Inhibitory effects of imidazolines on histamine liberation from human leukocytes and on tracheal smooth muscle tone.

Antigen-induced IgE-mediated release of histamine from human leukocytes, an in vitro model of allergic reactions, was blocked by imidazole and imidazole-compounds such as oxymetazoline and clonidine. The H-2-antihistamines antagonized this effect of imidazolines. Alpha- and H-1-receptor blocking agents did not antagonize the effect. The contractile effects of the imidazolines were tested on tracheal preparations from the cow and guinea-pig. Imidazole was found to be a rather potent contracting agent, while oxymetazoline only caused weak contractions. Clonidine relaxed the tracheal muscles, when used in the concentration range which were inhibitory in the leukocyte experiments. The contractions caused by imidazolines were non-competitively inhibited by clemastine, while the relaxing effects were blocked by a combination of propranolol, phentolamine and cimethidine. The results suggest that imidazolines which inhibit histamine release and relax bronchial smooth muscles may be of therapeutic importance in the treatment of human allergic disorders.