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181.
1. Hydroxypropyl-beta-cyclodextrin (HP-beta-CD) increases the stability of the oxazolidine prodrug toward hydrolysis. 2. The binding constant (Kb) and rate constant (Kc) for the hydrolysis of the prodrug-HP-beta-CD complex were calculated from the kinetic data. 3. Ion-spray mass spectra confirmed prodrug-HP-beta-CD complexation. 4. Mass spectral and kinetic data indicated 1:1 stoichiometry for the complex. 5. A significant elevation of locomotor activity in rats was observed when either (-)-ephedrine or the prodrug was administered by either the intraperitoneal or the oral route. 6. Addition of HP-beta-CD potentiated the central nervous system effect of both (-)-ephedrine and the prodrug when administered intraperitoneally. However, when the drugs were administered orally, HP-beta-CD caused a decrease in activity. 相似文献
182.
Ingram S.G. Linfield E.H. Brown K.M. Jones G.A.C. Ritchie D.A. Kelly M.J. 《Electron Devices, IEEE Transactions on》1995,42(6):1065-1069
A vertical hot electron transistor incorporating a two-dimensional electron gas (2DEG) base has been fabricated in the GaAs-AlGaAs materials system. The difficulties caused by the need to form selective ohmic contacts to the different conducting layers have been overcome using a combination of in situ focused ion beam (FIB) isolation and molecular beam epitaxial (MBE) regrowth. This has allowed a high yield of working devices to be achieved with a typical common emitter current gain of hFE=6 at low temperatures 相似文献
183.
KG Davey AD Holmes EM Johnson A Szekely DW Warnock 《Canadian Metallurgical Quarterly》1998,36(4):926-930
The FUNGITEST method (Sanofi Diagnostics Pasteur, Paris, France) is a microplate-based procedure for the breakpoint testing of six antifungal agents (amphotericin B, flucytosine, fluconazole, itraconazole, ketoconazole, and miconazole). We compared the FUNGITEST method with a broth microdilution test, performed according to National Committee for Clinical Laboratory Standards document M27-A guidelines, for determining the in vitro susceptibilities of 180 isolates of Candida spp. (50 C. albicans, 50 C. glabrata, 10 C. kefyr, 20 C. krusei, 10 C. lusitaniae, 20 C. parapsilosis, and 20 C. tropicalis isolates) and 20 isolates of Cryptococcus neoformans. Overall, there was 100% agreement between the methods for amphotericin B, 95% agreement for flucytosine, 84% agreement for miconazole, 83% agreement for itraconazole, 77% agreement for ketoconazole, and 76% agreement for fluconazole. The overall agreement between the methods exceeded 80% for all species tested with the exception of C. glabrata (71% agreement). The poorest agreement between the results for individual agents was seen with C. glabrata (38% for fluconazole, 44% for ketoconazole, and 56% for itraconazole) and C. tropicalis (50% for miconazole). The FUNGITEST method misclassified as susceptible 2 of 12 (16.6%) fluconazole-resistant isolates, 2 of 10 (20%) itraconazole-resistant isolates, and 4 of 8 (50%) ketoconazole-resistant isolates of several Candida spp. Further development of the FUNGITEST procedure will be required before it can be recommended as an alternative method for the susceptibility testing of Candida spp. or C. neoformans. 相似文献
184.
