ヒスタミン受容体、ヒスタミンレセプター

WordNet

amine formed from histidine that stimulates gastric secretions and dilates blood vessels; released by the human immune system during allergic reactions
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

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ヒスタミン(子宮収縮・血圧降下の薬)
=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）』「2015/08/31 03:14:50」(JST)

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The histamine receptors are a class of G protein–coupled receptors with histamine as their endogenous ligand.^[1]

There are four known histamine receptors:

H₁ receptor
H₂ receptor
H₃ receptor
H₄ receptor

Comparison

Histamine receptors
Receptor	Mechanism	Function	Antagonists
H₁	G_q	ileum contraction modulate circadian cycle itching systemic vasodilatation bronchoconstriction (allergy-induced asthma)	H₁-receptor antagonists Diphenhydramine Loratadine Cetirizine Fexofenadine Clemastine
H₂	G_s ↑ Ca²⁺	speed up sinus rhythm Stimulation of gastric acid secretion Smooth muscle relaxation Inhibit antibody synthesis, T-cell proliferation and cytokine production	H₂-receptor antagonists Ranitidine Cimetidine Famotidine Nizatidine
H₃	G_i	Decrease Acetylcholine, Serotonin and Norepinephrine Neurotransmitter release in CNS Presynaptic autoreceptors	H₃-receptor antagonists ABT-239 Ciproxifan Clobenpropit Thioperamide
H₄	G_i	mediate mast cell chemotaxis.^[2]	H₄-receptor antagonists Thioperamide JNJ 7777120

There are several splice variants of H₃ present in various species. Though all of the receptors are 7-transmembrane g protein coupled receptors, H₁ and H₂ are quite different from H₃ and H₄ in their activities. H₁ causes an increase in PIP₂ hydrolysis, H2 stimulates gastric acid secretion, and H3 mediates feedback inhibition of histamine.

References

^ Hill SJ, Ganellin CR, Timmerman H, Schwartz JC, Shankley NP, Young JM, Schunack W, Levi R, Haas HL (1997). "International Union of Pharmacology. XIII. Classification of histamine receptors". Pharmacol. Rev. 49 (3): 253–78. PMID 9311023.
^ Hofstra CL, Desai PJ, Thurmond RL, Fung-Leung WP (2003). "Histamine H₄ receptor mediates chemotaxis and calcium mobilization of mast cells". J. Pharmacol. Exp. Ther. 305 (3): 1212–21. doi:10.1124/jpet.102.046581. PMID 12626656.

External links

"Histamine Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
Holger Stark: Histamine Receptors, BIOTREND Reviews No. 01, November 2007
The Histamine Receptor
Histamine Receptor at the US National Library of Medicine Medical Subject Headings (MeSH)

UpToDate Contents

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1. 肥満細胞由来のメディエーター mast cell derived mediators
2. 制吐剤の特性 characteristics of antiemetic drugs
3. アレルギーのin vitro検査の概要 overview of in vitro allergy tests
4. 胃酸分泌の生理学 physiology of gastric acid secretion
5. 肝性脳症：病因 hepatic encephalopathy pathogenesis

English Journal

Efficacy of leukotriene receptor antagonist with anti-H1 receptor antagonist plus anti-H2 receptor antagonist for treatment of refractory chronic idiopathic urticaria.

Wan KS1, Chang YS.
The Journal of dermatological treatment.J Dermatolog Treat.2014 Dec;25(6):459-61. doi: 10.3109/09546634.2013.849791. Epub 2013 Nov 5.
BACKGROUND: The efficacy of the combination of leukotriene receptor antagonist (LRA) and H1 antihistamine was similar to the synergistic regimen of H1 and H2 antihistamine for treatment of chronic idiopathic urticaria (CIU). However, the effective rates of these two regimens were only 53.3% and 63.3
PMID 24192062

Disruption of histamine H2 receptor slows heart failure progression through reducing myocardial apoptosis and fibrosis.

Zeng Z1, Shen L1, Li X1, Luo T1, Wei X1, Zhang J1, Cao S1, Huang X1, Fukushima Y2, Bin J1, Kitakaze M, Xu D1, Liao Y1.
Clinical science (London, England : 1979).Clin Sci (Lond).2014 Oct 1;127(7):435-48. doi: 10.1042/CS20130716.
Histamine H2 receptor (H2R) blockade has been reported to be beneficial for patients with chronic heart failure (CHF), but the mechanisms involved are not entirely clear. In the present study, we assessed the influences of H2R disruption on left ventricular (LV) dysfunction and the mechanisms involv
PMID 24655024

Histamine regulates the inflammatory response of the tunicate Styela plicata.

García-García E1, Gómez-González NE1, Meseguer J1, García-Ayala A1, Mulero V2.
Developmental and comparative immunology.Dev Comp Immunol.2014 Oct;46(2):382-91. doi: 10.1016/j.dci.2014.05.017. Epub 2014 Jun 2.
Histamine is stored inside hemocytes of the tunicate Styela plicata (Chordata, Tunicata, Ascidiacea), but no evidence on its role in the regulation of the immune response of this species has been reported. We examined whether histamine participated in the regulation of inflammation and host defense
PMID 24892817

Japanese Journal

Pharmacology : Vasomotor Effects of Acetylcholine, Bradykinin, Noradrenaline, 5-Hydroxytryptamine, Histamine and Angiotensin Ⅱ on the Mouse Basilar Artery

ISLAM Md. Zahorul,WATANABE Yutaka,NGUYEN Ha Thi Thanh [他]
The journal of veterinary medical science 76(10), 1339-1345, 2014-10
NAID 40020245132

30aPS-115 ヒスタミン受容体の分子内情報伝達機構に関する理論的研究(30aPS 領域12ポスターセッション,領域12(ソフトマター物理・化学物理・生物物理))

石井裕子,石倉孝一,倭剛久
日本物理学会講演概要集 69(1-2), 426, 2014-03-05
NAID 110009835080

Molecular Determinants Responsible for Sedative and Non-sedative Properties of Histamine H₁-Receptor Antagonists

Uesawa Yoshihiro,Hishinuma Shigeru,Shoji Masaru
Journal of pharmacological sciences 124(2), 160-168, 2014-02
NAID 40019992567

Related Pictures

★リンクテーブル★

リンク元	「ヒスタミン受容体」「ヒスタミンレセプター」

「ヒスタミン受容体」

　　[★]

英: histamine receptor
関: ヒスタミン、抗ヒスタミン薬、受容体

7回膜貫通型受容体。Gタンパク質共役型受容体。

H1R：平滑筋、血管内皮、神経→血管拡張、血管透過性↑、気管収縮、知覚神経刺激によるかゆみ・痛み
H2R：胃、心臓、中枢、リンパ→胃酸分泌促進
H3R：中枢、気道、消化管。ヒスタミン合成やNeuro transmitterの遊離抑制
H4R：リンパ球をはじめとする免疫炭層細胞、骨髄、脾臓。機能は不明

H1Rはα1受容体と似ている。Gαqと共役している
H2Rはβ1受容体と似ている。Gαsと共役している