histamine H1 receptor

H1受容体

WordNet

1. the 8th letter of the Roman alphabet (同)h
2. amine formed from histidine that stimulates gastric secretions and dilates blood vessels; released by the human immune system during allergic reactions
3. a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response

PrepTutorEJDIC

1. hydrogenの化学記号
2. 鉛筆の硬度 / 《俗》heroin
3. ヒスタミン(子宮収縮・血圧降下の薬)
4. =sense organ / 受信装置

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/05/23 12:58:18」(JST)

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Histamine receptor H1
Histamine H1 receptor in complex with doxepin(PDB entry 3RZE)
Available structures PDB Ortholog search: PDBe, RCSB List of PDB id codes 3RZE
Identifiers
Symbols	HRH1 ; H1-R; hisH1
External IDs	OMIM: 600167 MGI: 107619 HomoloGene: 668 IUPHAR: 262 ChEMBL: 231 GeneCards: HRH1 Gene
Gene ontology Molecular function • G-protein coupled receptor activity • histamine receptor activity Cellular component • plasma membrane • integral component of plasma membrane Biological process • inflammatory response • G-protein coupled receptor signaling pathway • phospholipase C-activating G-protein coupled receptor signaling pathway • memory • visual learning • positive regulation of inositol trisphosphate biosynthetic process • regulation of vascular permeability • positive regulation of vasoconstriction • inositol phosphate-mediated signaling • regulation of synaptic plasticity • eosinophil chemotaxis • cellular response to histamine Sources: Amigo / QuickGO
RNA expression pattern
More reference expression data
Orthologs
Species	Human	Mouse
Entrez	3269	15465
Ensembl	ENSG00000196639	ENSMUSG00000053004
UniProt	P35367	P70174
RefSeq (mRNA)	NM_000861	NM_001252642
RefSeq (protein)	NP_000852	NP_001239571
Location (UCSC)	Chr 3: 11.18 – 11.31 Mb	Chr 6: 114.4 – 114.48 Mb
PubMed search	[1]	[2]

The H₁ receptor is a histamine receptor belonging to the family of Rhodopsin-like G-protein-coupled receptors. This receptor, which is activated by the biogenic amine histamine, is expressed throughout the body, to be specific, in smooth muscles, on vascular endothelial cells, in the heart, and in the central nervous system. The H₁ receptor is linked to an intracellular G-protein (G_q) that activates phospholipase C and the phosphatidylinositol (PIP2) signaling 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 H₁ receptor ligands in structure-based virtual screening studies.

Role in inflammation

The production of prostaglandin E2 synthase induces the release of histamine from neurons, causing systemic vasodilation, along with increased cell permeability due to its action on H1 receptors.

Neurophysiology

Histamine H₁ 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.

In the cortex, activation of H₁ receptors leads to inhibition of cell membrane potassium channels. This depolarizes the neurons and increases the resistance of the neuronal cell membrane, bringing the cell closer to its firing threshold and increasing the excitatory voltage produced by a given excitatory current. H₁ receptor antagonists, or antihistamines, produce drowsiness because they oppose this action, reducing neuronal excitation.

