Igel, Patrick and Dove, Stefan and Buschauer, Armin (2010) Histamine H4 receptor agonists. Bioorganic & Medicinal Chemistry Letters 20 (24), pp. 7191-7199.
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Since its discovery ten years ago the histamine H4 receptor (H4R) has attracted attention as a potential drug target, for instance, for the treatment of inflammatory and allergic diseases. Potent and selective ligands including agonists are required as pharmacological tools to study the role of the H4R in vitro and in vivo. Many H4R agonists, which were identified among already known histamine receptor ligands, show only low or insufficient H4R selectivity. In addition, the investigation of numerous H4R agonists in animal models is hampered by species-dependent discrepancies regarding potencies and histamine receptor selectivities of the available compounds, especially when comparing human and rodent receptors. This article gives an overview about structures, potencies and selectivities of various compounds showing H4R agonistic activity and summarizes the structure-activity relationships of selected compound classes.
|Date:||15 December 2010|
|Institutions:||Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)|
|Projects:||GRK 760, Graduiertenkolleg Medizinische Chemie|
|Keywords:||H4 receptor selectivity; acylguanidines; arylbenzimidazoles; clozapine analogues; cyanoguanidines; indoles; oximes|
|Subjects:||500 Science > 570 Life sciences|
500 Science > 540 Chemistry & allied sciences
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||Yes|
|Owner:||Prof. Armin Buschauer|
|Deposited On:||18 Oct 2010 14:39|
|Last Modified:||17 Nov 2010 17:27|