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ASP8477, a fatty acid amide hydrolase inhibitor, exerts analgesic effects in rat models of neuropathic and dysfunctional pain

Tetsuo Kiso, Tomonari Watabiki, Toshihiro Sekizawa. Eur J Pharmacol. 2020;881:173194.

Laboratory studyOther animalsWith ASP8477 (a FAAH inhibitor that raises brain PEA and OEA, tested alone)

This study tested palmitoylethanolamide together with ASP8477 (a FAAH inhibitor that raises brain PEA and OEA, tested alone). Its results cannot be assigned to palmitoylethanolamide alone. More combination studies.

Design
Laboratory study
Subjects
Rats with spinal nerve ligation, chronic constriction injury or reserpine-induced myalgia, and mice with chemically induced allodynia (numbers not stated in the abstract)
Dose used in the study
ASP8477 by mouth, single and four-week repeated dosing; doses not stated in the abstract
Duration
Single doses and 4 weeks repeated dosing
What was measured
Mechanical allodynia, thermal hyperalgesia, cold allodynia and muscle pressure thresholds; duration of effect; ex vivo brain FAAH inhibition; brain OEA and PEA levels; acute pain tests.

What the authors reported

The study found:

  • ASP8477 reduced mechanical allodynia after single and four-week dosing with similar improvement, improved thermal and cold hypersensitivity, and restored muscle pressure thresholds.
  • The effect lasted at least 4 hours, matching brain FAAH inhibition and raised OEA and PEA.
  • It also reduced AMPA-, NMDA-, prostaglandin- and bicuculline-induced allodynia in mice, but did not affect acute pain.

Limits of this study

Rat and mouse pain models; they cannot show effect in people. PEA was not given; it rose as a result of FAAH inhibition. The conflict statement attached to this record names Salvatore Cuzzocrea, who is not an author, so it appears misfiled; the compound's sponsor is not stated in the abstract.

Source

PubMed 32445705 · doi:10.1016/j.ejphar.2020.173194

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.