Day: November 18, 2022

Guariglia, A. published the artcileMetabolic effects of a natriuretic-uricosuric drug, Ticrynafen, in man, Related Products of benzothiophene, the main research area is Ticrynafen urate sodium potassium metabolism; acid base equilibrium Ticrynafen.

Ticrynafen (I) [40180-04-9] (500 mg) has a maximal diuretic and natriuretic effect in human subjects during the 1st 2 and 3 days after treatment, resp. A significant natriuretic effect was also observed in subjects with reduced glomerular filtration rates. During a period of maximum water and Na+ excretion, the urinary K+ losses were not significant. The urinary K+ losses were only late, after the maximal natriuretic effect. The observed changes in acid-base balance indicated that the development of metabolic acidosis was related to K+ depletion and that it might be prevented by administration of K+-sparing diuretics. Increases in blood and urine uric acid [69-93-2] were observed in all subjects treated with I, including patients with reduced glomerular filteration rates.

International Congress Series published new progress about Ticrynafen urate sodium potassium metabolism; acid base equilibrium Ticrynafen. 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, Related Products of benzothiophene.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Freis, Edward published the artcileComparative effects of ticrynafen and hydrochlorothiazide in the treatment of hypertension, Application of 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, the main research area is ticrynafen hydrochlorothiazide hypertension.

Two dose levels of ticrynafen (I) [40180-04-9], a new uricosuric diuretic, and of hydrochlorothiazide [58-93-5] were randomly assigned double-blind to 240 men with initial diastolic blood pressures in the range of 95 to 114 mm Hg. A dose of 500 mg of I once daily exerted an antihypertensive effect comparable to that of 50 or 100 mg of hydrochlorothiazide. Whereas serum uric acid [69-93-2] levels rose in patients treated with hydrochlorothiazide, they fell markedly in those receiving I. Otherwise, both diuretics produced similar chem. changes in serum. Patients tolerated I as well as they did hydrochlorothiazide over a period of 6 mo of observation, and there was no evidence of serious toxicity or loss of therapeutic effect with I. This antihypertensive agent, in appropriate doses, appears to be as effective and well tolerated as hydrochlorothiazide, and in addition I prevents hyperuricemia.

New England Journal of Medicine published new progress about ticrynafen hydrochlorothiazide hypertension. 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, Application of 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Kahela, Paavo published the artcilePolymorphism of tienilic acid, Safety of 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, the main research area is polymorphism tienilic acid.

One amorphous and 3 crystalline forms of tienilic acid (I) [40180-04-9] were characterized by using IR spectroscopy and X-ray diffraction. Form A is stable at room temperature, while forms B and C and the amorphous form are metastable. Form B changes to form A near the m.p. and the amorphous form into form C at 120°. Further, during mech. grinding, the mixed form containing forms A and B changes to form A and the amorphous form into form C.

Acta Pharmaceutica Fennica published new progress about polymorphism tienilic acid. 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, Safety of 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Shinosaki, Toshihiro published the artcileStop-flow studies on tubular transport of uric acid in rats, Synthetic Route of 40180-04-9, the main research area is kidney tubule urate transport uricosuric.

A stop-flow technique using pyrazinoic acid (PZO)-treated and -untreated rats was devised to evaluate drug effects on bi-directional transport of uric acid in the tubules. Constant venous infusion of test drugs to PZO-untreated rats was used to estimate their inhibitory effects on urate secretion, while their inhibitory effects on urate reabsorption was studied by i.v. administration as a bolus to PZO-treated rats. Probenecid, tienilic acid and R(+)-enantiomer of S-8666, which is the uricosuric component of a new uricosuric diuretic, decreased the (Tua/Pua)/(Tin-Pin) value in the distal and proximal tubules by inhibiting urate secretion in PZO-untreated rats. On the other hand, all of these drugs increased the (Tua/Pua)/(Tin/Pin) value in the tubules in PZO-treated rats, which suggested that they also inhibited the reabsorptive flux of urate. This stop-flow technique in rat kidney showed the possibilities of bi-directional inhibition by these drugs of urate transport in the tubules.

