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The adenosine receptor antagonist, 8-phenyltheophylline, causes diuresis and saliuresis in the rat 总被引:2,自引:0,他引:2
The diuretic and adenosine antagonist actions of two alkylxanthines have been compared in the conscious rat. 8-Phenyltheophylline (10 mg kg-1) antagonized adenosine-induced bradycardia in the rat for at least 3 h whereas enprofylline (10 mg kg-1) had no effect on this response. 8-Phenyltheophylline (10 mg kg-1) evoked diuresis and saliuresis in the rat whereas enprofylline (10 mg kg-1) had no effect on excretory parameters. These results indicate that the diuretic action of some alkylxanthines may be related to adenosine antagonism. 相似文献
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R.P. Butt J.P. Huggins D. Greiling B. Hopkins S. Gaboardi D. Winslow M. Ronald S. Lewis S. Ward E. Levett J. Owen F. Burslem M. Collis S. Bailey P.V. Fish G. Whitlock S. Billotte K. James A. Mcelroy J. Blagg 《International journal of experimental pathology》2004,85(1):A20-A21
Introduction Fibrosis is a component of many tissue pathologies leading to loss of normal tissue function, primarily due to excessive collagen deposition. Collagen is deposited following cleavage of the C- and N- terminal peptides from the pro-collagen molecule. The cleavage of the globular C-peptide by PCP reduces solubility of the fibrillar collagen molecule, resulting in deposition of insoluble collagen. Increased insoluble collagen deposition is a feature of all organ fibroses, with inhibition of this process, a key potential anti-fibrotic mechanism. The aim of this work was to discover potent and selective PCP inhibitors as experimental, topically applied, anti-fibrotic drugs for clinical evaluation.
Materials and methods PCP was cloned from human osteosarcoma cells and enzymatic activity demonstrated using a PCP-specific peptide cleavage assay. Activities were confirmed by measuring cleavage of [3 H]C-peptide from type-I pro-collagen. A cell-based fibroplasias model was employed to demonstrate compound efficacy using collagen deposition, liberated C-peptide and histological endpoints. The activities of PCP inhibitors in fibroblast and epithelial in vitro cell proliferation and migration assays, and selectivity vs. a panel of MMPs were also determined.
Discussion In summary, we have identified and characterized potent and selective inhibitors of PCP for progression to clinical studies for investigation as a treatment paradigm for fibrotic disease.
Materials and methods PCP was cloned from human osteosarcoma cells and enzymatic activity demonstrated using a PCP-specific peptide cleavage assay. Activities were confirmed by measuring cleavage of [
Discussion In summary, we have identified and characterized potent and selective inhibitors of PCP for progression to clinical studies for investigation as a treatment paradigm for fibrotic disease.
Results 相似文献
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M Kaplan HJ Vreman C Hammerman C Leiter B Rudensky MG MacDonald DK Stevenson 《Acta paediatrica (Oslo, Norway : 1992)》1998,87(4):455-457
The incidence (%) of hyperbilirubinemia (serum bilirubin ≥257 μmol/l) was similar in neonates with a combination of ABO incompatibility and glucose-6-phosphate dehydrogenase (G-6-PD) deficiency (45%), with ABO incompatibility (54%) or G-6-PD deficiency (37%), alone (ns). Carboxyhemoglobin values, corrected for inspired CO, were similarly elevated in all three groups (0.87 ± 0.32%, 0.82 ± 0.29%, 0.76 ± 0.18%, respectively, ns), but correlated with bilirubin only in those with ABO incompatibility alone. ABO-incompatible/G-6-PD-deficient neonates, compared with those with either condition alone, are not at increased risk for hemolysis or hyperbilirubinemia. 相似文献
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A 4-wk interval-type training program incorporating omni-kinetic equipment and stationary cycling elicited an increase in the absolute and relative VO2max of an active group of young boys. The improvement in aerobic function was independent of the training protocols of high velocity-low resistance and low velocity-high resistance. However, the training programs failed to increase anaerobic function as measured by an "all-out" cycle test in which power output was calculated in watts and watts per kilogram for 0- to 15-s and 15- to 30-s work periods. Changes in aerobic and anaerobic functions were independent of physiological maturity as determined by serum testosterone level (ng X dl-1). 相似文献
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Vanessa S. Sakalidis Alethea Rea Sharon L. Perrella Jacki McEachran Grace Collis Jennifer Miraudo Stuart A. Prosser Lisa Y. Gibson Desiree Silva Donna T. Geddes 《Nutrients》2021,13(6)
During the COVID-19 pandemic, breastfeeding women have experienced restricted access to support, placing them at increased risk of mental health concerns and limited breastfeeding assistance. This study investigated the effect of the pandemic on feeding choices and maternal wellbeing amongst breastfeeding mothers living in Australian and New Zealand. We conducted a cross-sectional online survey that examined feeding methods, maternal mental wellbeing, worries, challenges, and positive experiences during the pandemic. Most women were exclusively breastfeeding (82%). Partial breastfeeding was associated with perceived low milk supply and longer pregnancy duration during the pandemic. Reduced mental health and wellbeing was associated with lower levels of family functioning, increased perceived stress, and perinatal anxiety. Longer pregnancy duration during the pandemic was associated with lower mental health wellbeing scores, while higher perceived stress scores were reported for regions with higher COVID-19 infection rates and women with perceived low milk supply. Women reported that the pandemic resulted in less pressure and more time for family bonding, while worries about the pandemic, family health, and parenting challenges were also cited. Mental health concerns of breastfeeding women appear to be exacerbated by COVID-19, highlighting a critical need for access to mental health and broader family support during the pandemic. 相似文献