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Summary— KR31080 (2-butyl-5-methyl-6-(1-oxopyridin-2-yl)-3-[[2'-(1H-tetrazol-5-yl) biphenyl-4-yl]methyl]-3H-imidazo[4,5-b] pyridine) is a potent inhibitor of angiotensin type 1 (AT1 ) receptors in rabbit aorta and human recombinant AT1 receptors. In the isolated rabbit thoracic aorta, KR31080 caused a nonparallel shift to the right of the concentration-response curves to angiotensin II (All) with decreased maximal response (pD'2 = 10.1 ± 0.1), but had no effect on the contractile response induced by norepinephrine. KR31080 inhibited specific [125 I]AII binding to rabbit aortic membranes (AT, receptors) and [125 I][Sar1 , Ile8 ]AII binding to human recombinant AT1 receptors in a concentration-dependent manner with IC50 values of 0.84 ± 0.08 nM and 1.92 ± 0.15 nM, respectively, but did not inhibit specific [125 I)AII binding to bovine cerebellum membranes (ÀT2 receptors). In the Scatchard analysis, KR31080 interacted with rabbit aortic AT1 receptors in a competitive manner, similar to losartan. These results demonstrate that KR31080 is a potent and AT1 selective angiotensin receptor antagonist which exerts a competitive antagonism in the [125 I]AII binding assay and insurmountable AT1 receptor antagonism in the functional study. 相似文献
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Leena Joseph R. Anuradha R. Nathuram V. V. Shaha M. C. Abani 《Applied radiation and isotopes》2003,59(5-6):359-362
National intercomparisons of activity measurements of 131I, a radioisotope widely used for diagnosis and therapy of thyroid related ailments, were initiated in 1979 as a quality assurance program, towards improving radiation safety procedures and related dosimetry in Nuclear Medicine Centres (NMCs) in India. Oral administration of a known quantity of radioiodine to patients requires accurate radioactivity measurements to be performed on a well-calibrated isotope calibrators. Under or over estimation of the activity due to a faulty or uncalibrated isotope calibrator could provide misleading results. Calibration of isotope calibrators and the traceablity of subsequent measurements to the national standards laboratory is one of the essential basic radiation safety requirement of the IAEA. In view of the stringent quality assurance requirements for activity measurements imposed by Atomic Energy Regulatory Board, a National Intercomparison Program was initiated and to date ten such intercomparison programs have been conducted by the Radiation Safety Systems Division, of the Bhabha Atomic Research Centre. This program has benefited the participants by making their measurements traceable to the National Primary Standards. Over the years there has been a marked increase in the number of NMCs participating in the intercomparison programs. As a result, the number of institution showing large deviation from the correct value has decreased considerably over the years. This program thus, has enabled participating NMCs to check their isotope calibrators so as to ensure proper delivery of radiation dose to the patients and hence to optimise patient exposure. 相似文献
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Praloy Chakraborty P Shakuja A Kundra Anil Jain Shivendra Singh S Anuradha Anil Agarwal Premashish Kar 《Tropical gastroenterology》2004,25(4):170-171
A 14-year-old male presented with abdominal pain, diarrhoea and a sensation of something prolapsing through the anus during defecation, and was found to have diffuse colonic polyposis. There was no evidence of mucocutaneous hyperpigmentation and family history was negative, suggesting a diagnosis of non-familial juvenile polyposis. Histological analysis of multiple endoscopic biopsies showed features typical of juvenile or retention type (hamartomatous) lesions: dilated cystic glands lined by mucocus-secreting epithelium and prominent, inflamed and congested lamina propria. However, admixed with these features, focal areas of atypical adenomatous changes were recognized. Even the intervening normal-looking colonic mucosa showed some dysplastic changes. These findings indicate that hamartomatous and atypical adenomatous epithelial changes can co exist in non-familial juvenile polyposis and the latter may confer a risk of malignant transformation in this otherwise non-neoplastic disease. 相似文献
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H S Randhawa Anuradha Chowdhary K Preeti Sinha T Kowshik V K Vijayan 《Medical mycology》2006,44(4):343-348
