| Carrier-mediated serotonin release induced by d-fenfluramine: studies with human neuroblastoma cells transfected with a rat serotonin transporter. | |
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MedLine Citation:
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PMID: 9225308 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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M Cinquanta; T Ratovitski; D Crespi; M Gobbi; T Mennini; R Simantov |
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Publication Detail:
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Type: In Vitro; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Neuropharmacology Volume: 36 ISSN: 0028-3908 ISO Abbreviation: Neuropharmacology Publication Date: 1997 Jun |
Date Detail:
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Created Date: 1997-08-18 Completed Date: 1997-08-18 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 0236217 Medline TA: Neuropharmacology Country: ENGLAND |
Other Details:
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Languages: eng Pagination: 803-9 Citation Subset: IM |
Affiliation:
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Istituto di Ricerche Farmacologiche Mario Negri, Milan, Italy. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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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:
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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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