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Literature DB >> 9140140

An affinity-modulating site on neuronal monoamine transport proteins.

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 effect 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 implication for the reuptake of monoamines released during synaptic activity.

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Year: 1997 PMID： 9140140 DOI： 10.1111/j.1600-0773.1997.tb00396.x

Source DB: PubMed Journal: Pharmacol Toxicol ISSN： 0901-9928

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Cited

13 in total

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4. Steric hindrance mutagenesis in the conserved extracellular vestibule impedes allosteric binding of antidepressants to the serotonin transporter.

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6. Rapid and sustained antidepressant properties of an NMDA antagonist/monoamine reuptake inhibitor identified via transporter-based virtual screening.

Authors: Jeffery N Talbot; Laura M Geffert; Jessica E Jorvig; Ruben I Goldstein; Cienna L Nielsen; Nicholas E Wolters; Mary Ellen Amos; Caitlin A Munro; Elizabeth Dallman; Maddalena Mereu; Gianluigi Tanda; Jonathan L Katz; Martín Indarte; Jeffry D Madura; Hailey Choi; Rehana K Leak; Christopher K Surratt
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Review 10. Discovery of novel-scaffold monoamine transporter ligands via in silico screening with the S1 pocket of the serotonin transporter.

Authors: Tammy L Nolan; Laura M Geffert; Benedict J Kolber; Jeffry D Madura; Christopher K Surratt
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