See also

• Antihistamine – H₁-receptor antagonists

References

Further reading

• Mitsuchashi M, Payan DG (1989). "Molecular and cellular analysis of histamine H1 receptors on cultured smooth muscle cells.". J. Cell. Biochem. 40 (2): 183–92. doi:10.1002/jcb.240400207. PMID 2670975. 
• Braman SS (1987). "Histamine receptors in the lung.". N Engl Reg Allergy Proc 8 (2): 116–20. doi:10.2500/108854187778994446. PMID 2886904. 
• Hill SJ, Ganellin CR, Timmerman H et al. (1997). "International Union of Pharmacology. XIII. Classification of histamine receptors.". Pharmacol. Rev. 49 (3): 253–78. PMID 9311023.  CS1 maint: Explicit use of et al. (link)
• Holden CA, Chan SC, Norris S, Hanifin JM (1988). "Histamine induced elevation of cyclic AMP phosphodiesterase activity in human monocytes.". Agents Actions 22 (1–2): 36–42. doi:10.1007/BF01968814. PMID 2891264. 
• Moguilevsky N, Varsalona F, Noyer M et al. (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". Eur. J. Biochem. 224 (2): 489–95. doi:10.1111/j.1432-1033.1994.00489.x. PMID 7925364.  CS1 maint: Explicit use of et al. (link)
• Fukui H, Fujimoto K, Mizuguchi H et al. (1994). "Molecular cloning of the human histamine H1 receptor gene". Biochem. Biophys. Res. Commun. 201 (2): 894–901. doi:10.1006/bbrc.1994.1786. PMID 8003029.  CS1 maint: Explicit use of et al. (link)
• Le Coniat M, Traiffort E, Ruat M et al. (1994). "Chromosomal localization of the human histamine H1-receptor gene". Hum. Genet. 94 (2): 186–8. doi:10.1007/bf00202867. PMID 8045566.  CS1 maint: Explicit use of et al. (link)
• De Backer MD, Gommeren W, Moereels H et al. (1994). "Genomic cloning, heterologous expression and pharmacological characterization of a human histamine H1 receptor". Biochem. Biophys. Res. Commun. 197 (3): 1601–8. doi:10.1006/bbrc.1993.2662. PMID 8280179.  CS1 maint: Explicit use of et al. (link)
• Hishinuma S, Young JM (1996). "Characteristics of the binding of [3H]-mepyramine to intact human U373 MG astrocytoma cells: evidence for histamine-induced H1-receptor internalisation". Br. J. Pharmacol. 116 (6): 2715–23. doi:10.1111/j.1476-5381.1995.tb17232.x. PMC 1909113. PMID 8590995. 
• Max SI, Chowdhury BA, Fraser CM (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 et al. (1998). "Structure of the human histamine H1 receptor gene". Biochem. J. 335 (3): 663–70. PMC 1219830. PMID 9794809.  CS1 maint: Explicit use of et al. (link)
• Horváth BV, Szalai C, Mándi Y et al. (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". Immunol. Lett. 70 (2): 95–9. doi:10.1016/S0165-2478(99)00126-1. PMID 10569698.  CS1 maint: Explicit use of et al. (link)
• Wang KY, Arima N, Higuchi S et al. (2000). "Switch of histamine receptor expression from H2 to H1 during differentiation of monocytes into macrophages". FEBS Lett. 473 (3): 345–8. doi:10.1016/S0014-5793(00)01560-X. PMID 10818238.  CS1 maint: Explicit use of et al. (link)
• Oda T, Morikawa N, Saito Y et al. (2001). "Molecular cloning and characterization of a novel type of histamine receptor preferentially expressed in leukocytes". J. Biol. Chem. 275 (47): 36781–6. doi:10.1074/jbc.M006480200. PMID 10973974.  CS1 maint: Explicit use of et al. (link)
• Brew OB, Sullivan MH (2002). "Localisation of mRNAs for diamine oxidase and histamine receptors H1 and H2, at the feto-maternal interface of human pregnancy". Inflamm. Res. 50 (9): 449–52. doi:10.1007/PL00000269. PMID 11603849. 
• Gutzmer R, Langer K, Lisewski M et al. (2002). "Expression and function of histamine receptors 1 and 2 on human monocyte-derived dendritic cells". J. Allergy Clin. Immunol. 109 (3): 524–31. doi:10.1067/mai.2002.121944. PMID 11898002.  CS1 maint: Explicit use of et al. (link)
• Idzko M, la Sala A, Ferrari D et al. (2002). "Expression and function of histamine receptors in human monocyte-derived dendritic cells". J. Allergy Clin. Immunol. 109 (5): 839–46. doi:10.1067/mai.2002.124044. PMID 11994709.  CS1 maint: Explicit use of et al. (link)

External links

• "Histamine Receptors: H₁". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. 

UpToDate Contents

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• 1. Mast cell-derived mediators
• 2. 胃酸分泌の生理学 physiology of gastric acid secretion
• 3. 制吐剤の特性 characteristics of antiemetic drugs
• 4. アレルギーのin vitro検査の概要 overview of in vitro allergy tests
• 5. 肥満細胞：表面受容体とシグナル伝達 mast cells surface receptors and signal transduction

English Journal

• Simultaneous optimization of pH and binary organic composition by grid form modeling of the retention behavior in reversed-phase ultra high-performance liquid chromatography.

• Sasaki T1, Todoroki K2, Toyo'oka T3.
• Journal of pharmaceutical and biomedical analysis.J Pharm Biomed Anal.2017 Nov 30;146:251-260. doi: 10.1016/j.jpba.2017.08.047. Epub 2017 Sep 1.
• PMID 28888712

• Hyperosmolarity evokes histamine release from ileum mucosa by stimulating a cholinergic pathway.

