* Paper based on a talk at the symposium entitled `In vivo pharmacology in drug discovery and development' at The Royal Veterinary and Agricultural University, Copenhagen, Denmark, September 10, 2004.
The Pharmacology of Citalopram Enantiomers: The Antagonism by R-Citalopram on the Effect of S-Citalopram*
Article first published online: 8 AUG 2006
Basic & Clinical Pharmacology & Toxicology
Volume 99, Issue 2, pages 91–95, August 2006
How to Cite
Sánchez, C. (2006), The Pharmacology of Citalopram Enantiomers: The Antagonism by R-Citalopram on the Effect of S-Citalopram. Basic & Clinical Pharmacology & Toxicology, 99: 91–95. doi: 10.1111/j.1742-7843.2006.pto_295.x
- Issue published online: 8 AUG 2006
- Article first published online: 8 AUG 2006
- (Received August 1, 2005; Accepted September 20, 2005)
Abstract: Recent results on the in vivo and in vitro pharmacology of escitalopram are summarised. The exact molecular mechanism by which R-citalopram inhibits the effect of S-citalopram on the serotonin transporter remains to be elucidated. Preliminary evidence indicates an effect of R-citalopram on the association of escitalopram with the high affinity primary site, and on its dissociation from the serotonin transporter, via an allosteric mechanism. Escitalopram can be considered as an allosteric serotonin reuptake inhibitor. This serotonin dual action in binding to two sites on the serotonin transporter (both the primary site and the allosteric site) is hypothesised to be responsible for a longer binding to, and therefore greater inhibition of the serotonin transporter by escitalopram.