Interfacial properties of a direct bonded Nd-doped YVO4 and YVO4 single crystal

Laser crystal bonding of a neodymium-doped yttrium orthovanadate (Nd : YVO₄) and a non-doped yttrium orthovanadate (YVO₄) crystal as a cold finger has been demonstrated. Instead of a traditional chemical treatment, a newly developed dry etching process was applied to the preparation for contact of mechanically polished surfaces. In the subsequent heat treatment process, stable heating at 873 K was required to prevent precipitation at the bonded interface. The bonded interface of 3 mm×3 mm was investigated by optical scattering and wavefront distortion measurements. The scattering density around the bonded interface was less than 4.6×10⁶/cm³ and the wavefront distortion caused by the bonded region was assumed to be around 0.04 at 633 nm. Additional magnified inspection showed that atoms in the bonded region were well arranged with the same regularity as the bulk crystal. The diffusion coefficient of Nd³⁺ ions in the YVO₄ crystal was estimated at 2.3×10^–23 m²/s at 873 K.     

加载频率对中温环境下疲劳裂纹扩展的影响

由于材料或环境的因素,加载频率对疲劳裂纹扩展速率将产生很大的影响,以工业Ｔｉ为对象,研究了中等温度环境下疲劳裂纹扩展性能及加载频率的影响,并用弹、粘塑性理论对其进行了理论上的探讨,基于该理论导出的本构关系和利用有限元方法,对裂纹尖端的应力应变进行了分析,结果表明,粘塑性应变范围和Ｊ积分范围可作为裂纹扩展的控制参数,能很好地反映加载频率对裂纹扩展的影响。     

Contributions of Mobile and Bonded Molecules to Dynamic Friction of Nanometer-Thick Perfluoropolyether Films Coated on Magnetic Disk Surfaces

To protect the interface against intermittent head–disk contact in hard disk drives, nanometer-thick perfluoropolyether (PFPE) films consisting of both “bonded” and “mobile” molecules are applied on the disk surfaces. Because of their different adsorption states and mobility, the bonded and mobile molecules are supposed to contribute differently to friction properties, which directly impact the stability of ultra-low flying head–disk interfaces. By measuring the friction force at light loads and low to high speeds as a function of bonded and mobile film thicknesses, we studied the contributions of bonded and mobile molecules to the dynamic friction of nanometer-thick PFPE films. We found that the friction coefficient of lubricant films without or with less bonded molecules increased as a power function of sliding speed, whereas that of lubricant films with more bonded molecules increased logarithmically with sliding speed. We suggest that these results can be explained by the following mechanisms: the dynamic friction of lubricant films without and with less bonded molecules is dominated by shear thinning behavior of mobile molecules, while that of lubricant films with more bonded molecules is governed by bonded molecules which lead to boundary lubrication.     

Preformulation studies of EFdA,a novel nucleoside reverse transcriptase inhibitor for HIV prevention

4′-Ethynyl-2-fluoro-2′-deoxyadenosine (EFdA) is a novel nucleoside analog of great interest because of its superior activity against wild-type and multidrug-resistant HIV-1 strains, and favorable safety profiles in vitro and in vivo. The aim of this work was to provide preformulation information of EFdA important for delivery system development. A simple, accurate and specific reverse-phase high performance liquid chromatographic (RP-HPLC) method with UV detection was developed for quantification of EFdA. In addition, physicochemical characterizations including pH solubility profile, octanol/water partition coefficient (Log P_o/w), DSC analysis, field emission scanning electron microscopy, and stability studies under various conditions were conducted. EFdA existed in planar or flake shape, with a melting point of ～130?°C, and had a pH dependent solubility. The log P_o/w value of EFdA was ?1.19. The compound was stable upon exposure to pH levels from 3 to 9 and showed good stability at elevated temperature (65?°C). In vitro cytotoxicity assessments were performed in two different epithelial cell lines. In cell-based studies, the EFdA selectivity index (50% cytotoxic concentration [CC₅₀] values/50% effective concentration [EC₅₀]) was found to be greater than 1?×?10³. Permeability studies using cell- and tissue-based models showed that EFdA had an apparent permeability coefficient (P_app)??6?cm/s and that the paracelluar pathway was the dominant transport route for EFdA. Overall, EFdA possesses favorable characteristics for further formulation development.     

Mechanism of beta-adrenergic receptor upregulation induced by ACE inhibition in cultured neonatal rat cardiac myocytes: roles of bradykinin and protein kinase C

BACKGROUND: Although bradykinin is thought to contribute to the effects of ACE inhibitors on the cardiovascular system, its precise role remains to be elucidated. Evidence suggests that bradykinin might be important in the upregulation of beta-adrenergic receptors (beta-ARs) induced by ACE inhibitors, and the role of bradykinin in this effect has now been investigated with cultured neonatal rat cardiac myocytes. METHODS AND RESULTS: The density of beta-ARs on the myocyte surface was determined with a binding assay with [3H]CGP-12177. Incubation of cultured myocytes for 24 hours with the ACE inhibitor captopril (1 micromol/L) increased beta-AR density by 35% and enhanced the response of cells to isoproterenol but not to forskolin. Neither an angiotensin-II type 1 (AT1) receptor antagonist, CV-11974, nor angiotensin-I affected beta-AR density. However, the bradykinin B2 receptor antagonist Hoe 140 abolished the effect of captopril on beta-AR upregulation in a dose-dependent manner. The protein kinase C inhibitor staurosporine (20 nmol/L) but neither indomethacin nor L-NAME also inhibited captopril-induced upregulation of beta-ARs. Exogenous bradykinin increased the spontaneous beating frequency of cultured myocytes and Hoe 140 abolished this effect. Bradykinin level in the medium increased 1.4-fold by the treatment of cultured myocytes with captopril for 24 hours. CONCLUSIONS: The results suggest that captopril enhances beta-AR responsiveness by inducing beta-AR upregulation and that the latter effect is mediated by activation of bradykinin B2 receptors and protein kinase C. These observations also offer insight into the different roles of ACE inhibitors and AT1 receptor antagonists in the treatment of heart failure.     

Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists

A series of novel 6-fluorochroman derivatives was prepared and evaluated as antagonists for the 5-HT1A receptor. N-2-[[(6-Fluorochroman-8-yl)oxy]ethyl]-4-(4-methoxyphenyl)butylami ne (3; J. Med. Chem. 1997, 40, 1252-1257) was chosen as a lead, and structural modifications were done on the aliphatic portion of the chroman ring, the tether linking the middle amine and the terminal aromatic ring, the aromatic ring, and lastly the amine. Radioligand binding assays proved that the majority of the novel compounds behaved as good to excellent ligands at the 5-HT1A receptor, some of which were selective with respect to alpha1-adrenergic and D2-dopaminergic receptors. The antagonist activity of the compounds was assessed in the forskolin-stimulated adenylate cyclase assays in CHO cells expressing the human 5-HT1A receptors. Among the modifications attempted, introduction of an oxo or an optically active hydroxy moiety at the chroman C-4 position was effective in ameliorating the receptor selectivity. Six analogues were selected through the in vitro screens and further evaluated for their in vivo activities. A 4-oxochroman derivative (31n), having a terminal 1, 3-benzodioxole ring, demonstrated antagonist activities toward 8-OH-DPAT-induced behavioral and electrophysiological responses in rats.     

Presence of platelet-activating factor in pyuria in humans

The relationship between the occurrence of platelet-activating factor (PAF) and neutrophils in urine from patients with urinary tract infection was examined. PAF was detected in human pyuria, when leukocyte levels reached at least 300 cells/μL (n=45), but not in normal urine (n=12). The amount of PAF found in pyuria, measured by platelet aggregation assay, was 0.01 to 13.3 pmol/mL. A close correlation was seen between the amount of PAF present and the number of urinary leukocytes (p<0.01, r=0.70). The leukocytes in pyuria consisted almost entirely of neutrophils (96±4%, mean ±S.D.). Our findings suggest that the occurrence of PAF is associated with the accumulation of neutrophils in urine. Based on a paper presented at the Third International Conference on Platelet-Activating Factor and Structurally Related Alkyl Ether Lipids, Tokyo, Japan, May 1989.     