Advances in Experimental Medicine and Biology published new progress about Gout. 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, Synthetic Route of 40180-04-9.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Gibson, T. published the artcileTienilic acid in the treatment of gout and hypertension, Recommanded Product: 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, the main research area is tienilic acid gout hypertension; health hazard tienilic acid.

Tienilic acid (I) [40180-04-9] (125 mg, twice daily) was given to patients with hypertension and gouty arthritis. In hypertensive patients, the supine and standing diastolic values declined progressively from 101 to 92 and 102 to 94 mm/Hg resp., over a period of 4 wk. There was a significant decrease in serum uric acid and K. I decreased hyperuricemic levels in gouty patients by 50%. Precipitation of acute gout by I probably reflects its profound effect on blood uric acid levels.

Advances in Experimental Medicine and Biology published new progress about Gout. 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, Recommanded Product: 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Fehring, Susan I. published the artcileEffect of the glutathione S-transferase inhibitor, tienilic acid, on biliary excretion of sulfobromophthalein, Product Details of C13H8Cl2O4S, the main research area is tienilate interaction sulfobromophthalein biliary excretion; glutathione transferase inhibitor sulfobromophthalein biliary excretion.

Tienilic acid, a phenoxyacetic acid diuretic, reduces the amount of total sulfobromophthalein (BSP) excretion in the isolated perfused rat liver (IPRL). This reduction was primarily by reduction in excretion of conjugated BSP, with excretion of unchanged BSP being relatively unaffected. TA also reduces the amount of conjugated BSP formed in vitro, indicating that its effect in the IPRL may be by means of inhibiting the glutathione S-transferase enzymes involved in the formation of the conjugate. It would appear that a reduction in the biliary excretion of BSP cannot be taken to be an indication of reduced liver function in a general sense.

Chemico-Biological Interactions published new progress about Bile. 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

Zou, Tingting published the artcileFlavour precursor peptide from an enzymatic beef hydrolysate Maillard reaction-II: Mechanism of the synthesis of flavour compounds from a sulphur-containing peptide through a Maillard reaction, Application of 3-Acetylthiophene, the main research area is beef hydrolyzate Maillard reaction product dimethylthiazole isobutylpyrazine.

This study aims to investigate the Maillard reaction products (MRPs) generated between enzymic beef hydrolyzated sulfur-containing oligopeptides and xylose subjected to heat treatment. The priority of the meat aroma contribution is Cys-Gly-Val > GSH > Leu-Cys, whereas Val-Met is relatively Maillard inert. Two peptide-specific aroma compounds, namely, 2-Isobutylpyrazine and 4-butyl-2,5-dimethylthiazole, were produced in a Leu-Cys Maillard reaction system at pH 5.5, showing that the dipeptides with Leu in the N-terminus exhibited high Maillard reactivity. The carbon source and generation pathway of the aroma-active compounds were demonstrated by carbohydrate module labeling (CAMOLA). A new pyrazine generation pathway with xylose-contributed C2 was proposed using this method specifically. Ultra-performance liquid chromatog.-electrospray ionization/quadrupole-time-of-flight tandem mass spectrometry (UPLC-ESI-Q-TOF MS/MS) was then used to analyze the peptide-specific MRPs to reveal the peptide cleavage, cyclization, and crosslinking with other reactants and intermediates. The main results of this study include that crosslinking between reactants and their intermediates largely occurred in a peptide-specific Maillard reaction; its oligopeptide-specific MRPs were first demonstrated; and the crosslinking products from cyclopeptides and two xyloses and/or their fragments were observed for the first time.

LWT–Food Science and Technology published new progress about Beef. 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, Application of 3-Acetylthiophene.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Ahokas, J. T. published the artcileInhibition of soluble glutathione S-transferase by diuretic drugs, Formula: C13H8Cl2O4S, the main research area is diuretic liver glutathione transferase inhibition; toxicity diuretic glutathione transferase.

