Document Detail


Carrier-mediated serotonin release induced by d-fenfluramine: studies with human neuroblastoma cells transfected with a rat serotonin transporter.
MedLine Citation:
PMID:  9225308     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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 (1 nM. 0.5 microM (dF) and and 5 microM (IF), respectively) which are similar to those found in rat brain synaptosomes. d-Fenfluramine (0.5 and 10 microM) also stimulates tritium release from NMB-rSERT cells preloaded with [3H-]-5-HT. The d-fenfluramine-induced [3H-]5-HT release is blocked by 0.3 microM 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 microM 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.
Authors:
M Cinquanta; T Ratovitski; D Crespi; M Gobbi; T Mennini; R Simantov
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Publication Detail:
Type:  In Vitro; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Neuropharmacology     Volume:  36     ISSN:  0028-3908     ISO Abbreviation:  Neuropharmacology     Publication Date:  1997 Jun 
Date Detail:
Created Date:  1997-08-18     Completed Date:  1997-08-18     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0236217     Medline TA:  Neuropharmacology     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  803-9     Citation Subset:  IM    
Affiliation:
Istituto di Ricerche Farmacologiche Mario Negri, Milan, Italy.
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MeSH Terms
Descriptor/Qualifier:
Animals
Calcium / pharmacology
Carrier Proteins / genetics*
Citalopram / pharmacology
Fenfluramine / pharmacology*
Humans
Membrane Glycoproteins / genetics*
Membrane Transport Proteins*
Nerve Tissue Proteins*
Neuroblastoma / genetics,  metabolism*
Potassium / pharmacology
Rats
Serotonin / metabolism*
Serotonin Plasma Membrane Transport Proteins
Serotonin Uptake Inhibitors / pharmacology*
Transfection
Tumor Cells, Cultured
Chemical
Reg. No./Substance:
0/Carrier Proteins; 0/Membrane Glycoproteins; 0/Membrane Transport Proteins; 0/Nerve Tissue Proteins; 0/SLC6A4 protein, human; 0/Serotonin Plasma Membrane Transport Proteins; 0/Serotonin Uptake Inhibitors; 0/Slc6a4 protein, rat; 458-24-2/Fenfluramine; 50-67-9/Serotonin; 59729-33-8/Citalopram; 7440-09-7/Potassium; 7440-70-2/Calcium

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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