Sonawane, N. D.’s team published research in Journal of Pharmaceutical Sciences in 94 | CAS: 307510-92-5

Journal of Pharmaceutical Sciences published new progress about 307510-92-5. 307510-92-5 belongs to thiazolidine, auxiliary class Membrane Transporter/Ion Channel,CFTR, name is 4-((4-Oxo-2-thioxo-3-(3-(trifluoromethyl)phenyl)thiazolidin-5-ylidene)methyl)benzoic acid, and the molecular formula is C24H26ClNO4, Category: thiazolidine.

Sonawane, N. D. published the artcileIn vivo pharmacology and antidiarrheal efficacy of a thiazolidinone CFTR inhibitor in rodents, Category: thiazolidine, the publication is Journal of Pharmaceutical Sciences (2005), 94(1), 134-143, database is CAplus and MEDLINE.

A small-mol. inhibitor of the cystic fibrosis transmembrane conductance regulator (CFTR), 3-[(3-trifluoromethyl)phenyl]-5-[(4-carboxyphenyl)methylene]-2-thioxo-4-thiazolidinone (CFTRinh-172), reduces enterotoxin-induced intestinal fluid secretion in rodents. Here, we study CFTRinh-172 pharmacol. and antidiarrheal efficacy in rodents using 14C-labeled CFTRinh-172, liquid chromatog./mass spectrometry, and a closed intestinal loop model of fluid secretion. CFTRinh-172 was cleared primarily by renal glomerular filtration without chem. modification. CFTRinh-172 accumulated in liver within 5 min after i.v. infusion in mice, and was concentrated fivefold in bile over blood. At 30-240 min, CFTRinh-172 was found mainly in liver, intestine, and kidney, with little detectable in the brain, heart, skeletal muscle, or lung. Pharmacokinetic anal. in rats following i.v. bolus infusion showed a distribution volume of 770 mL with redistribution and elimination half-times of 0.14 h and 10.3 h, resp. CFTRinh-172 was stable in hepatic microsomes. Closed-loop studies in mice indicated that a single i.p. injection of 20 μg CFTRinh-172 inhibited fluid accumulation at 6 h after cholera toxin by >90% in duodenum and jejunum, ∼60% in ileum and <10% in colon. No toxicity was seen after high-dose CFTRinh-172 administration (3 mg/kg/day in two daily doses) in mice over the first 6 wk of life. The metabolic stability, enterohepatic recirculation, slow renal elimination, and intestinal accumulation of CFTRinh-172 account for its efficacy as an antidiarrheal.

Journal of Pharmaceutical Sciences published new progress about 307510-92-5. 307510-92-5 belongs to thiazolidine, auxiliary class Membrane Transporter/Ion Channel,CFTR, name is 4-((4-Oxo-2-thioxo-3-(3-(trifluoromethyl)phenyl)thiazolidin-5-ylidene)methyl)benzoic acid, and the molecular formula is C24H26ClNO4, Category: thiazolidine.

Referemce:
https://en.wikipedia.org/wiki/Thiazolidine,
Thiazolidine – ScienceDirect.com