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Table 4 H3 Receptor Antagonists

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

Receptor

H3

Signal conduction through

Gi/o

Location of receptors

Mainly expressed on presynaptic nerves in the peripheral sympathetic adrenergic system and histaminergic nerves in the central nervous system. Receptors can be found in airways and gastrointestinal tract

Chromosome location

20q13.33

Signal conduction induces

Decreased cyclic AMP, induction MAP kinase

Antagonists (reverse agonists)

None available clinically: Thioperamide, alobenpropit, and others Very little data regarding effect of H1 antagonists on the H3 receptor are available (13)

Activities

Opposes bronchoconstriction and gastric acid; suppression of norepinephrine release at presynaptic nerve endings

Nasal symptoms produced

Can produce nasal decongestion by blocking effect of histamine on adrenergic postsynaptic receptors