ALIASES HRH1, H1-R, H1R, HH1R, hisH1, histamine receptor H1
EXTERNAL IDS OMIM: 600167 MGI: 107619 HomoloGene: 668 GeneCards: HRH1
GENE LOCATION (HUMAN)
BAND 3p25.3 START 11,137,093 bp
END 11,263,557 bp
GENE LOCATION (MOUSE)
BAND 6 E36 53.05 cM START 114,397,936 bp
END 114,483,296 bp
RNA EXPRESSION PATTERN
More reference expression data
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
SPECIES HUMAN MOUSE
NM_000861 NM_001098211 NM_001098212 NM_001098213
NM_001252642 NM_001252643 NM_008285 NM_001317124 NM_001317125
NP_000852 NP_001091681 NP_001091682 NP_001091683
NP_001239571 NP_001239572 NP_001304053 NP_001304054 NP_001304055
LOCATION (UCSC) Chr 3: 11.14 – 11.26 Mb Chr 3: 114.4 – 114.48 Mb
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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 (Gq) 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) and used to discover new histamine H1 receptor ligands in structure-based virtual screening studies.
* 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 H1 receptor as well as by agonists that bind at the receptor. H1-antihistamines have been shown to attenuate NF-κB expression and mitigate certain inflammatory processes in associated cells.
The tuberomammillary nucleus is a histaminergic nucleus that strongly regulates the sleep-wake cycle. 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.
* Antihistamine – H1-receptor antagonists
* ^ A B C GRCh38:
* ^ 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.
* 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). "