An Affinity‐Modulating Site on Neuronal Monoamine Transport Proteins
- 1 April 1997
- journal article
- Published by Wiley in Basic & Clinical Pharmacology & Toxicology
- Vol. 80 (4) , 197-201
- https://doi.org/10.1111/j.1600-0773.1997.tb00396.x
Abstract
The dissociation rates of [3H]nisoxetine, [3H]GBR 12935 and [3H]citalopram from, respectively, the rat brain noradrenaline, dopamine and 5‐HT transporters were found to be markedly affected by several drugs. Sertraline strongly attenuated the rate of dissociation of [3H]nisoxetine from the noradrenaline transporter, while citalopram strongly attenuated that of [3H]citalopram from the 5‐HT transporter. The effects of both drugs were stereospecific. Less potent affinity‐modulating drugs were identified with regards to [3H]GBR 12935 dissociation from the dopamine transporter. All three neuronal monoamine transporters may thus have specific affinity‐modulating sites which change the function of the transporters with possible implications for the reuptake of monoamines released during synaptic activity.Keywords
This publication has 19 references indexed in Scilit:
- Isolation and Characterization of an Endogenous Peptide from Rat Brain Interacting Specifically with the Serotonergic 1B Receptor SubtypesPublished by Elsevier ,1996
- Chronic fluoxetine treatment upregulates 5‐HT uptake sites and 5‐HT2 receptors in rat brain: An autoradiographic studySynapse, 1993
- [3H]Paroxetine binding in rat frontal cortex strongly correlates with [3H]5-HT uptake: Effect of administration of various antidepressant treatmentsNeuropharmacology, 1993
- Serotonin Receptors in the Brain of Rats Treated Chronically with Imipramine or RU24969: Support for the 5‐HT1BReceptor Being a 5‐HT AutoreceptorBasic & Clinical Pharmacology & Toxicology, 1992
- Affinity modulation of [3H]imipramine, [3H]paroxetine and [3H]citalopram binding to the 5-HT transporter from brain and plateletsEuropean Journal of Pharmacology: Molecular Pharmacology, 1991
- [3H]Citalopram Binding to Brain and Platelet Membranes of Human and RatJournal of Neurochemistry, 1991
- Inhibitory and regulatory binding sites on the rat brain serotonin transporter: molecular weight of the [3H]paroxetine and [3H]citalopram binding proteinsEuropean Journal of Pharmacology: Molecular Pharmacology, 1990
- Effect of chronic treatment with selective monoamine oxidase inhibitors and specific 5-hydroxytryptamine uptake inhibitors on [3h]paroxetine binding to cerebral cortical membranes of the ratNeuropharmacology, 1987
- Biochemical and Pharmacological Characterization of [3H]GBR 12935 Binding In Vitro to Rat Striatal Membranes: Labeling of the Dopamine Uptake ComplexJournal of Neurochemistry, 1987
- Serotonin uptake inhibitors differentially modulate high affinity imipramine dissociation in human platelet membranesLife Sciences, 1985