[General pharmacology of BMY-28100]

General pharmacological properties of BMY-28100, a new semisynthetic oral cephalosporin, were studied in experimental animals. The obtained results are summarized as follows: 1. BMY-28100 had no effect on gross behavior and the central nervous system in mice and rats nor on EEG activities in rabbits. 2. BMY-28100 did not affect the smooth muscle isolated from rats, guinea pigs or rabbits nor did it influence ganglionic transmission in cats. 3. Effects of BMY-28100 on the atrium and heart isolated from guinea pigs were not obvious. Several parameters of the cardiovascular system were examined and found unchanged by administration of BMY-28100 to rabbits. 4. In the digestive system, BMY-28100 had no effect on charcoal meal transport in the small intestine of mice. In rats, however, gastric secretion was reduced at a dose level of 125 mg/kg or higher and bile secretion was enhanced at a dose level of 500 mg/kg. 5. BMY-28100 had no effect on neuromuscular transmission in rabbits and showed no local anesthetic activity in guinea pigs. 6. BMY-28100 decreased urine volume and urinary excretion of electrolytes in dose-dependent manners in rats. Sulfobromophthalein excretion in rats was inhibited only at the highest dose tested. BMY-28100 had no effect on blood coagulation and red blood cell resistance in rats or rabbits. BMY-28100 revealed no antiinflammatory activity in rats. 7. BMY-28167, a trans-isomer of BMY-28100, had no or weak effects on some of above test systems when compared with BMY-28100. These results suggest that BMY-28100 has hardly any pharmacological properties leading to severe adverse reactions in clinical use.