Histamine H1 Receptors and Affinity Analyses in Human Nasal Mucosa in Cases of Nasal Allergy

Abstract

An increased number (density) or sensitivity (affinity) of histamine H₁ receptors could cause an increase of allergic symptoms. Using the specific H₁ receptor blocker ³H-mepyramine, we have demonstrated for the first time an H₁ receptor number (Bmax) and a binding affinity (Kd) in guinea pig and human nasal mucosa. H₁ antihistamines inhibited ³H-mepyramine binding in nasal mucosa at low concentrations, while H₂ antihistamines inhibited at extremely high concentrations, indicating that ³H-mepyramine binding sites represent H₁ receptors in nasal mucosa. Bmax and Kd values were not significantly different among the nonallergic sinusitis, vasomotor rhinitis, or the nasal allergy group, suggesting that H₁ receptors do not change quantitatively and qualitatively in allergic nasal mucosa. There was no significant correlation between H₁ receptor number and clinical data (IgE, peripheral eosinophils, RAST). These data suggest that H₁ receptor number and affinity are not main etiological and pathophysiological factors in nasal allergy.

Keywords

histamine receptors nasal allergy nasal mucosa

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