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Histamine
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== Mechanism of action == In humans, histamine exerts its effects primarily by binding to [[G protein-coupled receptor|G protein-coupled]] [[histamine receptors]], designated H<sub>1</sub> through H<sub>4</sub>.<ref name="Histamine receptors" /> {{As of|2015}}, histamine is believed to activate ligand-gated chloride channels in the brain and intestinal epithelium.<ref name="Histamine receptors" /><ref name="FGID mast cell" /> {| class="wikitable" |+ Biological targets of histamine in the human body |- ! {{nowrap|[[G-protein coupled receptor]]}} !! Location !! Function !! <small>Sources</small> |- <!-- HRH1 --> | style="text-align:center" | [[Histamine H1 receptor|{{nowrap|Histamine H<sub>1</sub>}} receptor]] | style="vertical-align:top"| {{bull}}'''CNS''': Expressed on the [[dendrite]]s of the output neurons of the histaminergic [[tuberomammillary nucleus]], which projects to the [[Dorsal raphe nucleus|dorsal raphe]], [[locus coeruleus]], and additional structures.<br /> {{bull}}'''Periphery''': [[Smooth muscle]], [[endothelium]], [[mast cells]], sensory nerves | style="vertical-align:top"| {{bull}} '''CNS''': [[Sleep-wake cycle]] (promotes wakefulness), [[body temperature]], [[nociception]], [[endocrine system|endocrine homeostasis]], regulates [[appetite]], involved in cognition<br /> {{bull}}'''Periphery''': Causes [[bronchoconstriction]], bronchial [[smooth muscle]] contraction, urinary bladder contractions, [[vasodilation]], promotes hypernociception ([[visceral hypersensitivity]]), involved in [[itch|itch perception]] and [[urticaria]]. | <ref name="Histamine receptors" /><ref name="FGID mast cell">{{cite journal | vauthors = Wouters MM, Vicario M, Santos J | title = The role of mast cells in functional GI disorders | journal = Gut | volume = 65 | issue = 1 | pages = 155–68 | date = January 2016 | pmid = 26194403 | doi = 10.1136/gutjnl-2015-309151 | doi-access = free }}</ref><ref>{{cite journal | vauthors = Blandina P, Munari L, Provensi G, Passani MB | title = Histamine neurons in the tuberomamillary nucleus: a whole center or distinct subpopulations? | journal = Frontiers in Systems Neuroscience | volume = 6 | pages = 33 | year = 2012 | pmid = 22586376 | pmc = 3343474 | doi = 10.3389/fnsys.2012.00033 | doi-access = free }}</ref><ref name="Urinary Bladder">{{cite journal | vauthors = Stromberga Z, Chess-Williams R, Moro C | title = Histamine modulation of urinary bladder urothelium, lamina propria and detrusor contractile activity via H1 and H2 receptors | journal = Scientific Reports | volume = 9 | issue = 1 | pages = 3899 | date = March 2019 | pmid = 30846750 | pmc = 6405771 | doi = 10.1038/s41598-019-40384-1 | bibcode = 2019NatSR...9.3899S }}</ref><ref name="Histamine mediated autocrine signal">{{cite journal | vauthors = Pal S, Gasheva OY, Zawieja DC, Meininger CM, Gashev AA J | title = Histamine mediated autocrine signalling in mesenteric perilymphatic mast cells | journal = Am J Physiol Regul Integr Comp Physiol | volume = 318 | issue = 3 | pages = 590–604 | date = January 2020 | pmid = 31913658 | doi = 10.1152/ajpregu.00255.2019 | pmc = 7099465 | s2cid = 210119438 }}</ref> |- <!-- HRH2 --> | style="text-align:center" | [[Histamine H2 receptor|{{nowrap|Histamine H<sub>2</sub>}} receptor]] | style="vertical-align:top"| {{bull}}'''CNS''': [[Dorsal striatum]] ([[caudate nucleus]] and [[putamen]]), [[cerebral cortex]] (external layers), [[hippocampal formation]], [[dentate nucleus]] of the [[cerebellum]]<br /> {{bull}}'''Periphery''': Located on [[parietal cells]], [[vascular smooth muscle cells]], [[neutrophils]], [[mast cells]], as well as on cells in the [[heart]] and [[uterus]] | style="vertical-align:top"| {{bull}}'''CNS''': Not established (note: most known H<sub>2</sub> receptor ligands are unable to cross the [[blood–brain barrier]] in sufficient concentrations to allow for neuropsychological and behavioral testing)<br /> {{bull}}'''Periphery''': Primarily involved in vasodilation and stimulation of [[gastric acid]] secretion. Urinary bladder relaxation. Modulates gastrointestinal function. | <ref name="Histamine receptors" /><ref name="FGID mast cell" /><ref name="IUPHAR HRH2">{{cite web |title=H<sub>2</sub> receptor |url=http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=263 |work=IUPHAR/BPS Guide to Pharmacology |publisher=International Union of Basic and Clinical Pharmacology |access-date=20 March 2017 |vauthors=Maguire JJ, Davenport AP |date=29 November 2016 |url-status=dead |archive-url=https://web.archive.org/web/20170321084255/http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=263 |archive-date=21 March 2017 }}</ref><ref name="Histamine mediated autocrine signal"/> |- <!-- HRH3 --> | style="text-align:center" | [[Histamine H3 receptor|{{nowrap|Histamine H<sub>3</sub>}} receptor]] | Located in the [[central nervous system]] and to a lesser extent [[peripheral nervous system]] tissue | [[Autoreceptor]] and [[heteroreceptor]] functions: decreased [[neurotransmitter]] release of histamine, [[acetylcholine]], [[norepinephrine]], [[serotonin]]. Modulates nociception, gastric acid secretion, and food intake. | <ref name="Histamine receptors" /> |- <!-- HRH4 --> | style="text-align:center" | [[Histamine H4 receptor|{{nowrap|Histamine H<sub>4</sub>}} receptor]] | Located primarily on [[basophil]]s and in the [[bone marrow]]. It is also expressed in the [[thymus]], [[small intestine]], [[spleen]], and [[colon (anatomy)|colon]]. | Plays a role in mast cell [[chemotaxis]], itch perception, cytokine production and secretion, and visceral hypersensitivity. Other putative functions (e.g., inflammation, allergy, cognition, etc.) have not been fully characterized. || <ref name="Histamine receptors">{{cite journal | vauthors = Panula P, Chazot PL, Cowart M, Gutzmer R, Leurs R, Liu WL, Stark H, Thurmond RL, Haas HL | display-authors = 6 | title = International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors | journal = Pharmacological Reviews | volume = 67 | issue = 3 | pages = 601–55 | date = July 2015 | pmid = 26084539 | pmc = 4485016 | doi = 10.1124/pr.114.010249 }}</ref> |- ! scope="col" | [[Ligand-gated ion channel]] !! Location !! Function !! <small>Sources</small> |- | style="text-align:center" | {{nowrap|Histamine-gated}} {{nowrap|[[chloride channel]]}} | Putatively: CNS (hypothalamus, thalamus) and intestinal epithelium | Brain: Produces fast [[inhibitory postsynaptic potential]]s<br /> Intestinal epithelium: chloride secretion (associated with [[secretory diarrhea]]) | <ref name="Histamine receptors" /><ref name="FGID mast cell" /> |}
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