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1.
A composite was made by adsorption of the bisphosphonate [(3-dimethylamino-1-hydroxypropylidene)-1,1-bisphosphonate; dimethyl-APD] into an hydroxyapatite (HA) tube. Adsorbed dimethyl-APD did not change the bulk properties of the HA tube but the surface properties were altered. The amount of 0.1 mmol/L dimethyl-APD adsorbed into the HA tube was 0.78 ( ± 0.20) g after 4 weeks. The composite tube of HA and dimethyl-APD placed after extraction of teeth in the premolar regions of dogs were biocompatible, stable and bonded strongly and intimately to the alveolar bone. Although there was no bone resorption around the composite tubes, no conclusion can be drawn yet from this study as far as local inhibition of alveolar bone resorption is concerned.  相似文献   
2.
The authors examined associations of perceived similarity, actual similarity, and peer-rated similarity in personality with friendship intensity during the acquaintanceship process in a naturalistic setting. Self- and peer-rated personality data were gathered from undergraduates (mean age = 18.9) at 5 time points during the first year of university using a round-robin design. Whereas perceived similarity and peer-rated similarity in personality were concurrently associated with more friendship intensity for just-acquainted individuals, actual similarity in personality was not. Further, bidirectional cross-lagged associations between perceived similarity and friendship intensity were found. Peer-rated similarity was also associated with increases in friendship intensity, and this association was mediated by communication frequency. These results indicate that specific types of similarity in personality are differentially associated with friendship intensity during early phases of acquaintanceship in a real-life setting. Further, insight was provided in the direction of causality between similarity and attraction: Perceived and peer-rated similarity seem to breed friendship intensity, whereas friendship intensity seems to breed perceived similarity only. Finally, peers’ expectations seem to affect individuals’ communicative behaviors, which in turn affect friendship formation. (PsycINFO Database Record (c) 2010 APA, all rights reserved)  相似文献   
3.
In a 19-year longitudinal study, the 15% most inhibited and the 15% most aggressive children at ages 4-6 years were followed up until age 23 years and were compared with controls who were below average in preschool inhibition or aggressiveness. As adults, inhibited boys and girls were judged as inhibited by their parents and showed a delay in establishing a first stable partnership and finding a first full-time job. However, only the upper 8% in terms of inhibition tended to show internalizing problems, including self-rated inhibition. Aggressive boys showed an externalizing personality profile in the parental and self-judgments, were educational and occupational underachievers, and showed a higher adult delinquency rate than the controls, even after sex and socioeconomic status were controlled. The results suggest delayed social transitions without internalizing problems for most male and female inhibited children and a significant long-term risk of an externalizing profile for aggressive children. (PsycINFO Database Record (c) 2010 APA, all rights reserved)  相似文献   
4.
Studies conducted with the goal of discovering a second-generation platelet-activating factor (PAF) antagonist have identified a novel class of potent and orally active antagonists which have high aqueous solubility and long duration of action in animal models. The compounds arose from the combination of the lipophilic indole portion of Abbott's first-generation PAF antagonist ABT-299 (2) with the methylimidazopyridine heterocycle moiety of British Biotechnology's BB-882 (1) and possess the positive attributes of both of these clinical candidates. Structure-activity relationship (SAR) studies indicated that modification of the indole and benzoyl spacer of lead compound 7b gave analogues that were more potent, longer-lived, and bioavailable and resulted in the identification of 1-(N, N-dimethylcarbamoyl)-4-ethynyl-3-[3-fluoro-4-[(1H-2-methylimidazo[4,5-c] pyrid-1-yl)methyl]benzoyl]indole hydrochloride (ABT-491, 22 m.HCl) which has been evaluated extensively and is currently in clinical development.  相似文献   
5.
Inorganic polymer (IP) foams could be used as an alternative to commonly available cellular concretes. To do so, however, it is crucial to understand how the foaming kinetics and the final foam properties can be controlled and tailored to delivered the desired performance. The research reported in this article investigates the influence of the SiO2/Na2O ratio of the activating solution, addition time of foaming agent, and temperature, on the reaction kinetics and final properties of a porous IP. The IPs were formed by activating fayalite slag, a by-product of secondary copper production, with a sodium-silicate solution. Foaming was achieved by introducing metallic Al into the formulation, oxidizing it in the alkaline environment, liberating H2 gas, and entrapping it. Reaction kinetics were assessed using isothermal calorimetry, rheology, and a dedicated setup to record the foaming. The mechanical and physical properties of the foam were assessed via compressive strength and water absorption measurements. Microstructural analysis was undertaken using electron microscopy and computed tomography. The results showed that by decreasing the SiO2/Na2O ratio and/or increasing the temperature, the reaction kinetics were accelerated. Regarding the properties, postponing the initiation of the foaming led to more uniform and smaller pores, resulting in an increased compressive strength-to-density ratio.  相似文献   
6.
