scholarly journals Novel and High Affinity Fluorescent Ligands for the Serotonin Transporter Based on (S)-Citalopram

2014 ◽  
Vol 5 (6) ◽  
pp. 696-699 ◽  
Author(s):  
Vivek Kumar ◽  
Troels Rahbek-Clemmensen ◽  
Christian B. Billesbølle ◽  
Trine Nygaard Jorgensen ◽  
Ulrik Gether ◽  
...  
Keyword(s):  
Serotonin Transporter ◽  
High Affinity ◽  
Fluorescent Ligands

3β-(4-Ethyl-3-iodophenyl)nortropane-2β- carboxylic Acid Methyl Ester as a High-Affinity Selective Ligand for the Serotonin Transporter

1997 ◽  
Vol 40 (24) ◽  
pp. 3861-3864 ◽  
Author(s):  
Bruce E. Blough ◽  
Philip Abraham ◽  
Andrew C. Mills ◽  
Anita H. Lewin ◽  
John W. Boja ◽  
...  
Keyword(s):  
Carboxylic Acid ◽  
Methyl Ester ◽  
Serotonin Transporter ◽  
Acid Methyl Ester ◽  
High Affinity ◽  
Acid Methyl ◽  
Selective Ligand

Structural Studies on McN-5652-X (I), a High-Affinity Ligand for the Serotonin Transporter in Mammalian Brain.

ChemInform ◽  
2003 ◽  
Vol 34 (36) ◽  
Author(s):  
Bruce E. Maryanoff ◽  
David F. McComsey ◽  
Rina K. Dukor ◽  
Laurence A. Nafie ◽  
Teresa B. Freedman ◽  
...  
Keyword(s):  
Serotonin Transporter ◽  
Mammalian Brain ◽  
Structural Studies ◽  
High Affinity ◽  
Affinity Ligand ◽  
High Affinity Ligand

scholarly journals The mechanism of a high-affinity allosteric inhibitor of the serotonin transporter

2020 ◽  
Vol 11 (1) ◽  
Author(s):  
Per Plenge ◽  
Ara M. Abramyan ◽  
Gunnar Sørensen ◽  
Arne Mørk ◽  
Pia Weikop ◽  
...  
Keyword(s):  
Serotonin Transporter ◽  
High Affinity ◽  
Allosteric Inhibitor

Structural studies on McN-5652-X, a high-affinity ligand for the serotonin transporter in mammalian brain

2003 ◽  
Vol 11 (11) ◽  
pp. 2463-2470 ◽  
Author(s):  
Bruce E Maryanoff ◽  
David F McComsey ◽  
Rina K Dukor ◽  
Laurence A Nafie ◽  
Teresa B Freedman ◽  
...  
Keyword(s):  
Serotonin Transporter ◽  
Mammalian Brain ◽  
Structural Studies ◽  
High Affinity ◽  
Affinity Ligand ◽  
High Affinity Ligand

scholarly journals Transgenic elimination of high-affinity antidepressant and cocaine sensitivity in the presynaptic serotonin transporter

2011 ◽  
Vol 108 (9) ◽  
pp. 3785-3790 ◽  
Author(s):  
Brent J. Thompson ◽  
Tammy Jessen ◽  
L. K. Henry ◽  
Julie R. Field ◽  
Karen L. Gamble ◽  
...  
Keyword(s):  
Serotonin Transporter ◽  
High Affinity

Characterization of Novel Fluorescent Ligands with High Affinity for D1and D2Dopaminergic Receptors

1989 ◽  
Vol 52 (5) ◽  
pp. 1641-1644 ◽  
Author(s):  
Frederick J. Monsma ◽  
Anne C. Barton ◽  
Hee Chol Kang ◽  
Diana L. Brassard ◽  
Richard P. Haugland ◽  
...  
Keyword(s):  
High Affinity ◽  
Fluorescent Ligands

scholarly journals A Dualistic Conformational Response to Substrate Binding in the Human Serotonin Transporter Reveals a High Affinity State for Serotonin

2015 ◽  
Vol 290 (12) ◽  
pp. 7747-7755 ◽  
Author(s):  
Henriette Bjerregaard ◽  
Kasper Severinsen ◽  
Saida Said ◽  
Ove Wiborg ◽  
Steffen Sinning
Keyword(s):  
Serotonin Transporter ◽  
Substrate Binding ◽  
High Affinity

High-affinity paroxetine binding to the human placental serotonin transporter

1990 ◽  
Vol 259 (2) ◽  
pp. C196-C204 ◽  
Author(s):  
D. R. Cool ◽  
F. H. Leibach ◽  
V. Ganapathy
Keyword(s):  
Serotonin Transporter ◽  
Brush Border ◽  
Brush Border Membrane ◽  
Binding Capacity ◽  
Membrane Vesicles ◽  
Dependent Manner ◽  
High Affinity ◽  
Paroxetine Binding ◽  
Dose Dependent ◽  
Dissociation Constant Kd

We investigated the interaction of paroxetine, a nontricyclic antidepressant, with the serotonin transporter of the human placental brush-border membrane. Paroxetine bound to the purified placental brush-border membranes with a high affinity [dissociation constant (Kd) = 72 pM]. The maximal binding capacity (Bmax) was 3.9 pmol/mg protein. Imipramine, desipramine, and serotonin inhibited the binding in a dose-dependent manner with inhibition constant (Ki) values of 4.4 nM, 48.7 nM, and 1.77 microM, respectively, whereas reserpine, ketanserin, and 5-hydroxytryptophan did not have any effect. Imipramine and serotonin inhibited paroxetine binding by increasing the Kd with essentially no effect on Bmax. Binding of paroxetine to the membranes increased hyperbolically with increasing concentrations of Na+ in the assay medium. Cl- had little effect on the binding. The effect of Na+ was primarily to increase the affinity of the transporter for paroxetine with no effect on Bmax. The association constant (Ka) increased hyperbolically as the concentration of Na+ increased, indicating a 1Na+:1paroxetine stoichiometry. The maximal value for Ka was 12.1 +/- 2.5 x 10(12) M-1, and Kd for Na+ was 10.0 +/- 3.5 mM. Treatment of the membranes with tyrosyl group-specific reagents reduced the Na(+)-dependent binding, suggesting the involvement of tyrosyl residues in the binding process. This inhibition was, however, significantly reduced when treatment with the reagent was performed in the presence of Na+, suggesting that the reactive tyrosyl residues were located at or near the Na(+)-binding site. Paroxetine inhibited NaCl gradient-dependent serotonin uptake in placental brush-border membrane vesicles both at pH 6.5 and 7.5.(ABSTRACT TRUNCATED AT 250 WORDS)

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