Polyamine analogue regulation of NMDA MK-801 binding: a structure-activity study

A series of analogues and homologues of spermine were synthesized, and their impact on MK-801 binding to the N-methyl-D-aspartate (NMDA) receptor was evaluated. These tetraamines encompass both linear and cyclic compounds. The linear molecules include norspermine, N1, N11-diethylnorspermine, N1,N12-bis(2,2,2-trifluoroethyl)spermine, homospermine, and N1,N14-diethylhomospermine. The cyclic tetraamines consist of the piperidine analogues N1,N3-bis(4-piperidinyl)-1,3-diaminopropane, N1,N4-bis(4-piperidinyl)-1,4-diaminobutane, N1,N4-bis(4-piperidinylmethyl)-1,4-diaminobutane, and N1,N4-bis[2-(4-piperidinyl)ethyl]-1,4-diaminobutane and the pyridine analogues N1,N3-bis(4-pyridyl)-1,3-diaminopropane, N1,N4-bis(4-pyridyl)-1,4-diaminobutane, N1,N4-bis(4-pyridylmethyl)-1,4-diaminobutane, and N1,N4-bis[2-(4-pyridyl)-ethyl]-1,4-diaminobutane. This structure-activity set makes it possible to establish the importance of charge, intercharge distance, and terminal nitrogen substitution on polyamine-regulated MK-801 binding in the NMDA channel. Four families of tetraamines are included in this set: norspermines, spermines, homospermines, and tetraazaoctadecanes. Calculations employing a SYBYL modeling program revealed that the distance between terminal nitrogens ranges between 12.62 and 19.61 A. The tetraamines are constructed such that within families cyclics and acyclics have similar lengths but different nitrogen pKa's and thus different protonation, or charge, states at physiological pH. The pKa values for all nitrogens of each molecule and its protonation state at physiological pH are described. The modifications at the terminal nitrogens include introduction of ethyl and beta,beta,beta-trifluoroethyl groups and incorporation into piperidinyl or pyridyl systems. The studies clearly indicate that polyamine length, charge, and terminal nitrogen substitution have a significant effect on how the tetraamine regulates MK-801 binding to the NMDA receptor. Thus a structure-activity basis set on which future design of MK-801 agonists and antagonists can be based is now available.     

90°分束偏光镜光强分束比研究

给出了90°分束偏光镜的e,o光光强分束比的计算公式,以及光强分束比随光波长的变化曲线;在6328Å测得的光强分束比与计算值是一致的。     

面向大规模定制的虚拟设计研究

综述了大规模定制的范围经济性和面向大规模定制的基本设计方法，并提出了一个虚拟设计框架，该框架改变了传统的设计模式，利用先进的设计方法学和仿真支撑技术为产品开发提供了最大柔性和敏捷性。同时，它提供了一个多学科合作的设计环境，用户直接参与进设计循环中。最后，结合新型剑杆织机的开发，展示了一个能够支持新产品快速成功开发的虚拟设计环境。     

COIL中BHP浓度对发生O_2(~1△)的影响

本文实验研究了BHP的浓度对产生O2（1△）的影响。实验结果表明：当BHP浓度大于3.5M时，Cl2利用率以及O2（1△）的产率将不依赖于BHP浓度的变化而变化，同时，实验结果表明，使用低浓度的BHP对COIL的操作是可行的。     

Deoxyribonucleic acid vaccines encoding antigens with rapid proteasome-dependent degradation are highly efficient inducers of cytolytic T lymphocytes

We generated plasmid expression vectors encoding ubiquitin and beta-galactosidase (beta-gal) with different intervening amino acids, allowing for the production of processed protein products that have either stabilizing or destabilizing residues at their N-termini. P815 cells transfected with plasmids encoding beta-gal with a destabilizing N-terminus did not have detectable expression beta-gal unless they were treated with inhibitors specific for the proteasome. Inhibitors of other proteolysis pathways had no such effect. Nevertheless, transfectants expressing beta-gal with different amino acid residues were equally sensitive to cytolysis by a CTL clone specific for a beta-gal peptide presented in the context of H-2Ld. In contrast to vectors encoding native beta-gal, plasmid vectors encoding beta-gal with a destabilizing residue did not induce detectable anti-beta-gal Abs when injected into skeletal muscle of BALB/c mice. However, such vectors were significantly more effective than vectors encoding native beta-gal or beta-gal with a stabilizing residue in stimulating CTL specific for P13.2, a lacZ transfectant of P815. We conclude that incorporation of strategies that enhance proteasome-dependent degradation may generate DNA vaccines that are more effective in inducing cellular immunity against targeted Ags.     

对数型产量衰减曲线方程的建立与应用

在产量衰减曲线方程的基础上，通过数学推导，得到了一种对数型产量减曲线方程。方程既可以用来预测油气田整个开发阶段的指标，又可以比较准确的测算油气田的可采集量。对国内外一些油田的实际应用表明，对数型产量衰减曲线方程是十分实用和有效的。     

聚苯硫醚酰胺的合成与表征

用4-氯苯甲酰4′-氯苯胺和硫化钠为原料在常压下合成了聚苯硫醚酰胺,并对其进行了表征。结果表明所合成的产物为结晶性聚合物,并且有较高的热稳定性。     

无约束淬火机目标温度神经网络预报

淬火、控制冷却的冷却速度和目标温度是关系到钢板性能的关键因素 ,但由于冷却过程的水量、水温、辊道速度等对冷却目标温度的影响属多变量非线性过程 ,用简单的解析模型通常精度较低 ,难以达到精确控制的要求。采用人工神经网络技术对无约束淬火机目标温度进行快速预报 ,结果表明 ,预测精度高 ,快速准确     

变速铣削的试验研究

通过试验考证了变速铣削的减振效果和机床电机电流的波动幅度，试验结果表明，变速铣削同样具有明显的减振效果。机床电机电流虽有波动，但波动幅度不大，不会影响电机的正常使用，变速铣削具有良好的应用前景。