Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 7 of 7 for “"GBR 12909"”.
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Synthesis and Biological Evaluation of Novel GBR 12909 Tropane and Azetidine Hybrid Analogues
… affinity, selective dopamine transporter ligand GBR 12909 has served as a template for the design of two novel classes of dopamine transporter ligands. A series of 3-[2- (diarylmethoxyethyidenyl)]-N-substituted tropane derivatives were synthesized and the binding affinities of these compounds …
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Modeling of flexible drug-like molecules : qsar of GBR 12909 analog dat/sert selectivity
The dopamine reuptake inhibitor GBR 12909 and related dialkyl piperazine and piperidine analogs have been studied as agonist substitution therapies acting on the dopamine transporter (DAT) to treat cocaine addiction. Undesirable binding to the serotonin transporter (SERT) can vary greatly depending …
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Ligand-based drug design : I. conformational studies of GBR 12909 analogs as cocaine antagonists; II. 3d-QSAR studies of salvinorin a analogs as kappa opioid agonists
… of the flexible dopamine reuptake inhibitor, GBR 12909, may have potential usefulness in the treatment of cocaine abuse. As a first step in the 3D-QSAR modeling of the dopamine transporter (DAT)/serotonin transporter (SERT) selectivity of these compounds, conformational analysis of a …
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Analysis of molecular conformations using relative planes
… the conformations of DM324, a flexible analog of GBR 12909, a drug potentially useful in the treatment of cocaine abuse. The present work suggests that the Planes program could be potentially useful in the description of the relative orientation of pharmacophore features if the molecular …
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Ligand-based design of dopamine reuptake inhibitors : fuzzy relational clustering and 2-D and 3-D QSAR modleing
… large collection of conformations of a flexible GBR 12909 analogue was demonstrated by cluster analysis. Novel structurebased features that can be easily generalized to other molecules were developed and used for clustering. Since the feature space may or may not be Euclidean, a …
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Dopamine Transporter (DAT) and Metabotropic Glutamate Receptor 5 (MGLU5) Irreversible Probes for Identifying Anti-Psychostimulant Therapeutics
… Under the first aim, methylphenidate (MP) and GBR-12909 as non-tropane DAT inhibitors were structurally modified to contain a photoreactive group (e.g., aryl azide, benzophenone) and a tag (e.g., 125I, terminal alkyne, aliphatic azide). These compounds were then subjected to DAT pharmacological …
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Molecular Characterization of Dopamine Transporter Phosphorylation and Regulation
… stimulated DAT phosphorylation and DA transport. GBR 12909 suppressed PMA-induced DAT phosphorylation and internalization. Treatment with DA did not affect DAT phosphorylation while inducing PKC mediated DA transport down regulation. These results provide information on the potential for …