Histamine Receptors: Ligand Design, Pharmacology, and Therapeutic Applications

Dear Colleagues,

Histamine receptors are one of the most studied G protein-coupled receptors (GPCRs) and play crucial roles in various physiological and pathophysiological conditions, including allergic reactions (H₁R), gastric acid secretion (H₂R), cognitive functions, and CNS disorders, by modulating histamine and other neurotransmitter release (H₃R) or inflammatory conditions (H₄R). Furthermore, multi-target directed ligands (MTDLs) have become a significant target for diseases with complex pathogenesis.

This Special Issue aims to discuss cutting-edge advancements in research on histamine receptors and the role of new biologically active agents in novel therapeutic strategies, thereby expanding the knowledge of medicinal chemistry. We would like to publish studies that contribute to ligand design, synthesis, and understanding of the relationship between structure and activity (SAR), mode of action, and therapeutic applications. We encourage scientists to share both original and computational results of their research, as well as comprehensive reviews and short communications concerning histamine receptors and their ligands in this Special Issue. Furthermore, we believe that our Special Issue will inspire the scientific community worldwide. The subtopics may include a wide range of topics, but are not limited to the following:

• Design, synthesis, and structural modification of histamine receptor ligands;
• SAR of the histamine ligands;
• Target-based drug discovery;
• Pharmacological or pharmacokinetic evaluation of novel potent lead compounds and biologically active molecules;
• Alternative therapeutics: novelty and hopes;
• Multifunctional histamine receptor ligands in medicinal chemistry;
• Molecular mechanisms underlying the pharmacological actions of histamine ligands;
• Computational studies of histamine ligands that provide insight into the SAR of the novel molecules.

Dr. Marek Staszewski
Prof. Dr. Krzysztof Walczyński
Guest Editors

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