Detail of "114-86-3"

Reference

The mechanism of action of phenformin in starved rats

The mechanism of action of phenformin in starved rats. Evans, Peter F.; King, Laurence J.; Parke, Dennis V.; Margetts, George; Jones, William E. (Dep. Biochem., Univ. Surrey, Guildford/Surrey GU2 5XH, UK). Biochem. Pharmacol., 32(22), 3459-63 (English) 1983. CODEN: BCPCA6. ISSN: 0006-2952. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) In starved rats the ability of phenformin [114-86-3] to lower the blood glucose concn. after an i.p. glucose load, with a concomitant increase in blood lactate [50-21-5] concn., indicated that the drug was increasing the rate of anaerobic glycolysis. The results of expts. in which glucose and gluconeogenic precursors were given to starved rats were explained by a hypothesis for the mechanism of action of phenformin involving inhibition of certain NAD+-dependent dehydrogenases. Substrates with NAD+-linked oxidns. could be discriminated from those, like succinate [110-15-6], with FAD-linked oxidns., and succinate may be of use in the treatment of clin. lactic acidosis caused by biguanide drugs.Except for chemicals metioned above, 50-21-5 and 9035-82-9 are also used. .

The effects of phenformin on the transport and metabolism of sugars by the rat small intestine

The effects of phenformin on the transport and metabolism of sugars by the rat small intestine. Nicholls, Trevor J.; Leese, Henry J. (Dep. Biol., Univ. York, York YO1 5DD, UK). Biochem. Pharmacol., 33(5), 771-7 (English) 1984. CODEN: BCPCA6. ISSN: 0006-2952. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The effects of 0.25-10 mM phenformin [114-86-3] on sugar transport and metab. in rats were studied in a prepn. for the combined perfusion of the vascular bed and the lumen. At all concns., the effects of vascular phenformin were more pronounced than those of luminal phenformin. Phenformin inhibited galactose [59-23-4] transport across the intestine, the pattern of inhibition depending on whether the phenformin was added to the luminal or vascular compartments. The active accumulation of galactose in the mucosal epithelial cells was also abolished. There was a linear relationship between the percentage redn. in mucosal ATP levels and vascular phenformin concn. Phenformin reduced the rate of glucose [50-99-7] uptake from the lumen, and the proportion of this glucose which reached the vascular effluent. Most of the glucose which did not reach the vascular side could be accounted for by the formation of lactic acid. Vascular phenformin increased glucose uptake from the vascular medium by 88%, 97% of which could be accounted for by lactate formation. Phenformin was sequestered by the mucosa when added to the vascular, but not the luminal, perfusates. There was very little translocation of intact phenformin across the gut in either the mucosal or serosal direction. It is suggested that the effects of phenformin on the gut mainly derive from an inhibition of mitochondrial oxidative phosphorylation, with a small contribution from a direct effect on the brush border, more pronounced at high phenformin concns.In this experiment, several chemicals are used like 50-99-7 and 59-23-4 Thus, phenformin appears to delay sugar absorption in man. Further, the intestine may be a significant source of lactate prodn. in lactic acidosis. .