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。     

A technique for extracting physiological parameters and therequired input function simultaneously from PET image measurements:theory and simulation study

Positron emission tomography (PET) is an important tool for enabling quantification of human brain function. However, quantitative studies using tracer kinetic modeling require the measurement of the tracer time-activity curve in plasma (PTAC) as the model input function. It is widely believed that the insertion of arterial lines and the subsequent collection and processing of the biomedical signal sampled from the arterial blood are not compatible with the practice of clinical PET, as it is invasive and exposes personnel to the risks associated with the handling of patient blood and radiation dose. Therefore, it is of interest to develop practical noninvasive measurement techniques for tracer kinetic modeling with PET. In this paper, a technique is proposed to extract the input function together with the physiological parameters from the brain dynamic images alone. The identifiability of this method is tested rigorously by using Monte Carlo simulation. The results show that the proposed method is able to quantify all the required parameters by using the information obtained from two or more regions of interest (ROIs) with very different dynamics in the PET dynamic images. There is no significant improvement in parameter estimation for the local cerebral metabolic rate of glucose (LCMRGlc) if there are more than three ROIs. The proposed method can provide very reliable estimation of LCMRGlc, which is our primary interest in this study     

含钇奥氏体基堆焊焊条堆焊层研究

针对高温、磨损、热疲劳工况下服役零件的失效，研制了一种含稀土元素钇的奥氏体基沉淀强化型堆焊焊条，并对堆焊层组织与性能进行了较系统的研究。     

人工接地装置设计方法分析

本文系统地论述了人工接地装置的设计方法,修正了现有文献中有关论述的缺点和错误,提出了通过迭代求解方程组来设计人工接地装置的新方法。     

DX型数据采集与无线传输系统

DX型数据采集与无线传输系统能对油井压力、温度、载荷和流量等参数进行自动采集 ,并通过无线传输向总站提供实时参数 ,为及时决策提供信息。数据采集系统采用STD总线 ,测量精度高、故障低 ;无线传输系统采用短波电台和具有自动纠错功能的数传机 ,抗噪能力强、可靠性高。文章介绍了DX型数据采集与无线传输系统的组成、工作原理、功能和主要技术指标     

Investigation of the Interaction of Sodium Chloride and Two Amino Sulfonic Acids,HEPES and MOPSO,by EMF Measurements

Ionic interactions in the two systems NaCl-HEPES (N-2-hydroxyethylpiperazine-N′-2-ethanesulfonic acid) and NaCl-MOPSO (3-(N-Morpholino)-2-hydroxypropanesulfonic acid) have been studied in terms of their mutual influence on the respective activity coefficients of each component. Activity coefficients for each component of the two systems and for corresponding buffers are calculated from emf measurements of solutions containing NaCl, the aminosulfonic acid, and its conjugate base in a NalSE/solution/AgCl-Ag cell at 5, 15, 25, and 37 °C.     

钢的连铸用保护渣的表征

在钢的连铸过程中,结晶器保护渣的性质强烈地影响着铸造的行为、钢的质量、以及连铸工艺的环境.本研究采用高温显微技术来研究保护渣的熔化行为,采用液滴测试方法来测定保护渣的熔化速率.结果表明:自由碳是控制保护渣熔化行为的主要因素.熔化速率随碳的反应能力的增加而增加,随着碳含量的减少而增加.     

化工企业环境因素的评价

化工企业环境因素评价是建立环境管理体系的核心任务，化工企业生产过程的特点决定了其环境因素数量多、环境影响大、识别评价难、控制难度大。本文介绍了化工企业环境因素评价的技术方法和过程，可以为提高环境因素评价的科学性、客观性和充分性提供参考。     

浅论水电规划工作思路

在水电的前期设计阶段，规划专业的重要性显而易见。由于水电规划工作涉及专业很多，如果仅停留于规划专业本身，未必能解决问题。在规划工作中，既有定量的计算，也有定性的分析；既要站在国家的角度进行评价，也要进行企业的财务效益分析；既要考虑目前的现实情况，也要对未来的发展做出预测；既有企业的主观意志，也有自然、社会历史的限制。总之，规划专业是涉及多目标、多量纲的综合判断，若以局部来通观全体，则一定要流于片面的谬误。因此，水电规划工作须进行辩证的综合研究。