Detail of "10049-83-9"

Reference

Changes of muscle fiber thickness following diets of various types and administration of drugs in experimental animals

Changes of muscle fiber thickness following diets of various types and administration of drugs in experimental animals. Puzanova, Ludmila (Hyg. Med. Fac., Charles' Univ., Prague, Czech.). Acta Univ. Carol., Med., 22(3-4), 231-7 (English) 1976. CODEN: AUNCA9. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) In rats fed a low-protein, low-caloric diet from birth until day 40 neither Encephabol (pyrithioxine)(I) [10049-83-9] nor pyridoxine [65-23-6] (both drugs given 40 mg/kg/day from day 40 to day 50) altered skeletal muscle fiber thickness.

Biopharmaceutics of pyrithioxin

Biopharmaceutics of pyrithioxin. III. Blood concentration and urinary excretion profiles following oral administration of esters of pyrithioxin to dogs. Kitao, Kazuhiko; Yata, Noboru; Yamazaki, Masaru; Iwane, Junichi; Kamada, Akira (Fac. Pharm. Sci., Osaka Univ., Suita, Japan). Chem. Pharm. Bull., 25(6), 1350-6 (English) 1977. CODEN: CPBTAL. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) An attempt was made to det. and compare oral absorption characteristics of ester derivs. of pyrithioxin (I) [1098-97-1] filled in hard gelatin capsules after administration to dogs. Ester derivs. studied were pyrithioxin tetraacetate-2HCl (I-A-2HCl) [55422-93-0], pyrithioxin tetrapropionate-2HCl (I-P-2HCl) [10089-40-4], pyrithioxin tetrabutyrate-2HCl (I-B-2HCl) [64157-29-5], and pyrithioxin 4,4'-disuccinate-2HCl (I-S2HCl) [64124-25-0]. Blood concns. of 5'-desoxy-5'-methylsulfinylpyridoxol [20166-39-6] and urinary excretions of metabolites of I were studied following oral administration of esters. The increased bioavailability of I-P-2HCl, with the max. blood concn. 1.63 times larger and the total urinary excretion 1.47 times larger than those of pyrithioxin-2HCl [10049-83-9], is related to the high partition coeff. in octanol-pH 6.5 buffer. The insufficient bioavailability of I-S-2HCl appeared to be closely correlated with its lower partition coeff. and incomplete hydrolysis during absorption. The esters were considered to be hydrolyzed in intestinal fluid and/or in the intestinal membrane and the parent drug, I, permeated through the intestinal tract. The uptake of 14C-labeled glucose into the brain of the mouse was studied with I-A-2HCl and I-S-2HCl, with only I-A-2HCl giving a significant increase of glucose through the blood-brain barrier similar to that of I-2HCl.