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Discovery of Dermorphin-Based Affinity Labels with Subnanomolar Affinity for Mu Opioid Receptors+

Sinha, Bhaswati
; 
Cao, Zhengyu
; 
Murray, Thomas F.
; 
Aldrich, Jane V.
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Abstract
A 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.
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Date
2009-12-10
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American Chemical Society
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Medicinal Chemistry Scholarly Works
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Sinha, 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/jm9007592
URI
https://hdl.handle.net/1808/23589
DOI
10.1021/jm9007592
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