HRH1 Membrane Protein Introduction

Introduction of HRH1

Histamine H1 receptor (H1R or HRH1), is an integral membrane protein which in human is encoded by HRH1 gene. It is recognized as a histamine receptor belonging to the family of rhodopsin-like G-protein-coupled receptors and is predominantly expressed in smooth muscles, on vascular endothelial cells, in the heart, and in the central nervous system. This receptor is activated by the biogenic amine histamine. HRH1 is linked to an intracellular G-protein (Gq) that activates phospholipase C and the inositol triphosphate (IP3) signaling pathway.

Function of HRH1 Membrane Protein

HRH1 or H1R is activated by endogenous histamine, which is a ubiquitous messenger molecule that is released from enterochromaffin-like cells, mast cells, and neurons. In vascular endothelial cells, stimulation of H1Rs results in the synthesis and release of several neurochemicals and neuromodulators including platelet-activating factor, prostacyclin, and nitric oxide (NO). In addition, stimulation of the H1 receptor leads to changes in vascular permeability, particularly the postcapillary venule as a consequence of endothelial cell contraction, which due to contraction of terminal venules, the release of catecholamine from adrenal medulla, and neurotransmission in the central nervous system. The stimulation of H1R-induced contraction is mediated by inositol 1,4,5-triphosphate-induced mobilization of intracellular calcium. It has been reported to be associated with multiple processes, such as memory and learning, circadian rhythm, and thermoregulation. It is also known to be involved in the pathophysiology of allergic diseases such as asthma, atopic dermatitis, anaphylaxis, and allergic rhinitis. Thus, H1R has been regarded as a useful target for developing anti-allergy drugs.

Fig.1 Structure of H1R membrane protein.

Application of HRH1 Membrane Protein in Literature

1. Morioka E., et al. Histamine regulates molecular clock oscillations in human retinal pigment epithelial cells via H1 receptors. Front Endocrinol (Lausanne). 2018, 9:108. PubMed ID: 29615980
   
   

   Authors in this group focused on regulatory mechanisms of the circadian clocks in vertebrate eyes. And the present results indicated histaminergic control of the molecular clock via H1R in retinal pigment epithelial cells.

2. Stoddart L. A., et al. Development of novel fluorescent histamine H1-receptor antagonists to study ligand-binding kinetics in living cells. Sci Rep. 2018, 8(1):1572. PubMed ID: 29371669
   
   

   This study was carried out to investigate the particular clinical utility of H1R in allergic rhinitis and urticaria. The findings indicated that the kinetics of these fluorescent ligands could also be monitored in membrane preparations providing new opportunities for future drug discovery applications.

3. Solís K. H., et al. The histamine H1 receptor participates in the increased dorsal telencephalic neurogenesis in embryos from Diabetic rats. Front Neurosci. 2017, 11:676. PubMed ID: 29311766
   
   

   In this article, the participation of histamine and H1R on the increased dorsal telencephalic neurogenesis was explored. This study opened a new perspective on the participation of HA and H1R receptor in early corticogenesis in health and disease.

4. Veglia E., et al. Histamine type 1-receptor activation by low dose of histamine undermines human glomerular slit diaphragm integrity. Pharmacol Res. 2016, 114:27-38. PubMed ID: 27751877
   
   

   The data demonstrated that histamine, via the H1R, modified SD morphological and functional integrity, in part, by decreasing the expression of ZO-1 and P-cadherin.

5. Lieb S., et al. Label-free versus conventional cellular assays: Functional investigations on the human histamine H1 receptor. Pharmacol Res. 2016, 114:13-26. PubMed ID: 27751876
   
   

   The results of this article confirmed the value of the label-free methods, DMR and ECIS, for the characterization of H1R ligands. Both noninvasive techniques were complementary to each other, but cannot fully replace reductionist signaling pathway focused assays.

HRH1 Preparation Options

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