Tags

Type your tag names separated by a space and hit enter

Antagonists and substrates differentially regulate serotonin transporter cell surface expression in serotonergic neurons.
Eur J Pharmacol. 2010 Mar 10; 629(1-3):63-7.EJ

Abstract

The serotonin transporter (SERT) terminates serotonergic neurotransmission by the rapid removal of serotonin (5-hydroxytryptamine, 5-HT) from the extracellular space back into serotonergic neurons. SERT therefore controls the concentration of extracellular 5-HT, and thus one mechanism to regulate the efficacy of serotonergic neurotransmission is via modulation of the density of SERT molecules on the cell membrane. We have studied the effects of prolonged exposure to various selective serotonin re-uptake inhibitors (SSRIs), as well as cocaine and the transport substrates 5-HT and 3,4-methylenedioxy-methamphetamine (MDMA), on SERT cell surface expression in cultured serotonergic neurons. This was achieved via quantification of the amount of cell surface-expressed SERT molecules using antibody detection combined with confocal laser scanning microscopy. Our results show that exposure to the SSRIs citalopram, fluoxetine, sertraline and paroxetine all induced SERT internalization, but with different efficacies. The substrates 5-HT and MDMA also induced SERT internalization, while cocaine elevated SERT cell surface expression.

Authors+Show Affiliations

Biochemical Laboratory, Central Institute of Mental Health, J5, 68159 Mannheim, Germany.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

20006597

Citation

Kittler, Katharina, et al. "Antagonists and Substrates Differentially Regulate Serotonin Transporter Cell Surface Expression in Serotonergic Neurons." European Journal of Pharmacology, vol. 629, no. 1-3, 2010, pp. 63-7.
Kittler K, Lau T, Schloss P. Antagonists and substrates differentially regulate serotonin transporter cell surface expression in serotonergic neurons. Eur J Pharmacol. 2010;629(1-3):63-7.
Kittler, K., Lau, T., & Schloss, P. (2010). Antagonists and substrates differentially regulate serotonin transporter cell surface expression in serotonergic neurons. European Journal of Pharmacology, 629(1-3), 63-7. https://doi.org/10.1016/j.ejphar.2009.12.010
Kittler K, Lau T, Schloss P. Antagonists and Substrates Differentially Regulate Serotonin Transporter Cell Surface Expression in Serotonergic Neurons. Eur J Pharmacol. 2010 Mar 10;629(1-3):63-7. PubMed PMID: 20006597.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Antagonists and substrates differentially regulate serotonin transporter cell surface expression in serotonergic neurons. AU - Kittler,Katharina, AU - Lau,Thorsten, AU - Schloss,Patrick, Y1 - 2009/12/16/ PY - 2009/10/19/received PY - 2009/11/19/revised PY - 2009/12/07/accepted PY - 2009/12/17/entrez PY - 2009/12/17/pubmed PY - 2010/3/31/medline SP - 63 EP - 7 JF - European journal of pharmacology JO - Eur. J. Pharmacol. VL - 629 IS - 1-3 N2 - The serotonin transporter (SERT) terminates serotonergic neurotransmission by the rapid removal of serotonin (5-hydroxytryptamine, 5-HT) from the extracellular space back into serotonergic neurons. SERT therefore controls the concentration of extracellular 5-HT, and thus one mechanism to regulate the efficacy of serotonergic neurotransmission is via modulation of the density of SERT molecules on the cell membrane. We have studied the effects of prolonged exposure to various selective serotonin re-uptake inhibitors (SSRIs), as well as cocaine and the transport substrates 5-HT and 3,4-methylenedioxy-methamphetamine (MDMA), on SERT cell surface expression in cultured serotonergic neurons. This was achieved via quantification of the amount of cell surface-expressed SERT molecules using antibody detection combined with confocal laser scanning microscopy. Our results show that exposure to the SSRIs citalopram, fluoxetine, sertraline and paroxetine all induced SERT internalization, but with different efficacies. The substrates 5-HT and MDMA also induced SERT internalization, while cocaine elevated SERT cell surface expression. SN - 1879-0712 UR - https://www.unboundmedicine.com/medline/citation/20006597/Antagonists_and_substrates_differentially_regulate_serotonin_transporter_cell_surface_expression_in_serotonergic_neurons_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0014-2999(09)01131-5 DB - PRIME DP - Unbound Medicine ER -