We have reported earlier that Aspergillus fumigatus is inhibited in vitro by Candida albicans which also interferes in its isolation from sputum experimentally seeded with predetermined graded inocula of the two fungi. It was further shown that this interference was neutralized by employing peptone glucose agar with incorporation of fluconazole which is more inhibitory to C. albicans than to A. fumigatus. This communication embodies the results of evaluation of peptone glucose fluconazole agar (PGFA) as a selective culture medium for rapid and enhanced isolation of A. fumigatus from sputum of patients clinically suspected of aspergillosis with C. albicans colonization in the respiratory tract. Of the 23 sputum specimens and one broncho-alveolar lavage collected from 15 suspected aspergillosis patients, A. fumigatus was isolated from all (100%) on PGFA as against only 19 specimens (79%) that proved to be positive on the control PGA medium (P<0.05). The greater efficacy of PGFA than that of PGA was further evident from the 2-fold higher A. fumigatus mean colony count (8.2+/-1.87) on the former medium than on the latter (3.7+/-1.00), and this difference was found to be statistically significant (P<0.05). Besides, A. fumigatus colonies were macroscopically recognizable within 2-3 days on PGFA at 28 degrees C in strong contrast to 5-7 days required on PGA. Based upon these observations, PGFA is recommended for wider application as a selective medium for rapid and enhanced recovery of A. fumigatus from sputum of patients clinically suspected of aspergillosis with C. albicans colonization in their respiratory tract. 相似文献
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SUMMARY Elevated plasma levels of Lp(a) do seem to influence the progression of atherosclerosis. Evidence is emerging that certain apo(a) isoforms may be more atherogenic than others, and in transgenic mice free apo(a) has been shown to be associated with accelerated atherosclerosis. Currently it is not known whether treating elevated Lp(a) levels will reduce progression of atherosclerosis and, as therapeutic options are limited, mass screening of Lp(a) levels in populations is not indicated. The presence of raised Lp(a) levels, however, warrants aggressive treatment to reduce other cardiovascular risk factors. Continuing research to investigate the relationship of the apo(a) gene to other genes, including the plasminogen gene and apo(a)-related genes, will add further information pertaining to the evolution, function, regulation and clinical implications of Lp(a). 相似文献
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Macrophages are known to adhere to a plastic dish via beta2 integrin (CR3) and scavenger receptors. Although their functions such as phagocytosis, endocytosis, and nitric oxide production have been investigated on adherent macrophages in vitro, very little is known about intracellular signals triggered by adhesion to a plastic dish. Recently we reported that the mRNA level of krox-20/egr-2 was significantly increased in rat alveolar macrophages following exposure to fibrous titanium dioxide particles. In the present study we report that up-regulation of krox-20/egr-2 gene expression following adhesion to a plastic dish and homophilic adhesion in rat alveolar macrophages and rat macrophage cell line, NR8383. The mRNA level of krox-20/egr-2 increased with a peak 1 hr after adhesion to a plastic dish in both cell types. Piceatannol inhibited tyrosine-phosphorylation of Syk and decreased both adhesion and krox-20/egr-2 mRNA level. In contrast staurosporine, a serine/threonine kinase inhibitor, increased adherence of macrophages and yet prohibited the adhesion-dependent increase in krox-20/egr-2 gene expression. When NR8383 cells are cultured in suspension, the cells aggregated naturally and produced cell clumps. The mRNA level of krox-20/egr-2 also increased in response to the homophilic intercellular adhesion. The increased mRNA level of krox-20/egr-2 was not caused by inflammatory stimuli, because lipopolysaccharide did not affect the aggregation-dependent up-regulation of krox-20/egr-2 gene. The up-regulation of krox-20/egr-2 gene due to the homophilic cell aggregation was also inhibited either by piceatannol or staurosporine. Those results suggest that krox-20/egr-2 gene expression is triggered by sensing non-specific and homophilic cellular adhesion and the following phosphorylation of signal transducing proteins including Syk and staurosporine-inhibitable kinases. 相似文献
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Baishnab C. Singh Basanta K. Misra Anuradha Rout Nigamananda Mallick M. K. Rout 《Macromolecular chemistry and physics.》1979,180(4):953-958
The kinetics and mechanism of the inhibiting action of toluene on the Ce(IV) initiated polymerization of acrylonitrile were studied together with the effects of [M], [Ce(IV)], [Toluene], [HClO4], [NaClO4], and [Acetic acid] on the rate of polymerization. The values of composite rate constant kkt/kpkoki for toluene (and substituted toluenes) was calculated by plotting [M]/Rp versus [M]?1. A very significant observation in the present study was that the plot of [M]/Rp versus [M]?1 gave a negative intercept, which seems to be a general observation for all inhibiting substrates. On the basis of the experimental data, it could be concluded that the benzyl radical obtained by hydrogen abstraction, and not a chain transfer, is responsible for the inhibition. 相似文献