| Title |
Radiosynthesis and first preclinical evaluation of the novel norepinephrine transporter pet-ligand [11C]ME@HAPTHI
|
|---|---|
| Published in |
EJNMMI Research, June 2015
|
| DOI | 10.1186/s13550-015-0113-3 |
| Pubmed ID | |
| Authors |
Christina Rami-Mark, Neydher Berroterán-Infante, Cecile Philippe, Stefanie Foltin, Chrysoula Vraka, Alexander Hoepping, Rupert Lanzenberger, Marcus Hacker, Markus Mitterhauser, Wolfgang Wadsak |
| Abstract |
The norepinephrine transporter (NET) has been demonstrated to be relevant to a multitude of neurological, psychiatric and cardiovascular pathologies. Due to the wide range of possible applications for PET imaging of the NET together with the limitations of currently available radioligands, novel PET tracers for imaging of the cerebral NET with improved pharmacological and pharmacodynamic properties are needed. The present study addresses the radiosynthesis and first preclinical evaluation of the novel NET PET tracer [(11)C]Me@HAPTHI by describing its affinity, selectivity, metabolic stability, plasma free fraction, blood-brain barrier (BBB) penetration and binding behaviour in in vitro autoradiography. [(11)C]Me@HAPTHI was prepared and displayed outstanding affinity and selectivity as well as excellent in vitro metabolic stability, and it is likely to penetrate the BBB. Moreover, selective NET binding in in vitro autoradiography was observed in human brain and rat heart tissue samples. All preclinical results and radiosynthetic key-parameters indicate that the novel benzothiadiazole dioxide-based PET tracer [(11)C]Me@HAPTHI is a feasible and improved NET radioligand and might prospectively facilitate clinical NET imaging. |
X Demographics
The data shown below were collected from the profile of 1 X user who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 11 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 11 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 4 | 36% |
| Student > Master | 2 | 18% |
| Researcher | 2 | 18% |
| Professor | 1 | 9% |
| Student > Bachelor | 1 | 9% |
| Other | 1 | 9% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 3 | 27% |
| Medicine and Dentistry | 3 | 27% |
| Agricultural and Biological Sciences | 1 | 9% |
| Physics and Astronomy | 1 | 9% |
| Neuroscience | 1 | 9% |
| Other | 1 | 9% |
| Unknown | 1 | 9% |
Attention Score in Context
This research output has an Altmetric Attention Score of 4. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 23 May 2016.
All research outputs
#7,216,867
of 22,811,321 outputs
Outputs from EJNMMI Research
#131
of 556 outputs
Outputs of similar age
#86,361
of 266,634 outputs
Outputs of similar age from EJNMMI Research
#4
of 8 outputs
Altmetric has tracked 22,811,321 research outputs across all sources so far. This one has received more attention than most of these and is in the 67th percentile.
So far Altmetric has tracked 556 research outputs from this source. They receive a mean Attention Score of 2.5. This one has done well, scoring higher than 75% of its peers.
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We're also able to compare this research output to 8 others from the same source and published within six weeks on either side of this one. This one has scored higher than 4 of them.