Prandota, J. published the artcileBinding of tienilic acid (Diflurex) to human serum albumin and to plasma of normal subjects and uremic patients, Quality Control of 40180-04-9, the main research area is tienilate binding plasma protein uremic; serum albumin tienilate binding uremic.
The binding of tienilic acid (TA)(I) [40180-04-9], a new diuretic, to human serum albumin (HSA) and to the plasma of uremic patients under treatment with hemodialysis was measured. At a total concentration of 4.5 μg/mL (expected therapeutic concentration), the unbound fraction of TA to 4% HSA and to normal plasma was 0.49% and 0.6%, resp. The degree of binding was approx. the same from 0.5 to 132 μg/mL of total drug concentration The free fraction of TA increased about 2-fold when total concentration of the drug increased from 0.5 to 192 μg/mL. TA has 2 classes of binding sites. The effect of ionic strength and pH on the binding of TA to HSA indicate that the drug is bound mainly by hydrophobic interaction. Acetylsalicylic acid (300 μg/mL), bilirubin (10 mg%), and palmitic acid (2:1 molar ratio with HSA) decreased TA binding. Reduced drug plasma protein binding was observed in uremic patients. No correlation was found between the unbound fraction of TA and the uremic serum albumin, creatinine, or blood urea concentrations Following an i.v. injection of heparin [9005-49-6], the free fraction of TA in uremic plasma rose from 1.7% to 4.5% after 10 min. of hemodialysis. This could be explained, at least partially, by the increased uremic plasma free fatty acids to albumin molar ratio.
European Journal of Drug Metabolism and Pharmacokinetics published new progress about Blood serum albumins. 40180-04-9 belongs to class benzothiophene, name is 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, and the molecular formula is C13H8Cl2O4S, Quality Control of 40180-04-9.
Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem