Histamine Receptor Ligands in Medicinal Chemistry

Dear Colleagues,

Pharmacological studies have confirmed the existence of four histamine receptors. Histamine plays a pathophysiological role in allergy via H₁R and a key physiological role in the control of gastric acid secretion via H₂R. Both receptors remain valuable in the treatment of allergic diseases and duodenal ulcers. The marketed H₃R antagonist is useful in narcolepsy, but further studies are investigating the use of H₃R ligands in some CNS disorders, i.e., memory or learning deficits including Prader–Willi syndrome, or epilepsy and obesity, are investigated. H₄R ligands are promising compounds that act on the immune system and have the potential to be used in asthma and inflammation. Certain histamine receptor ligands with additional pharmacological targets modulate acetylcholine, dopamine, norepinephrine, serotonin, γ-aminobutyric acid, dopamine levels, and even breast cancer cell proliferation, often leading to the discovery of multipotent compounds. Histamine and its receptors continue to be of interest to medicinal chemists and pharmacologists, and the recently described crystal structure of H₃R may also increase the interest in the search for new ligands.

We encourage all scientists to contribute their research results on histamine receptors and their ligands to this Special Issue. Review papers are also welcome. The subtopics of a submitted manuscript may include, but are not limited to, the following:

• The discovery and structural modification of histamine receptor ligands;
• Target-based drug discovery;
• The pharmacological or pharmacokinetic evaluation of potent histamine receptors ligands;
• Alternative therapeutics: novelty and hopes;
• Multifunctional histamine receptor ligands in medicinal chemistry;
• Bio- and chemo-informatics, molecular modeling histamine receptors, and their ligands.

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

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