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

European Neuropsychopharmacology

Volumn 15, Issue 2, 2005, Pages 193-198

  Chen, Fenghua ^a   Larsen, Mads Breum ^a   Sánchez, Connie ^b   Wiborg, Ove ^a  

^a AARHUS UNIVERSITY HOSPITAL   (Denmark)

^b H LUNDBECK A S   (Denmark)

Author keywords

COS 1 cell membrane; Dissociation rate; Escitalopram; Human SERT; SSRI

Indexed keywords

3BETA (4 IODOPHENYL) 2BETA TROPANECARBOXYLIC ACID METHYL ESTER I 125; CITALOPRAM; ESCITALOPRAM; FLUOXETINE; FLUOXETINE H 3; IODINE 125; PAROXETIN H 3; PAROXETINE; RADIOLIGAND; SEROTONIN; SEROTONIN TRANSPORTER; SEROTONIN UPTAKE INHIBITOR; SERTRALINE; UNCLASSIFIED DRUG; VENLAFAXINE; VENLAFAXINE H 3;

ALLOSTERISM; ARTICLE; BINDING AFFINITY; BINDING SITE; CELL MEMBRANE; CHEMICAL INTERACTION; COMPARATIVE STUDY; ENANTIOMER; HUMAN; HUMAN CELL; PRIORITY JOURNAL; STEREOCHEMISTRY;

EID: 13244262698     PISSN: 0924977X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.euroneuro.2004.08.008     Document Type: Article

References (12)

1. S. Chalon, J. Tarkiainen, L. Garreau, H. Hall, P. Emond, J. Vercouillie, L. Farde, P. Dasse, K. Varnas, J.C. Besnard, C. Halldin, and D. Guilloteau Pharmacological characterization of N,N-dimethyl-2-(2-amino-4-methylphenylthio) benzylamine as a ligand of the serotonin transporter with high affinity and selectivity J. Pharmacol. Exp. Ther. 304 2002 81 87
2. J. Hyttel, K.P. Bøgesø, J. Perregaard, and C. Sánchez The pharmacological effect of citalopram resides in the (S)-(+)-enantiomer J. Neural Transm. 88 1992 157 160
3. O.V. Mortensen, A.S. Kristensen, and O. Wiborg Species-scanning mutagenesis of the serotonin transporter reveals residues essential in selective, high-affinity recognition of antidepressants J. Neurochem. 79 2001 237 247
4. A. Mørk, M. Kreilgaard, and C. Sánchez The R-enantiomer of citalopram counteracts escitalopram-induced increase in extracellular 5-HT in the frontal cortex of freely moving rats Neuropharmacology 45 2003 167 173
5. M.J. Owens, D.L. Knight, and C.B. Nemeroff Second-generation SSRIs: human monoamine transporter binding profile of escitalopram and R-fluoxetine Biol. Psychiatry 50 2001 345 350
6. 3H]paroxetine binding to platelet and neuronal membranes Eur. J. Pharmacol. 119 1985 1 8
7. P. Plenge, and E.T. Mellerup An affinity-modulating site of neuronal monoamine transporter protein Pharmacol. Toxicol. 80 1997 197 201
8. 3H] citalopram binding to the 5-HT transporter from brain and platelets Eur. J. Pharmacol. 206 1991 243 250
9. C. Sánchez R-Citalopram attenuates anxiolytic effects of escitalopram in a rat ultrasonic vocalisation model Eur. J. Pharmacol. 464 2003 155 158
10. C. Sánchez, P. Gruca, E. Bien, and M. Papp R-Citalopram counteracts the anxiolytic-like effect of escitalopram in a rat conditioned fear model Pharmacol. Biochem. Behav. 75 2003 903 907
11. C. Sánchez, P. Gruca, and M. Papp R-Citalopram counteracts the antidepressant-like effect of escitalopram in a rat chronic mild stress model of depression Behav. Pharmacol. 14 2003 465 470
12. L.P. Wennogle, and L.R. Meyerson Serotonin uptake inhibitors differentially modulate high affinity imipramine dissociation in human platelet membranes Life Sci. 36 1985 1541 1550