Functional expression of mammalian opioid receptors in insect cells and high-throughput screening platforms for receptor ligand mimetics

Lepidopteran cell lines have been engineered to constitutively express high levels of mouse opioid receptors either alone or in combination with human G16 protein. Biochemical and pharmacological studies demonstrate that these lines contain all the mediator G proteins and downstream effectors required for opioid receptor function, including phospholipase C, and that expression of exogenous G16 does not contribute significantly to increased receptor responses upon activation. The activation of the phospholipase C pathway in the transformed cells upon stimulation with known receptor ligands results in easily and quantitatively measurable increases in free intracellular calcium, which can be monitored by automated fluorescent methods, while the addition of specific antagonists blocks the agonist-induced responses. Therefore, the transformed lepidopteran cell lines can be used as sensitive high-throughput screening platforms for fast detection of opioid receptor ligand mimetics (agonists and antagonists) in collections of natural products and synthetic compounds.Received 3 December 2004; received after revision 3 February 2005; accepted 10 February 2005L. Swevers and E. Morou contributed equally to this work.     

Physicochemical profiling in drug research: a brief survey of the state-of-the-art of experimental techniques

This review begins with a general presentation of the new paradigm of drug discovery, with its emphasis on the rapid identification and elimination of compounds with unsuitable physicochemical and pharmacokinetic properties. The focus of the paper is on the various experimental methods used to determine such key physicochemical properties as ionization, lipophilicity and distribution in isotropic and anisotropic systems, solubility, and permeability across artificial membranes. Both traditional and high-throughput methods are presented and their limits highlighted. The text concludes with the trade-off between quantity/speed in high-throughput screening techniques versus greater data quality in the more labor-intensive methods. Received 23 April 2002; received after revision 25 June 2002; accepted 11 July 2002 RID="*" ID="*"Corresponding author.     

豫西南蓝石棉成矿地质特征

蓝石棉矿床属世界一种珍贵和稀有的矿产资源,是国防及尖端工业的一种重要矿物原料。我国是全世界性能优良的蓝石棉产地之一,豫西南地区是我国最好的一个蓝石棉成矿带。本文主要论述该矿带的成矿地质特征,该矿带蓝石棉矿床的产出与偏碱基性火山岩、基性和酸性侵入岩与围岩的接触带以及断裂构造有着极为密切的联系。     

一种基于关联预测的车间生产计划的最优分解方法

提出一种基于关联预测的柔性自动化车间（ＦＡＷ）生产计划的最优分解方法。文中首先建立关联方程有延迟的车间计划分解数学模型，然后推导基于关联预测的计划分解算法，证明算法可行的必要条件，编制相应软件，进行算例研究。与现有的计划分解方法相比，本文的方法更适于将ＣＩＭＳ／ＭＲＰⅡ下达给ＦＡＷ的中期计划最优分解成ＦＡＷ中各ＦＭＳ执行的短期计划，尤其适合ＦＭＳ之间的工件传输需经过出入库并有一步延迟的情况。     

Color image computer desktop printing system

Color image printing technique on ink jetting printer is introduced. Color shading method such as dithering, Amplitude Modulation (AM) screening and Frequency Modulation (FM) screening is presented. Some solutions to the problems with FM screening are given. An application program under Windows is developed. Supported by the International Cooperation Project (Japan Asahi High Tec Co. Ltd) Sun Xiaoan: born in July 1967, Ph. D     

Teratogenicity screening in standardized chick embryo culture: Effects of dexamethasone and diphenylhydantoin

Summary Teratogenic and toxic effects of DXM and DPH were tested using a standardized chick embryo culture. Survival, growth and malformations were scored with respect to the drug concentrations used. DXM (>10^–8 mol/l) inhibited the differentiation of the extraembryonic blood circulation and induced craniofacial anomalies. DPH (>1.5 10^–5 mol/l) induced cardiomegaly, craniofacial and somitic anomalies. Both drugs were lethal at 10^–3 mol/l. Comparison of results obtained with 8 drugs shows that the method has a good discriminative power and specificity and that it can be used as a simple, reliable and economical primary screening test, making it possible to reduce the use of animals in toxicological studies.Supported by the grant 4.790.0.84.17 from the Swiss National Science Foundation.     

五氯酚钠生物降解菌的初步筛选

用五氯酚钠浓度梯度培养基平板,从土样中筛选五氯酚钠耐受菌;再以五氯酚钠为唯一碳源进行摇瓶培养,筛选五氯酚钠降解菌。以不同浓度的五氯酚钠药物培养基对五氯酚钠降解菌的耐受能力进行测定。结果筛选出对五氯酚钠的耐受能力为0.8 g/L的菌株,并能以五氯酚钠为唯一碳源生长的细菌3株。     

维吾尔族新生儿苯丙酮尿症(PKU)的筛查及诊断

本文用纸片法采取新疆维吾尔自治区12527名维吾尔族新生儿足跟血三滴,采用细菌抑制法测定血片中血液苯丙氨酸的含量,进而筛查维吾尔族新生儿苯丙酮尿症患儿.本次抽样筛查共发现苯丙酮尿症患儿9例.初步确定维吾尔族新生儿苯丙酮尿症的发病率为0.718‰,高于我国内地的新生儿苯丙酮尿症发病率(0.33‰).应在新疆维吾尔自治区建立以地区妇幼保健院为中心的筛查网,对维吾尔族及其他民族的新生儿进行苯丙酮尿症筛查和治疗.