HRH2 Membrane Protein Introduction

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 G_s, and It is a potent stimulant of cAMP production.

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

1. Adelborg K., et al. Use of histamine H2 receptor antagonists and outcomes in patients with heart failure: a nationwide population-based cohort study. Clin Epidemiol. 2018, 10:521-530. PubMed ID: 29765253
   
   

   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.

2. Saheera S., et al. Histamine-2 receptor antagonist famotidine modulates cardiac stem cell characteristics in hypertensive heart disease. PeerJ. 2017, 5:e3882. PubMed ID: 29038754
   
   

   Authors in this group suggested that the histamine 2 receptor antagonist modulated cardiac stem cells characteristics, in addition to being cardioprotective.

3. Kennedy L., et al. Blocking H1/H2 histamine receptors inhibits damage/fibrosis in Mdr2_-/- mice and human cholangiocarcinoma tumorigenesis. Hepatology. 2018. PubMed ID: 29601088
   
   

   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.

4. Chaudhary A., et al. Docking-based screening of Ficus religiosa phytochemicals as inhibitors of human histamine H2 receptor. Pharmacogn Mag. 2017, 13(Suppl 3):S706-S714. PubMed ID: 29142437
   
   

   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.

5. Patel K. S., et al. Renal transplant acute rejection with lower mycophenolate mofetil dosing and proton pump inhibitors or histamine-2 receptor antagonists. Pharmacotherapy. 2017, 37(12):1507-1515. PubMed ID: 28976570
   
   

   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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