The S-enantiomer of R,S-citalopram, increases inhibitor binding to the human serotonin transporter by an allosteric mechanism. Comparison with other serotonin transporter inhibitors.

@article{Chen2005TheSO,
  title={The S-enantiomer of R,S-citalopram, increases inhibitor binding to the human serotonin transporter by an allosteric mechanism. Comparison with other serotonin transporter inhibitors.},
  author={Fenghua Chen and Mads Breum Larsen and Connie S{\'a}nchez and Ove Wiborg},
  journal={European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology},
  year={2005},
  volume={15 2},
  pages={193-8}
}
The interaction of the S- and R-enantiomers (escitalopram and R-citalopram) of citalopram, with high- and low-affinity binding sites in COS-1 cell membranes expressing human SERT (hSERT) were investigated. Escitalopram affinity for hSERT and its 5-HT uptake inhibitory potency was in the nanomolar range and approximately 40-fold more potent than R-citalopram. Escitalopram considerably stabilised the [3H]-escitalopram/SERT complex via an allosteric effect at a low-affinity binding site. The… CONTINUE READING

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