Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors.
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ABSTRACT:
SUBMITTER: Sinha B
PROVIDER: S-EPMC2788677 | biostudies-literature | 2009 Dec
REPOSITORIES: biostudies-literature
Publications
Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors.
Sinha Bhaswati B Cao Zhengyu Z Murray Thomas F TF Aldrich Jane V JV
Journal of medicinal chemistry 20091201 23
A series of potent electrophilic affinity labels (IC(50) = 0.1-5 nM) containing either a bromoacetamide or isothiocyanate based on the mu opioid receptor (MOR) selective peptide dermorphin were prepared. All four analogues exhibited wash resistant inhibition of [(3)H]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. ...[more]
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