ARTICLE | Targets & Mechanisms

Pain out of the brain

September 30, 2010 7:00 AM UTC

Achieving analgesia without cognitive and behavioral side effects has been a holy grail for companies developing pain therapeutics, but separating the desirable and undesirable effects of analgesics has been a challenge for compounds that act in the CNS. Now, a team of Italian and American researchers may have sidestepped the problem with a molecule, URB937, that works entirely in the periphery.1

URB937, a p-hydroxyphenyl-O-arylcarbamate, targets fatty acid amide hydrolase (FAAH), an enzyme that degrades the lipid molecule anandamide,which in turn activates cannabinoid receptors on sensory neurons in the periphery and on a range of other neurons in the brain. Inhibiting FAAH raises natural anandamide levels and leads to long-term cannabinoid receptor activation and pain relief...