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北京石油化工学院2026年研究生招生接收调剂公告
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armea

木虫之王 (著名写手)


[资源] Pharmacokinetic Profiling in Drug Research

Pharmacokinetic Profiling in Drug Research: Biological, Physicochemical, and Computational Strategies
By Bernard Testa, Stefanie D. Krämer, Heidi Wunderli-Allenspach, Gerd Folkers



Publisher:   Wiley-VCH
Number Of Pages:   500
Publication Date:   2006-03-31
ISBN-10 / ASIN:   3906390357
ISBN-13 / EAN:   9783906390352
Binding:   Hardcover



Informatics and robotics are the workhorses of a technological revolution in drug research. On them are based combinatorial chemistry, which yields compounds by the many thousands, and high-throughput bioassays, which screen them for activity. The results are avalanches of 'hits', which invade the databases like swarms of locusts. But far from being a plague, these innumerable compounds become a blessing if properly screened for 'drugability', i.e., for 'drug-like' properties such as good pharmacokinetic (PK) behavior. Pharmacokinetic profiling of bioactive compounds has, thus, become a sine qua non condition for cherry-picking the most promising hits. Just as important, but less visible, are the structure-property and structure-ADME relations, which emerge from PK profiling and provide useful feedback when designing new synthetic series. As a result, the screening, design, and optimization of pharmacokinetic properties has become the bottleneck and a major challenge in drug research. To shorten the time-consuming development and high rate of attrition of active compounds ultimately doomed by hidden pharmacokinetic defects, powerful biological, physicochemical, and computational approaches are being developed, whose objectives are to increase the clinical relevance of drug design and to eliminate as soon as possible compounds with unfavorable physicochemical properties and pharmacokinetic profiles.

The profiling of ADME properties (absorption, distribution, metabolism, and excretion) is the topic of this book. Following the extraordinary success of the previous work ('Pharmacokinetic Optimization in Drug Research: Biological, Physicochemical, and Computational Strategies', Eds. B. Testa, H. van de Waterbeemd, G. Volkers, R. Guy, Verlag Helvetica Chimica Acta, Z? 2001, 655 pages), there was a need for an essentially new edition focusing on the latest theoretical and technological breakthroughs. In this unique work, international authorities and practicing experts from academia and industry offer state-of-the-art presentations of concepts, methods and technologies now in use or development in drug research. The biological strategies emphasized in the book include cell cultures, drug-metabolizing enzymes, transporters and plasma protein binding. The physicochemical strategies focus on artificial membrane-permeability assays, on solubility and lipophilicity and related molecular properties as factors and predictors of pharmacokinetic behavior, and on stability and solid-state properties. Computational strategies comprize the exploration of property spaces, pharmacophore searching to predict biotransformation and enzyme inhibition, and expert systems to process biopharmaceutical profiling data.

In addition to its 28 chapters, the book includes a CD-ROM containing the invited lectures, oral communications, and posters (in full version) presented at the Third LogP Symposium, 'Physicochemical and Biological Profiling in Drug Research', held at the Federal Institute of Technology (ETH) of Z?in March 2004.
http://rapidshare.com/files/103299275/PHAPIDR.rar
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wzgynkmlhf

金虫 (著名写手)


下了以后只有3K多,打不开,说是数据损坏了。我两个链接都试过的。
8楼2008-04-16 22:22:24
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yinjj

金虫 (职业作家)


★★★★★ 五星级,优秀推荐

good book
2楼2008-03-30 20:41:26
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daoke2005

铁杆木虫 (著名写手)


★★★★★ 五星级,优秀推荐

收下了,谢谢!
3楼2008-03-31 21:33:53
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lotus86

新虫 (初入文坛)


★★★ 三星级,支持鼓励

,谢谢啊。。。辛苦了啊。。
4楼2008-04-01 09:57:07
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