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Pharmaceuticals
Special Issues
Neuroactive Compounds
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Neuroactive Compounds

A special issue of Pharmaceuticals (ISSN 1424-8247).

Deadline for manuscript submissions: closed (31 December 2010) | Viewed by 23529

Special Issue Editor

Dr. Maurice Tangui

E-Mail Website
Guest Editor
INSERM U. 710, University of Montpellier 2, CEDEX 5, 34095 Montpellier, France
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Research in Neuroscience has never been so active, taking benefits from recent developments in functional imaging, molecular biology and transgenesis, or improvements in animals’ cognitive behavioral analyses. Paradoxically, validation of new therapeutic strategies and marketing of really innovative medicine against pathologies with major social issues like Alzheimer’s disease and related neurodegenerative disorders, ischemic insults, depression, or schizophrenia mark time and do not find way out in a near future. Drug development pipelines of pharmaceutical companies remain alarmingly empty.
This combined Special Issue of Molecules and Pharmaceuticals, on Neuroactive Compounds, will offer an unique forum to present the chemistry, pharmacology and therapeutic opportunities offered by new and innovative molecular series in all areas of neuropharmacology and neuroscience. I strongly encourage authors to submit papers for this special issue, within the scope of Molecules and Pharmaceuticals, and I hope that the fields covered will allow to rise our hopes in seeing soon the validation of breakthrough treatments in central pathologies of major concern.

Dr. Tangui Maurice
Guest Editor

Keywords

  • psychoactive drugs
  • neuroprotective agents
  • antidepressant
  • anxiolytics
  • anti-stress drugs
  • brain imaging tools
  • brain penetration
  • blood-brain barrier agents

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Published Papers (2 papers)

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Review

381 KiB  
Review
Neuroactive Multifunctional Tacrine Congeners with Cholinesterase, Anti-Amyloid Aggregation and Neuroprotective Properties
by Maria Kozurkova, Slavka Hamulakova, Zuzana Gazova, Helena Paulikova and Pavol Kristian
Pharmaceuticals 2011, 4(2), 382-418; https://doi.org/10.3390/ph4020382 - 18 Feb 2011
Cited by 67 | Viewed by 10996
Abstract
The review summarizes research into the highly relevant topics of cholinesterase and amyloid aggregation inhibitors connected to tacrine congeners, both of which are associated with neurogenerative diseases. Various opinions will be discussed regarding the dual binding site inhibitors which are characterized by increased [...] Read more.
The review summarizes research into the highly relevant topics of cholinesterase and amyloid aggregation inhibitors connected to tacrine congeners, both of which are associated with neurogenerative diseases. Various opinions will be discussed regarding the dual binding site inhibitors which are characterized by increased inhibitor potency against acetylcholin/butyrylcholine esterase and amyloid formation. It is suggested that these compounds can both raise levels of acetylcholine by binding to the active site, and also prevent amyloid aggregation. In connection with this problem, the mono/dual binding of the multifunctional derivatives of tacrine, their mode of action and their neuroprotective activities are reported. The influence of low molecular compounds on protein amyloid aggregation, which might be considered as a potential therapeutic strategy in the treatment of Alzheimer’s disease is also reported. Finally, attention is paid to some physico-chemical factors, such as desolvation energies describing the transfer of the substrate solvated by water, the metal-chelating properties of biometals reacting with amyloid precursor protein, amyloid beta peptide and tau protein. Full article
(This article belongs to the Special Issue Neuroactive Compounds)
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916 KiB  
Review
Nanomedicine Faces Barriers
by Paul Debbage and Gudrun C. Thurner
Pharmaceuticals 2010, 3(11), 3371-3416; https://doi.org/10.3390/ph3113371 - 28 Oct 2010
Cited by 23 | Viewed by 11936
Abstract
Targeted nanoparticles have the potential to improve drug delivery efficiencies by more than two orders of magnitude, from the ~ 0.1% which is common today. Most pharmacologically agents on the market today are small drug molecules, which diffuse across the body’s blood-tissue barriers [...] Read more.
Targeted nanoparticles have the potential to improve drug delivery efficiencies by more than two orders of magnitude, from the ~ 0.1% which is common today. Most pharmacologically agents on the market today are small drug molecules, which diffuse across the body’s blood-tissue barriers and distribute not only into the lesion, but into almost all organs. Drug actions in the non-lesion organs are an inescapable part of the drug delivery principle, causing “side-effects” which limit the maximally tolerable doses and result in inadequate therapy of many lesions. Nanoparticles only cross barriers by design, so side-effects are not built into their mode of operation. Delivery rates of almost 90% have been reported. This review examines the significance of these statements and checks how far they need qualification. What type of targeting is required? Is a single targeting sufficient? What new types of clinical challenge, such as immunogenicity, might attend the use of targeted nanoparticles? Full article
(This article belongs to the Special Issue Neuroactive Compounds)
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