Histamine H4 receptor agonists.

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Igel P, Dove S, Buschauer A

Histamine H4 receptor agonists.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7191-9. doi: 10.1016/j.bmcl.2010.10.041. Epub 2010 Oct 14.

PubMed ID

21044842 [ View in PubMed

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Abstract

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.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Clozapine	Histamine H4 receptor	Protein	Humans	No	Agonist	Details