Design and synthesis of cyanamides as potent and selective N-acylethanolamine acid amidase inhibitors
Laboratory studyHumansOther animals
- Design
- Laboratory study
- Subjects
- Enzyme and plasma stability assays with human and rodent material; no animals or people treated
- Dose used in the study
- Not applicable; no palmitoylethanolamide was given
- Duration
- Not stated in the abstract
- What was measured
- Potency of new azetidine-nitrile (cyanamide) compounds against human NAAA, the enzyme that breaks down palmitoylethanolamide; selectivity against FAAH, MGL, ABHD6 and cathepsin K; plasma stability.
What the authors reported
The study found:
- Key compounds inhibited human NAAA at single-digit nanomolar concentrations with more than 100-fold selectivity over the other enzymes tested.
- The authors also identified dual NAAA-FAAH inhibitors.
- Several compounds had plasma half-lives above 2 hours in human and rodent plasma.
Limits of this study
A chemistry and enzyme study; no effect on pain or inflammation in animals or people was tested. Palmitoylethanolamide itself was not given. Funding and conflicts not stated in the abstract.
Source
PubMed 31761726 · doi:10.1016/j.bmc.2019.115195
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.