduction from the extracellular to the intracellular environment occurs as the GCPR becomes activated after binding of a specific ligand or agonist. A subunit of the G - protein subsequently dissociates and affects intracellular messaging including downstream signaling accomplished through various intermediaries such as cyclic AMP, cyclic GMP, calcium, and nuclear factor kappa B ( NF - κB ), a ubiquitous transcription factor thought to play an important role in immune - cell chemotaxis, proinflammatory cytokine production, expression of cell adhesion molecules, and other allergic and inflammatory conditions. 1, 8, 12, 30 -- 32... For example, the H1 - receptor promotes NF - κB in both a constitutive and agonist - dependent manner and all clinically available H1 - antihistamines inhibit constitutive H1 - receptor - mediated NF - κB production... Importantly, because antihistamines can theoretically behave as inverse agonists or neutral antagonists, they are more properly described as H1 - antihistamines rather than H1 - receptor antagonists. 15 Jump up ^ Passani MB, Lin JS, Hancock A, Crochet S, Blandina P ( Dec 2004 ). `` The histamine H3 receptor as a novel therapeutic target for cognitive and sleep disorders ''. Trends in Pharmacological Sciences. 25 ( 12 ) : 618 -- 25. doi : 10.1016 / j. tips. 2004.10. 003. PMID 15530639. Jump up ^ Malenka RC, Nestler EJ, Hyman SE ( 2009 ). `` Chapter 6 : Widely Projecting Systems : Monoamines, Acetylcholine, and Orexin ''. In Sydor A, Brown RY. Molecular Neuropharmacology : A Foundation for Clinical Neuroscience ( 2nd ed. ). New York : McGraw - Hill Medical. pp. 175 -- 176. ISBN 9780071481274. Within the brain, histamine is synthesized exclusively by neurons with their cell bodies in the tuberomammillary nucleus ( TMN ) that lies within the posterior hypothalamus. There are approximately 64000 histaminergic neurons per side in humans. These cells project throughout the brain and spinal cord. Areas that receive especially dense projections include the cerebral cortex, hippocampus, neostriatum, nucleus accumbens, amygdala, and hypothalamus... While the best characterized function of the histamine system in the brain is regulation of sleep and arousal, histamine is also involved in learning and memory... It also appears that histamine is involved in the regulation of feeding and energy balance. Further reading Mitsuchashi M, Payan DG ( Jun 1989 ). `` Molecular and cellular analysis of histamine H1 receptors on cultured smooth muscle cells ''. Journal of Cellular Biochemistry. 40 ( 2 ) : 183 -- 92. doi : 10.1002 / jcb. 240400207. PMID 2670975. Braman SS ( 1987 ). `` Histamine receptors in the lung ''. New England and Regional Allergy Proceedings. 8 ( 2 ) : 116 -- 20. doi : 10.2500 / 108854187778994446. PMID 2886904. Hill SJ, Ganellin CR, Timmerman H, Schwartz JC, Shankley NP, Young JM, Schunack W, Levi R, Haas HL ( Sep 1997 ). `` International Union of Pharmacology. XIII. Classification of histamine receptors ''. Pharmacological Reviews. 49 ( 3 ) : 253 -- 78. PMID 9311023. Holden CA, Chan SC, Norris S, Hanifin JM ( Oct 1987 ). `` Histamine induced elevation of cyclic AMP phosphodiesterase activity in human monocytes ''. Agents and Actions. 22 ( 1 -- 2 ) : 36 -- 42. doi : 10.1007 / BF01968814. PMID 2891264. Moguilevsky N, Varsalona F, Noyer M, Gillard M, Guillaume JP, Garcia L, Szpirer C, Szpirer J, Bollen A ( Sep 1994 ). `` 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 ''. European Journal of Biochemistry / FEBS. 224 ( 2 ) : 489 -- 95. doi : 10.1111 / j. 1432 - 1033.1994. 