• Wang B1, An N2, Shaikh AS3, Wang H1, Xiao L1, Liu H1, Li J1, Zhao D4.
• Biochemical and biophysical research communications.Biochem Biophys Res Commun.2017 Nov 18;493(2):1037-1042. doi: 10.1016/j.bbrc.2017.09.093. Epub 2017 Sep 19.
• PMID 28939039

• Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H1 receptor antagonists for use in allergic rhinitis.

• Procopiou PA1, Ford AJ2, Gore PM3, Hancock AP3, Hodgson ST3, Holmes DS3, Looker BE3, Vile S3, Clark KL2, Saunders KA2, Slack RJ2, Watts CJ4.
• Bioorganic & medicinal chemistry letters.Bioorg Med Chem Lett.2017 Nov 1;27(21):4914-4919. doi: 10.1016/j.bmcl.2017.09.020. Epub 2017 Sep 9.
• PMID 28958623

Japanese Journal

• Histidine augments the suppression of hepatic glucose production by central insulin action.

• Kimura Kumi,Nakamura Yusuke,Inaba Yuka,Matsumoto Michihiro,Kido Yoshiaki,Asahara Shun-ichiro,Matsuda Tomokazu,Watanabe Hiroshi,Maeda Akifumi,Inagaki Fuyuhiko,Mukai Chisato,Takeda Kiyoshi,Akira Shizuo,Ota Tsuguhito,Nakabayashi Hajime,Kaneko Shuichi,Kasuga Masato,Inoue Hiroshi
• Diabetes 62(7), 2266-2277, 2013-07-00
• … Inhibition of HGP by histidine was also blocked by ICV administration of a histamine H1 receptor antagonist. … Therefore, histidine activates hepatic STAT3 and suppresses HGP via central histamine action. …
• NAID 120005334015

• Effect of Azelastine on Cardiac Repolarization of Guinea-Pig Cardiomyocytes, hERG K+ Channel, and Human L-type and T-type Ca2+ Channel

• Park Mi-Hyeong,Ho Lee Seung,Hyun Chu Dae,Hee Won Kwang,Hee Choi Bok,Choe Han,Jo Su-Hyun
• Journal of Pharmacological Sciences, 2013
• … Azelastine is a second generation histamine H1–receptor antagonist used as an anti-asthmatic and anti-allergic drug that can induce QT prolongation and torsades de pointes. …
• NAID 130003362736

• Combination of Leukotoriene Receptor Antagonist With Antihistamine Has an Additive Suppressive Effect on the Up-regulation of H1-Receptor mRNA in the Nasal Mucosa of Toluene 2,4-Diisocyanate-Sensitized Rat

• Kuroda Wakana,Kitamura Yoshiaki,Mizuguchi Hiroyuki,Miyamoto Yuko,Kalubi Bukasa,Fukui Hiroyuki,Takeda Noriaki
• Journal of Pharmacological Sciences, 2013
• … An attempt was made to clarify the additive suppressive effects of pranlukast, a cysteinyl leukotriene–receptor (LTR) antagonist, in combination with chlorpheniramine, an antihistamine, on the up-regulation of histamine H1–receptor (H1R) mRNA in toluene 2,4-diisocyanate (TDI)-sensitized rats. …
• NAID 130003362697

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★リンクテーブル★

リンク元	「H1受容体」「ヒスタミンH1受容体」
拡張検索	「histamine H1 receptor antagonist」
関連記事	「H1」「H」

「H1受容体」

　　[★]

英

H1 receptor

同

ヒスタミンH1受容体 ヒスタミンH1レセプター histamine H1 receptor

関

[[]]

• アレルギー反応に関与するヒスタミン受容体サブタイプ

「ヒスタミンH1受容体」

　　[★]

英

histamine H1 receptor

関

H1受容体、ヒスタミンH1レセプター

「histamine H1 receptor antagonist」

　　[★]

• ヒスタミンH1受容体遮断薬、ヒスタミンH1受容体拮抗薬

関

antihistamine、H1 blocker、histamine H1 antagonist

「H1」

　　[★]

• ヒストンのサブユニット　→　ヒストンH1
• ヒスタミンの受容体 H1受容体
• 癌の分類において肝転移有りを示す。
• 視床束 thalamic fasciculus

関

H, H0, HX

• 胃癌の病期分類に用いられている。
• 肝転移の有無を示す。
• 肝転移を認める。

「H」

　　[★]

• 食道裂孔
• ヒスチジン
• 水素