Histamine receptors and the conjunctiva

PURPOSE OF REVIEW: The purpose of this review is to evaluate the effect of histamine on various receptors in the conjunctiva. A Medline search from 1980 was performed on the histamine receptor subtypes H1, H2 and H3 in the human conjunctiva. RECENT FINDINGS: In the conjunctiva, histamine has been shown to induce various physiological and immunological changes through both H1 and H2 receptor stimulation. Histamine binding to conjunctival H1 receptors through the phospholipase C-dependent inositol phosphate pathway leads to the symptom of pruritus while histamine stimulation of the conjunctival H2 receptors has been indirectly shown to cause vasodilation. SUMMARY: The effect of histamine on conjunctival H1 receptors appears to be the primary target for ocular allergy treatment as it is primarily involved in ocular pruritus. The exact interaction of the conjunctival H2 receptors appears to work in a complementary fashion to the H1 receptor in controlling other features of ocular allergy such as vasodilation and injection. Thus, oral and topical antihistamines with multiple histamine receptor binding activities may provide an improved treatment paradigm for the various signs and symptoms of ocular allergy. The histamine H1, H2 and H3 receptor affinities of ketotifen, pyrilamine, and epinastine appear to have the strongest H1 and H2 affinities.