JP Edwards SJ West CL Pooley KB Marschke LJ Farmer TK Jones 《Canadian Metallurgical Quarterly》1998,8(7):745-750
Typhoid fever is often associated with abnormal liver biochemical tests, but severe hepatic involvement with a clinical feature of acute hepatitis is a rare complication. There have been more than 150 cases of salmonella hepatitis reported from both developed and developing countries. The documented incidence varies widely from less than 1% to 26% patients with enteric fever. The possible associated factors for development of salmonella hepatitis are virulence of the organisms, delayed treatment and poor general health of the patients. The pathogenesis of severe hepatic involvement in salmonella infection may be multifactorial and includes endotoxin, local inflammatory and/or host immune reactions. Clinical jaundice in salmonella hepatitis usually occurs within the first 2 weeks of the febrile illness. Hepatomegaly and moderate elevation of transaminase levels are common findings. Extreme hepatic dysfunction with hepatic encephalopathy is a rare coexisting complication in salmonella hepatitis. A positive culture for salmonella from blood or stool is essential to differentiate salmonella hepatitis from other causes of acute hepatitis. Hepatic pathology is characterized by the presence of typhoid nodules with marked hyperplasia of reticuloendothelial cells. The prognosis is usually good as salmonella hepatitis responds well to a specific antibiotic therapy and juandice resolves with clinical improvement. The clinical course can be severe with a mortality rate as high as 20%, particularly with delayed treatment or in patients with other complications of salmonella infection. As enteric fever is a common infection, the recognition of salmonella hepatitis is of clinical importance. 相似文献
185.
BT Heelan S Osman A Blyth L Schnorr T Jones AJ George 《Canadian Metallurgical Quarterly》1998,66(8):1101-1103
BACKGROUND: We investigated the potential of predicting allograft rejection by measuring the ability of graft-infiltrating cells to take up 2-[18F]fluoro-2-deoxyglucose ([18F]FDG). This molecule is a positron emitting glucose analogue that is taken up by metabolically active cells and can be detected using positron emission tomography. METHODS: Uptake of [18F]FDG during an alloresponse was measured both in vitro in mixed lymphocyte cultures and in vivo using allogeneic and syngeneic skin grafts. RESULTS: Uptake of [18F]FDG was seen in a mixed lymphocyte reaction. Using a mouse skin graft model, we found that mean [18F]FDG uptake was 1.5-2 times higher in allografts than in syngeneic grafts; the increase in uptake correlated with the level of T-cell infiltrate seen histologically. CONCLUSION: Assessing the metabolic activity of graft-infiltrating cells with [18F]FDG may be useful in the prediction of graft rejection episodes. 相似文献
186.
Eighty beef crossbred steers with an average weight of 493 kg (4·66 kg SD) were allocated at random to one of five treatments to assess the effects of withholding feed and water on carcass shrinkage and meat quality. The five treatments were: slaughter from the feedlot (T1); and 12, 24, 36 and 48 h periods without feed and water prior to slaughter (T2-5).Weights were taken of the live animal and the carcass to monitor shrinkage along with relevant meat quality measurements. There were no treatment differences (P > 0·05) in initial farm weight, but plant weight shrinkage increased from 31gkg(-1) for T1 to 106 g kg(-1) for T5. Warm carcass weight decreased (P < 0·05) from 278·8 kg for T1, to 270·7 kg for T3 and 261·9 kg for T5. Liver, alimentary tract components, hide and head decreased as a proportion of farm weight as time without feed and water increased. Muscle pH at 6 days post mortem was increased (P < 0·05) in T3-5 compared to T1, with the result that muscle colour became darker, and steaks had less drip loss. Shear values increased (P < 0·05) from 6·3 kg in T1 to 7·7 kg in T4 and T5 indicating an increase in muscle toughness as time without feed and water increased. It was concluded that steers lose live weight rapidly within the first 24 h without feed and water, and that these relatively short periods of time (24 h) can have detrimental effects on carcass shrinkage and muscle quality. 相似文献
187.
H. O. Menlove M. M. Fowler E. Garcia M. C. Miller M. A. Paciotti R. R. Ryan S. E. Jones 《Journal of Fusion Energy》1990,9(4):495-506
Experiments using high-efficiency neutron detectors have detected neutron emission from various forms of Pd and Ti metal in pressurized D2 gas cells and D2O electrolysis cells. Four independent neutron detectors based on3He gas tubes were used. Both random neutrons (0.05–0.2 n/s) and time-correlated neutron bursts (10–280 n) of 100-s duration were measured using time-correlation counting techniques. The majority of the neutron burst events occurred at –30°C as the samples were warming up from the liquid nitrogen temperature. 相似文献
188.
