Minor, Steve’s team published research in Research Communications in Chemical Pathology and Pharmacology in 1979-07-31 | CAS: 40180-04-9

Research Communications in Chemical Pathology and Pharmacology published new progress about Diuresis. 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, Category: benzothiophene.

Minor, Steve published the artcileThe effects of ticrynafen in the rat, Category: benzothiophene, the main research area is ticrynafen diuresis uricosuria.

The i.v. infusion of ticrynafen (I) [40180-04-9] (50 mg/kg/h) in rats had no effect on glomerular filtration rate, but increased the urine flow from 4.4 μL/min/g kidney to 19.2; urinary Na excretion increased from 0.14 μEq/min/g kidney to 2.35 and urate [69-93-2] excretion from 2.8 μg/min/g kidney to 4.0. There was no change in the urinary phosphate excretion. In awake animals, I administration decreased the free water clearance from 6.47 to 3.50, but no change in free water reabsorption was observed Thus, I is a uricosuric and diuretic agent in the rat. The natriuresis appears to derive from an inhibitory action of this agent in the cortical diluting segment of the nephron. In comparison to a related uricosuric diuretic, MK-196, I is less potent with respect to both its uricosuric and diuretic properties in the rat.

Research Communications in Chemical Pathology and Pharmacology published new progress about Diuresis. 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, Category: benzothiophene.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Zakidou, Panagiota’s team published research in Molecules in 2021 | CAS: 1468-83-3

Molecules published new progress about Acidity. 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, HPLC of Formula: 1468-83-3.

Zakidou, Panagiota published the artcileSingle Origin Coffee Aroma: From Optimized Flavor Protocols and Coffee Customization to Instrumental Volatile Characterization and Chemometrics, HPLC of Formula: 1468-83-3, the main research area is coffee aroma flavor instrumental volatile characterization chemometrics; GC-MS; HCA; HS-SPME; Heatmap; Maillard reaction; PCA; chemometrics; coffee cupping; flavor; geographical origin.

In this study, the aroma profile of 10 single origin Arabica coffees originating from eight different growing locations, from Central America to Indonesia, was analyzed using Headspace SPME-GC-MS as the anal. method. Their roasting was performed under temperature-time conditions, customized for each sample to reach specific sensory brew characteristics in an attempt to underline the customization of roast profiles and implementation of sep. roastings followed by subsequent blending as a means to tailor cup quality. A total of 138 volatile compounds were identified in all coffee samples, mainly furan (∼24-41%) and pyrazine (∼25-39%) derivatives, many of which are recognized as coffee key odorants, while the main formation mechanism was the Maillard reaction. Volatile compounds’ composition data were also chemometrically processed using the HCA Heatmap, PCA and HCA aiming to explore if they meet the expected aroma quality attributes and if they can be an indicator of coffee origin. The desired brew characteristics of the samples were satisfactorily captured from the volatile compounds formed, contributing to the aroma potential of each sample. Furthermore, the volatile compounds presented a strong variation with the applied roasting conditions, meaning lighter roasted samples were efficiently differentiated from darker roasted samples, while roasting degree exceeded the geog. origin of the coffee. The coffee samples were distinguished into two groups, with the first two PCs accounting for 73.66% of the total variation, attributed mainly to the presence of higher quantities of furans and pyrazines, as well as to other chem. classes (e.g., dihydrofuranone and phenol derivatives), while HCA confirmed the above results rendering roasting conditions as the underlying criterion for differentiation.

Molecules published new progress about Acidity. 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, HPLC of Formula: 1468-83-3.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Ahokas, J. T.’s team published research in IRCS Medical Science in 1984-10-31 | CAS: 40180-04-9

IRCS Medical Science published new progress about Cytosol. 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.

Ahokas, J. T. published the artcileThe effect of tienilic acid on paracetamol toxicity, Related Products of benzothiophene, the main research area is tienilate paracetamol toxicity glutathione transferase.

Tienilic acid (I) [40180-04-9] inhibited the activity of mouse liver cytosolic glutathione-S-transferase (GSH-t) [50812-37-8] in vitro, with inhibition ranging 23-48%. In mice, the administration of paracetamol (II) [103-90-2] (302 mg/kg, i.p.), a drug normally detoxified through conjugation by the GSH-t system, along with I (40 mg/kg, i.p.) did not result in an increase of II toxicity. Thus, the interaction between II and a strong GSH-t inhibitor, I, does not lead to enhanced II toxicity. Results are discussed with respect to II detoxification via GSH-t.

IRCS Medical Science published new progress about Cytosol. 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

 

Dan, Takashi’s team published research in European Journal of Pharmacology in 1990-10-23 | CAS: 40180-04-9

European Journal of Pharmacology published new progress about Anions. 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.

Dan, Takashi published the artcileUricosurics inhibit urate transporter in rat renal brush border membrane vesicles, Application of 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, the main research area is uricosuric urate transporter kidney brush border.

It has been proposed that a urate-anion exchanger system in brush border membrane vesicles (BBMV), which mediates hydroxyl ion (OH-) gradient-dependent urate uptake, is the most likely route for the mediation of urate transport in the first step of urate reabsorption in the proximal tubules. Luminal drugs which inhibit urate reabsorption would inhibit the transport of urate into the cell by blocking the urate-anion exchanger. To confirm this hypothesis, the inhibitory effects of well-known uricosuric drugs on the OH-/urate exchange in BBMV were studied. The rank order of potency was benzbromarone > tienilic acid > sulfinpyrazone > probenecid, which is consistent with clin. doses in man. AA-193 (5-chloro-7,8-dihydro-3-phenylfuro[2,3-g]-1,2-benzisoxazole-7-carboxylic acid), an excellent candidate for a uricosuric, exerted the most potent inhibition on urate uptake (Ki = 0.12 μM). In contrast with that by stilbene disulfonates, the inhibition by AA-193 or benzbromarone was reversible.

European Journal of Pharmacology published new progress about Anions. 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

 

Ullrich, Karl J.’s team published research in Kidney International in 1989-07-31 | CAS: 40180-04-9

Kidney International published new progress about Anions. 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.

Ullrich, Karl J. published the artcileContraluminal organic anion and cation transport in the proximal renal tubule: V. Interaction with sulfamoyl- and phenoxy diuretics, and with β-lactam antibiotics, SDS of cas: 40180-04-9, the main research area is kidney tubule contraluminal ion transport; xenobiotic ion transport kidney tubule; antibiotic ion transport kidney tubule; diuretic ion transport kidney tubule.

In order to study the interaction of sulfamoyl- and phenoxy-diuretics as well as of β-lactam antibiotics with the contraluminal anion and cation transport systems, the inhibitory potency of these substances against the influx of [3H]p-aminohippurate, [14C]succinate, [35S]sulfate, and [3H]N1-methylnicotinamide into cortical tubular cells were determined The results show that the probenecid, the diuretics furosemide, piretanide, hydrochlorothiazide, acetazolamide, ethacrynic, and tielinic acid, and the β-lactam antibiotics of the penicillin and cephalosporin type interact with the anion and cation transport systems in a predictable fashion.

Kidney International published new progress about Anions. 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

 

Lemieux, G.’s team published research in Nephron in 1979 | CAS: 40180-04-9

Nephron published new progress about Kidney. 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, HPLC of Formula: 40180-04-9.

Lemieux, G. published the artcileThe renal handling of tienilic acid (ticrynafen), a new diuretic with uricosuric properties, HPLC of Formula: 40180-04-9, the main research area is tienilic acid diuresis kidney; ticrynafen diuresis mechanism.

Tienilic acid (I) [40180-04-9] was highly bound to plasma proteins of dogs at 37° (>95% at drug concentrations of 3.0-20.0 mg/dL). Thus, glomerular filtration of the drug is negligible and I must reach the kidney at the antiluminal site of the tubule. During free-flow studies, the clearance of I at stable plasma concentrations (3.0-20.0 mg/dL) ranged from 11-22% of glomerular filtration. These values are 3-5 times greater than that accounted for by filtration of the drug alone and are highly suggestive of tubular secretion. Secretion becomes more apparent during alkalinization of the urine when the clearance of I may rise to 40 and even 100% of glomerular filtration. During stop-flow studies, the urine over plasma ratio of the drug (U/P TA) over that of creatinine (U/P Cr) decreased along the nephron indicating progressive reabsorption. At equivalent plasma concentration, I markedly depressed p-aminohippuric acid (PHA) transport in the proximal tubule. When plasma I concentration was kept low (5 mg/dL) and PAH concentration was raised to 30 mg/dL, the (U/P TA)/(U/P Cr) dropped by 50%. These results indicate active secretion of I in the proximal tubule followed by passive pH dependent reabsorption along the nephron. The drug is transported through the common organic acid pathway by a carrier having higher affinity for I than for PAH.

Nephron published new progress about Kidney. 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, HPLC of Formula: 40180-04-9.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Oker-Blom, Christian’s team published research in Toxicology Letters in 1980 | CAS: 40180-04-9

Toxicology Letters published new progress about Blood. 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.

Oker-Blom, Christian published the artcileToxicological studies on tienilic acid in rats, Safety of 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, the main research area is tienilic acid toxicity; sex tienilic acid toxicity.

The subacute oral toxicity of tienilic acid (I) [40180-04-9] in male and female rats was studied. Animals were given 0, 30, 120, and 480 mg I/kg as a 3% gum arabic suspension for 28 days. At 30 mg I/kg, blood pressure and serum uric acid [69-93-2] decreased. At the 2 higher dose levels, a slight decrease in Hb and an increase in serum glutamic-pyruvic transaminase [9000-86-6] activity was noticed, and there was a significant increase in the liver weight and serum Mg concentration of male rats, while the liver weight of female rats increased only slightly. One microscopic examination, unicellular necrosis of small groups of liver cells was noted, together with focal round-cell infiltration and some stasis of the 2 higher dose levels in some animals. I had no noticeable effects on other organs or parameters.

Toxicology Letters published new progress about Blood. 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

 

Ahmed, Nahed K.’s team published research in Journal of Pharmacology and Experimental Therapeutics in 1979-04-30 | CAS: 40180-04-9

Journal of Pharmacology and Experimental Therapeutics published new progress about Brain. 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, Quality Control of 40180-04-9.

Ahmed, Nahed K. published the artcileComparison and characterization of mammalian xenobiotic ketone reductases, Quality Control of 40180-04-9, the main research area is drug metabolism ketone reductase enzyme; liver kidney ketone drug reduction.

Rabbit liver extracts catalyzed the reduction of the ketone group of the following drugs: oxisuran [27302-90-5], metyrapone [54-36-4], naloxone [465-65-6], naltrexone [16590-41-3], 3,7-dimethyl-1-(5-oxohexyl)-xanthine (3,7-DMX) [6493-05-6], and daunorubicin [20830-81-3]. The reductases catalyzing these reactions were extracted from rabbit liver and characterized. Significant activity was also extracted from human liver, but rat and mouse livers had very low levels of the ketone reductases. Although reductase activity occurs mainly in the liver and kidney, detectable activity was also observed in spleen, lung, and brain. All drug reductases displayed an acid pH optimum, had an absolute requirement for NADPH as cofactor, and occurred primarily as cytoplasmic enzymes. Although the reductases elute from gel filtration chromatog. in slightly different volumes, all enzymes have mol. weights in the range of 32,000 to 38,000 daltons. The drug reductases were not significantly inhibited by phenobarbital or by pyrazole, suggesting that the ketone reductases exist as a class of enzymes distinct from aromatic aldehyde reductases and classical alc. dehydrogenase. The ketone reductases were inhibited by the plant flavonoid quercitrin. Isoelec. focusing resolved drug reductases into multiple forms. The major activities for 3,7-DMX, oxisuran, and metyrapone focused as a single sym. coincident peak with a pI of 4.8, whereas the majority of naloxone and naltrexone reductases focused as heterogeneous bands above pH 6.0. Minor forms of most of the drug reductases were also evident.

Journal of Pharmacology and Experimental Therapeutics published new progress about Brain. 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, Quality Control of 40180-04-9.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Acosta, Daniel’s team published research in Toxicology Letters in 1982-03-31 | CAS: 40180-04-9

Toxicology Letters 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, HPLC of Formula: 40180-04-9.

Acosta, Daniel published the artcileLack of cytotoxicity of ticrynafen in primary cultures of rat liver cells, HPLC of Formula: 40180-04-9, the main research area is tricrynafen cytotoxicity liver.

Primary cultures of hepatocytes obtained from neonatal Sprague-Dawley rats were grown in arginine-deficient, ornithine-supplemented medium to inhibit fibroblastic overgrowth and to selectively isolate relatively pure cultures of parenchymal hepatocytes. This system of primary hepatocytes was used to study the potential cytotoxicity of ticrynafen (I) [40180-04-9] by measuring cytoplasmic enzyme leakage, cell viability, and total protein per culture dish. Hepatic cultures were treated with the drug in concentrations ranging from 10-3 M to 10-6 M and for durations from 2 to 8 h. The results of the study indicate that ticrynafen was minimally toxic to the hepatocytes.

Toxicology Letters 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, HPLC of Formula: 40180-04-9.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Hildebrandt, E.’s team published research in Journal of Pharmacy and Pharmacology in 1984-09-30 | CAS: 40180-04-9

Journal of Pharmacy and 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, Application of 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid.

Hildebrandt, E. published the artcileIndirect inhibition of vitamin K epoxide reduction by salicylate, Application of 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, the main research area is salicylate vitamin K epoxide reductase.

Salicylate  [69-72-7] antagonizes the vitamin K  [12001-79-5]-dependent biosynthesis of clotting factors in the rat and produces an elevation of the ratio of vitamin K epoxide  [25486-55-9] to vitamin K in the liver. Vitamin K epoxide is reduced to vitamin k by a vitamin K epoxide reductase  [55963-40-1], and 1 mM salicylate was required to cause a 50% inhibition of the dithiothreitol-dependent in-vitro reduction of vitamin K epoxide by this enzyme. This enzyme was, however, inhibited 50% by as little as 70-80 μM salicylate when reducing equivalent for the reaction were furnished by endogenous cytosolic reductants. This effect on the cytosolic reductant supply was shown to be unrelated to a previously demonstrated inhibition of DT-diaphorase by salicylate. The concentrations of salicylate at which significant inhibitory effects are exerted are in-vitro (50-100 μM) are below the 200 μM levels observed in the livers of rats given an anticoagulating dose of salicylate.

Journal of Pharmacy and 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, Application of 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem