Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways

…, SM Keenan, S Kortagere, KM Wannemacher…

Index: Peng, Youyi; Zhang, Qiang; Arora, Sonia; Keenan, Susan M.; Kortagere, Sandhya; Wannemacher, Kenneth M.; Howells, Richard D.; Welsh, William J. Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 17 p. 6442 - 6450

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Citation Number: 10

Abstract

A novel family of 1, 3, 5-trisubstituted 1, 2, 4-triazoles was discovered as potent and selective ligands for the δ opioid receptor by rational design. Compound 5b exhibited low-nanomolar in vitro binding affinity (IC50= 5.8 nM), excellent selectivity for the δ opioid receptor over the alternative μ and κ opioid receptors, full agonist efficacy in receptor down-regulation and MAP kinase activation assays, and low-efficacy partial agonist activity in stimulation of ...