Histamine H4 receptor agonists

Since its discovery 10 years ago the histamine H(4) receptor (H(4)R) 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 t...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010-12, Vol.20 (24), p.7191-7199
Main Authors: IGEL, Patrick, DOVE, Stefan, BUSCHAUER, Armin
Format: Article
Language:English
Subjects:
Animals
Benzimidazoles - chemistry
Binding Sites
Biological and medical sciences
Clozapine - chemistry
Guanidines - chemistry
Histamine and antagonists. Allergy
Humans
Ligands
Medical sciences
Mice
Miscellaneous
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Oximes - chemistry
Pharmacology. Drug treatments
Receptors, G-Protein-Coupled - agonists
Receptors, G-Protein-Coupled - genetics
Receptors, G-Protein-Coupled - metabolism
Receptors, Histamine - genetics
Receptors, Histamine - metabolism
Receptors, Histamine H4
Structure-Activity Relationship
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Summary:Since its discovery 10 years ago the histamine H(4) receptor (H(4)R) 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 H(4)R in vitro and in vivo. Many H(4)R agonists, which were identified among already known histamine receptor ligands, show only low or insufficient H(4)R selectivity. In addition, the investigation of numerous H(4)R 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 H(4)R agonistic activity and summarizes the structure-activity relationships of selected compound classes.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.10.041