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A novel analgesic dipeptide from bovine brain is a possible Met-enkephalin releaser

Abstract

It is generally accepted that morphine exerts its analgesic effect by binding to specific opiate receptors in the brain and spinal cord1. Since Hughes et al.2 isolated and identified two endogenous pentapeptides, Met- and Leu-enkephalin, from the brain and found that they acted as agonists at opiate receptors, α-, β- and γ-endorphins, larger peptides than enkephalins and having morphine-like activity, have been identified in either the brain or pituitary of various species1. Several studies have demonstrated that enkephalins possess analgesic properties and that they are distributed in the pain-mediated pathways in the central nervous system. These findings suggest that enkephalins are important neurotransmitters or neuromodulators regulating pain transmission. We now report the isolation of a novel substance which has a Met-enkephalin releasing action. Our findings suggest the possibility of a regulating mechanism for the release of endogenous opioid peptides, especially Met-enkephalin

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Takagi, H., Shiomi, H., Ueda, H. et al. A novel analgesic dipeptide from bovine brain is a possible Met-enkephalin releaser. Nature 282, 410–412 (1979). https://doi.org/10.1038/282410a0

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