Noradrenaline dopamine-reuptake inhibitors

2012 ◽  
pp. 58-66
Author(s):  
Peter Silverstone
Keyword(s):  
Dopamine Reuptake

Effects of dopamine reuptake inhibitors on food- and cocaine-maintained responding: I. Dependence on unit dose of cocaine.

1995 ◽  
Vol 3 (3) ◽  
pp. 219-231 ◽  
Author(s):  
John R. Glowa ◽  
Francis H. E. Wojnicki ◽  
Dorota Matecka ◽  
John D. Bacher ◽  
Robert S. Mansbach ◽  
...  
Keyword(s):  
Dopamine Reuptake ◽  
Unit Dose

scholarly journals Thermostabilization and purification of the human dopamine transporter (hDAT) in an inhibitor and allosteric ligand bound conformation

2018 ◽  
Author(s):  
Vikas Navratna ◽  
Dilip K. Tosh ◽  
Kenneth A. Jacobson ◽  
Eric Gouaux
Keyword(s):  
Dopamine Transporter ◽  
Limiting Factor ◽  
Molecular Architecture ◽  
Secondary Active Transport ◽  
Reward Seeking ◽  
Dopamine Reuptake ◽  
Seeking Behavior ◽  
Chemical Messenger ◽  
Hormonal Release ◽  
Detergent Micelles

AbstractThe human dopamine transporter(hDAT) plays a major role in dopamine homeostasis and regulation of neurotransmission by clearing dopamine from the extracellular space using secondary active transport. Dopamine is an essential monoamine chemical messenger that regulates reward seeking behavior, motor control, hormonal release, and emotional response in humans. Psychostimulants such as cocaine primarily target the central binding site of hDAT and lock the transporter in an outward-facing conformation, thereby inhibiting dopamine reuptake. The inhibition of dopamine reuptake leads to accumulation of dopamine in the synapse causing heightened signaling. In addition, hDAT is implicated in various neurological disorders and disease-associated neurodegeneration. Despite its significance, the molecular architecture of hDAT and its various conformational states are poorly understood. Instability of hDAT in detergent micelles has been a limiting factor in its successful biochemical, biophysical, and structural characterization. To overcome this hurdle, first we identified ligands that stabilize hDAT in detergent micelles. Then, we screened ∼200 single residue mutants of hDAT using high-throughput scintillation proximity assay, and identified a thermostable variant(I248Y). Here we report a robust strategy to overexpress and successfully purify a thermostable variant of hDAT in an inhibitor and allosteric ligand bound conformation.

scholarly journals Prolonged High Fat Diet Reduces Dopamine Reuptake without Altering DAT Gene Expression

PLoS ONE ◽  
2013 ◽  
Vol 8 (3) ◽  
pp. e58251 ◽  
Author(s):  
Jackson J. Cone ◽  
Elena H. Chartoff ◽  
David N. Potter ◽  
Stephanie R. Ebner ◽  
Mitchell F. Roitman
Keyword(s):  
Gene Expression ◽  
High Fat Diet ◽  
High Fat ◽  
Dopamine Reuptake

Melatonin receptors limit dopamine reuptake by regulating dopamine transporter cell-surface exposure

2018 ◽  
Vol 75 (23) ◽  
pp. 4357-4370 ◽  
Author(s):  
Abla Benleulmi-Chaachoua ◽  
Alan Hegron ◽  
Marine Le Boulch ◽  
Angeliki Karamitri ◽  
Marta Wierzbicka ◽  
...  
Keyword(s):  
Cell Surface ◽  
Dopamine Transporter ◽  
Melatonin Receptors ◽  
Dopamine Reuptake

Singular value decomposition of torsional angles of analogs of the dopamine reuptake inhibitor GBR 12909

2006 ◽  
Vol 27 (5) ◽  
pp. 609-620 ◽  
Author(s):  
Anna Fiorentino ◽  
Deepangi Pandit ◽  
Kathleen M. Gilbert ◽  
Milind Misra ◽  
Rose Dios ◽  
...  
Keyword(s):  
Singular Value Decomposition ◽  
Reuptake Inhibitor ◽  
Singular Value ◽  
Gbr 12909 ◽  
Dopamine Reuptake ◽  
Dopamine Reuptake Inhibitor ◽  
Value Decomposition ◽  
Torsional Angles

scholarly journals Temporal Expression of Mutant LRRK2 in Adult Rats Impairs Dopamine Reuptake

2011 ◽  
Vol 7 (6) ◽  
pp. 753-761 ◽  
Author(s):  
Hongxia Zhou ◽  
Cao Huang ◽  
Jianbin Tong ◽  
Weimin C Hong ◽  
Yong-Jian Liu ◽  
...  
Keyword(s):  
Temporal Expression ◽  
Adult Rats ◽  
Dopamine Reuptake ◽  
Mutant Lrrk2

scholarly journals Electrophysiology and Behavioral Assessment of the New Molecule SMe1EC2M3 as a Representative of the Future Class of Triple Reuptake Inhibitors

Molecules ◽  
2019 ◽  
Vol 24 (23) ◽  
pp. 4218 ◽  
Author(s):  
Koprdova ◽  
Csatlosova ◽  
Durisova ◽  
Bogi ◽  
Majekova ◽  
...  
Keyword(s):  
Forced Swim Test ◽  
Behavioral Assessment ◽  
Dopamine Neurons ◽  
Neuroleptic Drug ◽  
Swim Test ◽  
Forced Swim ◽  
Reuptake Inhibition ◽  
Immobility Time ◽  
Dopamine Reuptake

SMe1EC2M3 is a pyridoindole derivative related to the neuroleptic drug carbidine. Based on the structural similarities of SMe1EC2M3 and known serotonin (5-HT), norepinephrine, and dopamine reuptake inhibitors, we hypothesized that this compound may also have triple reuptake inhibition efficacy and an antidepressant-like effect. PreADMET and Dragon software was used for in silico prediction of pharmacokinetics and pharmacodynamics of SMe1EC2M3. Forced swim test was used to evaluate its antidepressant-like effects. Extracellular in vivo electrophysiology was used to assess 5-HT, norepinephrine, and dopamine reuptake inhibition efficacy of SMe1EC2M3. PreADMET predicted reasonable intestinal absorption, plasma protein binding, and blood-brain permeability for SMe1EC2M3. Dragon forecasted its efficiency as an antidepressant. Using behavioral measurements, it was found that SMe1EC2M3 decreased immobility time and increase swimming time during the forced swim test (FST). Electrophysiological investigations showed that SMe1EC2M3 dose-dependently suppressed the excitability of 5-HT neurons of the dorsal raphe nucleus (DRN), norepinephrine neurons of the locus coeruleus (LC), and dopamine neurons of the ventral tegmental area (VTA). The SMe1EC2M3-induced suppression of 5-HT, norepinephrine, and dopamine neurons was reversed by the antagonists of serotonin-1A (5-HT1A; WAY100135), α-2 adrenergic (α2, yohimbine), and dopamine-2 receptors (D2, haloperidol), respectively. We conclude that SMe1EC2M3 is prospective triple 5-HT, norepinephrine, and dopamine reuptake inhibitor with antidepressant-like properties, however future studies should be performed to complete the pharmacological profiling of this compound.

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