Carrier-mediated serotonin release induced by d-fenfluramine: Studies with human neuroblastoma cells transfected with a rat serotonin transporter

M. Cinquanta, T. Ratovitski, D. Crespi, M. Gobbi, T. Mennini, R. Simantov

Research output: Contribution to journalArticle

13 Citations (Scopus)

Abstract

The NMB human neuronal cell line, transfected with a newly prepared plasmid expressing rat serotonin transporter (NMB-rSERT), shows specific [3H]5-HT uptake which is blocked by citalopram and fenfluramine (F) stereoisomers with IC50 values (I nM, 0.5 μM (dF) and 5 μm (IF), respectively) which are similar to those found in rat brain synaptosomes. d- Fenfluramine (0.5 and 10 μM) also stimulates tritium release from NMB-rSERT cells preloaded with [3H-]-5-HT. The d-fenfluramine-induced [3H-15-HT release is blocked by 0.3 μM citalopram and is dependent on the density of SERT expressed per cell, but is not affected by removal of Ca++ ions from the incubation medium. Manipulation of the Na+ gradient across the plasma membrane (replacing 60 mM NaCl with an equimolar concentration of KCl or choline) also induced [3H-]5-HT release from NMB-rSERT cells, which was inhibited by 0.3 μM citalopram. These results, together with the finding that NMB rSERT cells preloaded with 500 nM unlabelled 5-HT take up [3H-]d- fenfluramine, make NMB-rSERT cells a valuable tool for studying the transporter-mediated exchange release induced by amphetamine derivatives.

Original languageEnglish
Pages (from-to)803-809
Number of pages7
JournalNeuropharmacology
Volume36
Issue number6
DOIs
Publication statusPublished - Jun 1997

Fingerprint

Fenfluramine
Serotonin Plasma Membrane Transport Proteins
Neuroblastoma
Serotonin
Citalopram
Stereoisomerism
Tritium
Synaptosomes
Amphetamine
Choline
Inhibitory Concentration 50
Plasmids
Cell Membrane
Ions
Cell Line
Brain

Keywords

  • d-fenfluramine
  • Serotonin release
  • Serotonin transporter
  • Transfected human neuroblastoma cells

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Drug Discovery
  • Pharmacology

Cite this

Carrier-mediated serotonin release induced by d-fenfluramine : Studies with human neuroblastoma cells transfected with a rat serotonin transporter. / Cinquanta, M.; Ratovitski, T.; Crespi, D.; Gobbi, M.; Mennini, T.; Simantov, R.

In: Neuropharmacology, Vol. 36, No. 6, 06.1997, p. 803-809.

Research output: Contribution to journalArticle

Cinquanta, M. ; Ratovitski, T. ; Crespi, D. ; Gobbi, M. ; Mennini, T. ; Simantov, R. / Carrier-mediated serotonin release induced by d-fenfluramine : Studies with human neuroblastoma cells transfected with a rat serotonin transporter. In: Neuropharmacology. 1997 ; Vol. 36, No. 6. pp. 803-809.
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