Postdoctoral Research Associate
University of Florida
Synthesis of Bicyclic Analogs of the Kappa Opioid Receptor Antagonist Arodyn
The acetylated dynorphin A analog arodyn (Ac[Phe1,2,3,Arg4,D-Ala8]Dyn A(1-11)-NH2) exhibits potent and selective kappa opioid receptor antagonism. While cyclization can impart metabolic stability, increase binding affinity, and/or improve permeability, bicyclization imparts additional conformational constraint which can further enhance metabolic stability.