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Antinociceptive Profile of ARN19702, (2-Ethylsulfonylphenyl)-[(2S)-4-(6-fluoro-1,3-benzothiazol-2-yl)-2-methylpiperazin-1-yl]methanone, a Novel Orally Active N-Acylethanolamine Acid Amidase Inhibitor, in Animal Models

Yannick Fotio, Oscar Sasso, Roberto Ciccocioppo, Daniele Piomelli. J Pharmacol Exp Ther. 2021 Aug;378(2):70-76.

Laboratory studyOther animals

Design
Laboratory study
Subjects
Male mice and male rats in models of acute, inflammatory and neuropathic pain
Dose used in the study
ARN19702, an oral NAAA inhibitor, in a dose range; 30 mg/kg oral for the reward and motor tests. Palmitoylethanolamide itself was not given
Duration
Not stated in the abstract
What was measured
Formalin nocifensive response; hypersensitivity after carrageenan, paw incision, sciatic nerve ligation and paclitaxel; conditioned place preference; exploratory motor behaviour.

What the authors reported

This laboratory study found:

  • Oral ARN19702 reduced formalin responses and hypersensitivity in the inflammatory, incision and nerve-ligation models in mice in a dose-dependent way, and reduced paclitaxel neuropathy pain in rats without subacute tolerance.
  • At 30 mg/kg it did not produce place preference or change motor behaviour.
  • NAAA breaks down palmitoylethanolamide, so the drug acts by preserving the body's own PEA.

Limits of this study

Rodent models; they cannot show effect in people. PEA was not given directly. One author is an inventor on patent applications for NAAA inhibitors owned by the University of California, Irvine.

Source

PubMed 33986036 · doi:10.1124/jpet.121.000674

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.