WordNet

the 8th letter of the Roman alphabet (同)h
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

hydrogenの化学記号
鉛筆の硬度 / 《俗》heroin
=sense organ / 受信装置

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/08/14 00:23:40」(JST)

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The H₁ 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 H₁ receptor is linked to an intracellular G-protein (G_q) that activates phospholipase C and the phosphatidylinositol (PIP2) 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)^[3] and used to discover new histamine H₁ receptor ligands in structure-based virtual screening studies.^[4]

Role in inflammation

The expression of NF-κB, the transcription factor that regulates inflammatory processes, is promoted by the constitutive activity of the H₁ receptor as well as by agonists that bind at the receptor.^[5] H₁-antihistamines have been shown to attenuate NF-κB expression and mitigate certain inflammatory processes in associated cells.^[5]

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.^[6]

The tuberomammillary nucleus is a histaminergic nucleus that strongly regulates the sleep-wake cycle.^[7] H₁-antihistamines that cross the blood-brain barrier inhibit H₁ receptor activity on neurons that project from the tuberomammillary nucleus. This action is responsible for the drowsiness effect associated with these drugs.

References

^ "Human PubMed Reference:".
^ "Mouse PubMed Reference:".
^ 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.
^ 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.
^ ^a ^b 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
^ 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.
^ 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.

External links

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

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English Journal

Central histaminergic transmission modulates the ethanol induced anxiolysis in mice.

Verma L1, Jain NS2.
Behavioural brain research.Behav Brain Res.2016 Oct 15;313:38-52. doi: 10.1016/j.bbr.2016.07.012. Epub 2016 Jul 9.
Intrigued by the report demonstrating an increase in brain histamine levels by ethanol administration and central histamine transmission to affect the anxiety related behaviors, the present study examined the permissive role of central histaminergic transmission in the acute anxiolytic-like effect o
PMID 27401108

Histamine regulates murine primary dendritic cell functions.

Schenk H1, Neumann D1, Kloth C1,2.
Immunopharmacology and immunotoxicology.Immunopharmacol Immunotoxicol.2016 Oct;38(5):379-384. Epub 2016 Aug 10.
OBJECTIVE AND DESIGN: The modulation of antigen uptake and activation of dendritic cells (DCs) by histamine may function as a regulator of inflammation. Therefore, we sought to determine the impact of histamine on antigen uptake by and activation of murine DCs.MATERIAL AND METHODS: DCs from spleen a
PMID 27560832

Biomimetic contact lenses eluting olopatadine for allergic conjunctivitis.

González-Chomón C1, Silva M2, Concheiro A1, Alvarez-Lorenzo C3.
Acta biomaterialia.Acta Biomater.2016 Sep 1;41:302-11. doi: 10.1016/j.actbio.2016.05.032. Epub 2016 May 21.
Combination of the ability of contact lenses (CLs) to act as a physical barrier against airborne antigen and to serve as a sustained depot of antihistaminic drugs may improve the efficiency of treatments of some ocular allergic diseases. The aim of this work was to develop CLs that exhibit affinity
PMID 27221794

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. … Hepatic STAT3 phosphorylation after histidine ICV administration was attenuated in histamine H1 receptor knockout (Hrh1KO) mice but not in neuron-specific insulin receptor knockout (NIRKO) mice. …
NAID 120005334015

Central role of the exchange factor GEF-H1 in TNF-α–induced sequential activation of Rac, ADAM17/TACE, and RhoA in tubular epithelial cells

Waheed Faiza,Dan Qinghong,Amoozadeh Yasaman,Zhang Yuqian,Tanimura Susumu,Speight Pam,Kapus András,Szászi Katalin
Molecular Biology of the Cell 24(7), 1068-1082, 2013-04-01
… Transactivation of the epidermal growth factor receptor (EGFR) by tumor necrosis factor-α (TNF-α) is a key step in mediating RhoA activation and cytoskeleton and junction remodeling in the tubular epithelium. … TNF-α stimulates both Rac and RhoA through the guanine nucleotide exchange factor (GEF)-H1 but by different mechanisms. …
NAID 120005231330

Monitoring Genetic Diversity of Influenza A(H1N1)pdm09 Virus Circulating during the Post-Pandemic Period in Turkey

Guldemir Dilek,Kalaycioglu Atila T.,Altas A. Basak,Korukluoglu Gulay,Durmaz Riza
Japanese Journal of Infectious Diseases 66(4), 299-305, 2013
… The aimes of the present study were to monitor genetic alterations in the hemagglutin (HA) gene and oseltamivir resistance-related alterations in the neuraminidase (NA) gene of influenza A(H1N1)pdm09 viral isolates detected during the post-pandemic period in Turkey. … A total of 2601 clinical specimens obtained from suspected cases of influenza A(H1N1)pdm09 viral infections were analyzed by real-time reverse transcription polymerase chain reaction. …
NAID 130003381692

Related Pictures

★リンクテーブル★

リンク元	「H1受容体」「H1レセプター」
拡張検索	「histamine H1 receptor antagonist」
関連記事	「H1」「H」

「H1受容体」

HRH1
Available structures
PDB	Ortholog search: PDBe RCSB
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: 3269
Gene ontology
Molecular function	• histamine receptor activity; • signal transducer activity; • G-protein coupled receptor activity;
Cellular component	• integral component of membrane; • nucleoplasm; • membrane; • integral component of plasma membrane; • plasma membrane; • cytoplasm;
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 synaptic transmission; • inflammatory response; • visual learning; • signal transduction; • memory; • positive regulation of vasoconstriction;
	Sources:Amigo / QuickGO
RNA expression pattern
	; ;
	More reference expression data
Orthologs
	3269
	15465
	ENSG00000196639
	ENSMUSG00000053004
	P35367
	P70174
	NM_000861; NM_001098211; NM_001098212; NM_001098213
NM_001252642; NM_001252643; NM_008285; NM_001317124; NM_001317125;
	NM_001317126
	NP_000852.1; NP_001091681.1; NP_001091682.1; NP_001091683.1
NP_001239571.1; NP_001239572.1; NP_032311.2; NP_001304053.1; NP_001304054.1;
	NP_001304055.1
	Wikidata
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