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Title: A selective small molecule NOP (ORL-1 receptor) partial agonist for the treatment of anxiety. Author: Ross TM, Battista K, Bignan GC, Brenneman DE, Connolly PJ, Liu J, Middleton SA, Orsini M, Reitz AB, Rosenthal DI, Scott MK, Vaidya AH. Journal: Bioorg Med Chem Lett; 2015 Feb 01; 25(3):602-6. PubMed ID: 25556095. Abstract: Small molecule (1) has been identified as a selective partial agonist of Opioid Receptor Like-1 (ORL-1) with potential utility for the treatment of anxiety and other disorders. Nociceptin (orphanin FQ) is an endogenous peptide ligand that binds to ORL-1, however it does not bind the classical δ, μ and κ opioid receptors with high affinity. The synthesis of 1 involved using a molecular diversity approach, to rapidly advance a library of compounds for biological testing. A lead selective potent partial agonist (35-fold ORL-1/Mu) progressed to ORL-1 (NOP or OP4) proof of concept testing in advanced studies. The synthetic approach and biological data for the related chemical series will be presented.[Abstract] [Full Text] [Related] [New Search]