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X Demographics
Mendeley readers
Attention Score in Context
| Title |
In Vitro Functional Characterization of GET73 as Possible Negative Allosteric Modulator of Metabotropic Glutamate Receptor 5
|
|---|---|
| Published in |
Frontiers in Pharmacology, April 2018
|
| DOI | 10.3389/fphar.2018.00327 |
| Pubmed ID | |
| Authors |
Sarah Beggiato, Andrea C. Borelli, Maria C. Tomasini, M. Paola Castelli, Nicholas Pintori, Roberto Cacciaglia, Antonella Loche, Luca Ferraro |
| Abstract |
The present study was aimed to further characterize the pharmacological profile of N-[4-(trifluoromethyl) benzyl]-4-methoxybutyramide (GET73), a putative negative allosteric modulator (NAM) of metabotropic glutamate subtype 5 receptor (mGluR5) under development as a novel medication for the treatment of alcohol dependence. This aim has been accomplished by means of a series of in vitro functional assays. These assays include the measure of several down-stream signaling [intracellular Ca++ levels, inositol phosphate (IP) formation and CREB phosphorylation (pCREB)] which are generally affected by mGluR5 ligands. In particular, GET73 (0.1 nM-10 μM) was explored for its ability to displace the concentration-response curve of some mGluR5 agonists/probes (glutamate, L-quisqualate, CHPG) in different native preparations. GET73 produced a rightward shift of concentration-response curves of glutamate- and CHPG-induced intracellular Ca++ levels in primary cultures of rat cortical astrocytes. The compound also induced a rightward shift of concentration response curve of glutamate- and L-quisqualate-induced increase in IP turnover in rat hippocampus slices, along with a reduction of CHPG (10 mM)-induced increase in IP formation. Moreover, GET73 produced a rightward shift of concentration-response curve of glutamate-, CHPG- and L-quisqualate-induced pCREB levels in rat cerebral cortex neurons. Although the engagement of other targets cannot be definitively ruled out, these data support the view that GET73 acts as an mGluR5 NAM and support the significance of further investigating the possible mechanism of action of the compound. |
X Demographics
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Switzerland | 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 15 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 15 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Researcher | 6 | 40% |
| Student > Ph. D. Student | 3 | 20% |
| Student > Doctoral Student | 2 | 13% |
| Student > Bachelor | 1 | 7% |
| Unknown | 3 | 20% |
| Readers by discipline | Count | As % |
|---|---|---|
| Neuroscience | 4 | 27% |
| Biochemistry, Genetics and Molecular Biology | 2 | 13% |
| Agricultural and Biological Sciences | 1 | 7% |
| Pharmacology, Toxicology and Pharmaceutical Science | 1 | 7% |
| Psychology | 1 | 7% |
| Other | 3 | 20% |
| Unknown | 3 | 20% |
Attention Score in Context
This research output has an Altmetric Attention Score of 1. 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 07 April 2018.
All research outputs
#20,480,611
of 23,041,514 outputs
Outputs from Frontiers in Pharmacology
#10,259
of 16,366 outputs
Outputs of similar age
#291,042
of 329,678 outputs
Outputs of similar age from Frontiers in Pharmacology
#239
of 388 outputs
Altmetric has tracked 23,041,514 research outputs across all sources so far. This one is in the 1st percentile – i.e., 1% of other outputs scored the same or lower than it.
So far Altmetric has tracked 16,366 research outputs from this source. They receive a mean Attention Score of 5.0. This one is in the 1st percentile – i.e., 1% of its peers scored the same or lower than it.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 329,678 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 1st percentile – i.e., 1% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 388 others from the same source and published within six weeks on either side of this one. This one is in the 1st percentile – i.e., 1% of its contemporaries scored the same or lower than it.