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 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.
Department of Pharmaceutical/Medicinal Chemistry, Faculty of Chemistry and Pharmacy, University of Regensburg, Regensburg, Germany.
Patrick
P
Igel
Stefan
S
Dove
Armin
A
Buschauer
D000818:Animals; D001562:Benzimidazoles / Q000737:chemistry; D001665:Binding Sites; D003024:Clozapine / Q000737:chemistry; D006146:Guanidines / Q000737:chemistry; D006801:Humans; D008024:Ligands; D051379:Mice; D010091:Oximes / Q000737:chemistry; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000235:genetics / Q000378:metabolism; D011968:Receptors, Histamine / Q000235:genetics / Q000378:metabolism; D000074040:Receptors, Histamine H4; D013329:Structure-Activity Relationship
D001562:Benzimidazoles; D006146:Guanidines; C418607:HRH4 protein, human; D008024:Ligands; D010091:Oximes; D043562:Receptors, G-Protein-Coupled; D011968:Receptors, Histamine; D000074040:Receptors, Histamine H4; D003024:Clozapine; C004711:dicyandiamido