Indoxyl derivatives of drug metabolites

Summary Indoxyl derivatives were detected as minor products among the urinary metabolites of two trial drugs, a benzodiazepine (GP 55 129) and a benzophenone (CGP 11 952). Their structures were elucidated by NMR and mass spectroscopy. Presumably, metabolites containing potential aldehyde functions react spontaneously with endogenous indoxyl. Such derivatives have not hitherto been encountered in drug metabolism.     

芦岭矿采空区煤炭自燃发火与开采技术关系的试验研究

采用了包括多点热电偶测定采空区遗煤温度、应用六氟化硫气体示踪和测定漏风压差等综合技术手段研究分析了漏风分布规律。结果发现,遗煤温度变化受漏风温度和漏风强度影响较大;停采线漏风的量及漏风时间受主要进、回风道的布置以及采掘接替安排的影响。由于采用无煤柱开采技术,三个相邻阶段的采空区之间连通,存在漏风,最后又从开采技术上提出了防火措施。     

The melatonin rhythm: both a clock and a calendar

The paper briefly reviews the data which shows that the circadian production and secretion of melatonin by the pineal gland can impart both daily, i.e., clock, and seasonal, i.e., calendar, information to the organism. The paper summarizes the 3 patterns of nocturnal melatonin production that have been described. Clearly, regardless of the pattern of nocturnal melatonin production a particular species normally displays, the duration of nightime elevated melatonin is proportional to the duration of the night length. Since daylength under natural conditions changes daily the melatonin rhythm, which adjusts to the photoperiod sends time of year information to the organism. The melatonin receptors which subserve the clock message sent by the pineal gland in the form of a melatonin cycle may reside in the biological clock itself, namely, the suprachiasmatic nuclei (SCN). The melatonin receptors that mediate seasonal changes in reproductive physiology are presumably those that are located on the pars tuberalis cells of the anterior pituitary gland. Besides these receptors which likely mediate clock and calendar information, melatonin receptors have been described in other organs. Interestingly, the distribution of melatonin receptors is highly species-specific. Whereas the clock and calendar information that the melatonin cycle imparts to the organism relies on cell membrane receptors, a fact that is of some interest considering the high lipophilicity of melatonin, recent studies indicate that other functions of melatonin may require no receptor whatsoever.     

地下感应式通信理论的研究

本文研究了地下矿井内,电波沿巷道内线缆传播的可行性及单线波模的传播与衰减规律,研究巷道内电小天线与线缆之间的耦合情况,从而为实际工作提供理论依据。     

Catecholamine metabolism in the vas deferens and the adrenal gland with special reference to the central catecholamine-depleted state

Experiments were carried out to elucidate the role of central catecholamines in regulating catecholamine metabolism in the vas deferens and adrenal gland of the rat. Rats were injected intracerebroventricularly (i.c.v.) with either vehicle or 6-hydroxydopamine (6-OHDA). Groups of animals pretreated with vehicle or 6-OHDA (i.c.v.) were injected intraperitoneally (i.p.) with alpha-methyl-para-tyrosine (AMT), a tyrosine hydroxylase inhibitor. Catecholamine turnover rates were estimated by determining norepinephrine or epinephrine content after administrating AMT.Central norepinephrine and dopamine contents decreased significantly (p<0.05) after treatment with 6-OHDA and AMT. The norepinephrine content of the vas deferens of rats pretreated with 6-OHDA was markedly reduced (p<0.001) after administration of AMT, whereas that of the vehicle-treated rats remained unchanged. Administration of 6-OHDA had no effect on the norepinephrine or epinephrine content of the adrenal gland.The present results indicate that central monoaminergic neurons have an inhibitory effect on the adrenergic neurons of the vas deferens. In contrast, this inhibitory regulation does not appear to be exerted on the adrenal glands.     

Increased assembly of cytoskeletal proteins associated with the transformation of human liver cells into fibroblast-like cells.

A topoisomerase II inhibitor, novobiocin, and a deacetylase inhibitor, butyrate, synergistically transformed human liver cells into fibroblast-like cells. This morphological change was associated with an increased production of procollagen type III peptide and a simultaneous assembly of actin, tubulin, vimentin and cytokeratin. Novobiocin and butyrate had no marked effect on the phosphorylation state of cytokeratin proteins, but synergistically enhanced [3H]acetate uptake. From these results, it can be speculated that protein acetylation plays an important role in inducing the assembly of cytoskeletal proteins and the morphological transformation of human liver cells.     

中国南海海绵化学成份研究Ⅱ—B·C

从中国南海西沙群岛永胜岛附近海域采集到的一种海绵(种属未定)分离到两种新的三羟基长链酰胺类化合物S—Ⅱ(C_(49)H_(99)NO_4,M=765,m.p.138-140℃)和S—Ⅲ(C_(45)H_(93)NO_4,M=723,m.p.92—93℃),通过对它们的IR,MS,~1HNMR,~(13)CNMR及~(13)CNMR DEPT等波谱数据分析,S—Ⅱ和S—Ⅲ的结构分别确定为N-(1-乙基-3,22-二羟基)二十二烷基-2-甲基-4-羟基二十四脂肪酸酰胺和N-(1-羟甲基-2-乙基-4-甲基-3,18-二羟基)十九烷基—二十三脂肪酸酰胺。     

精测安培表内阻的新方法——电桥伏安法

本文提出了精测安培表内阻的新方法,并将其与其它测量方法进行了比较。     

水电工程规划设计方案的自动生成及评价

本文介绍了在水电工程规划设计时，如何利用三次自然样条插值函数在有限个方案的基础上自动生成无限多个方案，然后采用多目标综合决策模型在其中选择最优方案的一种方法．文中还给出了程序流程，并以某水电站正常蓄水位选择作为实例，对方法进行了验证，结果与专家决策完全吻合．