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  • Title: Synthesis of 3H-Tyr-D-Ala-Gly-N(Me)Phe chloromethyl ketone--an opioid affinity label.
    Author: Varga E, Tóth G, Hepp J, Benyhe S, Simon J, Medzihradszky K, Borsodi A.
    Journal: Neuropeptides; 1988 Oct; 12(3):135-9. PubMed ID: 2853836.
    Abstract:
    A radioactive enkephalin affinity reagent, selective for the mu opioid receptor subtype, was synthesized by a fragment condensation method. 3H-BOC-Tyr-D-Ala-Gly-OH was prepared by catalytic tritiation of the protected iodinated tripeptide. The protected tritiated tripeptide and N(Me)Phe-CH2Cl were condensed by the mixed anhydride method. The protecting group was removed by HCl/acetic acid. The tritiated tetrapeptide has a specific radioactivity of 56.8 Ci/mmole (2.1 TBq/mmole).
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