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At least 397 records · Page 22Linked to original sources

[Activation of the blood kallikrein-kinin system in disseminated intravascular coagulation in rats. The significance of the pulmonary component and an attempt at correction with aspirin].

It has been shown that the development in animals of disseminated intravascular coagulation (DIC) caused by long-term intravenous infusion of thrombin was accompanied by appreciable activation of the kallikrein-kinin system, being characteristic of acute pathological processes. In the initial stages of the process development, prekallikrein and kallikrein inhibitor were observed to be secreted from the lungs to arterial blood. Further development of DIC led to the depletion of the reserves of the kinin system. Pretreatment with a single low dose of acetylsalicylic acid considerably reduced the total animals' lethality and postponed blood kinin system activation determined by the development of DIC.

4-Aminobenzoic Acid↗

Serine esterase inhibitor reduces contractions with isolated trachea and lung strips from guinea pigs induced by phospholipase A2.

The regulation of the phospholipid metabolism (arachidonic acid (AA) cascade) plays a key role in the pathogenetic mechanisms of the various forms of bronchial asthma. This pathogenetic mechanism offers also important therapeutic implications. Since AA liberation is modulated by phospholipase A2 (PLP-A2) the authors studied the effects of PLP-A2 on guinea pig airways under in vitro conditions and their responses to action of protease inhibitor. Experiments were performed in organ bath with lung strips and tracheal spirals from male guinea pigs. PLP-A2 caused in both models dose-dependent contractions. Para-aminomethyl-benzoic acid reduced PLP-A2-induced contractions in lung strips and trachea in a similar way. This reduction is apparently due to inhibition of AA liberation. These experimental findings underline the relevance of AA cascade to pathogenesis of bronchoconstriction and bronchial hyperreactivity. They support the clinical effectiveness of para-aminomethylbenzoic acid demonstrated earlier. The search for new potential antiasthmatic drugs with the site of action on AA liberation from phospholipids requires in vitro test systems. Guinea pig airway preparations proved to be a suitable in vitro model. The inhibition of PLP-A2 by protease inhibitors seems to be a principal (corticosteroid-like) way for modulation of bronchoconstriction.

4-Aminobenzoic Acid↗

[Effectiveness of the calcium antagonist nifedipine and the protease inhibitor with plasmin inactivating effect para-aminomethylbenzoic acid on stress-induced bronchial asthma].

In 15 asthmatics (7 females, 8 males, average age 23.3 years) the efficacy of the calcium antagonist nifedipine (Corinfar) and of PAMBA on the exercise-induced asthma was investigated. The patients underwent for 6 minutes a submaximal exercise (80 +/- 5% of the age-related maximum pulse rate) on the bicycle ergometer or by free running. Nifedipine exhibited a highly significant inhibition of the exercise-induced bronchial obstruction (p less than 0.001). Under the PAMBA-medication no significant differences could be stated in comparison to the exercise test without medicament (p greater than 0.5). A standardization of the exercise tests is to be aspired to.

4-Aminobenzoic Acid↗

[Circulating cardiac antigens in animals with experimental myocardial infarct undergoing malaben pharmacotherapy].

It has been established in chronic experiments on rats that during experimental myocardial infarction, the blood has a complex of heart antigens (up to 250 micrograms/ml). In untreated animals, a high content of heart antigens remains unchanged for a month, slightly diminishing in the second half of the observation period. During malaben treatment, the concentration of heart antigens and duration of their circulation in the blood noticeably decreases which evidences the reduction of the focus of necrosis in the myocardium. It is inferred that determination of the blood content of heart antigens may serve as diagnostic criterion and prognostic test in coronary heart disease subjected to drug therapy.

4-Aminobenzoic Acid↗

Bentiromide as a test of exocrine pancreatic function in adult patients with pancreatic exocrine insufficiency. Determination of appropriate dose and urinary collection interval.

A dose-ranging crossover study of orally administered bentiromide was conducted in 47 patients with chronic pancreatic disease and 61 healthy volunteers. Four doses (100 mg, 500 mg, 1 g, and 5 g) and postdosing urine collection periods (0-3, 0-6, 0-12, and 0-24 h) were studied. Of these, the 500-mg dose and 0-6-h urine collection period afforded maximal separation of urinary arylamine excretion rates between the two populations. At this dose and collection period, the lower limit of normal (mean - 2 SD) for the control group was 57%; none of the healthy volunteers had 6-h arylamine excretion rates less than 50%. The agent was well tolerated except at the 5-g dose level, where nausea, vomiting, and diarrhea were common. Bentiromide appears to be a useful agent in the assessment of exocrine pancreatic function.

