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Margaric Acid Decreases PIEZO2 Mediated Pain

Summary
Investigators at the National Center for Complimentary and Integrative Health (NCCIH) and the University of Tennessee Health and Science Center have shown that administration of margaric acid can ameliorate pain induced by a variety of noxious stimuli in mice. In vitro and ex vivo studies in human and murine neural cells indicate that the mechanism of action of margaric acid is mediated by PIEZO2 (Piezo-type mechanosensitive ion channel component 2) function. NCCIH seeks research co-development partners and/or licensees for methods of using the fatty acid, margaric acid to treat pain.
NIH Reference Number
E-081-2020
Product Type
Keywords
  • National Center for Complimentary and Integrative Health, NCCIH, Pain, Fatty Acid, Margaric Acid, Allodynia, PIEZO2, Migraine, Neuropathy, Chronic Inflammation, Vásquez, Chesler
Collaboration Opportunity
This invention is available for licensing and co-development.
Contact
Description of Technology

Some existing therapies for treatment of pain are administered systematically and have significant side effects, such as addiction and drowsiness. Alternative therapy that does not impair normal touch function could be used to treat pain caused by mechanical injury or chronic inflammation. Administration of margaric acid was shown to ameliorate pain in mouse models of pain. In vitro data shows that margaric acid counteracts PIEZO2 (Piezo-type mechanosensitive ion channel component 2) potentiation evoked by bradykinin (i.e. a peptide that promotes inflammation) by reducing the mechanocurrents up to non-inflammatory levels. Margaric acid seems to be specific to target mechanical pain as it does not significantly alter the electric excitability of mice dorsal root ganglia neurons or human iPSC-derived neurons. It mainly decreases action potential firing evoked by mechanical stimulation.

The National Center for Complimentary and Integrative Health (NCCIH) seeks licensees and/or commercial partners to develop topical formulations of margaric acid to treat allodynia, neuropathy, and pain caused by chronic inflammation.  

E-081-2020 - PIEZO2 channel under different physiological conditions

 

 

 

 

 

 

 

 

 

 

 

 

Potential Commercial Applications
  • Treatment of pain caused by mechanical injury
  • Treatment of pain caused by chronic inflammation (e.g., rheumatoid arthritis)
  • Treatment of allodynia
Competitive Advantages
  • Not addictive
  • Topical application
  • Fewer side effects
Inventor(s)

Valeria Vasquez Ph.D., Alexander Chesler Ph.D. (NCCIH), Julio Cordero-Morales Ph.D., Luis Romero

Development Stage
Publications

Romero LO, et al. A dietary fatty acid counteracts neuronal mechanical sensitization  [PMID 32561714]

Patent Status
  • U.S. Provisional: U.S. Provisional Patent Application Number 62/976,014 , Filed 13 Feb 2020
Therapeutic Area
Updated
Thursday, September 3, 2020