A heterocyclic compound CE-103 inhibits dopamine reuptake and modulates dopamine transporter and dopamine D1-D3 containing receptor complexes

@article{Sase2016AHC,
  title={A heterocyclic compound CE-103 inhibits dopamine reuptake and modulates dopamine transporter and dopamine D1-D3 containing receptor complexes},
  author={Ajinkya S. Sase and Y. D. Aher and Sivaprakasam R. Saroja and Minu Karthika Ganesan and Sunetra Sase and Marion Holy and Harald Höger and Vasiliy A. Bakulev and Gerhard F. Ecker and Thierry Langer and Harald H. Sitte and Johann Jakob Leban and Gert Lubec},
  journal={Neuropharmacology},
  year={2016},
  volume={102},
  pages={186-196}
}
A series of compounds have been reported to enhance memory via the DA system and herein a heterocyclic compound was tested for working memory (WM) enhancement. 2-((benzhydrylsulfinyl)methyl)thiazole (CE-103) was synthesized in a six-step synthesis. Binding of CE-103 to the dopamine (DAT), serotonin (SERT) and norepinephrine (NET) transporters and dopamine reuptake inhibition was tested as well as blood brain permeation and a screen for GPCR targets. 60 male Sprague Dawley rats were divided into… Expand
View on Elsevier
doi.org
12 Citations
Highly Influential Citations
1
Background Citations
1
Methods Citations
1
Results Citations
1

12 Citations

Citation Type

Citation Type

A novel heterocyclic compound targeting the dopamine transporter improves performance in the radial arm maze and modulates dopamine receptors D1-D3
TLDR
Dopamine re-uptake inhibition along with modulations in dopamine receptors are proposed as potential underlying mechanisms and CE-111 was identified as effective to improve memory performance in the RAM. Expand
A novel heterocyclic compound improves working memory in the radial arm maze and modulates the dopamine receptor D1R in frontal cortex of the Sprague-Dawley rat
TLDR
CE‐125 as a probably non‐neurotoxic compound and specific reuptake inhibitor was shown to increase performance (WMI) and modulation of the dopaminergic system is proposed as a possible mechanism of action. Expand
A daily single dose of a novel modafinil analogue CE-123 improves memory acquisition and memory retrieval
TLDR
Dopamine reuptake inhibition by CE‐123 may represent a novel and improved stimulant therapeutic for impairments of cognitive functions and enhance memory performance in a rat model. Expand
Heterocyclic Analogues of Modafinil as Novel, Atypical Dopamine Transporter Inhibitors.
TLDR
A series of compounds were showing higher activities on the DAT and a higher selectivity toward DAT versus serotonin and norepinephrine transporters than modafinil and the absence of neurotoxicity of a representative analogue may encourage further preclinical studies of the above-mentioned compounds. Expand
Structure Activity Relationships of Novel Thiazole-Based Modafinil Analogues Acting at Monoamine Transporters.
TLDR
A series of compounds based on scaffolds provided several new selective DAT inhibitors and gave valuable insights into the structure activity relationships, whereby S-configuration on both generally exerting the highest activity and selectivity on DAT. Expand
CE-123, a novel dopamine transporter inhibitor, attenuates locomotor hyperactivity and improves cognitive functions in rat model of fetal alcohol spectrum disorders
TLDR
Findings provide support that CE-123 may be a useful intervention for same of the deficits associated with neonatal ethanol exposure and inhibited the hyperactivity and ameliorated the impairment of reversal learning in alcohol-exposed rats. Expand
R-Modafinil exerts weak effects on spatial memory acquisition and dentate gyrus synaptic plasticity
TLDR
The results support the notion that LTP-like synaptic plasticity processes could be one of the factors contributing to the cognitive enhancing effects of spatial memory traces and D1R may play an important regulatory role in these processes. Expand
Decreased hippocampal homoarginine and increased nitric oxide and nitric oxide synthase levels in rats parallel training in a radial arm maze
TLDR
Findings indicate that hArg is linked to NO formation in hippocampus but not in FL and is paralleling spatial memory in the RAM. Expand
In vivo reduction of striatal D1R by RNA interference alters expression of D1R signaling-related proteins and enhances methamphetamine addiction in male rats
TLDR
It is indicated that reduced D1R expression in the DS increases vulnerability to methamphetamine addiction-like behavior, and this is accompanied by striatal alterations in the expression of DAT and D1r signaling proteins and is independent of the subcellular localization of these proteins. Expand
Aversive Learning Deficits and Depressive-Like Behaviors Are Accompanied by an Increase in Oxidative Stress in a Rat Model of Fetal Alcohol Spectrum Disorders: The Protective Effect of Rapamycin
TLDR
The results show that neonatal ethanol exposure leads to deficits in context-dependent fear learning and depressive-like behavior in adult rats that were associated with increased oxidative stress parameters in the hippocampus and prefrontal cortex, which suggests its usefulness as a preventive therapy in disorders connected with prenatal ethanol exposure. Expand
...
1
2
...