Among several high-ceiling diuretics (bumetanide  [28395-03-1], ethacrynic acid  [58-54-8], furosemide  [54-31-9], indacrynic acid  [56049-88-8], and tienilic acid  [40180-04-9]) only ethacrynic acid was conjugated in vitro to GSH in rat liver cytosol. Ethacrynic, indacrynic, and tienilic acids were all potent inhibitors of glutathione S-aryltransferase  [50812-37-8] in the same preparation; glutathione S-alkyltransferase  [50812-37-8] and glutathione S-epoxide transferase  [50812-37-8] activities were also inhibited by these diuretics, but to a lesser extent. The most potent enzyme inhibitors are related in structure to ethacrynic acid. These observations are discussed with respect to the effect this enzyme inhibition may have on the toxicity of diuretics as well as the toxicity of other coadministered drugs which are also detoxified by the glutathione S-transferase  [50812-37-8] pathway.

Biochemical Pharmacology published new progress about Liver. 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, Formula: C13H8Cl2O4S.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Dayan, J. published the artcileStudy of the mutagenic activity of 6 hepatotoxic pharmaceutical drugs in the Salmonella typhimurium microsome test, and the HGPRT and sodium-potassium ATPase system in cultured mammalian cells, SDS of cas: 40180-04-9, the main research area is hepatotoxic drug mutagenicity.

Several pharmaceutical drugs show strong hepatotoxicity during therapeutic use: aminophenazone  [58-15-1], clofibrate  [637-07-0], nifuroxazide  [965-52-6], oxamniquine  [21738-42-1], perhexiline maleate  [6724-53-4], and tienilic acid  [40180-04-9]. Their mutagenicity was assessed in the Ames test on 6 strains of S. typhimurium, and in V79 Chinese hamster lung cells with a rat-hepatocyte-mediated metabolic activation system and the hypoxanthine-guanine phosphoribosyl transferase test and the Na+/K+ ATPase assay. Nifuroxazide was pos. in the Ames test in 2 Salmonella strains (TA100 and TA100 Frl). In the hepatocyte-mediated mammalian V79 cell system, nifuroxazide, clofibrate, and aminophenazone were neg. Oxamniquine and tienilic acid were pos. with and without metabolic activation in tests for ouabain and 6-thioguanine resistance. Perhexiline maleate was neg. for the direct induction of 6-thioguanine resistance without metabolic activation, and pos. after metabolization mediated by primary rat hepatocytes. These results suggest the need for some caution in the use of some pharmaceutical drugs because of hepatotoxicity and because 3 out of 6 drugs were shown to be slightly mutagenic in mammalian cells.

Mutation Research, Genetic Toxicology Testing published new progress about Liver. 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, SDS of cas: 40180-04-9.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Dansette, P. M. published the artcileHydroxylation and formation of electrophilic metabolites of tienilic acid and its isomer by human liver microsomes: catalysis by a cytochrome P450 IIC different from that responsible for mephenytoin hydroxylation, Related Products of benzothiophene, the main research area is tienilate isomer metabolism liver microsome; cytochrome P450 tienilate isomer metabolism liver.

Tienilic acid (TA; I) is metabolized by human liver microsomes in the presence of NADPH with the major formation of 5-hydroxytienilic acid (5-OHTA) which is derived from the hydroxylation of the thiophene ring of TA. Besides this hydroxylation, TA is oxidized into reactive metabolites which covalently bind to microsomal proteins. Oxidation of an isomer of tienilic acid (TAI) by human liver microsomes, gives a much high level of covalent binding to proteins. Both covalent binding of TA and TAI metabolites are almost completely suppressed in the presence of glutathione. These three activities of human liver microsomes (TA 5-hydroxylation, covalent binding of TA and TAI metabolites) seem dependent on the same cytochrome P 450 of the IIC subfamily, since (i) antibodies against human liver cytochromes P 450 IIC strongly inhibit these three activities, (ii) there is a clear correlation between these activities in various human liver microsomes, and (iii) TA acts as a competitive inhibitor for TAI activation into electrophilic metabolites (Ki ≃ 25 μM) and TAI inhibits TA 5-hydroxylation. However cross inhibition experiments indicate that tienilic acid hydroxylation and mephenytoin hydroxylation, a typical reaction of some human liver P 450 IIC isoenzymes, are not catalyzed by the same member of the P 450 IIC subfamily.

Biochemical Pharmacology published new progress about Liver. 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, Related Products of benzothiophene.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem