Design, synthesis and in vivo evaluation of sodium 2-benzyl-chloromalonates as new central nervous system depressants

MedChemComm ◽  
2015 ◽  
Vol 6 (8) ◽  
pp. 1427-1437 ◽  
Author(s):  
Andreia Aguiar Vieira ◽  
Bruno Guimarães Marinho ◽  
Luana Gonçalves de Souza ◽  
Patricia Dias Fernandes ◽  
José D. Figueroa-Villar
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Acute Toxicity ◽  
Sleep Deprivation ◽  
High Solubility ◽  
In Vivo Evaluation ◽  
Design Synthesis ◽  
Solubility In Water ◽  
Low Levels

This work describes the design, synthesis and in vivo evaluation of new central nervous system depressing agents that show low levels of acute toxicity, high solubility in water, anxiolytic and hypnotic effects without sleep deprivation.

scholarly journals Chemical Delivery System of MIBG to the Central Nervous System: Synthesis, 11C-Radiosynthesis, and in Vivo Evaluation

2019 ◽  
Vol 10 (3) ◽  
pp. 352-357 ◽  
Author(s):  
Fabienne Gourand ◽  
Delphine Patin ◽  
Axelle Henry ◽  
Méziane Ibazizène ◽  
Martine Dhilly ◽  
...  
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Delivery System ◽  
In Vivo Evaluation ◽  
System Synthesis ◽  
Chemical Delivery System ◽  
The Central Nervous System

scholarly journals Murine Coronavirus Receptors Are Differentially Expressed in the Central Nervous System and Play Virus Strain-Dependent Roles in Neuronal Spread

2010 ◽  
Vol 84 (21) ◽  
pp. 11030-11044 ◽  
Author(s):  
Susan J. Bender ◽  
Judith M. Phillips ◽  
Erin P. Scott ◽  
Susan R. Weiss
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Demyelinating Disease ◽  
Hepatitis Virus ◽  
Cell Types ◽  
Cns Infection ◽  
The Central Nervous System ◽  
Coronavirus Infection ◽  
Low Levels

ABSTRACT Coronavirus infection of the murine central nervous system (CNS) provides a model for studies of viral encephalitis and demyelinating disease. Mouse hepatitis virus (MHV) neurotropism varies by strain: MHV-A59 causes mild encephalomyelitis and demyelination, while the highly neurovirulent strain JHM.SD (MHV-4) causes fatal encephalitis with extensive neuronal spread of virus. In addition, while neurons are the predominant CNS cell type infected in vivo, the canonical receptor for MHV, the carcinoembryonic antigen family member CEACAM1a, has been demonstrated only on endothelial cells and microglia. In order to investigate whether CEACAM1a is also expressed in other cell types, ceacam1a mRNA expression was quantified in murine tissues and primary cells. As expected, among CNS cell types, microglia expressed the highest levels of ceacam1a, but lower levels were also detected in oligodendrocytes, astrocytes, and neurons. Given the low levels of neuronal expression of ceacam1a, primary neurons from wild-type and ceacam1a knockout mice were inoculated with MHV to determine the extent to which CEACAM1a-independent infection might contribute to CNS infection. While both A59 and JHM.SD infected small numbers of ceacam1a knockout neurons, only JHM.SD spread efficiently to adjacent cells in the absence of CEACAM1a. Quantification of mRNA for the ceacam1a-related genes ceacam2 and psg16 (bCEA), which encode proposed alternative MHV receptors, revealed low ceacam2 expression in microglia and oligodendrocytes and psg16 expression exclusively in neurons; however, only CEACAM2 mediated infection in human 293T cells. Therefore, neither CEACAM2 nor PSG16 is likely to be an MHV receptor on neurons, and the mechanism for CEACAM1a-independent neuronal spread of JHM.SD remains unknown.

scholarly journals Synthesis and in vivo evaluation of 5-chloro-5-benzobarbiturates as new central nervous system depressants

2011 ◽  
Vol 22 (2) ◽  
pp. 364-371 ◽  
Author(s):  
Andreia A Vieira ◽  
Niele M Gomes ◽  
Maria E Matheus ◽  
Patricia D Fernandes ◽  
José D Figueroa-Villar
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
In Vivo Evaluation

Delivering FLT to the Central Nervous System by Means of a Promising Targeting System: Synthesis, [11C]Radiosynthesis, and in Vivo Evaluation

2017 ◽  
Vol 8 (11) ◽  
pp. 2457-2467 ◽  
Author(s):  
Fabienne Gourand ◽  
Mihaela-Liliana Ţînţaş ◽  
Axelle Henry ◽  
Méziane Ibazizène ◽  
Martine Dhilly ◽  
...  
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
In Vivo Evaluation ◽  
System Synthesis ◽  
The Central Nervous System

scholarly journals Protrudin functions as a scaffold in the endoplasmic reticulum to support axon regeneration in the adult central nervous system

2020 ◽  
Author(s):  
Veselina Petrova ◽  
Craig S. Pearson ◽  
James R. Tribble ◽  
Andrea G. Solano ◽  
Evan Reid ◽  
...  
Keyword(s):  
Central Nervous System ◽  
Endoplasmic Reticulum ◽  
Nervous System ◽  
Cortical Neurons ◽  
Binding Properties ◽  
Adult Central Nervous System ◽  
Low Levels ◽  
Cellular Components

SummaryAdult mammalian central nervous system axons have intrinsically poor regenerative capacity, so axonal injury has permanent consequences. One approach to enhancing regeneration is to increase the axonal supply of growth molecules and organelles. We achieved this by expressing the adaptor molecule Protrudin which is normally found at low levels in non-regenerative neurons. Elevated Protrudin expression enabled robust central nervous system regeneration both in vitro in primary cortical neurons and in vivo in the injured adult optic nerve. Protrudin overexpression facilitated the accumulation of endoplasmic reticulum, integrins and Rab11 endosomes in the distal axon, whilst removing Protrudin’s endoplasmic reticulum localization, kinesin-binding or phosphoinositide-binding properties abrogated the regenerative effects. These results demonstrate that Protrudin promotes regeneration by functioning as a scaffold to link axonal organelles, motors and membranes, establishing important roles for these cellular components in mediating regeneration in the adult central nervous system.

scholarly journals Protrudin functions from the endoplasmic reticulum to support axon regeneration in the adult CNS

2020 ◽  
Vol 11 (1) ◽  
Author(s):  
Veselina Petrova ◽  
Craig S. Pearson ◽  
Jared Ching ◽  
James R. Tribble ◽  
Andrea G. Solano ◽  
...  
Keyword(s):  
Central Nervous System ◽  
Endoplasmic Reticulum ◽  
Nervous System ◽  
Cortical Neurons ◽  
Binding Properties ◽  
Adaptor Molecule ◽  
Low Levels ◽  
Cellular Components

Abstract Adult mammalian central nervous system axons have intrinsically poor regenerative capacity, so axonal injury has permanent consequences. One approach to enhancing regeneration is to increase the axonal supply of growth molecules and organelles. We achieved this by expressing the adaptor molecule Protrudin which is normally found at low levels in non-regenerative neurons. Elevated Protrudin expression enabled robust central nervous system regeneration both in vitro in primary cortical neurons and in vivo in the injured adult optic nerve. Protrudin overexpression facilitated the accumulation of endoplasmic reticulum, integrins and Rab11 endosomes in the distal axon, whilst removing Protrudin’s endoplasmic reticulum localization, kinesin-binding or phosphoinositide-binding properties abrogated the regenerative effects. These results demonstrate that Protrudin promotes regeneration by functioning as a scaffold to link axonal organelles, motors and membranes, establishing important roles for these cellular components in mediating regeneration in the adult central nervous system.

Neuropharmacological Profile and Chemical Analysis of Moroccan Ormenis mixta L.

2018 ◽  
Vol 16 (S1) ◽  
pp. S55-S64
Author(s):  
G. Hajjaj ◽  
A. Bahlouli ◽  
M. Tajani ◽  
K. Alaoui ◽  
Y. Cherrah ◽  
...  
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Body Weight ◽  
Traditional Medicine ◽  
Behavioral Tests ◽  
Phytochemical Screening ◽  
Activity Profile ◽  
Acute Toxicity Study ◽  
Pharmacological Studies

Ormenis mixta L. is traditionally used for central nervous system (CNS)-related diseases. Its anti-stress properties have received attention in Moroccan traditional medicine and aromatherapy. However, no pharmacological studies have yet been undertaken on this plant in Morocco. The present study provides a preliminary phytochemical screening and psychopharmacological profile of the essential oil and aqueous extract from Ormenis mixta L. by using behavioral tests in vivo, at graded doses. The result of this research shows that Ormenis mixta L. was safe up to 2 g/kg b.w. (body weight) in the acute toxicity study, possesses potential psychostimulant effect, and has antianxiety and antidepressant-like activity. This activity profile of Ormenis mixta L. was similar to the typical psychostimulant, caffeine. The exact mechanism of action underlying this stimulant-like effect should be clarified with further detailed studies. These results explained the extensive use of Ormenis mixta L. as a traditional medicine in Morocco.

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