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Table 5 H4 Receptor Antagonists

From: The Role of Antihistamines in the Treatment of Vasomotor Rhinitis

Receptor

H4

Signal conduction through

Gi/o and G15/16

Location of receptors

Eosinophils, neutrophils, basophils, mast cells, spleen, liver, lung colon, epicanthus, and bone marrow

Chromosome location

18q11.2

Signal conduction induces

Decreased cyclic AMP, MAP kinase induction, phospholipase C activation, formation of diacylglycerol, calcium mobilization

Antagonists (reverse agonists)

None available clinically: Has homology with H3 receptor and is also antagonized by same drugs

Activities

Chemotaxis and chemokinesis of mast cells and eosinophils; enhancement of the activity of other chemoattractants (eg, chemokines) on eosinophils; upregulation of adhesion molecules

Nasal symptoms produced

Since histamine can up regulate inflammation on cells such as eosinophils, H4 antagonists may have a beneficial role in this regard