In the previous report, B-64114 derivatives were proven to have similar potent antiinflammatory activity to that of phenylbutazone. In this paper, the general pharmacological activities of B-64114-Ca were examined in comparison with phenylbutazone. The acute toxicity of B-64114-Ca was weaker than that of phenylbutazone. Toxic action of phenylbutazone was inhibition on the heart function, but on the other hand, B-64114-Ca did not hinder the heart function and showed mainly inhibitory action on the respiration. It was found that B-64114-Ca was almost similar or less to phenylbutazone in such activities as analgesic, hypothermic and antipyretic effects and lack hypnotic potentiation and anti-convulsive effects. It may be, therefore, considered to be extremely low in the effects on the central nervous system. B-64114-Na showed temporary hypotensive effect and it was also found to only slightly affect the cardiac movement and capillary vessels. It was free of any effects on the blood sodium and potassium levels, urinary sodium and potassium outputs, and urine volume and blood coagulation times. It did not affect the intestinal movement and did not show the antagonistic effects on such mediators as histamine, acetylcholine, serotonin and so on. It was found that B-64114-Na has the local irritation and B-64114-Ca caused the stomach ulcer, but these activities were similar or weaker to those of phenylbutazone. From the above results, it may be thought that B-64114-Ca is valuable of clinical usage as nonsteroid anti-inflammatory agent which is lower in toxicity and in side effects than phenylbutazone.
