氟哌啶醇季铵盐衍生物的合成及其对冠状动脉的作用

目的 :合成氟哌啶醇季铵盐衍生物并研究其对动物冠状动脉的作用。方法 :以氟哌啶醇为原料 ,将其与卤代烃在回流的情况下进行反应而得到其季铵盐衍生物。采用猪冠状动脉条生物测定法和Langendorff灌流法研究这些衍生物对冠状动脉的作用。结果 :合成了 7个新化合物 ( 1～ 7) ,其中化合物 7量效依赖地压低KCl所致的猪冠状动脉条收缩曲线 ,阻断较大剂量所致的冠状动脉条痉挛 ,并量效依赖地拮抗脑垂体后叶素所致的离体豚鼠心脏冠脉流量减少。结论 :化合物 7显示了良好的扩张冠状动脉的作用 ,值得进一步研究     

日晒海盐工人机体内高镁反应

报道福建某盐场从事日晒海盐生产人工机体内高镁对心血管系统的影响，通过现场空气、饮水、主良的镁含量测定，并对进入机体途径进行分析，得出空气、卤水接触、饮水为机体镁增高的主要来源。不同对象头发镁含量测定结果显示，以接触卤水、劳动强度大的盐工最高，并随机体内镁含量增高，出现血压偏低、心率减慢、心电图Ｐ－Ｒ间期延长、ＱＲＳ波增宽、Ｔ波高尖等机体高镁反应，与临床高镁血症相似。     

尿中83—1除草剂代谢产物的鉴定

本文采用高效液相色谱、质增、紫外和红外光谱对经83—1除草剂(2,4—二氯—6—硝基酚铵)染毒后大鼠尿液中出现的5种组分的化学结构进行了鉴定,并用纯品对照进行确证,发现组分Ⅴ为未代谢的农药母体,其余4种为代谢产物,依次为:二氯氨基酚、二氯氨基酚丙酮酸结合物、二氯羟氨基酚缩合物和二氯氨基酚葡萄糖醛酸结合物。     

中国西部地区儿童甲状腺肿大率、尿碘、盐碘变异程度的分析

目的 研究影响或导致儿童甲状腺肿大率(甲肿率)、尿碘、盐碘三项指标变异程度的因素。方法 用设计效率(DEFF)作为评价变异程度的指标。结果 在西部12省中，儿童甲肿率的DEFF在3．0左右的有9个省，占75．0％；尿碘水平的DEFF在1．0～3．5之间的有6个省，占50．0％；合格碘盐食用率的DEFF有11省在3．0以上。有4个省加碘盐覆盖率的DEFF在3．0左右。结论 除了充分考虑非抽样因素对甲肿率、尿碘、盐碘三项指标变异程度的影响外，还应对西部监测中样本的数量作进一步的推算，使样本量这一影响指标变异程度的主要因素更加科学、合理，从而为全国的碘缺乏病监测工作提供科学依据。     

An improved and highly standardised transformation procedure allows efficient production of single and multiple targeted gene-knockouts in a moss,<Emphasis Type="Italic"> Physcomitrella patens</Emphasis>

The moss Physcomitrella patens is the only land plant known to date with highly efficient homologous recombination in its nuclear DNA, making it a unique model for plant functional genomics approaches. For high-throughput production of knockout plants, a robust transformation system based on polyethylene glycol-mediated transfection of protoplasts was developed and optimised. Both the DNA conformation and pre-culture of plants used for protoplast isolation significantly affected transformation efficiencies. Employing a newly developed PCR high-throughput method, the gene-targeting efficiency in more than 1,000 plants transformed with different cDNA-based knockout constructs was determined and analysed with regard to the length and intron/exon structure of the homologous gene locus. Different targeting constructs, each containing an identical selectable marker gene, were applied as batch DNA in a single transformation experiment and resulted in double-knockout plants. Thus, the fast and efficient generation of multiple targeted gene-knockouts is now feasible in Physcomitrella.Communicated by U. Kück     

Contraluminal transport of organic cations in the proximal tubule of the rat kidney

In order to study the quantitative structure/activity relationship of organic cation transport across the contraluminal side of the proximal renal tubule cell, the stopped-flow capillary microperfusion method was applied and the inhibitory potency (apparent K _i values) of different homologous series of substrates against N ¹-[³H]methylnicotinamide (NMeN⁺) transport was evaluated. Aniline and its ring- or N-substituted analogues as well as the aminonaphthalines do not interact with the contraluminal NMeN⁺ transporter except for the quaternary trimethylphenylammonium and pararosaniline, which bear a permanent positive charge, and for 1,8-bis-(dimethylamino)naphthaline, which forms an intramolecular hydrogen bond. If, however, one or more than one methylene group is interposed between the benzene ring and the amino group, the compounds interact with the contraluminal NMeN⁺ transporter in proportion to their hydrophobicity parameter, i.e. the octanol/water partition coefficient (log octanol). The catecholamines and other hydroxyl-substituted phenylethyl analogues also follow this rule. In addition, the N-heterocyclic pyridine, quinoline, isoquinoline and acridine analogues also interact with the contraluminal NMeN⁺ transporter, when their pK _a values are higher than 5.0, and, an inverse correlation between pK _a and log K _{i, NMeN} was observed. An exception to this rule are those hydroxy compounds of pyridine, quinoline and isoquinoline that show tautomerism. These compounds slightly inhibit NMeN⁺ transport despite low pK _a values. The quaternary nitrogen compounds of aniline and the N-heterocyclic analogues, as far as tested, all interact with the contraluminal NMeN⁺ transporter in relation to their hydrophobicity. The data indicate that the contraluminal NMeN⁺ transporter interacts with N-compounds according to their hydrophobicity and/or according to their basicity (affinity to protons). The reason for deviation of the aniline analogues and the OH-tautomeric heterocyclic N-compounds from this behaviour is discussed.     

Blutdruck,relatives Körpergewicht,Alkoholkonsum und Elektrolytausscheidung in der BRD und der DDR: Die Intersalt-Studie

Summary The relationships between body mass index (BMI) and age, alcohol consumption, 24-hr urinary electrolyte excretion, and BP were studied in 588 subjects from three German centers participating inIntersalt, a highly standardized, previously reported protocol. Men and women aged 20–59 were sampled in Bernried, FRG; Cottbus, GDR; and Heidelberg, FRG. The subjects from the three centers did not differ in BMI, level of education, physical activity, cigarette- or alcohol-consumption patterns, or urinary Cl excretion. Mean Na excretion was 167, 147, and 172 mmol/24 hr in Bernried, Cottbus, and Heidelberg, while mean K excretion was 72, 55, and 73 mmol/24 hr, respectively. The excretion of these electrolytes was significantly lower in Cottbus than in Bernried or Heidelberg. BMI increased progressively in men with age; in women BMI plateaued until the 5th decade, after which it increased to equal that of men. In individual centers, the excretion of electrolytes was correlated with BML Sodium and chloride excretion were highly correlated. The data from each individual center were fitted to a multiple regression model. Age, BMI, sex, and alcohol consumption entered the model.

     

Effects of intracarotid or intraruminal injections of NaCl or NaHCO3 on sodium appetite in goats.

Goats, which have been depleted of sodium by loss of parotid saliva from a parotid fistula, have been trained to press panels with their muzzles in order to obatin small volumes of 4% (0.5 M) sodium bicarbonate to drink. Normal goats display no appetite for 4% (0.5 M) bicarbonate solutions. Goats which were depleted of sodium were highly motivated to work for bicarbonate solutions without displaying a marked fall in plasma sodium levels. It was not possible to train sodium depleted goats to press the panels to obtain intracarotid injections of 3% (0.5 M) salt solutions. The continuous intracarotid injection of concentrated 23% (3.9 M) solutions of NaCl, which increased the level of Na⁺ ions in the cephalic circulation by 11 to 18 m-equiv./1., did not reduce the rate at which sodium depleted goats pressed the panel to obtain 4% (0.5 M) bicarbonate solutions to drink. It was not possible to train sodium depleted goats to press the panel switch in order to obtain intraruminal injections of 4% (0.5 M) bicarbonate solution.     

Homo- and heteromeric assembly of TRP channel subunits

Mammalian homologues of the Drosophila melanogaster transient receptor potential (TRP) channels are the second largest cation channel family within the superfamily of hexahelical cation channels. Most mammalian TRP channels function as homooligomers and mediate mono- or divalent cation entry upon activation by a variety of stimuli. Because native TRP channels may be multimeric proteins of possibly complex composition, it is difficult to compare cation conductances in native tissues to those of clearly defined homomeric TRP channel complexes in living cells. Therefore, the possibility of heteromeric TRP channel assembly has been investigated in recent years by several groups. As a major conclusion of these studies, most heteromeric TRP channel complexes appear to consist of subunit combinations only within relatively narrow confines of phylogenetic subfamilies. Although the general capability of heteromer formation between closely related TRP channel subunits is now clearly established, we are only beginning to understand whether these heteromeric complexes are of physiological significance. This review summarizes the current knowledge on the promiscuity and specificity of the assembly of channel complexes composed of TRPC-, TRPV- and TRPM-subunits of mammalian TRP channels.     

Adaptive modification of ingestive behavior in beach mice (Peromyscus polionotus).

The ability of an inland and beach race of the old-field mouse to use increasing concentrations of NaCl solutions was compared. Inland mice drank significantly more fluid at all concentrations than did beach mice. These differences became more pronounced as the salt concentration was increased. Food consumption was similar in both races while drinking water or a dilute salt solution, but beach mice ate significantly greater amounts when the concentration of salt was increased above 0.2 M. Weight losses on salt solutions were approximately equal in both races, although beach mice survived longer and tolerated the higher concentrations better. There was no difference in the ability of the races to concentrate urine or excrete Na⁺. When given a choice of distilled water or two salt solutions, beach mice consumed significantly more water (77%) than salt solutions (23%) whereas inland mice drank approximately equal amounts of water (54%) and salt solutions (46%). When deprived of anything to drink, beach mice almost stopped eating for the first two days while inland mice did not reduce their food consumption as quickly and died sooner. Thus, it appears that adaptive modifications of ingestive behavior are important for survival in habitats where salt accumlates and summer droughts may be a problem.