Evaluation of the Bronchodilating and Antiallergic Properties of a Beta-Adrenoceptor Stimulant, KWD 2131, in Asthmatic Patients

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Abstract
KWD 2131 (1-(3,5-dihydroxyphenyl)-(1,1-dimethyl-2-hydroxyethyl-amino)ethanol sulfate) is a .beta.-adrenoceptor stimulating compound that is equipotent to terbutaline with regard to inhibition of anaphylactic histamine release from guinea pig lung tissue but less potent than terbutaline as a cardioaccelerator in this species. KWD 2131 was .apprx. 5-10 times less potent than terbutaline as a cardioaccelerator, tremorogenic and bronchodilator agent on s.c. injection in man. S.c. injection of KWD 2131 in a subthreshold dose for bronchodilatation, i.e., 0.3 mg or 0.6 mg, given prior to a bronchial provocation test with specific allergen had no protective effect on the changes in specific airway conductance and peak expiratory flow in a double-blind cross-over study in 12 patients with allergic asthma. KWD 2131 probably has a less selective antiallergic activity in man as compared to guinea pig. The methodology employed for the evaluation is useful for the characterization of antiallergic drugs with bronchodilator properties.