Journal
BIOLOGICAL PSYCHIATRY
Volume 50, Issue 5, Pages 345-350Publisher
ELSEVIER SCIENCE INC
DOI: 10.1016/S0006-3223(01)01145-3
Keywords
escitalopram; S-citalopram; R-fluoxetine; antidepressant; serotonin; enantiomer; binding; uptake
Categories
Ask authors/readers for more resources
Background: Single isomers of the selective serotonin reuptake inhibitors citalopram (escitalopram, S-citalopram) and fluoxetine (R-fluoxetine) are currently under development for the treatment of depression and other psychiatric disorders. Previous studies conducted in laboratory animals have revealed that the biological effects on serotonin reuptake for citalopram reside in the S enantiomer. In contrast, both enantiomers of fluoxetine contribute to its biological activity. Methods: In the present study, the potency and selectivity of escitalopram, R-fluoxetine, and all of the other currently available selective serotonin reuptake inhibitors were compared for binding affinity at the human serotonin, norepinephrine, and dopamine transporters and several select neurotransmitter receptors using radioligand binding assays. Results: Both escitalopram and R-fluoxetine were potent inhibitors of the serotonin transporter (K-i = 1.1 and 1.4 nmol/L, respectively). Escitalopram was the most serotonin transporter-selective compound tested and was similar to 30-fold more potent than R-citalopram. Conclusions: As noted previously, paroxetine and sertraline possess moderate affinity (< 50 nmol/L) for the human norepinephrine transporter and dopamine transporter, respectively. R-Fluoxetine, unlike the other selective serotonin reuptake inhibitors, possesses moderate affinity (K-i = 64 nmol/L) for the serotonin 2C receptor. Potential clinical correlates of these unique attributes of escitalopram and R-fluoxetine are discussed. Biol Psychiatry 2001;50: 345-350 (C) 2001 Society of Biological Psychiatry.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available