Babbs C.F. Fearnot N.E. Marchosky J.A. Moran C.J. Jones J.T. Plantenga T.D. 《IEEE transactions on bio-medical engineering》1990,37(7):662-672
This paper describes simulation of steady-state intratumoral temperatures achieved by a simple modality of local heat therapy: interstitial treatment with parallel arrays of warmed, conductive heating elements. During "conductive heating" power is directly deposited only in the interstitial probes. Adjacent tissue is warmed by heat conduction. Simulations of interstitial conductive heating involved solution of the bioheat transfer equation on a digital computer using a finite difference model of the treated tissue. The simulations suggest that when the complete temperature distributions for conductive interstitial hyperthermia are examined in detail, substantial uniformity of the temperature distributions is evident. Except for a thin sleeve of tissue surrounding each heating element, a broad, flat central valley of temperature elevation is achieved, with a well defined minimum temperature, very close to modal and median tissue temperatures. Because probes are inserted directly in tumor tissue, the thin sleeve of overheated tissue would not be expected to cause normal tissue complications. The temperature of the heated probes must be continuously controlled and increased in the face of increased blood flow in order to maintain minimum tumor temperature. However, correction for changes in blood flow is possible by adjusting probe temperature according to a feedback control scheme, in which power dissipation from each probe is the sensed input variable. Conductive interstitial heating with continually controlled probe temperature deserves investigation as a technique for local hyperthermia therapy. 相似文献
189.
The effect of rapid solidification on the corrosion behaviour in aerated 0.001 M NaCl solution of Mg-Al alloys containing 9.6 to 23.4wt% AI has been investigated in comparison with chill-cast material. Polarization studies show that rapid solidification decreases corrosion current by up to two orders of magnitude corresponding to a corrosion rate of 6 to 11 mil y–1. Increasing the aluminium content in solid solution by rapid solidification gave rise to a steep increase in pitting potential between 10 and 23 wt% Al and resulted in development of an anodic plateau at 30Acm–2 attributable to magnesium depletion for the alloy surface and formation of a protective film. Chemical analysis of the electrolyte as a function of dissolution time for the rapidly solidified material indicated that initially only magnesium dissolved and that this dissolution of magnesium ceased within 2 to 5 min. The results indicate the formation of an aluminium-enriched interdiffusion zone at the surface underlying a more stable surface oxide than for ingot-processed Mg-Al-based alloys. 相似文献
190.
Kallwass Helmut K.W.; Surewicz Witold K.; Parris Wendy; Macfarlane Emma L.A.; Luyten Marcel A.; Kay Cyril M.; Gold Marvin; Jones J.Bryan 《Protein engineering, design & selection : PEDS》1992,5(8):769-774
Lactate dehydrogenases are of considerable interest as stereospecificcatalysts in the chemical preparation of enantiomerically pure-hydroxyacid synthons. For such applications in synthetic organicchemistry it would be desirable to have enzymes which tolerateelevated temperatures for prolonged reaction times, to increaseproductivity and to extend then applicability to poor substrates.Here, two examples are reported of significant thermostabilizations,induced by sitedirected mutagenesis, of an already thermostableprotein, the L-lactate dehydrogenase (EC 1.1.1.27
[EC]
, 35 kDa permonomer subunit) from Bacillus stearothermophilus. Thermal inactivationof this enzyme is accompanied by irreversible unfolding of thenative protein structure. The replacement of Argl71 by Tyr stabilizesthe enzyme against thermal inactivation and unfolding. Thisstabilizing effect appears to be based on improved interactionsbetween the subunits in the core of the active dimeric or tetramericforms of the enzyme. The thermal stability of L-lactate dehydrogenasevariants with an active site Arg residue, either in the 171(wild-type) or in the 102 position, is further increased bysulfate ions. The two stabilizing effects are additive, as foundfor the Argl71Tyr/ Gln1O2Arg double mutant, for which the stabilityof the protein in 100 mM sulfate solution reaches that of L-lactatedehydrogenases from extreme thermophiles. All mutant proteinsretain significant catalytic activity, both in the presenceand absence of stnhilfoing salts, and are viable catalysts inpreparative scale reactions. 相似文献