酮洛芬及其手性对映体的研究进展

<正> 自1898年人们成功合成阿司匹林以来,已经发展出一类结构不同,作用及机理相似,效果可靠,并具有广泛的非特异性抗炎、适度镇痛和解热作用的非甾体抗炎药(NSAIDs)。非甾体抗炎药中,大多数是手性药物,而手性药物在目前临床应用的药物中占有很大的比例,常用的700多种药物有一半至少含有1个手性中心,其中90％使用外消旋体。很多内源性大分     

药物手性、药理作用与新药开发

简要介绍了手性药物在药效学和药动学方面的差异。并就一些手性药物的对映体生物作用特点异和构体间的关系等最新发现加以扼要综述。以供用药和开发新药参考。     

药物手性、药理作用与新药开发

简要介绍了手性药物在药效学和药动学方面的差异。并就一些手性药物的对映体生物作用特点异和构体间的关系等最新发现加以扼要综述。以供用药和开发新药参考。     

手性药物的药动学、药效学及不良反应

本文探讨手性药物的代谢动力学及药效学特征,阐明其药理活性和不良反应实质。结果表明有些手性药物在临床上的应用是有益的,有些则会造成不良后果。因此,通过对手性药物的深入研究,对临床合理应用手性药物具有重要的意义。     

手性药物分析方法研究进展

综述了近10年来手性药物分离检测方法的发展,包括高效液相色谱法、气相色谱法、毛细管电泳法,以及超临界流体色谱法等,旨在为该领域的进一步发展提供参考。     

氟比洛芬对映异构体手性拆分研究进展

手性药物氟比洛芬(flurbiprofen)是一种非甾体类抗炎药,其化学结构见图1.目前市场上销售及临床应用的是其消旋体,其两种光学异构体具有截然不同的药理活性[1-4],其中S型能更有效地抑制环氧化酶,是消炎镇痛的主要成分,R型虽无抗炎作用,但近期研究证明,R型能抑制Aβ-42的表达,并且在体内不会转化为(S)-氟比洛芬,目前已进入治疗前列腺癌和阿尔兹海默病的Ⅲ期临床研究.此外,外消旋氟比洛芬的胃肠不良反应因R对映体的存在而增加.     

阿莫达非尼对映异构体的手性HPLC法检测

建立了HPLC法拆分莫达非尼,并检测阿莫达非尼的(S)-型异构体.使用α-酸性糖蛋白(AGP)手性固定相,以0.05 mol/L乙酸铵水溶液(含3%异丙醇,pH 6.8)为流动相,检测波长225 nm,阿莫达非尼与其(S)-型异构体分离完全,前者的检测限为0.05μg/ml.     

手性药物对映体选择性的药代动力学和药效学与临床合理用药

手性药物对映体选择性的药代动力学和药效学与临床合理用药＊芮建中吴锦芳１庞晓东２综述凌树森审校（南京军区南京总医院临床药理科，南京２１０００２中国图书分类号Ｒ９６２；Ｒ９６９．１；Ｒ９６９．６手性（Ｃｈｉｒａｌｉｔｙ）是生物系统的基本特征，在人体内核酸...     

药物的手性与药效

近年来，随着分子生物学和受体理论的发展以及各种测定有机分子立体结构方法的进一步完善，使人们对体内有机化合物在分子水平上的相互作用有了更多、更深入的认识，从而对手性药物不同旋光异构体所产生的不尽相同的药效也能从作用机理上更清晰地进行阐明，使人们不断地认...     

手性药物对映体在药效学与药代动力学的相互作用

当手性药物以外消旋体供药用时，其对映体间就可能发生药效学和药代动力学的相互作用。本文综述了手性药物对映体间的药效学和药代动力学相互作用及其对手性药物药效学和药代动力学立体选择性的影响。     

Chirality and drugs

The two enantiomers of a chiral drug may have vastly different pharmacodynamic and pharmacokinetic properties. As a result, the research and development of chiral drugs raises specific problems some of which are discussed here. Thus, various pharmacokinetic interactions may involve two enantiomers, as seen for example when one enantiomer inhibits the metabolism of the other and modifies its effects. A different situation occurs when a third compound stereoselectively inhibits the metabolism of one of the two enantiomers. Another problem examined here results from the lack of configurational stability of some chiral drugs, a little known phenomenon whose consequences can be of pharmacological or pharmaceutical significance depending on the rate of the reaction of racemization or epimerisation. In-depth investigations are needed before choosing between a eutomer or a racemate.     

Chirality influences the effects of linalool on physiological parameters of stress

The specific physiological responses induced by inhaling R-(-)- as well as S-(+)-linalool in 24 human subjects undergoing experimental stress were investigated in this study. Various physiological parameters of the autonomous nervous system (heart rate, blood pressure, electrodermal activity) as well as the endocrine system (salivary cortisol) were monitored. The study clearly indicated that odorants can modulate salivary cortisol levels, with both linalool enantiomers exerting relaxing effects. Concerning blood pressure and heart rate, S-(+)-linalool acted as an activating agent in contrast to electrodermal activity. R-(-)-linalool proved to be stress-relieving as determined by heart rate. In conclusion, the results revealed that (1) chirality crucially influences the physiological effects of odorants and that (2) odorants may act differently on certain physiological parameters.     

乳酸环丙沙星注射液与6种药物配伍的稳定性

本文选用６种常用药物与乳酸环丙沙星注射液配伍。在２５℃时观察混合液的外观性状、ｐＨ值、紫外光谱吸收度的变化，以判断其任用后的稳定性，为临床用药提供参考。     

Species difference and characterization of intestinal esterase on the hydrolizing activity of ester-type drugs

The ability of the esterase from intestine was studied for hydrolysis of ester-type drugs during absorption. The intestinal esterase is present in the absorption sites in the intestine and hydrolyzes to a large extent during the absorption. In a study of the dietary effect on intestinal esterase, the esterase activity increased in rats fed a high-fat diet, decreased in those fasted or fed a fat-free diet, whereas the esterase activity in the rat treated with phenobarbital showed no marked change. Thus the esterase from intestinal mucosa appears to be characteristically quite different from hepatic esterase. The esterase from human intestine was characterized and compared with esterase from rats, mice, rabbits, guinea pigs and dogs. There was a difference in the substrate specificity of the esterase and there were significant species differences in the electrophoretic behavior of the enzyme among the species tested. These results indicate that intestinal esterase from humans differs characteristically from esterases in experimental animals.     

从临床疗效角度谈原研药和仿制药的区别

目的:从临床疗效的角度对原研药与仿制药的区别进行介绍并探讨引起疗效差别可能的原因。方法:在ISI Web of Knowledge、PubMed、Science Direct和中国知网数据库中检索原研药与仿制药对比的相关中英文文献,并对文章进行分析。结果:通过对检索到的相关文献进行分析,我们发现在癫痫、帕金森、精神疾病、器官移植、心血管和感染疾病方面的仿制药与原研药相比存在一定差异。结论:对于部分药物而言,作为评价仿制药上市的标准——生物等效性(bioequivalence,BE)试验尚不能替代临床疗效的等效性。制剂因素是两种药品疗效差异的根本原因。     

海洋来源的微管去稳定剂抗肿瘤药物研究进展

摘要：微管是细胞骨架重要组成成分,是筛选抗肿瘤药物的重要靶标。海洋生态系统的极端环境使海洋生物具备产生独特 化学结构和生理活性天然产物的能力,为新药发现提供了物质基础。本文主要综述了1972-2021年从海洋生物中分离鉴定的成 药性较好的微管去稳定剂抗肿瘤药物的研究进展,总结了活性化合物来源、构效关系,临床研究进展,化学全合成及衍生物的 研究情况等,以期为医药工作者提供新的研究思路,推进靶向微管海洋抗肿瘤药物的发展。     

Microplastic exposure and effects in aquatic organisms: A physiological perspective

The impact of microplastics (MPs) on aquatic life, given their ubiquitous presence in the water compartment, represents a growing concern. Consistently, scientific knowledge is advancing rapidly, although evidence on actual adverse effects is still highly fragmented. This paper summarizes the recent literature on MP impacts on aquatic organisms in an attempt to link routes of uptake, possible alterations of physiological processes, and outcomes at different levels of biological organization. Animal feeding strategies and MP biodistribution is discussed, alongside with relevant effects at molecular, cellular, and systemic level. Pathways from animal exposure to apical physiological responses are examined to define the relevance of MPs for animal health, and to point out open questions and research gaps. Emphasis is given to emerging threats posed by leaching of plastic additives, many of which have endocrine disruption potential. The potential role of MPs as substrates for microorganism growth and vehicle for pathogen spreading is also addressed.