Abstract
This review addresses pharmacological, structural and functional relationships among H2-histamine receptors and H1-histamine receptors in the mammalian heart. The role of both receptors in the regulation of force and rhythm, including their electrophysiological effects on the mammalian heart, will then be discussed in context. The potential clinical role of cardiac H2-histamine-receptors in cardiac diseases will be examined. The use of H2-histamine receptor agonists to acutely increase the force of contraction will be discussed. Special attention will be paid to the potential role of cardiac H2-histamine receptors in the genesis of cardiac arrhythmias. Moreover, novel findings on the putative role of H2-histamine receptor antagonists in treating chronic heart failure in animal models and patients will be reviewed. Some limitations in our biochemical understanding of the cardiac role of H2-histamine receptors will be discussed. Recommendations for further basic and translational research on cardiac H2-histamine receptors will be offered. We will speculate whether new knowledge might lead to novel roles of H2-histamine receptors in cardiac disease and whether cardiomyocyte specific H2-histamine receptor agonists and antagonists should be developed.
Highlights
Many reviews on histamine receptors have been published (Marone et al, 2014; Panula et al, 2015; Marino and Levi 2018; Zhang et al, 2018), few up-to-date reviews have focused on cardiac histamine receptors
The present review study focuses on H2-histamine receptors because they are relevant for the positive inotropic and positive chronotropic effects of histamine in the human heart
These results indicate that H2-histamine receptors couple in the heart via stimulatory GTP-binding proteins to activate adenylyl cyclase and via inhibitory GTP-binding proteins to inhibit the activity of adenylyl cyclase (Figure 2)
Summary
Many reviews on histamine receptors have been published (Marone et al, 2014; Panula et al, 2015; Marino and Levi 2018; Zhang et al, 2018), few up-to-date reviews have focused on cardiac histamine receptors. The most recent review was published by Hattori et al, in 2017. The present work reviews the most recent works on this topic in the relevant literature. The “histamine” molecule was named by Fühner (1912) based on its chemical structure, which is β-imidazolyl-amin(e). Histamine was first synthesised by two chemists from Freiburg im Breisgau using a battery of structurally similar compounds (Windaus and Vogt 1907) without studying their presence or function in animals. Histamine was shown to increase the cardiac force of contraction, to increase the beating rate of the heart and to induce
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have