GENERAL PHARMACOLOGY OF CS-807
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We studied the pharmacology of CS-807 and R-3746, an active metabolite. Cefaclor was used as a reference compound.<BR>The doses of CS-807 administered, orally or intraduodenally, were up to 2000mg/kg in mice and rats, and 1000mg/kg in rabbits, cats and dogs.<BR>The concentrations of R-3746 <I>in vitro</I> were up to 10<SUP>-4</SUP> or 10<SUP>-3</SUP>g/ml.<BR>On the central nervous system, CS-807 showed no significant effect. Namely, gross behavior, locomotor activity, thiopental-induced anesthesia, electroshock-or bemegride-induced convulsions, and muscle coordination in mice, gross behavior and spontaneous electroencephalogram in rats and body temperature in rabbits were not influenced by CS-807.<BR>On the respiratory, cardiovascular and autonomic nervous systems, CS-807 showed no significant effect. Namely, respiration, blood pressure, heart rate, carotid blood flow, electrocardiogram and blood pressure response to norepinephrine, acetylcholine or carotid artery occlusion in anesthetized dogs, contraction of the nictitating membrane induced by electrical stimulation of the cervical sympathetic nerve in anesthetized cats, and the beat rate and contractile force of isolated guinea pig atrium and papillary muscle were not influenced by CS-807 or R-3746.<BR>Movement and tone of isolated guinea pig tracheal muscle, rabbit ileum, rat was deferens, and pregnant or non-pregnant uterus were not influenced by R-3746. R-3746 showed no spasmolytic effect against acetylcholine, histamine or norepinephrine in isolated guinea pig ileum or rat was deferens.<BR>Gastric secretion in rats was slightly but significantly reduced by an intraduodenal dose of 2000mg/kg of CS-807, though at 500mg/kg no significant effect was observed. Intestinal propulsion and defecation time in mice were not influenced by CS-807.<BR>On the urinary excretion system, an oral dose of 2000mg/kg of CS-807 caused a slight but significant decrease in urine volume and increase in potassium excretion and urine osmotic pressure in rats. At 500mg/kg, a slight increase in urine osmotic pressure was observed.<BR>On the blood, CS-807 showed no significant effect. Namely, haemolysis of human blood, coagulation and platelet aggregation in rats were not influenced by CS-807 or R-3746. Isolated rat phrenic nerve-diaphragm preparation and blood glucose levels in rats were not influenced by CS-807 or R-3746. CS-807 or R-3746 caused neither local anesthesia in guinea pig cornea nor local irritation in rabbit eye mucosa.<BR>As shown above, significant effects of CS-807 were observed only at 2000mg/kg but not at 500mg/kg, which presumably would be 60-120 times the clinical dose (200-400mg/day). This suggests that CS-807 would not cause any serious adverse effects clinically.
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公益社団法人 日本化学療法学会 | 論文
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