Novel N-acylethanolamine acid amidase inhibitor shows promise as a potential analgesic agent in animal models

2023-04-22 13:29:19 By : admin
cannabinol (THC), CBD, pain relief, N-acylethanolamine acid amidase (NAAA), ARN19702, neuropathic pain, inflammatory pain, analgesic drugs.

Pain is one of the most commonly reported symptoms among individuals worldwide. It can be caused by various factors, including neuropathic and inflammatory conditions. While traditional analgesic drugs like nonsteroidal anti-inflammatory drugs (NSAIDs) are available to treat pain, they often come with adverse effects such as addiction and sedation.
Antinociceptive profile of ARN19702 (2-ethylsulfonylphenyl)-[(2S)-<a href='/4/'>4</a>-(<a href='/6/'>6</a>-fluoro-1,3-benzothiazol-2-yl)-2-methylpiperazin-1-yl]methanone), a novel orally active N-acylethanolamine acid amidase inhibitor, in animal models | Journal of Pharmacology and Experimental Therapeutics


Researchers are thus exploring alternative molecular targets for the discovery of novel analgesic drugs without the addictive and sedative potential of traditional drugs. One potential target is N-acylethanolamine acid amidase (NAAA), an enzyme that stops the physiological actions of a fatty acid substance called palmitoylethanolamide (PEA).

NAAA inhibitors like ARN19702 have been shown to produce protective effects against multiple sclerosis in mice. In a recent study published in the Journal of Pharmacology and Experimental Therapeutics, researchers evaluated the antinociceptive profile of ARN19702 in mouse and rat models of acute and neuropathic pain.

The study found that oral administration of ARN19702 attenuated the nocifensive response and hypersensitivity in mice elicited by intraplantar formalin injection, intraplantar carrageenan injection, paw incision, and sciatic nerve ligation. In rats, ARN19702 reduced nociception associated with paclitaxel-induced neuropathy without the development of sub-acute antinociceptive tolerance.

Notably, ARN19702 did not produce place-preference or alter exploratory motor behavior in male mice, suggesting that it lacks the rewarding potential and sedative effects often associated with traditional analgesic drugs.

The findings of this study suggest that NAAA is a promising molecular target for the development of efficacious analgesic drugs devoid of addictive and sedative potential. Alternative therapies like CBD and THC, which are derived from the cannabis plant, have also shown promising results in the treatment of neuropathic and inflammatory pain.

CBD, in particular, has gained popularity due to its ability to relieve pain without causing the psychoactive effects associated with THC. CBD works by interacting with the body's endocannabinoid system, which is responsible for regulating various physiological processes, including pain sensation.

Several studies have shown that CBD can effectively reduce pain levels in individuals with neuropathic and inflammatory conditions like multiple sclerosis, arthritis, and fibromyalgia. However, more research is needed to fully understand the mechanisms by which CBD produces its analgesic effects.

In conclusion, NAAA inhibitors like ARN19702 and alternative therapies like CBD and THC are promising avenues for the development of novel analgesic drugs without the adverse effects of traditional drugs. As research in this field continues, we may see more effective and safe treatments for individuals suffering from chronic pain.