References

SHOWING 1-10 OF 79 REFERENCES
Salvinorin A regulates dopamine transporter function via a kappa opioid receptor and ERK1/2-dependent mechanism
TLDR
Co-immunoprecipitation and BRET studies revealed that DAT and KOR exist in a complex and SalA exposure caused a rapid and significant increase of the FRET signal, suggesting that the formation of KOR and DAT complexes is promoted in response to KOR activation. Expand
Powerful Cocaine-Like Actions of 3,4-Methylenedioxypyrovalerone (MDPV), a Principal Constituent of Psychoactive ‘Bath Salts’ Products
TLDR
The data show that MDPV is a monoamine transporter blocker with increased potency and selectivity for catecholamines when compared with cocaine, and may provide a mechanism to explain the adverse effects observed in humans taking high doses of ‘bath salts’ preparations. Expand
A selective dopamine reuptake inhibitor improves prefrontal cortex-dependent cognitive function: Potential relevance to attention deficit hyperactivity disorder
TLDR
Observations suggest that benztropine analogs may be efficacious in the treatment of ADHD or other disorders associated with PFC dysfunction, and provide a strong rationale for future research focused on the neural mechanisms contributing to the cognition-enhancing actions and the potential clinical utility of AHN 2-005 and related compounds. Expand
Ventral hippocampal dopamine D1 and D2 systems and spatial working memory in rats
TLDR
Clear evidence is provided that hippocampal D2 activity is positively related to working memory performance, while evidence for D1 systems is less compelling. Expand
Memory facilitation produced by dopamine agonists: Role of receptor subtype and mnemonic requirements
TLDR
The results suggest that the memory-improving properties of DA agonists on tasks sensitive to both hippocampal and caudate lesions are mediated by the D2 receptor. Expand
Regulation of Dopamine Transporter Function and Cell Surface Expression by D3 Dopamine Receptors*
TLDR
It is demonstrated that D3 receptors regulate dopamine transporter function and a novel mechanism by which D3 receptor regulate extracellular dopamine concentrations is identified. Expand
Strain differences in the distribution of dopamine transporter sites in rat brain
TLDR
Differences in the density and distribution of DAT sites in WKY rats may lead to altered modulation of synaptic DA levels in the cell body and mesolimbic regions, thereby contributing to the noted depression-like behaviors reported in this rat strain. Expand
The N Terminus of Monoamine Transporters Is a Lever Required for the Action of Amphetamines*
TLDR
It is concluded that the N terminus of monoamine transporters acts as a lever that sustains reverse transport. Expand
Performance- and task-dependent effects of the dopamine D1/D5 receptor agonist SKF 38393 on learning and memory in the rat.
TLDR
The results suggest that dopamine D(1)/D(5) receptor activation has performance- and task-dependent effects on cognitive function. Expand
Dose-dependent effects of the dopamine D1 receptor agonists A77636 or SKF81297 on spatial working memory in aged monkeys.
  • J. Cai, A. Arnsten
  • Psychology, Medicine
  • The Journal of pharmacology and experimental therapeutics
  • 1997
TLDR
The selective dopamine D1 receptor full agonists A77636 and SKF81297 were examined in aged monkeys for effects on the working memory functions of the PFC and the improvement and impairment in performance were reversed by pretreatment with the D1 receptors antagonist, SCH23390. Expand
...
1
2
3
4
5
...