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Syntheses of several tripeptide analogues of leupeptin containing C-terminal argininal, lysinal, or ornithinal units are presented. The synthetic analogues were tested as inhibitors of trypsin, plasmin, and kallikrein. (Benzyloxycarbonyl)-L-leucyl-L-leucyl-L-argininal (2a) was significantly less effective as an inhibitor of trypsin and plasmin activity than leupeptin. (Benzyloxycarbonyl)-L-leucyl-L-leucyl-L-lysinal (2e) and (benzyloxycarbonyl)-L-leucyl-L-leucyl-L-ornithinal (2i) display different inhibition characteristics than (benzyloxycarbonyl)-L-leucyl-L-leucyl-L-argininal (2a). While (benzyloxycarbonyl)-L-leucyl-L-leucyl-L-argininal (2a) showed moderate inhibition of all three enzymes tested, (benzyloxycarbonyl)-L-leucyl-L-leucyl-L-lysinal (2e) was less effective as an inhibitor of trypsin and plasmin activity. Of the three enzymes tested, (benzyloxycarbonyl)-L-leucyl-L-leucyl-L-ornithinal (2i) showed significant inhibition of kallikrein activity only. Modifications made in the composition and sequence of the P2 and P3 amino acids also resulted in variations in the inhibitory activity of the analogues. In general, plasmin showed a strong preference for inhibitors which contain an L-phenylalanyl-L-leucyl or an L-leucyl-L-valyl unit in the P2 and P3 positions. 相似文献
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The techniques specific to peroperative fluorocholangiography are discussed based on an experience of 632 cholangiograms and an estimation has been made of the associated radiation doses to staff and patients. Rapid and accurate information can be obtained during fluorocholangiography using appropriate techniques with acceptably low radiation hazards. 相似文献
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Valery L Feigin Craig S Anderson Anthony Rodgers Neil E Anderson Alistair J Gunn 《Journal of clinical neuroscience》2002,9(5):502-507
Current treatment of acute stroke remains unsatisfactory. This review presents experimental and clinical data which suggest that mild induced hypothermia could be a potent and practicable neuroprotective treatment of acute ischaemic stroke and intracerebral haemorrhage. Hypothermia, if proven to be safe, effective and widely practicable in patients with acute stroke, could have an enormous positive impact on reducing the burden of stroke worldwide. Critical issues that will need to be considered in a well designed randomised controlled trial of induced hypothermia in acute stroke patients are discussed. 相似文献
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Prediction of choledocholithiasis using a pocket microcomputer 总被引:4,自引:0,他引:4
T V Taylor C P Armstrong S Rimmer S B Lucas J Jeacock A A Gunn 《The British journal of surgery》1988,75(2):138-140
A computerized method, using a small pocket computer, has been used to predict the presence of choledocholithiasis in a prospective series of 239 patients undergoing cholecystectomy. From an initial data base of 424 patients 36 factors were evaluated and the most important 2 of these were determined by multivariate analysis for use in the prospective analysis. Satisfactory operative cholangiograms were a prerequisite to evaluation of the statistical method and were obtained in 90.4 per cent of cases. Using the computerized method a common bile duct stone would have been overlooked in only 1 patient but 17 unnecessary explorations would have been carried out. The overall accuracy of the computerized method was 92.5 per cent. When the method was applied to a further study of 97 patients from a separate centre the overall accuracy was 85.6 per cent. If the method was used to aid selective use of operative cholangiography, cholangiograms would be performed in 20 per cent and stones would be overlooked in less than 1 per cent. 相似文献
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Brandon JC; Teplick SK; Haskin PH; Sammon JK; Muhr WF; Hofmann AF; Gambescia RA; Zitomer N 《Radiology》1988,166(3):665-667
The authors describe their experience with methyl tertiary butyl ether (MTBE) in a larger series of patients than previously reported in order to acquaint physicians with both its effectiveness for dissolution of common bile duct calculi and the limitations of its use. Ten patients with 13 biliary calculi underwent percutaneous stone dissolution treatment with the experimental cholesterol solvent, MTBE. Three stones completely dissolved within 30 minutes, seven were reduced in size, and three were visibly unaffected. All stones not completely dissolved were easily extracted by means of a stone basket except for one in a patient taken to surgery. Although MTBE perfusion is an effective technique for management of biliary calculi, practitioners should be aware that its use is quite time consuming and its odor difficult to control. 相似文献