Synthesis and biological activity of novel small peptides with aminophosphonates moiety as NOP receptor ligands
Amino Acids, ISSN: 0939-4451, Vol: 39, Issue: 5, Page: 1537-1543
2010
- 34Citations
- 12Captures
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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.
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Metrics Details
- Citations34
- Citation Indexes34
- 34
- CrossRef27
- Captures12
- Readers12
- 12
Article Description
The aim of the present study was the synthesis and the biological screening of new analogs of Ac-RYYRWK-NH, modified at the N-terminal with 1-[(methoxyphosphono)methylamino]cycloalkanecarboxylic acids. The four newly synthesized ligands for the nociceptin/orphanin FQ (N/OFQ) receptor (NOP) have been prepared by solid-phase peptide synthesis-Fmoc-strategy. These compounds were tested for agonistic activity in vitro on electrically stimulated smooth-muscle preparations isolated from vas deferens of Wistar rats. Our data showed that substitution of Arg at position 1 with aminophosphonates moiety decreased significantly the affinity of ligands to the NOP receptor. Furthermore, the enlargement of the cycle (with 5-8 carbon atoms) additionally diminished both the activity and the selectivity for NOP-receptor. © 2010 Springer-Verlag.
Bibliographic Details
http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=78449280631&origin=inward; http://dx.doi.org/10.1007/s00726-010-0624-1; http://www.ncbi.nlm.nih.gov/pubmed/20499257; http://link.springer.com/10.1007/s00726-010-0624-1; https://dx.doi.org/10.1007/s00726-010-0624-1; https://link.springer.com/article/10.1007/s00726-010-0624-1; http://www.springerlink.com/index/10.1007/s00726-010-0624-1; http://www.springerlink.com/index/pdf/10.1007/s00726-010-0624-1
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