HRH3 Membrane Protein Introduction

Introduction of HRH3

Histamine H3 receptor (H3R or HRH3), is an integral membrane protein which in human is encoded by HRH3 gene. It is recognized as a histamine receptor belonging to the family of rhodopsin-like G-protein-coupled receptors. H3Rs are primarily expressed in the central nervous system and to a lesser extent the peripheral nervous system. The gene sequence for H3Rs expresses only about 22% and 20% homology with H1Rs and H2Rs respectively. Among all the four histamine receptors, H3R is distinguished for its almost exclusive expression in the nervous system and the large variety of isoforms generated by alternative splicing of the corresponding mRNA.

Function of HRH3 Membrane Protein

Similar with all histamine receptors, H3R is coupled to the Gi G-protein, so it results in inhibition of the formation of cAMP. H3R acts as autoreceptors on histaminergic terminals and heteroreceptors inhibiting neurotransmitter release on other types of terminals, and also controls histamine turnover by feedback inhibition of histamine synthesis and release. H3Rs have also been indicated to presynaptically inhibit the release of a number of other neurotransmitters (i.e. it acts as an inhibitory heteroreceptor) including, but probably not limited to dopamine, GABA, acetylcholine, noradrenaline, histamine, and serotonin. Besides, H3Rs are considered to play a part in the control of satiety. Since its involvement in the neuronal mechanism behind many cognitive H3R-disorders and especially its location in the central nervous system, H3Rs has attracted great interests as a therapeutic target for the treatment of several important neurologic and psychiatric disorders, such as Alzheimer and Parkinson diseases, Gilles de la Tourette syndrome, and addiction.

Fig.1 H3-receptor activation can result in the modulation of diverse signaling pathways. (Leurs, 2005)

Application of HRH3 Membrane Protein in Literature

1. Ito T., et al. Histamine H3 receptor density is negatively correlated with neural activity related to working memory in humans. EJNMMI Res. 2018, 8(1):48. PubMed ID: 29900481
   
   

   The findings of this article elucidated the role of H3 receptors in working memory and indicated the potential of H3 receptors as a therapeutic target for the cognitive impairments associated with neuropsychiatric disorders.

2. Kotańska M., et al. The histamine H3 receptor inverse agonist pitolisant reduces body weight in obese mice. Naunyn Schmiedebergs Arch Pharmacol. 2018. PubMed ID: 29802412
   
   

   This study was carried out to investigate the influence of a histamine H3 receptor antagonist/inverse agonist in the high-fat and high-sugar diet-induced obesity model in mice and indicated that it had a favorable influence of body weight and improved glucose tolerance and the lipid profile in obese mice.

3. Alachkar A., et al. Anticonvulsant evaluation of novel non-imidazole histamine H3R antagonists in different convulsion models in rats. Pharmacol Biochem Behav. 2018, 170:14-24. PubMed ID: 29729290
   
   

   This article demonstrated the potential of non-imidazole H3R antagonists as novel antiepileptic drugs (AEDs) either for single use or in addition to currently available epilepsy medications.

4. Liu Y., et al. Visualization of the activation of the histamine H3 receptor (H3R) using novel fluorescence resonance energy transfer biosensors and their potential application to the study of H3R pharmacology. FEBS J. 2018. PubMed ID: 29701013
   
   

   Authors of this article have built an H3R biosensor which can visualize the activation of receptor through real-time structure changes and which can obtain pharmacological kinetic data at the same time. The FRET (fluorescence resonance energy transfer) signals may allow the sensor to become a useful tool for screening compounds and optimizing useful ligands.

5. Eissa N., et al. The histamine H3 receptor antagonist DL77 ameliorates MK801-induced memory deficits in rats. Front Neurosci. 2018, 12:42. PubMed ID: 29483860
   
   

   The results indicated the potential involvement of H3Rs in modulating neurotransmitters related to neurodegenerative disorders, e.g., Alzheimer disease.

HRH3 Preparation Options

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Reference

1. Leurs R., et al. (2005). The histamine H 3 receptor: from gene cloning to H 3 receptor drugs. Nature reviews Drug discovery. 4(2), 107.

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