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W2083551552 abstract "Analogs of morphiceptin (Tyr-Pro-Phe-Pro-NH2), a mu-selective opioid receptor ligand, with position 3-modifications, including altered size, lipophilicity, and electronic character, while maintaining aromaticity were synthesized. The activity of the new analogs in in vitro assays and in in vivo hot-plate test of analgesia was compared and the results were consistent. [D-1-Nal3]Morphiceptin was the most potent analog of this series with a 26-fold increase in mu-opioid receptor affinity, a 15-fold potency increase in the GPI assay, and a significant potency increase in the hot-plate analgesic test, as compared with morphiceptin. [d-Qal3]Morphiceptin was found to be a weak antagonist in the GPI assay." @default.
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W2083551552 date "2004-07-01" @default.
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W2083551552 title "Opioid receptor binding and in vivo antinociceptive activity of position 3-substituted morphiceptin analogs" @default.
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W2083551552 doi "https://doi.org/10.1016/j.bbrc.2004.05.202" @default.
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