Relationship between pharmacological activity and blood level of a new anticholinergic agent, timepidium bromide...

Relationship between pharmacological activities and blood levels of a new anticholinergic agent (SA-504), as well as excretion, and distribution in the gastro-intestinal tract were investigated in cats. The time courses of inhibitory effect of SA-504 on gastric motility were closely related to those of blood levels of SA-504 after intragastric administration of 3H-labelled compound. Effects of SA-504 on the pupil of the eye, heart rate and blood pressure were much less than its inhibitory effects on gastric motility. The contents of 3H-SA-504 in the gastric wall were extremely high as compared with those in the blood and heart. About 23% of the radioactivity administered orally as 3H-SA-504 was excreted into the bile and 20% into the urine during a 24 hour period, suggesting that more than 40% of the dose is absorbed from the alimentary tract of cats within 24 hours.