Intravascular and Intracellular Hepatic Relaxivities of Superparamagnetic Particles: An Isolated and Perfused Organ Pharmacokinetics Study

The relative contributions of intravascular and intracellular compartments to the proton transverse relaxation of the isolated and excised rat liver were determined during the phagocytosis of superparamagnetic particles. The evolution of the proton transverse magnetization of the organ perfused with increasing doses of starch-coated magnetic microspheres was followed up using a Carr–Purcell–Meiboom–Gill sequence with various echo times. From the multiexponential fit of the echo train, the amplitudes and the relaxation ratesR₂of the liver tissue were obtained. The results clearly indicate that shortly after contrast medium administration, an internalization takes place which can be followed by the rapid and biphasic evolution of the transverse relaxation rate of the water protons. A very fast decaying component looking like an initial loss of the magnetization is observed together with an increase of the relaxation rate of the remaining water tissue. This regime is strongly dependent on both the echo time and the iron concentration, a behavior characteristic of the agglomeration of magnetic particles. The examination of the liver tissues by electron microscopy shows that this clustering arises in cytoplasmic vacuoles.     

Characterization of CNS disorders and evaluation of therapy using structural and functional MRI

Modern drug development requires technologies that allow rapid translation from the preclinical to the clinical stage. It is obvious that non-invasive imaging modalities such as magnetic resonance imaging (MRI) will play a central role in this regard. This article reviews the use of structural and functional MRI readouts for characterization of central nervous system (CNS) disorders and evaluation of the efficacy of potential CNS drugs. Examples comprise dementia of Alzheimer's type, cerebral ischemia, and neuroinflammation covering both clinical and preclinical aspects. In these examples MRI has been used to obtain relevant structural information on brain atrophy, on the location and extent of ischemic brain areas, and on the number and distribution of demyelinated plaques. These structural data are complemented by readouts assessing the functional consequences associated with the pathomorphological changes. In the last decade, MRI has evolved into a standard tool for the development of CNS drugs. With regard to target-specific/molecular imaging applications MRI is limited by its inherently low sensitivity; complementary imaging modalities utilizing optical and radionuclear reporter systems will thus be required.     

Synthesis of N-（α-Alkoxyalkyl）benzotriazoles Catalyzed by Acidic Ionic Liquid at Room Temperature

N-（α-Alkoxyalkyl）benzotriazoles were synthesized via the condensation of benzotriazole with various aldehydes and alcohols catalyzed by acidic ionic liquid [hmim]HSO4 at room temperature. The yield was up to 99%. This novel method was effective when triethoxymethane was utilized instead of alcohols. Moreover, acidic ionic liquid could be reused easily with no significant degradation of its catalytic activity.     

顺磁性聚酯金属配合物的合成及其驰豫性能的研究

本文通过二乙三胺五乙酸（ＤＴＰＡ）或乙二胺四乙酸（ＥＤＴＡ）的双酸酐与二元醇或二元酚进行聚合反应，制备了两个系列共１５种新的聚酯型大分子配体及其顺磁性金属配合物，用核磁、红外光谱以及元素分析表征了配体和配合物的结构。初步试验结果表明，与相应的小分子金属配合物相比，聚酯金属配合物具有较高的弛豫性能。     

Synthesis, binding affinity, and relaxivity of target-specific MRI contrast agents

Although magnetic resonance imaging (MRI) is one of the most important imaging modalities of the central nervous system (CNS), one of the main drawbacks of MRI is its limited specificity. This can potentially be partially alleviated by target-specific contrast agents. In the present paper we describe a simple high yield synthesis of two such gadolinium-based spiperone targeted MRI contrast agents, 1a and 1b. The R₁ relaxivities of 1a and 1b were evaluated and found to be 5.94 and 8.31 mM⁻¹ s⁻¹, respectively at 9.4T, while their R₂ relaxivities at the same magnetic field were found to be 18.05 and 22.60 mM⁻¹ s⁻¹, respectively. In addition and very importantly compound 1a, which is a gadolinium-based, spiperone-targeted MRI contrast agent, was found to preserve some of the spiperone affinity toward the dopamine D2 receptor. Compounds 1a and 1b thus represent potential agents for in vitro dopamine receptor imaging using MRI in experimental models. Electronic supplementary material The online version of this article (doi:) contains supplementary material, which is available to authorized users.     

