Study of influence of the glutamatergic concentration of [18F]FPEB binding to metabotropic glutamate receptor subtype 5 with N-acetylcysteine challenge in rats and SRM/PET study in human healthy volunteers

Dupont, Anne-Claire; Sérrière, Sophie; Barantin, Laurent; Vercouillie, Johnny; Tauber, Clovis; Gissot, Valérie; Bodard, Sylvie; Chicheri, Gabrielle; Chalon, Sylvie; Bonnet‐Brilhault, Frédérique; Santiago-Ribeiro, Pr Maria-Joao; Arlicot, Nicolas

doi:10.1038/s41398-020-01152-2

Cited by 8 publications

(5 citation statements)

References 56 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Another mGluR5 imaging agent, [ 18 F]FPEB, was discovered in preclinical research to have promising imaging characteristics for progression in human trials. Additional research revealed that [ 18 F]FPEB retained in the human brain followed a pattern similar to that of [ 11 C]ABP68 (Dupont et al, 2021). According to research, [ 11 C]ABP‐688 is recommended for drug challenge experiments aiming to describe glutamate neurotransmission, as [ 18 F]FPEB binding was found to be less responsive to rises in extracellular glutamate generated by ketamine injection.…”

Section: Methodsmentioning

confidence: 82%

Evaluation of advanced, pathophysiologic new targets for imaging of CNS

Singh

Srivastava

et al. 2023

Drug Development Research

View full text Add to dashboard Cite

The inadequate information about the in vivo pathological, physiological, and neurological impairments, as well as the absence of in vivo tools for assessing brain penetrance and the efficiency of newly designed drugs, has hampered the development of new techniques for the treatment for variety of new central nervous system (CNS) diseases. The searching sites such as Science Direct and PubMed were used to find out the numerous distinct tracers across 16 CNS targets including tau, synaptic vesicle glycoprotein, the adenosine 2A receptor, the phosphodiesterase enzyme PDE10A, and the purinoceptor, among others. Among the most encouraging are [ 18 F]FIMX for mGluR imaging, [ 11 C]Martinostat for Histone deacetylase, [ 18 F]MNI-444 for adenosine 2A imaging, [ 11 C]ER176 for translocator protein, and [ 18 F]MK-6240 for tau imaging. We also reviewed the findings for each tracer's features and potential for application in CNS pathophysiology and therapeutic evaluation investigations, including target specificity, binding efficacy, and pharmacokinetic factors. This review aims to present a current evaluation of modern positron emission tomography tracers for CNS targets, with a focus on recent advances for targets that have newly emerged for imaging in humans.

show abstract

Section: Methodsmentioning

confidence: 82%

Evaluation of advanced, pathophysiologic new targets for imaging of CNS

Singh

Srivastava

et al. 2023

Drug Development Research

View full text Add to dashboard Cite

show abstract

“…We may associate this effect with different mechanisms in previous studies on NAC [11,13,[32][33][34]. One of the prominent mechanisms in the occurrence of the anticonvulsant effect of NAC is the modulation of glutaminergic neurotransmission [8, 12,35]. It has been shown by previous studies that NAC participates in the function of maintaining extrasynaptic non-vesicular glutamate homeostasis.…”

Section: Discussionmentioning

confidence: 89%

N-acetyl cysteine: A new look at its effect on PTZ-induced convulsions

et al. 2023

View full text Add to dashboard Cite

Section: Discussionmentioning

confidence: 89%

N-acetyl cysteine: A new look at its effect on PTZ-induced convulsions

Egilmez

Pazarlar

Erdoğan

et al. 2022

Preprint

View full text Add to dashboard Cite

Introduction /Aim: Epilepsy is still widely investigated as a common neurological disease requiring pharmacologically effective agents. N-acetyl cysteine (NAC), the acetyl derivative of cysteine, has become a remarkable molecule with its role in both antioxidant and glutaminergic modulation. There are many points and processes waiting to be revealed regarding the role of NAC in epilepsy. Materials and Methods In this study, pentylenetetrazole (PTZ) was administrated to induce seizures. 30 minutes before the seizure-induced procedure, N-acetyl cysteine (NAC) was administered by intraperitoneally at doses of 300 and 600 mg/kg as pretreatment. There are 2 groups designed independently of each other with PTZ doses applied at different doses. These groups were formed in such a way that we evaluated the spike percentage with electroencephalography following 35 mg/kg PTZ, and behavioral observation following 70 mg/kg PTZ. As a biochemical analysis, malondialdehyde (MDA) which is an indicator of lipid peroxidation, was evaluated and superoxide dismutase (SOD) enzyme level was analyzed. Results There was a dose-dependent reduction in seizure stage and prolonged onset time of the first myoclonic jerk in rats with N-acetylcysteine pretreatment. EEG recordings resulted in a dose-dependent decrease in spike percentages. Both doses improved MDA and SOD levels, further the results indicate that the higher dose of NAC (600 mg/kg) was more effective. Conclusion In the light of all our findings, we can report that N-acetyl cysteine has been shown to be promising with its reducing effect on convulsions. In line with these results, it is obvious that it has a beneficial effect by preventing oxidative stress. Detailed and comparative studies are needed on the convulsion-reducing effect of N acetyl cysteine in epilepsy.

show abstract

Study of influence of the glutamatergic concentration of [18F]FPEB binding to metabotropic glutamate receptor subtype 5 with N-acetylcysteine challenge in rats and SRM/PET study in human healthy volunteers

Cited by 8 publications

References 56 publications

Evaluation of advanced, pathophysiologic new targets for imaging of CNS

Evaluation of advanced, pathophysiologic new targets for imaging of CNS

N-acetyl cysteine: A new look at its effect on PTZ-induced convulsions

N-acetyl cysteine: A new look at its effect on PTZ-induced convulsions

Contact Info

Product

Resources

About