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.
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References
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Hyttel, J., Bøgesø, K.P., Perregaard, J. et al. The pharmacological effect of citalopram resides in the (S)-(+)-enantiomer. J. Neural Transmission 88, 157–160 (1992). https://doi.org/10.1007/BF01244820
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DOI: https://doi.org/10.1007/BF01244820