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Synthesis, Molecular Modeling and Biological Evaluation of Metabolically Stable Analogues of the Endogenous Fatty Acid Amide Palmitoylethanolamide

Alessia D'Aloia, Federica Arrigoni, Renata Tisi, Alessandro Palmioli, Michela Ceriani, Valentina Artusa, Cristina Airoldi, Giuseppe Zampella, Barbara Costa, Laura Cipolla. Int J Mol Sci. 2020 Nov 28;21(23):9074.

Laboratory studyHumansOther animalsWith RePEA (a PEA analogue, tested alone and against PEA)

This study tested palmitoylethanolamide together with RePEA (a PEA analogue, tested alone and against PEA). Its results cannot be assigned to palmitoylethanolamide alone. More combination studies.

Design
Laboratory study
Subjects
Computer modelling; membrane samples containing FAAH; murine N9 microglial cells and human PMA-THP-1 cells stimulated with LPS
Dose used in the study
Not stated in the abstract
Duration
Not stated in the abstract
What was measured
Predicted and measured resistance of PEA analogues to FAAH hydrolysis (by 1H-NMR); inhibition of LPS-induced cytokine release in cultured cells

What the authors reported

The study found:

  • Modelling picked RePEA as the most accessible and FAAH-resistant analogue.
  • NMR showed RePEA was not broken down by FAAH, unlike PEA.
  • RePEA kept PEA's ability to inhibit LPS-induced cytokine release in both mouse microglia and human THP-1 cells.

Limits of this study

A chemistry and cell-culture study; it cannot show effect in people or animals treated in practice. The authors declare no conflict of interest.

Source

PubMed 33260658 · doi:10.3390/ijms21239074

Entry checked against the abstract on PubMed on 2026-09-22. The dose shown is the dose the researchers used. It is not a recommendation. How to read this page.