Advertisement

The pharmacological effect of citalopram resides in the (S)-(+)-enantiomer

  • J. Hyttel
  • K. P. Bøgesø
  • J. Perregaard
  • C. Sánchez
Short Communication

Summary

The enantiomers of citalopram and N-demethylcitalopram have been investigated. Based on the inhibition of 5-HT uptake in vitro and the potentiation of 1-5-HTP in vivo the pharmacological activity resides in the (+)-enantiomers (the eutomers) with the 1-(S) absolute configuration. In the 5-HT uptake test eudismic ratios of 167 and 6.6 are obtained for the enantiomers of citalopram and N-demethylcitalopram, respectively. The pharmacological profile of the eutomers of citalopram and N-demethylcitalopram very much resembles the profile of the respective racemates.

Keywords

Citalopram enantiomers 5-HT uptake 

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. Bøgesø KP, Perregaard J (1990) US Patent 4,943,590. Chem Abstr 113(9): 78150vGoogle Scholar
  2. Hyttel J (1978 a) Inhibition of3H-dopamine accumulation in rat striatal synaptosomes by psychotropic drugs. Biochem Pharmacol 27: 1063–1068Google Scholar
  3. Hyttel J (1978 b) Effect of a specific 5-HT uptake inhibitor, citalopram (Lu 10-171), on3H-5-HT uptake in rat brain synaptosomes. Psychopharmacology (Berlin) 60: 13–18Google Scholar
  4. Hyttel J (1982) Citalopram-pharmacological profile of a specific serotonin uptake inhibitor with antidepressant activity. Prog Neuropsychopharmacol Biol Psychiatry 6: 277–295Google Scholar
  5. Milne RJ, Goa KL (1991) Citalopram. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in depressive illness. Drugs 41: 450–477Google Scholar

Copyright information

© Springer-Verlag 1992

Authors and Affiliations

  • J. Hyttel
    • 1
  • K. P. Bøgesø
    • 1
  • J. Perregaard
    • 1
  • C. Sánchez
    • 1
  1. 1.Research & DevelopmentH. Lundbeck A/SCopenhagenDenmark

Personalised recommendations