The antagonism between analgesic antipyretic drugs and bradykinin was examined quantitatively, using the bronchoconstrictor response of guinea-pigs in vivo. The dose of bradykinin required to overcome antagonism by calcium acetylsalicylate increased with the dose of acetylsalicylate given, the ratio being roughly constant. Fifty times the quantity of acetylsalicylate which just antagonized bradykinin did not modify bronchoconstriction due to small doses of histamine, 5-hydroxytryptamine, or acetylcholine. A method of measuring the potency of this anti-bradykinin action was developed. Acetylsalicylic acid, phenylbutazone, amidopyrine, and phenazone had a high potency; paracetamol, cinchophen, sodium salicylate, and acetanilide had a moderate potency; and phenacetin, salicylamide, and 4-hydroxyisophthalic acid had little or none. Cortisone, hydrocortisone, aldosterone, amodiaquine, and morphine were ineffective o)r their action was non-specific. In sensitized guinea-pigs, an injection of antigen caused bronchospasm. This response was greatly lessened by pretreatment with mepyramine, but was not affected by calcium acetylsalicylate, lysergic acid diethylamide, or atropine. Acetylsalicylic acid, phenylbutazone, and amidopyrine did not specifically antagonize the action of bradykinin on the capillaries of guinea-pig skin in vivo, on guinea-pig ileum in vitro or on rat duodenum in vitro.Collier, Holgate, Schachter, and Shorley (1959Shorley ( , 1960 found that bradykinin causes bronchoconstriction in the guinea-pig, that small doses of acetylsalicylic acid, phenylbutazone and amidopyrine suppress this response without affecting those to histamine or 5-hydroxytryptamine, and that increasing the dose of bradykinin overcomes this suppression. Since the relationship between these analgesic and antipyretic drugs and bradykinin in its bronchoconstrictor action shows the main features of pharmacological antagonism, we thought it worth while to study this relationship quantitatively, to measure the potency of antagonism and to explore how effective were other antipyretic, analgesic, anti-inflammatory and anti-rheumatic drugs. Since bradykinin might take part in anaphylactic bronchospasm, we investigated whether pre-treatment with acetylsalicylate lessened the intensity of this spasm. We examined also whether the antagonists of bradykinin in its bronchoconstrictor action likewise antagonized some of its other actions. METHODS Materials.-Bradykinin was prepared by the action of crystalline trypsin on heated beef serum globulin and was purified chromatographically. The potencies of preparations, standardized against pure bradykinin obtained with trypsin (Elliott, Lewis, and Horton, 1960), ranged from 0.6 to 16 pxg. pure bradykinin/mg.Substances tested in acute experiments as antagonists of bradykinin are given in Table III, which shows the salts used. Histamine acid phosphate, 5-hydroxytryptamine creatinine sulphate and acetylcholine chloride were also employed as bronchoconstrictor agents and mepyramine maleate, lysergic acid di...