On resin click-chemistry-mediated synthesis of novel enkephalin analogues with potent anti-nociceptive activity
Scientific Reports, ISSN: 2045-2322, Vol: 9, Issue: 1, Page: 5771
2019
- 18Citations
- 33Captures
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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
- Citations18
- Citation Indexes18
- 18
- CrossRef14
- Captures33
- Readers33
- 33
Article Description
Here, we report the chemical synthesis of two DPDPE analogues 7a (NOVA1) and 7b (NOVA2). This entailed the solid-phase synthesis of two enkephalin precursor chains followed by a Cu -catalyzed azide-alkyne cycloaddition, with the aim of improving in vivo analgesic efficacy versus DPDPE. NOVA2 showed good affinity and selectivity for the μ-opioid receptor (K of 59.2 nM, EC of 12.9 nM, E of 87.3%), and long lasting anti-nociceptive effects in mice when compared to DPDPE.
Bibliographic Details
Springer Science and Business Media LLC
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