Plessas, C.’s team published research in European Journal of Drug Metabolism and Pharmacokinetics in 1980-06-30 | CAS: 40180-04-9

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, COA of Formula: C13H8Cl2O4S.

Plessas, C. published the artcileBinding of tienilic acid (Diflurex) to human plasma proteins and erythrocytes, COA of Formula: C13H8Cl2O4S, the main research area is tienilic acid protein binding; erythrocyte tienilic acid binding.

The binding of SKF-62698 (tienilic acid)(Diflurex)(I) [40180-04-9], a new antihypertensive agent with diuretic and uricosuric properties, to human plasma proteins, pure protein fractions, erythrocytes, as well as the effect of heparin [9005-49-6] on the degree of protein binding were measured. Different amounts of I (1 to 1000 μg) were incubated with 1 mL of either human plasma or phosphate buffer M/15 (pH 7.4), containing 47 mg of albumin, at 37° for 2 h. The degree of binding of I to plasma proteins and albumin, at plasma concentration (1-30 μg/mL) of the drug at therapeutic doses, was 99.4-98.5 and 95.8-94.2%, resp. In the case of albumin, a Scatchard plot showed 2 classes of binding sites (M1 = 0.5, K1 = 6.3 × 104/M; M2 = 8, K2 = 2.8 × 103/M). After incubation of 10 μg of drug with 8 mg of α-globulins, 8 mg of β-globulins or 7.4 mg of γ-globulins at 37°, pH 7.4 and ultrafiltration, the degree of binding was 83%, 44%, and 44%, resp. The distribution of I between erythrocytes and plasma ranges between 0.11-0.17 for concentrations of 1 to 15 μg/mL and between 0.17-0.10 for concentrations of 15 to 30 μg/mL under different exptl. conditions, heparin had no effect on the degree of binding of I to plasma proteins.

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, COA of Formula: C13H8Cl2O4S.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem