Tag: M.W=200-350

Ferrara, L A published the artcileLong term treatment with tienilic acid or thiazides: comparison of antihypertensive and metabolic effects., Quality Control of 40180-04-9, the main research area is .

A comparison has been made of arterial pressure and major metabolic parameters during long term treatment with tienilic acid and a hydrochlorothiazide-amiloride combination, using a randomized single-blind study without cross-over. A significant fall in systolic and diastolic blood pressure and no change in most biochemical parameters was observed with both drugs. Serum uric acid concentration was decreased during tienilic acid and was slightly increased whilst subjects took the hydrochlorothiazide-amiloride combination; serum potassium was slightly decreased on tienilic acid. No sign of hepatotoxicity was detected.

European journal of clinical pharmacology published new progress in MEDLINE about 40180-04-9, 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

Epstein, D L published the artcileNonsulfhydryl-reactive phenoxyacetic acids increase aqueous humor outflow facility., Name: 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, the main research area is .

PURPOSE: The phenoxyacetic acid, ethacrynic acid (ECA), has potential use in glaucoma therapy because it acts to increase aqueous outflow in vivo and in vitro. In human trabecular meshwork (HTM) cell culture, ECA acts to change cell shape and attachment, effects that have been correlated with microtubule (MT) alterations and chemical sulfhydryl (SH) reactivity. To further explore these actions, we evaluated two non-SH reactive phenoxyacetic acids, inadcrinone and ticrynafen, and the MT-disrupting drug vinblastine. METHODS: Excised bovine and porcine eyes were perfused and outflow facility measured. Calf pulmonary artery endothelial and HTM cells were grown in culture and cytoskeletal effects evaluated after drug treatment. RESULTS: Indacrinone, ticrynafen, and vinblastine all caused an increase in outflow facility. In contrast with ECA, the outflow effects of indacrinone and ticrynafen were not blocked by excess cysteine. Although indacrinone and ticrynafen produced changes in cell shape in vitro, the beta-tubulin staining pattern of treated cells was not altered. Vinblastine caused cell shape change and the expected MT disruption. CONCLUSIONS: Phenoxyacetic acids can increase aqueous outflow facility and alter HTM cell shape and attachment in vitro by a non-SH, non-MT mechanism (which is probably shared also by ECA). These findings suggest the possibility of a broader class of glaucoma drugs that may be directed at the HTM. An understanding of the cellular target for these drugs has implications both for potential glaucoma therapy and for the cytoskeletal mechanisms involved in normal outflow function.

Investigative ophthalmology & visual science published new progress in MEDLINE about 40180-04-9, 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, Name: 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Shinosaki, T published the artcileStop-flow studies on tubular transport of uric acid in rats., Computed Properties of 40180-04-9, the main research area is .

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 intravenous 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 kidneys 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 in MEDLINE about 40180-04-9, 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, Computed Properties of 40180-04-9.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Walker, R G published the artcileTienilic acid in the treatment of mild to moderate hypertension., Synthetic Route of 40180-04-9, the main research area is .

1. A double-blind crossover trial comparing the antihypertensive effect of tienilic acid and hydrochlorothiazide was conducted in thirty-eight patients with mild to moderate hypertension. 2. Tienilic acid was shown to be as effective as hydrochlorothiazide in controlling blood pressure. 3. Tienilic acid acid significantly lowered serum uric acid levels compared with both placebo and hydrochlorothiazide. 4. Tienilic acid was generally well tolerated but one patient developed acute renal failure due to acute allergic interstitial nephritis whilst taking the drug.

Clinical and experimental pharmacology & physiology published new progress in MEDLINE about 40180-04-9, 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

Salvetti, A published the artcileEffects of prostaglandins inhibition on changes in active and inactive renin induced by antihypertensive drugs., SDS of cas: 40180-04-9, the main research area is .

The behaviour of active (AR) and inactive (IR) renin was studied in 48 hypertensive patients (37 with uncomplicated essential hypertension and 11 with reno-vascular hypertension) treated with indomethacin alone or with AR stimulating (bumetanide, tienilic acid, captopril) and inhibiting (atenolol) drugs before and after indomethacin addition. In 10 pts indomethacin (50mg q.i.d./3 days) reduced (p less than 0.05) AR and to a lesser extent IR. In 6 pts bumetanide (1 mg) increased (p less than 0.05) only AR and this effect was abolished by indomethacin. In 6 pts tienilic acid (250 mg) increased (p less than 0.05) only AR and this action was unchanged by indomethacin. In 11 renovascular pts captopril (100mg) increased AR (p less than 0.01) and lesser IR and both these effects were uninfluenced by indomethacin. In 11 essential hypertensive pts captopril (25mg b.i.d./3 days) increased only AR (p less than 0.02), but after 1 year both AR and IR were increased (p less than 0.05) and these effects were abolished by indomethacin. In all the above reported protocols we did never find any inverse correlation between either AR and IR values or their induced changes. These data suggest that prostaglandins stimulate, even if not to a similar extent, both AR and IR and that drugs, which stimulate renin either through or independently of PGs, did not cause any apparent interconversion of plasma IR into AR. In 6 pts atenolol (100 mg daily/6 days) reduced AR (p less than 0.05) and tended to increase IR. Indomethacin addition further decreased AR and reduced IR (both p less than 0.05 vs atenolol alone): however the proportion (% of total) of IR was still reduced. These findings suggest that beta 1-adrenoreceptors blockade exerts a divergent effect on active and inactive renin and that this action is not influenced by PGs synthesis inhibition.

Clinical and experimental hypertension. Part A, Theory and practice published new progress in MEDLINE about 40180-04-9, 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

Maass, A R published the artcilePharmacokinetics and mode of action of tienilic acid., SDS of cas: 40180-04-9, the main research area is .

A review of the absorption, distribution, metabolism and excretion of ticrynafen (tienilic acid) in 8 animal species, including man, is presented. Although some species effects are apparent, ticrynafen absorption is essentially complete following oral administration. The compound is extensively bound to plasma proteins, primarily albumin. Consequently, tissue concentrations are generally lower than plasma concentrations. Plasma and whole body clearance of ticrynafen is rapid due both to metabolism and to extensive renal excretion of the compound and its metabolites. Male/female differences in renal excretion occur, with a subsequent effect on ticrynafen metabolism. Ticrynafen is an inhibitor of reabsorption of sodium and uric acid by the kidney. This inhibitory effect, within the renal tubular lumen, accounts for its diuretic and uricosuric activity and could account for its antihypertensive activity, although a direct effect has also been claimed. Ticrynafen is also a classical example of a competitive inhibitor of organic acid transport in the kidney and other organs. Much of the drug-drug interaction involving ticrynafen is understandable due to its effect on transport. However, potentiation of anticoagulant activity appears to involve some direct effects upon warfarin metabolism although ticrynafen, in general, is not an enzyme inducer or inhibitor. Toxicity of ticrynafen is low in all animal species.

Clinical and experimental hypertension. Part A, Theory and practice published new progress in MEDLINE about 40180-04-9, 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

Prandota, J published the artcileEffect of tienilic acid (Diflurex) on the binding of warfarin 14C to human plasma proteins., Product Details of C13H8Cl2O4S, the main research area is .

Tienilic acid (Diflurex), a new diuretic with a chemical structure close to that of ethacrynic acid, displaces significant amounts of warfarin from 2 g/l human albumin in vitro by a competitive mechanism. When physiologic concentrations of human albumin are used, or with human plasma there is no such interaction. Because excessive hypoprothrombinaemia and haemorrhage were reported in vivo when tienilic acid was added to oral coumarin anticoagulant therapy, it is advised to use another diuretic if necessary.

International journal of clinical pharmacology, therapy, and toxicology published new progress in MEDLINE about 40180-04-9, 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

Ambrosioni, E published the artcileEffects of tienilic acid used alone and in association with triamterene or amiloride on urinary excretion of electrolytes., Quality Control of 40180-04-9, the main research area is .

The K-sparing effects of amiloride (A) and triamterene (T) associated with tienilic acid (C) are studied, along with their effects on diuresis and on the urinary excretion of uric acid, Mg, Na, Cl, P, and Ca. Eighteen hospitalized patients, divided into two groups of nine, received the following dosages of the drugs. The first group took 250 mg of C (equivalent to 50 mg hydrochlorothiazide), 5 mg of A and 100 mg of T; the second received double doses of both A and T but the same dose of C. Each treatment was administered on 2 not necessarily consecutive days, so as to have a total of 6 days of treatment per patient according to a balanced randomized design identical for the two groups. The data were obtained from urine collected during the first 8 h after the drug was administered, and during the following 16 h. A and T showed a significant K-sparing effect (p less than 0.01) only for the second group, and only at the higher dosages were minor effects on the urinary excretion of uric acid, Mg, and Cl noted (p less than 0.05). The association of A or T with C was well tolerated, and no important side effects were observed.

International journal of clinical pharmacology, therapy, and toxicology published new progress in MEDLINE about 40180-04-9, 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

Rosendorff, C published the artcileThe treatment of mild to moderate essential hypertension with tienilic acid (ticrynafen)., Recommanded Product: 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, the main research area is .

This paper reports a clinical trial of tienilic acid, a new diuretic with uricosuric properties, in 23 patients with mild to moderate hypertension (standing diastolic blood pressure 90-120 mmHg). Tienilic acid was compared with hydrochlorothiazide in a variable-dose, double-blind cross-over study, and the duration of therapy was 8 weeks for each drug. The falls in blood pressure (systolic/diastolic) were: 11/11 mmHg supine and 17/11 mmHg standing for tienilic acid, and 8/12 mmHg supine and 9/17 mmHg standing for hydrochlorothiazide. There were no significant differences between the two drugs in their effect on blood pressure and heart rate, and regarding side-effects and laboratory results, except for serum uric levels (mean fall of 1,5 mg/dl with tienilic acid and mean increase of 1.1 mg/l with ydrochlorothiazide).

South African medical journal = Suid-Afrikaanse tydskrif vir geneeskunde published new progress in MEDLINE about 40180-04-9, 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

Riegelman, R K published the artcileWhat to do until the FDA arrives., Application In Synthesis of 40180-04-9, the main research area is .

The need for clinical monitoring to assure drug safety despite reliance on Food and Drug Administration testing is illustrated. The need to temper theory with clinical experience is exemplified by the recent examples of swine flu, resistant gonorrhea, and resistant pneumococcal infection. The potential for adverse effects to escape detection in animal studies and small-scale human trials is illustrated by the examples of ticrynafen, chloramphenicol, and diethylstilbestrol. The potential for unexpected side effects when established drugs are used in new ways is demonstrated by the examples of retrolental fibroplasia and vitamin D toxicity. The responsibilities of the medical profession and the individual practitioner include a healthy skepticism of newly introduced treatments, active participation in clinical monitoring, and maintenance of a system for chart retrieval when drugs are recalled or new effects reported.

Postgraduate medicine published new progress in MEDLINE about 40180-04-9, 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 In Synthesis of 40180-04-9.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem