The N -Methyl- d -aspartate Receptor Inhibitory Potencies of Aromatic Inhaled Drugs of Abuse: Evidence for Modulation by Cation-π Interactions
The Journal of Pharmacology and Experimental Therapeutics, ISSN: 0022-3565, Vol: 311, Issue: 1, Page: 14-21
2004
- 40Citations
- 23Captures
Metric Options: CountsSelecting the 1-year or 3-year option will change the metrics count to percentiles, illustrating how an article or review compares to other articles or reviews within the selected time period in the same journal. Selecting the 1-year option compares the metrics against other articles/reviews that were also published in the same calendar year. Selecting the 3-year option compares the metrics against other articles/reviews that were also published in the same calendar year plus the two years prior.
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Example: if you select the 1-year option for an article published in 2019 and a metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019. If you select the 3-year option for the same article published in 2019 and the metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019, 2018 and 2017.
Citation Benchmarking is provided by Scopus and SciVal and is different from the metrics context provided by PlumX Metrics.
Metrics Details
- Citations40
- Citation Indexes40
- CrossRef40
- 40
- Captures23
- Readers23
- 23
Article Description
Benzene and several close structural analogs are inhaled drugs of abuse with general anesthetic activity. By virtue of their π electron clouds, they may engage in attractive electrostatic interactions with cationic atomic charges on protein targets. In this study, we tested the hypothesis that inhaled drugs of abuse inhibit human N -methyl- d -aspartate (NMDA) receptors with potencies that correlate with their abilities to engage in cation-π interactions. Electrophysiological techniques were used to define the NR1/NR2B NMDA receptor inhibitory concentrations of volatile benzene analogs, and computer modeling was used to quantify their abilities to engage in cation-π interactions and their molecular volumes. In addition, each compound’s octanol/gas partition coefficient (a measure of hydrophobicity) was quantified. All 18 compounds inhibited human NR1/NR2B NMDA receptors reversibly and in a concentration-dependent manner. NMDA receptor inhibitory potency correlated strongly with the ability to engage in cation-π interactions, weakly with hydrophobicity, and was independent of molecular volume. This is consistent with the hypothesis that cation-π interactions enhance the binding of inhaled drugs of abuse to the NMDA receptor and suggests that the receptor binding site(s) for these drugs possesses significant cationic character.
Bibliographic Details
http://www.sciencedirect.com/science/article/pii/S0022356524315630; http://dx.doi.org/10.1124/jpet.104.069930; http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=4644353582&origin=inward; http://www.ncbi.nlm.nih.gov/pubmed/15166258; https://linkinghub.elsevier.com/retrieve/pii/S0022356524315630; https://dx.doi.org/10.1124/jpet.104.069930; https://jpet.aspetjournals.org/content/311/1/14
Elsevier BV
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