You are seeing a free-to-access but limited selection of the activity Altmetric has collected about this research output.
Click here to find out more.
X Demographics
Mendeley readers
Attention Score in Context
| Title |
Design and Synthesis of Novel Deuterated Ligands Functionally Selective for the γ‑Aminobutyric Acid Type A Receptor (GABAAR) α6 Subtype with Improved Metabolic Stability and Enhanced Bioavailability
|
|---|---|
| Published in |
Journal of Medicinal Chemistry, February 2018
|
| DOI | 10.1021/acs.jmedchem.7b01664 |
| Pubmed ID | |
| Authors |
Daniel E. Knutson, Revathi Kodali, Branka Divović, Marco Treven, Michael R. Stephen, Nicolas M. Zahn, Vladimir Dobričić, Alec T. Huber, Matheus A. Meirelles, Ranjit S. Verma, Laurin Wimmer, Christopher Witzigmann, Leggy A. Arnold, Lih-Chu Chiou, Margot Ernst, Marko D. Mihovilovic, Miroslav M. Savić, Werner Sieghart, James M. Cook |
| Abstract |
Recent reports indicate that α6β2/3γ2 GABAAR selective ligands may be important for the treatment of trigeminal orofacial pain and neuropsychiatric disorders with sensori-motor gating deficits. Based on 3 functionally α6β2/3γ2 GABAAR selective pyrazoloquinolinones, 42 novel analogs were synthesized and their in vitro metabolic stability and cytotoxicity as well as their in vivo pharmacokinetics, basic behavioral pharmacology, and effects on locomotion was investigated. Incorporation of deuterium into the methoxy substituents of the ligands increased their duration of action via improved metabolic stability and bioavailability, while their selectivity for the GABAAR α6 subtype was retained. 8b was identified as the lead compound with a substantially improved pharmacokinetic profile. The ligands allosterically modulated diazepam insensitive α6β2/3γ2 GABAARs and were functionally silent at diazepam sensitive α1β2/3γ2 GABAARs, thus no sedation was detected. In addition, these analogs were not cytotoxic, which render them interesting candidates for treatment of CNS disorders mediated by GABAAR α6β2/3γ2 subtypes. |
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 % |
|---|---|---|
| Philippines | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Practitioners (doctors, other healthcare professionals) | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 40 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 40 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Researcher | 5 | 13% |
| Student > Ph. D. Student | 3 | 8% |
| Student > Master | 3 | 8% |
| Student > Bachelor | 3 | 8% |
| Professor | 2 | 5% |
| Other | 8 | 20% |
| Unknown | 16 | 40% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 7 | 18% |
| Biochemistry, Genetics and Molecular Biology | 4 | 10% |
| Medicine and Dentistry | 4 | 10% |
| Agricultural and Biological Sciences | 2 | 5% |
| Unspecified | 2 | 5% |
| Other | 4 | 10% |
| Unknown | 17 | 43% |
Attention Score in Context
This research output has an Altmetric Attention Score of 7. 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 30 August 2022.
All research outputs
#4,616,531
of 23,202,641 outputs
Outputs from Journal of Medicinal Chemistry
#6,541
of 22,200 outputs
Outputs of similar age
#89,716
of 330,542 outputs
Outputs of similar age from Journal of Medicinal Chemistry
#45
of 142 outputs
Altmetric has tracked 23,202,641 research outputs across all sources so far. Compared to these this one has done well and is in the 79th percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 22,200 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 6.7. This one has gotten more attention than average, scoring higher than 70% of its peers.
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 330,542 tracked outputs that were published within six weeks on either side of this one in any source. This one has gotten more attention than average, scoring higher than 72% of its contemporaries.
We're also able to compare this research output to 142 others from the same source and published within six weeks on either side of this one. This one has gotten more attention than average, scoring higher than 65% of its contemporaries.