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Mendeley readers
Attention Score in Context
| Title |
Attaining in vivo selectivity of positive modulation of α3βγ2 GABAA receptors in rats: A hard task!
|
|---|---|
| Published in |
European Neuropsychopharmacology, June 2018
|
| DOI | 10.1016/j.euroneuro.2018.05.014 |
| Pubmed ID | |
| Authors |
Bojan Batinić, Tamara Stanković, Michael Rajesh Stephen, Revathi Kodali, Veera V. Tiruveedhula, Guanguan Li, Petra Scholze, Bojan D. Marković, Aleksandar Lj. Obradović, Margot Ernst, James M. Cook, Miroslav M. Savić |
| Abstract |
It is unclear whether GABAA receptors (GABAARs) that contain the α3-subunit are substantially involved in the anxiolytic effects of benzodiazepines (BDZs). In the present study, we tested YT-III-31, a newer BDZ ligand with functional preference for α3βγ2 GABAARs, in two paradigms of unconditioned anxiety, the open field and elevated plus maze in rats. The effective dose of YT-III-31 (2 mg/kg) displayed a clear anxiolytic-like profile, unhampered by sedative action, in both tests. At a higher dose (10 mg/kg), YT-III-31 induced ataxia in the rotarod and sedation in spontaneous locomotor activity test. The latter effect was preventable by flumazenil and βCCt, the non-selective and α1βγ2 GABAAR affinity-selective antagonist, respectively, demonstrating that sedative properties of YT-III-31, when attained, are mediated by the α1γ2 site. To elucidate the receptor substrate of subtle behavioral differences between YT-III-31 and diazepam, we approximated in vivo receptor potentiation for both ligands, based on estimated unbound concentrations in rat brains. Far different from diazepam, YT-III-31 has significantly lower affinity for the α1γ2 over other BDZ-sensitive sites, and at lower doses (1-2 mg/kg) was devoid of potentiation at α1βγ2 GABAARs. The approximation approach revealed a modest selectivity of YT-III-31 for α3γ2- in comparison to α2γ2 and α5γ2 binding sites, suggesting that its anxiolytic-like activity may not necessarily or predominantly reflect potentiation at α3βγ2 GABAARs. Nonetheless, as the anxiolytic effects are achievable at a dose devoid of any sedative potential, and having favorable safety (cytotoxicity) and metabolic stability profile, YT-III-31 represents a valuable candidate for further translational research. |
Mendeley readers
The data shown below were compiled from readership statistics for 13 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 13 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Researcher | 4 | 31% |
| Student > Ph. D. Student | 3 | 23% |
| Student > Master | 2 | 15% |
| Unspecified | 1 | 8% |
| Student > Bachelor | 1 | 8% |
| Other | 1 | 8% |
| Unknown | 1 | 8% |
| Readers by discipline | Count | As % |
|---|---|---|
| Neuroscience | 4 | 31% |
| Biochemistry, Genetics and Molecular Biology | 2 | 15% |
| Environmental Science | 1 | 8% |
| Unspecified | 1 | 8% |
| Medicine and Dentistry | 1 | 8% |
| Other | 3 | 23% |
| Unknown | 1 | 8% |
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 05 July 2018.
All research outputs
#22,767,715
of 25,382,440 outputs
Outputs from European Neuropsychopharmacology
#1,929
of 2,573 outputs
Outputs of similar age
#299,538
of 341,602 outputs
Outputs of similar age from European Neuropsychopharmacology
#36
of 58 outputs
Altmetric has tracked 25,382,440 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 2,573 research outputs from this source. They typically receive more attention than average, with a mean Attention Score of 8.2. 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 341,602 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 58 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.