Sinha, BhaswatiCao, ZhengyuMurray, Thomas F.Aldrich, Jane V.2017-04-062017-04-062009-12-10Sinha, B., Cao, Z., Murray, T. F., & Aldrich, J. V. (2009). Discovery of Dermorphin-Based Affinity Labels with Subnanomolar Affinity for Mu Opioid Receptors. Journal of Medicinal Chemistry, 52(23), 7372–7375. http://doi.org/10.1021/jm9007592https://hdl.handle.net/1808/23589A series of potent electrophilic affinity labels (IC50 = 0.1-5 nM) containing either a bromoacetamide or isothiocyanate based on the mu opioid receptor (MOR) selective peptide dermorphin were prepared. All four analogs exhibited wash resistant inhibition of [3H]DAMGO binding at subnanomolar to nanomolar concentrations, suggesting that these analogs bind covalently to MOR. To our knowledge these peptides are the highest affinity peptide-based affinity labels for MOR reported to date.This document is the Accepted Manuscript version of a Published Work that appeared in final form in the Journal of Medicinal Chemistry, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see http://dx.doi.org/10.1021/jm9007592.Article10.1021/jm9007592openAccess