MRI相关定量参数在肩峰下撞击综合征诊断中的价值及与肩关节功能、治疗效果的关系

为分析MRI相关定量参数对肩峰下撞击综合征(SIS)的诊断价值,本研究将56例SIS患者设为SIS组,同期56例健康体检者设为对照组,对比了两组对象的一般资料、肩关节功能评分(Constant评分)及MRI相关定量参数水平,探讨了 MRI定量参数与Constant评分、SIS发病相关影响因素、治疗效果的关系及对SIS的...     

东海区海岸带景观格局变化对生态系统服务价值的影响

对大尺度、长时序的海岸带景观格局和生态系统服务价值(ecosystem services value,ESV)的研究,有利于更好地促进区域生态系统保护工作的开展。以1990,1995,2000,2005,2010,2015年6期遥感影像解译结果为基础,对东海区海岸带景观格局变化特征和ESV时空演变进行了分析,并探讨了ESV与景观格局变化二者间的关系。结果表明,1990—2015年的25 a间,受人类活动的影响,东海区海岸带农田和海域面积大量减少,建设用地面积大幅增加;在所研究的5类地貌类型中,除中起伏山地外,其余地貌类型景观面积转移都较为剧烈。25 a间东海区海岸带斑块数量、斑块密度、边界密度、shannon多样性指数等不断增加,景观破碎化、复杂化、多样化增强。农田景观的最大斑块指数、形态指数、边界密度等变化均较大。东海区海岸带ESV呈先增加后减小的趋势,其中森林景观对ESV总量贡献最大;水文调节、生物多样性维持、气候调节、土壤保持、废物处理和气体调节是东海区海岸带主要的生态系统服务功能;在空间上表现出以单位面积中、低ESV为主导的空间分布,高、极高和极低ESV分布较少。研究区ESV总量与农田和海域以及水域和建设用地面积显著相关;与斑块密度、边界密度和形态指数呈显著负相关。同时,食物生产、气体调节、气候调节、土壤保持和生物多样性维持的服务价值与景观指数间均显著相关。     

磁共振成像谱仪梯度波形分析

梯度是磁共振成像（MRI）的关键环节.通过采集谱仪梯度波形信号并进行分析,提取出各通道波形的特征点,从而有助于快速准确地判断谱仪梯度硬件电路或脉冲序列编写是否存在问题.采用虚拟仪器LabVIEW软件控制高速采集卡DAQ-2005设计实现多路采集系统,对谱仪的梯度输出进行采集.通过对波形数据进行直方图统计、滤波、差分计算等分析,提取出波形的特征点,这些特征点包含时间与幅度信息.使用实验室自主研发的谱仪进行了多次实验,对该方法进行验证,证明了该方法的有效性,也为谱仪研制和脉冲序列开发提供了一种辅助测试方法.     

α-苯甲胺基-β-(3-吲哚基)-丙酸甲酯的合成

以L-色氨酸为原料经过4步得到α-苯甲胺基-β-(3-吲哚基)-丙酸甲酯,它是一种具有潜在的抗肿瘤活性的吲哚二酮哌嗪化合物的中间体,首先通过“酰氯法”合成L-色氨酸甲酯盐酸盐,再脱去盐酸,与苯甲醛发生缩合反应形成希夫碱,最后选择性还原,得目的产物,得率54.9%.     

金属-有机骨架材料二聚铜-苯-1，3，5-三羧酸酯中烷烃扩散机理的分子模拟研究

采用分子动力学方法研究了直链烷烃C₁—C₄在二聚铜-苯-1,3,5-三羧酸酯（Cu-BTC）中的扩散机理.首先计算了4种烷烃的自扩散系数,并进一步通过质心分布图与分子轨迹图详细讨论了主、次孔道中各种类型的扩散路径.研究结果表明,不同烷烃在Cu-BTC中表现出的不同或近似的宏观扩散速率,是由微观上受到不同的扩散路径阻力并偏好不同的扩散路径所造成的.这些信息可提高人们对该类材料的认识,并为材料的实际应用以及新材料设计提供理论指导. 关键词： 分子模拟 二聚铜-苯-1 5-三羧酸酯 烷烃 扩散机理