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Stereochemical Aspects of Drug Action and Disposition pp 91–112Cite as

Drug Racemization and Its Significance in Pharmaceutical Research

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Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 153))

Abstract

The presence of one or more elements of chirality (i.e., centers, axes or planes of chirality, and generally helicity) (Cahn et al. 1966; Testa 1979) in drug molecules generates specific properties which may be advantageous in some cases, but inevitably require special consideration and studies. Examples of advantages include the possibility of increased selectivity and the fact that chirality per se is an invaluable probe in molecular pharmacology and biochemistry (Testa 1989,1990; Testa and Trager 1990). In contrast, problems generated by stereoisomerism include the need for stereospecific synthetic and analytical methods, the influence of the degree of resolution on activity (Barlow et al. 1972), and the increased complexity of metabolic, pharmacological, and clinical studies (AriËns 1986; Testa et al. 1993a).

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Authors
  1. M. Reist
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  2. B. Testa
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  3. P.-A. Carrupt
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Editor information

Editors and Affiliations

  1. Institut für Klinische Pharmakologie, Dr. Margarete-Fischer-Bosch, Auerbachstr. 112, 70376, Stuttgart, Germany

    Michel Eichelbaum

  2. School of Pharmacy, University of Lausanne School of Pharmacy, 1015, Lausanne, Switzerland

    Bernard Testa

  3. Dept. of Clinical and Experimental Pharmacology, University of Adelaide, 5005, Adelaide, Australia

    Andrew Somogyi

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© 2003 Springer-Verlag Berlin Heidelberg

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Reist, M., Testa, B., Carrupt, PA. (2003). Drug Racemization and Its Significance in Pharmaceutical Research. In: Eichelbaum, M., Testa, B., Somogyi, A. (eds) Stereochemical Aspects of Drug Action and Disposition. Handbook of Experimental Pharmacology, vol 153. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-55842-9_4

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  • DOI: https://doi.org/10.1007/978-3-642-55842-9_4

  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-642-62575-6

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