Abstract: Sodium tanshinone Ⅱ-A sulfonate (danshen-201) is a new water-soluble derivative of tanshinone Ⅱ-A which was isolated from Salvia miltiorrhiza. In coronary patients danshen-201 ameliorated the anginal pain and the feeling of chest tightness, and improved the ischemic alterations in the electrocardiogram. This paper reports its effects on hypoxia in mice, hemodynamic studies in dogs and its metabolism in mice.In mice, an intraperitoneal injection of 200 mg/kg prolonged significantly the surviral time under hypoxia. The-rate of O₂ consumption was retarded than in control mice. The amount of-residual O₂ at death was less than in controls (p<0.05). When the ambient O₂ content was lowered to 6%, the lactic acid concentrations in heart and brain of control mice increased markedly, whereas those of treated (danshen-201 was given 1/2 hr previously) mice did not increase.In anesthetized dogs an intravenous injection of 20 mg/kg brought about mild elevation of blood pressure, cardiac output and work of the left ventricle. The changes in heart rate and peripheral vascular resistance, were insignificant.³⁵S-labeled danshen-201 was administered intravenously to mice. At 2 minutes the radioactivity in blood was found to be 75843 cpm/0.1 ml, lowered to 3785 cpm at 90 minutes. The average half-life was about 18 minutes. After 1 hr, the radioactivities were high in liver, lung and intestine, then came to heart and stomach, They all tended to decrease after 6 and 24 hrs. The radioactivities of the contents An the intestines ranked first for all times The amount was also considerable in gall-bladder. The excretion rates in urine and feces were 10.2% and 32%, resp., within 24 hrs; 4.5% and 24.1%, resp., on the 2nd day; and 1.8% and 19.6%, resp., on the 3rd day In the urine, danshen-201 per se as well as a metabolite were identified by both nonradioactive and radioactive thin-layer chromatography and autoradiography. This metabolite was found to have a basic-skeleton similar to the prototype of danshen-201 and seemed to have certain polar groups added.