N-desethyl-fluornitrazene

N-desethyl-fluornitrazene (DFNZ) is a novel, highly potent synthetic benzimidazole opioid of the nitazene class that acts as a selective superagonist of the μ-opioid receptor (MOR). Developed by researchers at the National Institute on Drug Abuse (NIDA) and the National Institutes of Health (NIH), DFNZ exhibits a unique pharmacological and pharmacokinetic profile characterized by impaired brain penetrance. This is due to its status as a substrate for the blood-brain barrier efflux transporters P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2), resulting in limited brain MOR occupancy at therapeutic doses. In preclinical rodent models, DFNZ produces robust analgesia for acute and inflammatory pain without inducing typical opioid-related adverse effects such as respiratory depression, tolerance, withdrawal, or high abuse liability. It also shows diminished efficacy at the MOR-galanin 1 receptor (GAL1) heteromer and has limited effects on dopamine neurotransmission in the nucleus accumbens, reducing its reinforcing properties.

Other names

N-desethyl-2-fluoroetonitazeneN-desethyl2-fluoroetonitazeneN-desethyl 2-fluoroetonitazeneN-desethyl-fluetonitazeneN-desethylfluornitrazene