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.     

人工接地装置设计方法分析

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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.     

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Improved coupled-mode theory of anisotropic optical waveguides

A coupled-mode equation for anisotropic waveguide systems of arbitrary cross section and general dielectric distribution is derived. Numerical results comparing the exact calculations to those of the method of Hardy et al. (Opt. Lett., vol.11, 742-4, 1986) show that the same accuracy can be obtained not only for TE, but also for TM mode coupling in the case of anisotropic waveguides, and the improved coupled-mode theory is applicable to the situation when moderately strong coupling occurs under the condition where the edge-to-edge separation of two coupled guides D₂ is about 0.1 μm     

用最优化方法和双水模型评价泥质砂岩储集层

本文从测井资料数字处理和解释的角度出发,在系统考察分析常用的各种最优化方法的基础上,认为采用抛物线插值法作一维搜索和变尺度法中的BFGS法作多维搜索相结合的最优化方法,用双水解释模型对泥质砂岩储集层进行评价是适宜的。为此编制了最优化测井解释程序,对胜利油田砂泥岩的测井资料进行了实际处理,并针对本地区的地质特点,对测井响应方程和解释参数的选择等重要问题进行了探讨。数字处理的结果表明,所获得的储集层参数和岩性矿物成分,与岩心分析资料和斯仑贝谢公司的GLOBAL程序处理结果相当吻合。证明它有较好的效果。     

我国建筑涂料技术进步简评

从以下诸方面简述我国建筑涂料的技术进步:⑴新品种涂料的研制开发;⑵加强对配套材料及施工技术的研究;⑶超细填料在涂料中的应用;⑷计算机自动配色技术;⑸产品标准的修订;⑹建筑涂料的实用范围扩大。     

浅谈高层建筑火灾扑救

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转移法色交换

将图Ｇ的着色由一种变为中一种，通常用Ｋｅｍｐｅ法以交换。但是，对于某些情况，用此法无效。针对这个问题，本文提出了一种转移法色交换，它适用于平面图着色，方法直观，清晰且有效。