Introduction of HRH2
Histamine H2 receptor (H2R or HRH2), alternatively known as Gastric receptor I, is an integral membrane protein, in human is encoded by the HRH2 gene. It is recognized as a histamine receptor belonging to the family 1 of G protein-coupled receptors and is predominantly expressed in gastric parietal cells, on vascular smooth muscle, neutrophils, in the heart, and in the central nervous system. HRH2 is positively coupled to adenylate cyclase via Gs, and It is a potent stimulant of cAMP production.
|Basic Information of HRH2|
|Protein Name||Histamine H2 receptor|
|Organism||Homo sapiens (Human)|
Function of HRH2 Membrane Protein
HRH2 is activated by endogenous histamine, which is a ubiquitous messenger molecule that is released from enterochromaffin-like cells, mast cells, and neurons. Activation of the HRH2 stimulates gastric acid secretion, which indicates the potential therapeutical target of anti-HRH2 for peptic ulcer disease and GERD (gastro-esophageal reflux disease). It also modulates gastrointestinal motility and intestinal secretion and is supposed to be involved in regulating cell growth and differentiation. HRH2 is a potent stimulant of cAMP production, which leads to activation of PKA (protein kinase A). PKA activity leads to phosphorylation of MLCK, reducing its activity, causing MLC of myosin being dephosphorylated by MLCP and thus inhibiting contraction. In addition, HRH2 is also involved in the suppression of several immune functions, such as the inhibition of neutrophil activation and chemotaxis. Some studies also report that HRH2 blockers are sufficed to exert powerful neuroprotective effects in spinal cord trauma.
Fig.1 Structure of family 1 G protein-coupled receptors membrane protein.
Application of HRH2 Membrane Protein in Literature
This study was carried out to investigate the potential effectiveness of histamine H2 receptor antagonists (H2RAs) in humans with heart failure. The findings indicated that in patients with heart failure, H2RA initiation was associated with 15%-20% lower mortality than PPI initiation.
Authors in this group suggested that the histamine 2 receptor antagonist modulated cardiac stem cells characteristics, in addition to being cardioprotective.
In this article, the results showed that inhibition of H1/H2HR reversed PSC (primary sclerosing cholangitis)-associated damage and decreased CCA (cholangiocarcinoma) growth, angiogenesis, and EMT; because PSC patients were at risk of developing CCA, using HR blockers may be therapeutic for these diseases.
This study was performed to screen antiulcer compounds from F. religiosa. The data showed that Lanosterol and α-amyrin may be a suitable therapeutic agent against histamine H2 receptor. This study facilitated initiation of the herbal drug discovery process for the antiulcer activity.
The purpose of this study was to evaluate clinical outcomes in renal transplant recipients receiving a lower MMF dose than previously studied (1.5 g/day) and either a PPI or histamine-2 receptor antagonist (H2RA). The results of the article showed that subjects on a PPI compared to an H2RA were not at increased risk of acute rejection within 1 year posttransplantation.
HRH2 Preparation Options
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