Respirerx Pharmaceuticals Inc.’s lead GABA-A receptor potentiator, KRM-II-81, has advanced to the next level of evaluation within the National...

Researchers from New York University College of Dentistry’s Pain Research Center in collaboration with the University of Pittsburgh found a candidate for chronic pain treatment among a library of 27 million compounds.

Monoacylglycerol lipase (MAGL), a member of the serine hydrolase family expressed in the brain and peripheral tissue, is a key enzyme in the hydrolysis of monoglycerides, converting 2-arachidonoyl glycerol (2-AG) into arachidonic acid and glycerol. MAGL inhibition has been previously shown to induce anxiolytic and analgesic phenotypes in animal models. Researchers from Janssen Pharmaceutica NV recently reported the discovery of novel noncovalent MAGL inhibitors.

Mu opioid receptors (MOR) agonists exert strong anti-nociceptive activity but their ability to cause tolerance and physical dependence are serious issues of concern and limit their use. The activation of another branch of opioid receptors discovered lately, the opioid-related nociceptin receptor 1 (OPRL1) has recently shown the ability to enhance MOR agonist-induced analgesia while limiting tolerance and side effects.

Researchers from Hefei Industrial Pharmaceutical Institute Co. Ltd. presented the discovery and preclinical evaluation of novel multifunctional inhibitors as potential anti-inflammatory and analgesic agents.