00489. x. PMID 7925364. Fukui H, Fujimoto K, Mizuguchi H, Sakamoto K, Horio Y, Takai S, Yamada K, Ito S ( Jun 1994 ). `` Molecular cloning of the human histamine H1 receptor gene ''. Biochemical and Biophysical Research Communications. 201 ( 2 ) : 894 -- 901. doi : 10.1006 / bbrc. 1994.1786. PMID 8003029. Le Coniat M, Traiffort E, Ruat M, Arrang JM, Berger R ( Aug 1994 ). `` Chromosomal localization of the human histamine H1 - receptor gene ''. Human Genetics. 94 ( 2 ) : 186 -- 8. doi : 10.1007 / bf00202867. PMID 8045566. De Backer MD, Gommeren W, Moereels H, Nobels G, Van Gompel P, Leysen JE, Luyten WH ( Dec 1993 ). `` Genomic cloning, heterologous expression and pharmacological characterization of a human histamine H1 receptor ''. Biochemical and Biophysical Research Communications. 197 ( 3 ) : 1601 -- 8. doi : 10.1006 / bbrc. 1993.2662. PMID 8280179. Hishinuma S, Young JM ( Nov 1995 ). `` Characteristics of the binding of ( 3H ) - mepyramine to intact human U373 MG astrocytoma cells : evidence for histamine - induced H1 - receptor internalisation ''. British Journal of Pharmacology. 116 ( 6 ) : 2715 -- 23. doi : 10.1111 / j. 1476 - 5381.1995. tb17232. x. PMC 1909113. PMID 8590995. Max SI, Chowdhury BA, Fraser CM ( Jun 1996 ). `` Sequence analysis of the 5 ' - untranslated region of the human H1 histamine receptor - encoding gene ''. Gene. 171 ( 2 ) : 309 -- 10. doi : 10.1016 / 0378 - 1119 ( 96 ) 00036 - 4. PMID 8666296. De Backer MD, Loonen I, Verhasselt P, Neefs JM, Luyten WH ( Nov 1998 ). `` Structure of the human histamine H1 receptor gene ''. The Biochemical Journal. 335 ( 3 ) : 663 -- 70. doi : 10.1042 / bj3350663. PMC 1219830. PMID 9794809. Horváth BV, Szalai C, Mándi Y, László V, Radvány Z, Darvas Z, Falus A ( Nov 1999 ). `` Histamine and histamine - receptor antagonists modify gene expression and biosynthesis of interferon gamma in peripheral human blood mononuclear cells and in CD19 - depleted cell subsets ''. Immunology Letters. 70 ( 2 ) : 95 -- 9. doi : 10.1016 / S0165 - 2478 ( 99 ) 00126 - 1. PMID 10569698. Wang KY, Arima N, Higuchi S, Shimajiri S, Tanimoto A, Murata Y, Hamada T, Sasaguri Y ( May 2000 ). `` Switch of histamine receptor expression from H2 to H1 during differentiation of monocytes into macrophages ''. FEBS Letters. 473 ( 3 ) : 345 -- 8. doi : 10.1016 / S0014 - 5793 ( 00 ) 01560 - X. PMID 10818238. Oda T, Morikawa N, Saito Y, Masuho Y, Matsumoto S ( Nov 2000 ). `` Molecular cloning and characterization of a novel type of histamine receptor preferentially expressed in leukocytes ''. The Journal of Biological Chemistry. 275 ( 47 ) : 36781 -- 6. doi : 10.1074 / jbc. M006480200. PMID 10973974. Brew OB, Sullivan MH ( Sep 2001 ). `` Localisation of mRNAs for diamine oxidase and histamine receptors H1 and H2, at the feto - maternal interface of human pregnancy ''. Inflammation Research. 50 ( 9 ) : 449 -- 52. doi : 10.1007 / PL00000269. PMID 11603849. Gutzmer R, Langer K, Lisewski M, Mommert S, Rieckborn D, Kapp A, Werfel T ( Mar 2002 ). `` Expression and function of histamine receptors 1 and 2 on human monocyte - derived dendritic cells ''. The Journal of Allergy and Clinical Immunology. 109 ( 3 ) : 524 -- 31. doi : 10.1067 / mai. 2002.121944. PMID 11898002. Idzko M, la Sala A, Ferrari D, Panther E, Herouy Y, Dichmann S, Mockenhaupt M, Di Virgilio F, Girolomoni G, Norgauer J ( May 2002 ). `` Expression and function of histamine receptors in human monocyte - derived dendritic cells ''. The Journal of Allergy and Clinical Immunology. 109 ( 5 ) : 839 -- 46. doi : 10.1067 / mai. 2002.124044. PMID 11994709. External links `` Histamine Receptors : H ''. