Ontology highlight
ABSTRACT:
SUBMITTER: Sinha B
PROVIDER: S-EPMC2788677 | biostudies-literature | 2009 Dec
REPOSITORIES: biostudies-literature
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]