4-Aminobenzoic Acid↗

Comparative studies on thrombin inhibitors in experimental microthrombosis.

The influence of thrombin inhibitors, which differ both in their chemical structure and type of inhibition on thrombin-induced microthrombosis was studied in rat lungs. The antithrombotically effective doses and blood levels of the compounds correlated with their kinetic constants for inhibition of thrombin. In preventing microthrombosis, some of the synthetic inhibitors tested surpassed the effectiveness of heparin and approached that of the naturally occurring inhibitor hirudin.

4-Aminobenzoic Acid↗

[Experimental induction of atherosclerosis in guinea pigs fed a cholesterol and vitamin D2-rich diet].

Atherosclerotic lesions of aorta and arteries were induced in guinea pigs fed a diet supplemented with 1% cholesterol and vitamin D2 (0.75 million IU/kg of diet) for 6 weeks. Histopathological observation revealed intimal proliferation and calcification of the intima and media, but no atheroma was present at the sites of arterial injury. However, the biochemical findings revealed accumulation of cholesterol, mainly esterified, and calcium in the aorta. Significant correlation between the calcium and phosphorus contents in the aorta indicates the presence of a probable calcium-phosphate complex. Synergism for the induction of atherosclerotic lesions was shown between high cholesterol and excess vitamin D2. Sodium 4-(hexadecylamino)benzoate (cetaben) (90 mg/kg/day, p.o.) and trisodium ethane-1-hydroxy-1,1-diphosphonate (EHDP) (5 mg/kg/day, s.c.) inhibited the development of atherosclerotic lesions induced in this manner. These effects were associated with a significant reduction of serum and aortic cholesterol levels and a significant elevation of HDL-cholesterol levels caused by cetaben, and a significant reduction in aortic calcium caused by EHDP. These two drugs and clofibrate, however, had no significant effect on the regression of pre-established atherosclerotic lesions.

4-Aminobenzoic Acid↗

Comparative study of the estimation of exocrine pancreatic function using p-(N-acetyl-L-tyrosyl)- and p-(N-benzoyl-L-tyrosyl)aminobenzoic acid.

A comparative study using the oral test with chymotrypsin substrates p-(N-acetyl-L-tyrosyl)- and p-(N-benzoyl-L-tyrosyl) aminobenzoic acid (Ac-Tyr-PAB and Bz-Tyr-PAB) was carried out in 43 adults divided into four groups comprising controls (n = 18), chronic pancreatitis (n = 13), after acute pancreatitis (n = 7), and celiac sprue (n = 4), after separate administration of both derivatives and determination of PABA urinary output in 6 and 8 hours. Both derivatives were diagnostically comparable. The specificity of both derivatives in the investigated group in 6 and 8 hours was 100%, and test sensitivity in patients with chronic pancreatitis, was in 6 hours 90.9% for Ac-Tyr-PAB and 72.7% for Bz-Tyr-PAB, and 8 hours 81.8% for both compounds. Differentiation between the controls and the chronic pancreatitis group was better in Ac-Tyr-PAB, as adjudged by the sensitivity and significance of the Student t-test criterion.

4-Aminobenzoic Acid↗

Chemical control of hyperfibrinolytic states by synthetic inhibitors of fibrinolytic enzymes.

The effects of two types of synthetic inhibitor of fibrinolytic enzymes (omega-aminocarboxylic acids, benzamidine derivatives) on intravascular fibrinolysis and fibrinogenolysis were studied in rats. Generalised primary fibrinogenolysis was produced by infusion of human plasminogen-streptokinase complex, secondary fibrinolysis was induced by infusion of the thrombin-like enzyme batroxobin. The inhibitors exerted different effects on the hyperfibrinolytic states. The omega-aminocarboxylic acids (PAMBA, AMCA) inhibited fibrinolysis more effective than fibrinogenolysis. In contrast, the benzamidines (APPA, NANP) were more potent inhibitors of fibrinogenolysis. Aprotinin examined for comparison behaved like the benzamidine derivatives.

4-Aminobenzoic Acid↗