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Three-dimensional pharmacology, a subject ranging from ignorance to overstatements.

Waldeck, Bertil LU (2003) In Pharmacology and Toxicology1987-01-01+01:002004-01-01+01:00 93(5). p.203-210
Abstract
Stereoselectivity has been known to play a role in drug action for 100 years or more. Nevertheless, chiral drugs have been developed and used as racemates, neglecting the fact that they comprise mixtures of two or more compounds which may have quite different pharmacological properties. A very limited access to pure enantiomers in the past has been responsible for this unsatisfactory state of affairs. During the last 20 years, significant achievements have made it possible to perform stereoselective synthesis and analysis. Today, novel chiral drugs are as a rule developed as single enantiomers. Yet, studies of old racaemic drugs are still designed, performed and published without mention of the fact that two or more compounds are involved.... (More)
Stereoselectivity has been known to play a role in drug action for 100 years or more. Nevertheless, chiral drugs have been developed and used as racemates, neglecting the fact that they comprise mixtures of two or more compounds which may have quite different pharmacological properties. A very limited access to pure enantiomers in the past has been responsible for this unsatisfactory state of affairs. During the last 20 years, significant achievements have made it possible to perform stereoselective synthesis and analysis. Today, novel chiral drugs are as a rule developed as single enantiomers. Yet, studies of old racaemic drugs are still designed, performed and published without mention of the fact that two or more compounds are involved. In recent years, a number of old racaemic drugs have been re-evaluated and re-introduced into the clinical area as the pure, active enantiomer (the eutomer). While in principle correct, the clinical benefit of this shift from a well established racaemate to a pure enantiomer often seems to be limited and sometimes exaggerated. Racaemic drugs with a deleterious enantiomer that does not contribute to the therapeutic effect (the distomer), may have been sorted out in the safety evaluation process. However, in the future any pharmacological study of racaemic drugs must include the pure enantiomers. This will generate new, valuable information on stereoselectivity in drug action and interaction (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Pharmacology and Toxicology1987-01-01+01:002004-01-01+01:00
volume
93
issue
5
pages
203 - 210
publisher
Wiley-Blackwell
external identifiers
  • pmid:14629731
  • wos:000187107300001
  • scopus:0346874450
ISSN
1600-0773
DOI
10.1046/j.1600-0773.2003.pto930502.x
language
English
LU publication?
yes
id
49b9981d-e344-4e54-ba7c-795deb40ac4e (old id 118746)
date added to LUP
2007-07-20 08:26:19
date last changed
2018-09-02 03:31:10
@article{49b9981d-e344-4e54-ba7c-795deb40ac4e,
  abstract     = {Stereoselectivity has been known to play a role in drug action for 100 years or more. Nevertheless, chiral drugs have been developed and used as racemates, neglecting the fact that they comprise mixtures of two or more compounds which may have quite different pharmacological properties. A very limited access to pure enantiomers in the past has been responsible for this unsatisfactory state of affairs. During the last 20 years, significant achievements have made it possible to perform stereoselective synthesis and analysis. Today, novel chiral drugs are as a rule developed as single enantiomers. Yet, studies of old racaemic drugs are still designed, performed and published without mention of the fact that two or more compounds are involved. In recent years, a number of old racaemic drugs have been re-evaluated and re-introduced into the clinical area as the pure, active enantiomer (the eutomer). While in principle correct, the clinical benefit of this shift from a well established racaemate to a pure enantiomer often seems to be limited and sometimes exaggerated. Racaemic drugs with a deleterious enantiomer that does not contribute to the therapeutic effect (the distomer), may have been sorted out in the safety evaluation process. However, in the future any pharmacological study of racaemic drugs must include the pure enantiomers. This will generate new, valuable information on stereoselectivity in drug action and interaction},
  author       = {Waldeck, Bertil},
  issn         = {1600-0773},
  language     = {eng},
  number       = {5},
  pages        = {203--210},
  publisher    = {Wiley-Blackwell},
  series       = {Pharmacology and Toxicology1987-01-01+01:002004-01-01+01:00},
  title        = {Three-dimensional pharmacology, a subject ranging from ignorance to overstatements.},
  url          = {http://dx.doi.org/10.1046/j.1600-0773.2003.pto930502.x},
  volume       = {93},
  year         = {2003},
}