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  • Title: Methionine oxidation enhances opioid activity of an enkephalin analog.
    Author: Kiritsy-Roy JA, Chan SK, Iwamoto ET.
    Journal: Life Sci; 1983 Feb 21; 32(8):889-93. PubMed ID: 6131372.
    Abstract:
    D-ala2-met-sulfoxide5-enkephalinamide, DALA(0), was synthesized by oxidizing the 5-methionine residue of D-ala2-met5-enkephalinamide (DALA). Antinociception was assessed on the hot-plate and catalepsy estimated using an immobility test in rats administered DALA, DALA(0) and morphine intraventricularly. By comparing areas under time-effect curves, DALA(0) was 30 times more antinociceptive and up to 40 times more cataleptogenic than DALA. For comparison, morphine induced one-tenth the antinociception and one-fortieth the immobility caused by DALA(0). These results demonstrate that the opiate activity of DALA is clearly enhanced by oxidation of its terminal methionine.
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