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

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• 作者：Bhaswati Sinha ; Zhengyu Cao ; Thomas F. Murray ; Jane V. Aldrich
• 刊名：Journal of Medicinal Chemistry
• 出版年：2009
• 出版时间：December 10, 2009
• 年：2009
• 卷：52
• 期：23
• 页码：7372-7375
• 全文大小：689K
• 年卷期：v.52,no.23(December 10, 2009)
• ISSN：1520-4804

文摘

A series of potent electrophilic affinity labels (IC₅₀ = 0.1−5 nM) containing either a bromoacetamide or isothiocyanate based on the μ opioid receptor (MOR) selective peptide dermorphin were prepared. All four analogues exhibited wash resistant inhibition of [³H]DAMGO binding at subnanomolar to nanomolar concentrations, suggesting that these analogues bind covalently to MOR. To our knowledge, these peptides are the highest affinity peptide-based affinity labels for MOR reported to date.