Nonionic polyoxyethylene type detergents (CxEy) are widely used to solubilize and purify membrane proteins. The detergent hydrophobic moiety (Cx) replaces phospholipids at exposed hydrophobic regions of the membrane proteins. During chromatography on an immobilized anti-Kell antibody to purify Kell protein (an integral erythrocyte protein), it was observed that the size of the polar head of an non ionic detergent added to the mobile phase appeared to influence the interaction of the detergent-protein complex with the immobilized antibody. Further studies were performed using another erythrocyte membrane protein, Glycophorin C and three anti-GPC monoclonal antibodies directed against three epitopes of the extracytoplasmic domain of the protein. The interaction of GPC with the three Protein A-coupled monoclonal antibodies was studied in the presence of three detergents C12E<9>, C13E<15> and C12E<23>. It was observed in batch mode and in column chromatography experiments that the adsorption of GPC to the immunoaffinity supports decreased as the size of the detergent polar head increased. Thus, the polyoxyethylene chain of a detergent might prevent the interaction of the detergent-protein complex with the immobilized antibody.  相似文献   
7.
The HIV-1 protease inhibitor ritonavir (ABT-538) undergoes cytochrome P450-mediated biotransformation in human liver microsomes to three major metabolites, Ml, M2 and M11, with wide interindividual variation in the rates of metabolite formation. The structures of these metabolites were determined with the use of electrospray ionization mass spectrometry. Chemical inhibition, metabolic correlation, immunoinhibition and metabolism by microsomes derived from specific CYP cDNA-transfected B-lymphoblastoid cell lines indicated that the CYP3A subfamily of enzymes was the major contributor to the formation of M1 and M11, whereas both CYP3A and CYP2D6 contributed to the formation of M2. None of the typical CYP3A substrates/inhibitors (e.g., ketoconazole, troleandomycin) were able to completely inhibit ritonavir metabolism, even at high concentrations. Ritonavir was found to be a potent inhibitor of CYP3A-mediated biotransformations (nifedipine oxidation, IC50) = 0.07 microM; 17alpha-ethynylestradiol 2-hydroxylation, IC50 = 2 microM; terfenadine hydroxylation, IC50 = 0.14 microM). Ritonavir was also found to be an inhibitor of the reactions mediated by CYP2D6 (IC50 = 2.5 microM) and CYP2C9/10 (IC50 = 8.0 microM). The results of this study indicate the potential for in vivo inhibition of the metabolism by ritonavir of drugs that are CYP3A, CYP2D6 and, to a lesser extent, CYP2C9/10 substrates.  相似文献   
8.
9.
In fundamental osteoporosis research precise and accurate assessment of the mineral quantity in histological bone sections is of particular importance when studying the local effects of implants releasing bone modulating agents. A potentially useful technique to estimate the bone mineral density (BMD) is dual-energy X-ray absorptiometry (DXA). A highly collimated (0.13 mm) Hologic 2000 with a line spacing and point resolution of 0.13 mm was used. The mineral content was measured in regions of 3.1 mm(2). A ceramic hydroxyapatite (CHA) phantom was developed as a reference standard. The phantom was made of a single-phase hydroxyapatite starting powder by compressing and sintering at 1000 degrees Celsius. The true density was 3.14 + or - 0.001 g/cm(3). The calcium/phosphorus ratio was close to the theoretical one of 1.67. The mean precision error expressed as the coefficient of variation (CV) of the mineral density (MD) measurements of the phantoms with thicknesses of 1, 2, and 3 mm was 0.2%. Embedded undecalcified alveolar bone sections of dogs (0.0015-1 mm in thickness) were scanned simultaneously with a phantom 1 mm in thickness. The precision error (CV) of the BMD measurements calculated by DXA for sections > or = 0.1 mm and with a BMD > or = 0.14 g/cm(2) was 0.81%. There was a linear relationship between the BMD calculated by DXA and the estimated BMD in the histological bone sections by means of the true density of the phantom. It is concluded that DXA using a standard CHA phantom is a precise and accurate method to measure MD changes as small as 1% in histological bone areas of 3.1 mm(2) provided that the loss or gain in BMD is > or = 0.14 g/cm(2).  相似文献   
10.
The design, synthesis, and molecular modeling studies of a novel series of azacyclic ureas, which are inhibitors of human immunodeficiency virus type 1 (HIV-1) protease that incorporate different ligands for the S1', S2, and S2' substrate-binding sites of HIV-1 protease are described. The synthesis of this series is highly flexible in the sense that the P1', P2, and P2' residues of the inhibitors can be changed independently. Molecular modeling studies on the phenyl ring of the P2 and P2' ligand suggested incorporation of hydrogen-bonding donor/acceptor groups at the 3' and 4-positions of the phenyl ring should increase binding potency. This led to the discovery of compound 7f (A-98881), which possesses high potency in the HIV-1 protease inhibition assay and the in vitro MT-4 cell culture assay (Ki = approximately 5 pM and EC50 = 0.002 microM). This compares well with the symmetrical cyclic urea 1 pioneered at DuPont Merck.  相似文献   
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