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Target intelligence / Profile preview
Histamine Receptor H2 (H2)
- Target
- H2
- Molecular classification
- GPCR, G protein-coupled receptor, Receptor
01
Overview
The histamine receptor H2 (H2) is a member of the rhodopsin-like family of G protein-coupled receptors (GPCRs). It primarily mediates the effects of histamine in stimulating gastric acid secretion, but also plays roles in regulating gastrointestinal motility, intestinal secretion, and possibly cell growth and differentiation.
- Other names
- HRH2
02
Mechanism of action
Upon activation by ligand binding (e.g., histamine), the receptor stimulates adenylate cyclase via Gs proteins → increases intracellular cAMP → activates protein kinase A → downstream phosphorylation events affecting cellular activity such as acid secretion from parietal cells.
03
Biological functions
Signal transductionRegulation of gastric acid secretionRegulation of gastrointestinal motilityRegulation of intestinal secretionsCell growth regulationCell differentiation
04
Disease associations
Gastroesophageal reflux disease (GERD)Peptic ulcersZollinger-Ellison syndromeAcid-related diseases
05
Safety considerations
Potential drug interactions with H2 receptor antagonistsRebound acid hypersecretion upon discontinuation of H2 receptor antagonists
06
Interacting drugs
Histamine
4 more in the full profile.
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