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Irreversible labelling of the opioid receptors by a melphalan-substituted (Met5)enkephalin-Arg-Phe derivative



Irreversible labelling of the opioid receptors by a melphalan-substituted (Met5)enkephalin-Arg-Phe derivative



European Journal of Pharmacology 373(2-3): 241-249



(Met5)enkephalin-Arg-Phe (Tyr-Gly-Gly-Phe-Met-Arg-Phe) was modified with the methyl esther of melphalan (Mel; 4-bis(2-chloroethyl)amino-L-phenylalanine) and the resulting compounds were studied for their opioid binding properties in guinea pig and rat brain membranes. Three new peptides, with a substitution of a single amino acid, were synthesized (Mel-Gly-Gly-Phe-Met-Arg-Phe, Tyr-Gly-Gly-Mel-Met-Arg-Phe and Tyr-Gly-Gly-Phe-Met-Arg-Mel).

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Accession: 010885746

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