Morpholine as a privileged structure: A review on the medicinal chemistry and pharmacological activity of morpholine containing bioactive molecules

AP Kourounakis, D Xanthopoulos… - Medicinal Research …, 2020 - Wiley Online Library
Morpholine is a heterocycle featured in numerous approved and experimental drugs as well
as bioactive molecules. It is often employed in the field of medicinal chemistry for its …

Histamine pharmacology: from Sir Henry Dale to the 21st century

E Tiligada, M Ennis - British Journal of Pharmacology, 2020 - Wiley Online Library
Histamine has been one of the most studied substances in medicine, playing a major role in
diverse (patho) physiological processes. It elicits its multifaceted modulatory functions by …

Histamine receptors and cancer pharmacology: an update

NA Massari, MB Nicoud… - British journal of …, 2020 - Wiley Online Library
In the present review, we will discuss the recent advances in the understanding of the role of
histamine and histamine receptors in cancer biology. The controversial role of the …

[HTML][HTML] NanoBRET binding assay for histamine H2 receptor ligands using live recombinant HEK293T cells

L Grätz, K Tropmann, M Bresinsky, C Müller… - Scientific Reports, 2020 - nature.com
Fluorescence/luminescence-based techniques play an increasingly important role in the
development of test systems for the characterization of future drug candidates, especially in …

[HTML][HTML] Alterations in histamine responses between juvenile and adult urinary bladder urothelium, lamina propria and detrusor tissues

Z Stromberga, R Chess-Williams, C Moro - Scientific Reports, 2020 - nature.com
Inflammatory mediators may have a role in various lower urinary tract disorders. Histamine is
known to induce significant increases in both the tension and frequency of spontaneous …

[HTML][HTML] Agonist Binding and G Protein Coupling in Histamine H2 Receptor: A Molecular Dynamics Study

M Conrad, CA Söldner, Y Miao, H Sticht - International Journal of …, 2020 - mdpi.com
The histamine H 2 receptor (H2R) plays an important role in the regulation of gastric acid
secretion. Therefore, it is a main drug target for the treatment of gastroesophageal reflux or …

Discovery of a G Protein-Biased Radioligand for the Histamine H2 Receptor with Reversible Binding Properties

K Tropmann, C Höring, N Plank… - Journal of Medicinal …, 2020 - ACS Publications
Currently employed histamine H2 receptor (H2R) radioligands possess several drawbacks,
for example, high non-specificity, insurmountable binding, or short half-life. We report the …

Human H1 receptor (HRH1) gene polymorphism is associated with the severity of side effects after desloratadine treatment in Chinese patients with chronic …

J Li, W Chen, C Peng, W Zhu, Z Liu, W Zhang… - The …, 2020 - nature.com
H1 nonsedating antihistamines, such as desloratadine, are first-line treatment options for
chronic spontaneous urticaria (CSU). However, desloratadine induces various degrees of …

[PDF][PDF] The clinical and psychopathological implications in the forms of hyperhistaminosis

G Perrotta - Online J Neuro Br Disord, 2020 - researchgate.net
The present work analyzes the clinical and psychopathological implications of
hyperhistaminosis, starting from the general consideration that, despite the recent scarcity of …

[HTML][HTML] Molecular dynamics of the histamine H3 membrane receptor reveals different mechanisms of GPCR signal transduction

LD Herrera-Zúñiga, LM Moreno-Vargas, L Ballaud… - Scientific reports, 2020 - nature.com
In this work, we studied the mechanisms of classical activation and inactivation of signal
transduction by the histamine H3 receptor, a 7-helix transmembrane bundle G-Protein …