Histamine H2 receptor

H₂ receptors are a type of histamine receptor found in many parts of the anatomy of humans and other animals. They are positively coupled to adenylate cyclase via G_s alpha subunit. It is a potent stimulant of cAMP production, which leads to activation of protein kinase A. PKA functions to phosphorylate certain proteins, affecting their activity. The drug betazole is an example of a histamine H₂ receptor agonist.

Function

Histamine is a ubiquitous messenger molecule released from mast cells, enterochromaffin-like cells, and neurons. Its various actions are mediated by histamine receptors H₁, H₂, H₃ and H₄. The histamine receptor H₂ belongs to the rhodopsin-like family of G protein-coupled receptors. It is an integral membrane protein and stimulates gastric acid secretion. It also regulates gastrointestinal motility and intestinal secretion and is thought to be involved in regulating cell growth and differentiation. Histamine may play a role in penile erection.

Tissue distribution

Histamine H₂ receptors are expressed in the following tissues:

Peripheral tissues

• Gastric parietal cells (oxyntic cells)
• Vascular smooth muscle
• Neutrophils
• Mast cells
• Heart
• Genitourinary system (uterus, bladder)

Central nervous system tissues

• Caudate–putamen
• Cerebral cortex (external layers)
• Hippocampal formation
• Dentate nucleus of the cerebellum

Physiological responses

Activation of the H₂ receptor results in the following physiological responses:

• Stimulation of gastric acid secretion (Target of anti-histaminergics (H₂ receptors) for peptic ulcer disease and GERD)
• Smooth muscle relaxation (Experimental histamine H₂ receptor agonist used for asthma and COPD)
• Inhibit antibody synthesis, T-cell proliferation and cytokine production
• Vasodilation – PKA activity causes phosphorylation of MLCK, decreasing its activity, resulting in MLC of myosin being dephosphorylated by MLCP and thus inhibiting contraction. The smooth muscle relaxation leads to vasodilation.
• Inhibition of neutrophil activation and chemotaxis

See also

• H₂-receptor antagonist
• Histamine H₁-receptor
• Histamine H₃-receptor
• Histamine H₄-receptor

External links

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