Thiagarajah, Jay R.’s team published research in Gastroenterology in 126 | CAS: 307510-92-5

Gastroenterology 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 C7H5FN2, Application In Synthesis of 307510-92-5.

Thiagarajah, Jay R. published the artcilePrevention of toxin-induced intestinal ion and fluid secretion by a small-molecule CFTR inhibitor, Application In Synthesis of 307510-92-5, the publication is Gastroenterology (2004), 126(2), 511-519, database is CAplus and MEDLINE.

Background & Aims: The cystic fibrosis transmembrane conductance regulator (CFTR) provides an important apical route for Cl– secretion across intestinal epithelia. A thiazolidinone-type CFTR blocker (CFTRinh-172) reduced cholera toxin-induced fluid accumulation in mouse intestinal loops. Here, we characterize the efficacy and pharmacodynamics of CFTRinh-172 in blocking cAMP and cGMP induced Cl–/fluid secretion in rodent and human intestine. Methods & Results: CFTRinh-172 inhibited cAMP and cGMP agonist induced short-circuit current by >95% in T84 colonic epithelial cells (KI ∼ 3 μmol/L) and in mouse and human intestinal sheets (KI ∼ 9 μmol/L). A single i.p. injection of CFTRinh-172 (200 μg) blocked intestinal fluid secretion in a rat closed-loop model by >90% for cholera toxin and >70% for STa Escherichia coli toxin. In mice, CFTRinh-172 (20 μg) inhibited cholera toxin-induced intestinal fluid secretion by 90% (persistence t1/2 ∼10 h, KI ∼ 5 μg) and STa toxin by 75% (KI ∼ 10 μg). Tissue distribution and pharmacokinetic studies indicated intestinal CFTRinh-172 accumulation facilitated by enterohepatic circulation. An oral CFTRinh-172 preparation reduced fluid secretion by >90% in a mouse open-loop cholera model. Conclusions: A small mol. CFTR blocker markedly reduced intestinal ion and fluid secretion caused by cAMP/cGMP-dependent bacterial enterotoxins. CFTR inhibition may thus reduce fluid secretion in infectious secretory diarrheas.

Gastroenterology 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 C7H5FN2, Application In Synthesis of 307510-92-5.

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