Aspirin-sensitive urticaria: provocation with a leukotriene receptor antagonist

The diagnosis of two patients with aspirin-induced urticaria (AIU) was confirmed by oral provocation with aspirin, other non-steroidal anti-inflammatory drugs, and food additives. Low doses of a novel leukotriene (LT) receptor antagonist, ONO-1078 (ONO, Japan) induced urticaria in these patients, while the same doses of ONO-1078 did not provoke any eruptions in 10 normal healthy volunteers or five patients with aspirin-unrelated chronic urticaria. This is the first report that a selective LTD4/LTE4 receptor antagonist that is effective as an antiasthmatic agent evoked urticaria in patients with AIU. Our observation suggests that the pathogenesis of AIU depends on the stimulation of LT receptors. The accumulation of results of anti-LT therapy may provide clues to resolve the pathogenetic mechanisms of this disorder.     

A PSK Group Modem for Satellite Communications

A PSK group modem which modulates and demodulates multiple PSK signals en bloc will play an important role in realizing a cost-effective satellite communications system based on the narrowband multicarrier PSK/FDMA technique. This paper briefly discusses its possible applications, and presents a developed PSK group modem including its algorithm, hardware design, and implementation. In the algorithm, filtering of respective PSK signals is effectively carried out by digital signal processing techniques applied to the digital transmultiplexer. Furthermore, in order to compensate for the difference between the operation timing of the PSK group modem and the symbol timing of each input/output data signal, digital signal processings based on a table-look-up method using ROM and a rate-conversion filter with adaptive weighting are proposed for the modulator and demodulator, respectively. An experimental 4-phase PSK group modem has been developed, and experiments have been conducted under various conditions. The measured performance of the developed hardware is also demonstrated.     

Regular network polyamide and copolyamide films from trimesic acid and aliphatic diamines

Regular network polyamide films made from trimesic acid (Y) and aliphatic diamines as well as copolyamide films made from hexamethylene diamine (6) and dodecamethylene diamine (12) with Y were prepared. Prepolymers obtained by melt polycondensation for a short period of time were cast from a DMF solution and successively post-polymerized at 300°C to form a network. The resultant films were transparent, flexible and insoluble in any solvents. Heat distortion temperature (T_h) measured by a penetration mode of thermomechanical analysis rapidly increased with increasing post-polymerization time, and then levelled out after 0.5–1 h. T_h was 238, 231, 232, 216, 207, 187, 176 and 163°C for 4Y, 5Y, 6Y, 7Y, 8Y, 9Y, 10Y and 12Y post-polymerized for 4h, respectively. Degrees of reaction estimated from the infrared absorbance of ester and methylene groups were 88 and 83% for 6Y and 12Y post-polymerized for 4h, respectively. Two diffraction peaks appeared in the wide angle X-ray scattering (WAXS) pattern, suggesting some ordered structure owing to the regular networks. Density increased with increasing post-polymerization time and was 1.266, 1.236, 1.214, 1.175, 1.162, 1.145, 1.130 and 1.107 g/cm³ for 4Y, 5Y, 6Y, 7Y, 8Y, 9Y, 10Y and 12Y post-polymerized for 4h, respectively. WAXS patterns of copolymer films of 12/6-Y suggested the continuous change of network structure with copolymer composition. It was found that comonomer disturbs the formation of ordered network structure, and decreases the packing of networks, thus decreasing density, T_h and tensile properties, and increasing dye absorption of copolymer films. From the dye absorption behavior, it was suggested that these regular network films could be utilized as membranes for the separation of molecules by varying the chain length between crosslinked sites.