1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine as a substrate of cytochrome P450 2D6: allosteric effects of NADPH-cytochrome P450 reductase

1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), a neurotoxin that produces Parkinsonism symptoms in man, has been examined as a substrate of recombinant human cytochrome P450 2D6. When cumene hydroperoxide is used as an oxygen and electron donor, a single product is formed, identified as 4-phenyl-1,2,3,6-tetrahydropyridine. The K(m) for formation of this product (130 microM) is in agreement with the dissociation constants for MPTP binding to the enzyme determined by optical and nuclear magnetic resonance (NMR) spectroscopy. When the reaction is carried out with nicotinamide adenine dinucleotide phosphate (reduced) (NADPH) and recombinant human NADPH-cytochrome P450 reductase, a second product, identified as 1-methyl-4-(4'-hydroxyphenyl)-1,2,3,6-tetrahydropyridine, is formed in addition to 4-phenyl-1,2,3,6-tetrahydropyridine. The K(m) values for formation of these two products are 19 microM and 120 microM, respectively. Paramagnetic relaxation experiments have been used to measure distances between the protons of bound MPTP and the heme iron, and these have been used to construct models for the position and orientation of MPTP in the active site. For the cytochrome alone, a single mode of binding was observed, with the N-methyl close to the heme iron in a position appropriate for the observed N-demethylation reaction. In the presence of the reductase, the data were not consistent with a single mode of binding but could be explained by the existence of two alternative orientations of MPTP in the active site. One of these, characterized by a dissociation constant of 150 microM, is essentially identical to that observed in the absence of the reductase. In the second, which has a K(d) of 25 microM, the MPTP is oriented so that the aromatic ring is close to the heme iron, in a position appropriate for p-hydroxylation leading to the formation of the product seen only in the presence of the reductase. In the case of codeine, another substrate for cytochrome P450 2D6, the addition of reductase had no effect on the nature of the product formed, the dissociation constant, or the orientation in the binding site. These observations show that NADPH-cytochrome P450 reductase has an allosteric effect on the active site of cytochrome P450 2D6 that affects the binding of some substrates but not others.     

激光辐照制备搪瓷涂层

激光辐照制备的搪瓷涂层表面粗糙,与金属基材结合牢固。一般由 Si,Al,Na,K,B,F,O等元素组成。在激光辐照过程中 K,Na 明显地挥发,从而在涂层中的含量明显减少;Co,Ni,主要分布在界面附近;Fe 元素也由基材进入涂层,呈梯度状分布,在界面过渡区含量很高,在涂层内含量很低。搪瓷涂层的形成与激光辐照参数,特别与激光功率间存在极为密切的关系;只有选用合理的参数,才能制得搪瓷涂层。     

Structure and Properties of Electroless Ni Deposits

The changes in structure and the hardness of two electroless deposited Ni-P alloy coatings (with P content of 1.5 and 9.5 wt pct) with heat treatment have been studied by XRD and TEM. The deposits containing 1.5 wt pct P can be represented as an fcc NiP supersaturated solid solution of 5~10 nm microcrystallites. whereas the deposits containing 9.5 wt pct P are amorphous. The heat treatment process induces crystallization of amorphous Ni to Ni phosphides and fcc Ni.Both of the deposits reach maximum hardness after annealing at 400℃ for 1 h. All coated steel specimens are inferior in fatigue strength to uncoated steel specimens mainly due to the poor fatigue resistance of the coating itself     

电子聚合物基体碳纳米管复合材料研究进展

电子聚合物是一种新型的功能材料，碳纳米管具有优异的力学性能和独特的电学性能等，是聚合物基体复合材料的理想增强体，按不同电子聚合物基体类型进行了归纳，评述了电子聚合物基体碳纳米管复合材料的制备，性能和应用等情况。     

The TDCPR Management Mode of Engineering Equipment

The Three Gorges Project is a very large project,and its structure is very complex.Interna-tional advanced engineering equipment is broadly used.The state of equipment running directly influ-ences project building qualities and limited time.According to the factud conditions of the Three Gor-ges Project,the characteristics of engineering equipment are analyzed.At the same time ,some theories about equipment management are induced ,and the TDCPR management mode of engineering equip-ment of the Three Gorges Project is put forwared in order to gain the aim of managing and using equip-ment well and speeding up the project construction.     

油砂地层中子-伽玛能谱Monte-Carlo模拟

本工作应用自行研制开发的中子 伽玛能谱测井的中子 伽玛射线随空间、能量、时间分布的蒙特卡罗模拟软件包计算了裸眼井、井眼里无下井仪器、油饱和砂岩地层、井眼注油条件下沿井轴和井壁的中子 伽玛射线随能量、时间分布及沿井轴和沿井壁的中子 伽玛射线能谱 ,研究了源距对中子 伽玛射线随能量、时间分布以及井轴与井壁中子 伽玛射线能谱的影响。     

广州中城广场主体工程施工技术

广州中城广场工程结构形式复杂，平面曲折多角。施工中在应用多种模板体系、泵送混凝土、无粘结预应力楼板及核心筒部分小平台滑模等方面，采用了多项新技术，保证了工程质量，加快了工程进度。     

榆树林油田砂岩储层敏感性研究

榆树林油田储层粘土矿物含量较高，各种注入条件和施工条件都会对该储层造成相应的伤害，应采取相应的防护措施，为防止速敏的发生，储层的注水速度应控制在临界流速（1.0mL/min）以下，在油井转注时，可先注入1.09PV的含粘土稳定剂的进行处理，以提高产量或注入量，注入阴离子表面活性剂配置的活性水再注入地层水，不能增加地层水的渗透率，该项试验研究对指导榆树林油田的开发具有重要的意义。     

超薄SiO2层的热生长

隧道小孔中超薄ＳｉＯ２的生长是ＥＥＰＲＯＭ电路制造的关键工艺之一。采用ＳＵＰＲＥＭ－Ⅲ工艺模拟程序对超薄ＳｉＯ２的热生长进行了工艺模拟，经过大量的工艺实验及优化，确定了超薄ＳｉＯ２的最佳生长条件，生长出的ＳｉＯ２性能良好，完全可满足ＥＥＰＲＯＭ研制的要求。     

活化剂在织物漂白中的应用研究

对活化剂TAED和PAG在棉织物常规高温双氧水漂白过程中的应用进行了研究与探讨，并且得出最佳工艺条件，即H2O2 3g／L，渗透剂1g／L，活化剂4g／L，pH为7．