Vinay, Patrick published the artcileMetabolism of tienilic acid (ticrynafen) in man. Pharmacokinetic and mass spectrometric studies, Product Details of C13H8Cl2O4S, the main research area is tienilic acid pharmacokinetics.
The pharmacokinetics and metabolism of tienilic acid (I) [40180-04-9] a new diuretic with uricosuric properties, were studied in human volunteers following single ingestion of 250, 500, or 1000 mg. I was found to be extensively (more than 98%) bound to plasma proteins but not to displace the fraction of urate bound to plasma proteins at the usual therapeutic dosage (250 to 500 mg). The uricosuric and natriuretic effects of I lasted 8-12 h. A peak concentration of 2.5, 4.2 or 10.1 mg/dL was noted in the plasma 2 h following ingestion of each dose. The apparent volume of distribution of the drug was close to that of plasma volume I disappeared rapidly from the plasma according to a first order kinetics and the plasma half-life ranged from 1.6-2.4 h. Gas chromatog. and mass spectrometric studies revealed that 21% of the ingested I is excreted as such in urine over 24 h. Three major metabolites of I were identified in urine: a monohydroxylated I [55901-78-5], a dihydroxylated I [75278-66-9], and a diacid I [66584-08-5]. Including metabolites, 36-47% of the drug was excreted in the urine within 24 h. No significant glucuro- or sulfoconjugation of the drug or its metabolites could be detected in the urine. Excretion of the drug and its metabolites was also noted in the bile. It is concluded that I is rapidly metabolized and excreted in humans with normal kidney and liver function.
European Journal of Drug Metabolism and Pharmacokinetics published new progress about tienilic acid pharmacokinetics. 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, Product Details of C13H8Cl2O4S.
Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem