Histamine receptor

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:

Comparison

Histamine receptors
ReceptorMechanismFunctionAntagonists
H1 Gq
H2 Gs
↑ cAMP2+
H3 Gi
H4 Gi

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. ↑ 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.
  2. ↑ 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.
  • "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)
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