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Cell surface receptor : G protein -- coupled receptors Class A : Rhodopsin - like Neurotransmitter Adrenergic α1 ( A D ) α2 ( A C ) β1 β2 β3 Purinergic Adenosine ( A1 A2A A2B A3 ) P2Y ( 1 5 6 8 9 10 11 12 13 14 ) Serotonin ( all but 5 - HT3 ) 5 - HT1 ( A F ) 5 - HT2 ( A C ) 5 - HT ( 4 5A 6 7 ) Other Acetylcholine ( M1 M2 M3 M4 M5 ) Dopamine D1 D2 D3 D4 D5 GHB receptor Histamine H1 H2 H3 H4 Melatonin ( 1A 1B 1C ) TAAR ( 1 5 6 8 9 ) Metabolites and signaling molecules Eicosanoid CysLT ( 1 2 ) LTB4 FPRL1 OXE Prostaglandin DP ( 1 2 ), EP ( 1 4 ), FP Prostacyclin Thromboxane Other Bile acid Cannabinoid ( CB1 CB2, GPR ( 18 55 119 ) ) EBI2 Estrogen Free fatty acid ( 1 4 ) Hydroxycarboxylic acids Lysophosphatidic acid ( 1 5 6 ) Lysophospholipid ( 1 5 6 7 8 ) Oxoglutarate PAF Sphingosine - 1 - phosphate ( 1 5 ) Succinate Peptide Neuropeptide B / W ( 1 2 ) FF ( 1 2 ) Y ( 1 5 ) Neuromedin ( B U ( 1 2 ) ) Neurotensin ( 1 2 ) Other Anaphylatoxin ( C3a C5a ) Angiotensin ( 1 2 ) Apelin Bombesin BRS3 GRPR NMBR ) Bradykinin ( B1 B2 ) Chemokine Cholecystokinin ( A B) Endothelin Formyl peptide ( 1 3 ) FSH Galanin ( 1 3 ) Gonadotropin - releasing hormone ( 1 2 ) Ghrelin Kisspeptin Luteinizing hormone / choriogonadotropin MAS ( 1 1L X1 X2 X3 X4 ) Melanocortin ( 1 5 ) MCHR ( 1 2 ) Motilin Opioid ( Delta Kappa Mu Nociceptin & Zeta, but not Sigma ) Orexin ( 1 2 ) Oxytocin Prokineticin ( 1 2 ) Prolactin - releasing peptide Relaxin ( 1 4 ) Somatostatin ( 1 5 ) Tachykinin ( 1 3 ) Thyrotropin Thyrotropin - releasing hormone Urotensin - II Vasopressin ( 1A 1B 2 ) Miscellaneous Orphan GPR ( 1 6 12 15 17 18 19 20 21 22 23 25 26 27 31 32 33 34 35 37 39 42 44 45 50 52 55 61 62 63 65 68 75 77 78 81 82 83 84 85 87 88 92 101 103 109A 109B 119 120 132 135 137B 139 141 142 146 148 149 150 151 152 153 160 161 162 171 173 174 176 177 182 183 ) Other Adrenomedullin Olfactory Opsin ( 3 5 1LW 1MW 1SW RGR RRH ) Protease - activated ( 1 4 ) SREB ( 1 3 ) Class B : Secretin - like Adhesion ADGRG ( 1 5 6 7 ) Orphan GPR ( 56 64 97 98 110 111 112 113 114 115 116 123 124 125 126 128 133 143 144 155 157 ) Other Brain - specific angiogenesis inhibitor ( 1 3 ) Cadherin ( 1 3 ) Calcitonin CALCRL CD97 Corticotropin - releasing hormone ( 1 2 ) EMR ( 1 3 ) Glucagon ( GR GIPR GLP1R GLP2R ) Growth - hormone - releasing hormone PACAPR1 GPR Latrophilin ( 1 ELTD1 ) Methuselah - like proteins Parathyroid hormone ( 1 2 ) Secretin Vasoactive intestinal peptide ( 1 2 ) Class C : Metabotropic glutamate / pheromone Taste TAS1R ( 1 3 ) TAS2R ( 1 5 7 8 9 10 13 14 16 19 20 30 31 38 39 40 41 42 43 45 46 50 60 Vomeronasal receptor ) Other Calcium - sensing receptor GABAB ( 1 2 ) Glutamate receptor ( Metabotropic glutamate ( 1 5 6 7 8 ) ) GPRC6A GPR ( 156 158 179 ) RAIG ( 1 4 ) Class F : Frizzled / Smoothened Frizzled Frizzled ( 1 5 6 7 8 9 10 ) Smoothened Smoothened Histamine receptor modulators Agonists : 2 - Pyridylethylamine Betahistine Histamine HTMT L - Histidine UR - AK49 Antagonists : First - generation : 4 - Methyldiphenhydramine Alimemazine Antazoline Azatadine Bamipine Benzatropine ( benztropine ) Bepotastine Bromazine Brompheniramine Buclizine Captodiame Carbinoxamine Chlorcyclizine Chloropyramine Chlorothen Chlorphenamine Chlorphenoxamine Cinnarizine Clemastine Clobenzepam Clocinizine Cloperastine Cyclizine Cyproheptadine Dacemazine Decloxizine Deptropine Dexbrompheniramine Dexchlorpheniramine Dimenhydrinate Dimetindene Diphenhydramine Diphenylpyraline Doxylamine Embramine Etodroxizine Etybenzatropine ( ethylbenztropine ) Etymemazine Fenethazine Flunarizine Histapyrrodine