The pharmacological effect of citalopram residues in the (S)-(+)-enantiomer.
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.
Hyttel
J
J
H. Lundbeck A/S, Research & Development, Copenhagen, Denmark.
Bøgesø
K P
KP
Perregaard
J
J
Sánchez
C
C
D006916:5-Hydroxytryptophan / Q000494:pharmacology; D000818:Animals; D015283:Citalopram / Q000494:pharmacology*; D008297:Male; D051379:Mice; D051381:Rats; D011919:Rats, Inbred Strains; D012701:Serotonin / Q000378:metabolism; D012702:Serotonin Antagonists / Q000494:pharmacology*; D013237:Stereoisomerism; D013574:Synaptosomes / Q000187:drug effects / Q000378:metabolism
D012702:Serotonin Antagonists; D015283:Citalopram; D012701:Serotonin; D006916:5-Hydroxytryptophan