cebranopadol-hemicitrate

Description: Cebranopadol hemicitrate, the hemicitrate salt of Cebranopadol (also known as GRT-6005), is a novel, first in class compound with potent agonist activity on ORL-1 (opioid receptor like -1) and the well established mu opioid receptor. Cebranopadol is an analgesic nociceptin/orphanin FQ peptide (NOP) that exhibits high potency and efficacy in several rat models of acute and chronic pain (tail-flick, rheumatoid arthritis, bone cancer, spinal nerve ligation, diabetic neuropathy) with ED50 values of 0.5-5.6 ug/kg after intravenous and 25.1 ug/kg after oral administration. It is being evaluated in clinical Phase 2 and Phase 3 trials for the treatment of chronic and acute pain. Recent evidence indicates that the combination of opioid and NOP receptor agonism may be a new treatment strategy for cocaine addiction.

References: J Pharmacol Exp Ther. 2014 Jun; 349(3):535-48; J Pharmacol Exp Ther. 2017 Sep; 362(3):378-384.

Related CAS:863513-91-1 (free); 863513-93-3 ((1alpha, 4alpha)stereoisomer)