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.     

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。     

粉末冶金铁基烧结炉的现状与展望

评述了国内外粉末冶金铁基烧结炉的发展动向和具体改进装备。即功能带设计、脱蜡装置,烧结带气氛控制,淬火带的设想,加热元件配置及新型可塑性耐火材料。     

用数采器对空压机进行状态监测预报

通过几个典型事例的分析、判断和处理，介绍了该厂怎样利用９１ｌ型数采器对２Ｄ１２—１００／８型空压机运行状态进行监测，以预报早期故障，为设备检修提供指导．     

Temperature dependence of hydrogenated amorphous silicon thin-film transistors

The temperature dependence characteristics of hydrogenated amorphous silicon thin-film transistors were investigated. The results indicate that as the temperature was increased, the threshold voltage and the field-effect mobility were first increased, and then decreased, which may be controlled by different mechanisms at low and high temperatures. In addition, if the temperature was higher than 420 K, the Fermi level was promoted to the degenerate-like states, the current channel always existed due to the temperature effect, and the threshold voltage became negative.     

Double-step generation of ellipses

The principle of double-step incremental generation of nonparametric curves on a discrete plane is used to develop a double-step algorithm for scan converting ellipses in sixteen separate segments. The algorithm iterates only half as many times as current algorithms, while each iteration demands the same number of operations or slightly fewer operations than M. Pitteway's (1967, 1985) algorithm (previously the fastest one). This marked gain in the speed of scan conversion is due to the fact that the middle pixel in a two-step increment is obtained without computation     

β放射性气体浓度计的新分度方法

本文介绍β放射性气体浓度计的一种新的分度方法——泄漏元件排气法。其特点是一只元件可分度放射性气体浓度计的许多读出数(甚至是几个量程),操作方便。     

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