请输入您要查询的百科知识:

 

词条 Histamine receptor
释义

  1. Comparison

  2. References

  3. External links

The histamine receptors are a class of G protein–coupled receptors which bind histamine as their primary 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 Gq
  • ileum contraction
  • modulate circadian cycle
  • itching
  • systemic vasodilatation
  • bronchoconstriction (allergy-induced asthma)
  • H1-receptor antagonists
    • Diphenhydramine
    • Loratadine
    • Cetirizine
    • Fexofenadine
    • Clemastine
    • Rupatadine
H2 Gs
↑ cAMP2+
  • 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 Gi
  • Decrease Acetylcholine, Serotonin and Norepinephrine Neurotransmitter release in CNS
  • Presynaptic autoreceptors
  • H3-receptor antagonists
    • ABT-239
    • Ciproxifan
    • Clobenpropit
    • Thioperamide
H4 Gi
  • 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

1. ^{{cite journal |vauthors=Hill SJ, Ganellin CR, Timmerman H, Schwartz JC, Shankley NP, Young JM, Schunack W, Levi R, Haas HL | title = International Union of Pharmacology. XIII. Classification of histamine receptors | journal = Pharmacol. Rev. | volume = 49 | issue = 3 | pages = 253–78 | year = 1997 | pmid = 9311023 | doi = | url = http://pharmrev.aspetjournals.org/cgi/content/abstract/49/3/253 }}
2. ^{{cite journal |vauthors=Hofstra CL, Desai PJ, Thurmond RL, Fung-Leung WP | title = Histamine H4 receptor mediates chemotaxis and calcium mobilization of mast cells | journal = J. Pharmacol. Exp. Ther. | volume = 305 | issue = 3 | pages = 1212–21 | year = 2003 | pmid = 12626656 | doi = 10.1124/jpet.102.046581 }}

External links

  • {{cite web | url = http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1287 | title = Histamine Receptors | accessdate = | date = | format = | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | pages = | language = | archiveurl = | archivedate = | quote = }}
  • Holger Stark: Histamine Receptors, BIOTREND Reviews No. 01, November 2007
  • The Histamine Receptor
  • {{MeshName|Histamine+Receptor}}
{{G protein-coupled receptors}}{{Histaminergics}}

2 : Integral membrane proteins|Histamine receptors

随便看

 

开放百科全书收录14589846条英语、德语、日语等多语种百科知识,基本涵盖了大多数领域的百科知识,是一部内容自由、开放的电子版国际百科全书。

 

Copyright © 2023 OENC.NET All Rights Reserved
京ICP备2021023879号 更新时间:2024/9/29 17:35:33