Homochlorcyclizine Hydroxyethylpromethazine Hydroxyzine Isopromethazine Isothipendyl Meclozine Medrylamine Mepyramine ( pyrilamine ) Mequitazine Methafurylene Methapyrilene Methdilazine Moxastine Orphenadrine Oxatomide Oxomemazine Perlapine Phenindamine Pheniramine Phenyltoloxamine Pimethixene Piperoxan Pipoxizine Promethazine Propiomazine Pyrrobutamine Talastine Thenalidine Thenyldiamine Thiazinamium Thonzylamine Tolpropamine Tripelennamine Triprolidine Second / third - generation : Acrivastine Alinastine Astemizole Azelastine Bamirastine Barmastine Bepiastine Bepotastine Bilastine Cabastinen Carebastine Cetirizine Clemastine Clemizole Clobenztropine Desloratadine Dorastine Ebastine Efletirizine Emedastine Epinastine Fexofenadine Flezelastine Ketotifen Latrepirdine Levocabastine Levocetirizine Linetastine Loratadine Mapinastine Mebhydrolin Mizolastine Moxastine Noberastine Octastine Olopatadine Perastine Pibaxizine Piclopastine Quifenadine ( phencarol ) Rocastine Rupatadine Setastine Sequifenadine ( bicarphen ) Talastine Temelastine Terfenadine Vapitadine Zepastine Others : Atypical antipsychotics ( e.g., aripiprazole, asenapine, brexpiprazole, clozapine, iloperidone, olanzapine, paliperidone, quetiapine, risperidone, RP - 5063, ziprasidone, zotepine ) Phenylpiperazine antidepressants ( e.g., hydroxynefazodone, nefazodone, trazodone, triazoledione ) Tetracyclic antidepressants ( e.g., amoxapine, loxapine, maprotiline, mianserin, mirtazapine, oxaprotiline ) Tricyclic antidepressants ( e.g., amitriptyline, butriptyline, clomipramine, desipramine, dosulepin ( dothiepin ), doxepin, imipramine, iprindole, lofepramine, nortriptyline, protriptyline, trimipramine ) Typical antipsychotics ( e.g., chlorpromazine, flupenthixol, fluphenazine, loxapine, perphenazine, prochlorperazine, thioridazine, thiothixene ) Unknown / unsorted : Azanator Belarizine Elbanizine Flotrenizine GSK1004723 Napactadine Tagorizine Trelnarizine Trenizine Agonists : Amthamine Betazole Dimaprit Histamine HTMT Impromidine L - Histidine UR - AK49 Antagonists : Bisfentidine Burimamide Cimetidine Dalcotidine Donetidine Ebrotidine Etintidine Famotidine Isolamtidine Lafutidine Lamtidine Lavoltidine ( loxtidine ) Lupitidine Metiamide Mifentidine Niperotidine Nizatidine Osutidine Oxmetidine Pibutidine Quisultazine ( quisultidine ) Ramixotidine Ranitidine Roxatidine Sufotidine Tiotidine Tuvatidine Venritidine Xaltidine Zolantidine Agonists : α - Methylhistamine Cipralisant Histamine Imetit Immepip Immethridine L - Histidine Methimepip Proxyfan Antagonists : A-349,821 A-423,579 ABT - 239 ABT - 652 AZD5213 Bavisant Betahistine Burimamide Ciproxifan Clobenpropit Conessine Enerisant GSK - 189,254 Impentamine Iodophenpropit Irdabisant JNJ - 5207852 MK - 0249 NNC 38 - 1049 PF - 03654746 Pitolisant SCH - 79687 Thioperamide VUF - 5681 Agonists : 4 - Methylhistamine α - Methylhistamine Histamine L - Histidine OUP - 16 VUF - 8430 Antagonists : JNJ - 7777120 Mianserin Seliforant Thioperamide Toreforant VUF - 6002 See also : Receptor / signaling modulators Monoamine metabolism modulators Monoamine reuptake inhibitors Retrieved from `` https://en.wikipedia.org/w/index.php?title=Histamine_H1_receptor&oldid=824622507 '' Categories : Genes on human chromosome 3 Histamine receptors Talk Contents About Wikipedia Cymraeg Deutsch Italiano Latina Português Русский Српски / srpski Srpskohrvatski / српскохрватски Українська Edit links This page was last edited on 8 February 2018, at 14 : 07 ( UTC ). 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Question: where are h1 receptors found in the body
Answer: smooth muscles