Development of Novel Local Analgesics for Management of Acute Tissue Injury Pain
Technical Report,01 Sep 2015,31 Aug 2018
Childrens Hospital Corporation Boston United States
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We aimed to develop novel, non-addictive, treatments for acute soft tissue and skeletal injuries, such as seen in battlefield trauma, without the problems associated with opioid drugs. We targeted the delivery of small, membrane impermeable, sodium channel blockers through large pore TRP channels, such as TRPV1. These channels act as the innate trigger of nociceptive and inflammatory pain and are open at the site of acute injury and during the phases of inflammatory pain that follow. During the funded period we completed in vitro pharmacological screening of 46 new chemical entities including exclusion of compounds with activity on cardiomyocytes and identified 5 that showed promise relative to the reference compound, QX-314. In vivo studies in acute inflammatory and post-surgical pain models identified BW031 as the most promising lead for future therapeutic exploration as treatment for battle wound and surgical injures.
- Medicine and Medical Research
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