scholarly journals PE2I: A Radiopharmaceutical for In vivo Exploration of the Dopamine Transporter

2008 ◽  
Vol 14 (1) ◽  
pp. 47-64 ◽  
Author(s):  
Patrick Emond ◽  
Denis Guilloteau ◽  
Sylvie Chalon
Keyword(s):  
1999 ◽  
Vol 26 (8) ◽  
pp. 897-903 ◽  
Author(s):  
David Stout ◽  
Andrej Petric ◽  
N. Satyamurthy ◽  
Quan Nguyen ◽  
Sung-Cheng Huang ◽  
...  
Keyword(s):  

2012 ◽  
Vol 224 (2) ◽  
pp. 337-345 ◽  
Author(s):  
Marcelo Q. Hoexter ◽  
Gustavo Fadel ◽  
André C. Felício ◽  
Mariana B. Calzavara ◽  
Ilza R. Batista ◽  
...  

2009 ◽  
Vol 19 (16) ◽  
pp. 4843-4845 ◽  
Author(s):  
Magnus Schou ◽  
Carsten Steiger ◽  
Andrea Varrone ◽  
Denis Guilloteau ◽  
Christer Halldin

Synapse ◽  
1997 ◽  
Vol 26 (1) ◽  
pp. 72-80 ◽  
Author(s):  
Patrick Emond ◽  
Sylvie Chalon ◽  
Lucette Garreau ◽  
Anne-Marie Dognon ◽  
Sylvie Bodard ◽  
...  
Keyword(s):  

2021 ◽  
Author(s):  
Marco Niello ◽  
Spyridon Sideromenos ◽  
Ralph Gradisch ◽  
Ronan O'Shea ◽  
Jakob Schwazer ◽  
...  

Abstract α-Pyrrolidinovalerophenone (αPVP) is a psychostimulant and drug of abuse associated with severe intoxications in humans. αPVP exerts long-lasting psychostimulant effects, when compared to the classical dopamine transporter (DAT) inhibitor cocaine. Here, we compared the two enantiomeric forms of αPVP, the R- and the S-αPVP, with cocaine using a combination of in silico, in vitro and in vivo approaches. We found that αPVP enantiomers substantially differ from cocaine in their binding kinetics. The two enantiomers differ from each other in their association rates. However, they show similar slow dissociation rates leading to pseudo-irreversible binding kinetics at DAT. The pseudo-irreversible binding kinetics of αPVP is responsible for the observed non-competitive pharmacology and it correlates with persistent psychostimulant effects in mice. Thus, the slow binding kinetics of αPVP enantiomers profoundly differ from the fast kinetics of cocaine both in vitro and in vivo, suggesting drug-binding kinetics as a potential driver of psychostimulant effects in vivo.


2020 ◽  
Vol 8 (5) ◽  
pp. 349-356
Author(s):  
Vera S. Kerstens ◽  
A. Varrone

Abstract Purpose The dopamine transporter (DAT) serves as biomarker for parkinsonian syndromes. DAT can be measured in vivo with single-photon emission computed tomography (SPECT) and positron emission tomography (PET). DAT-SPECT is the current clinical molecular imaging standard. However, PET has advantages over SPECT measurements, and PET radioligands with the necessary properties for clinical applications are on the rise. Therefore, it is time to review the role of DAT imaging with SPECT compared to PET. Methods PubMed and Web of Science were searched for relevant literature of the previous 10 years. Four topics for comparison were used: diagnostic accuracy, quantitative accuracy, logistics, and flexibility. Results There are a few studies directly comparing DAT-PET and DAT-SPECT. PET and SPECT both perform well in discriminating neurodegenerative from non-neurodegenerative parkinsonism. Clinical DAT-PET imaging seems feasible only recently, thanks to simplified DAT assessments and better availability of PET radioligands and systems. The higher resolution of PET makes more comprehensive assessments of disease progression in the basal ganglia possible. Additionally, it has the possibility of multimodal target assessment. Conclusion DAT-SPECT is established for differentiating degenerative from non-degenerative parkinsonism. For further differentiation within neurodegenerative Parkinsonian syndromes, DAT-PET has essential benefits. Nowadays, because of wider availability of PET systems and radioligand production centers, and the possibility to use simplified quantification methods, DAT-PET imaging is feasible for clinical use. Therefore, DAT-PET needs to be considered for a more active role in the clinic to take a step forward to a more comprehensive understanding and assessment of Parkinson’s disease.


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