Reactome | HRH2 binds HRH2 antagonists

HRH2 binds HRH2 antagonists

Stable Identifier

R-HSA-9692738

Type

Reaction [binding]

Species

Homo sapiens

Compartment

plasma membrane, extracellular region

ReviewStatus

5/5

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Signal Transduction (Homo sapiens)

- Signaling by GPCR (Homo sapiens)
  - GPCR ligand binding (Homo sapiens)
    - Class A/1 (Rhodopsin-like receptors) (Homo sapiens)
      - Amine ligand-binding receptors (Homo sapiens)
        
        Histamine receptors (Homo sapiens)
        
        HRH2 binds HRH2 antagonists (Homo sapiens)

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When bound to its endogenous ligand histamine, the histamine H2 receptor (HRH2) mediates mediates gastric acid secretion, gastrointestinal motility and intestinal secretion. HRH2 is also thought to be involved in regulating cell growth and differentiation (Panula et al. 2015). The HRH2 antagonists cimetidine (Black et al. 1972, Ganellin 1981), ranitidine (Brogden et al. 1982), nizatidine (Price & Brogden 1988) and famotidine (Campoli-Richards & Clissold 1986) are well established treatments (Baker et al. 2008) for patients presenting with dyspepsia, gastric or duodenal ulcers, or gastroesophageal reflux disease (Sigterman et al. 2013).

Literature References

PubMed ID	Title	Journal	Year
18157166	A study of antagonist affinities for the human histamine H2 receptor Baker, JG	Br. J. Pharmacol.	2008
4401751	Definition and antagonism of histamine H 2 -receptors Durant, CJ, BLACK, JW, Parsons, EM, Ganellin, CR, Duncan, WA	Nature	1972
6120235	1980 Award in Medicinal Chemistry: Medicinal chemistry and dynamic structure-activity analysis in the discovery of drugs acting at histamine H2 receptors Ganellin, R	J. Med. Chem.	1981