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Effects of the synthetic enkephalin analogue FK 33-824 in man

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Abstract

THE synthetic analogue of methionine enkephalin, FK 33-824, exerts a long-lasting and potent analgesic effect in animals after systemic and enteral administration1. In high doses it produces tolerance, cross-tolerance with morphine, and dependence in monkeys. Like β-endorphin, FK 33-824 produces akinaesia in rats and rabbits. All effects seen in animals can be abolished by naloxone. We report here on the results of the first studies performed with FK 33-824 in man (tolerance, electroencephalogram (EEG), endocrine profile and plasma levels), as a basis for future therapeutic studies.

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Authors and Affiliations

  1. Department of Experimental Therapeutics, Biological and Medical Research Division, Sandoz Ltd, CH-4002, Basle, Switzerland

    BEAT VON GRAFFENRIED, EMILIO DEL POZO & JIRI ROUBICEK

  2. Psychiatric Clinic Wil, CH-9500, Wil, Switzerland

    EVA KREBS & WALTER PÖLDINGER

  3. Medical University Clinic, D-78 Freiburg i.Br., FRG

    PETER BURMEISTER & LOTHAR KERP

Authors
  1. BEAT VON GRAFFENRIED
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  2. EMILIO DEL POZO
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  3. JIRI ROUBICEK
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  4. EVA KREBS
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  5. WALTER PÖLDINGER
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  6. PETER BURMEISTER
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  7. LOTHAR KERP
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VON GRAFFENRIED, B., DEL POZO, E., ROUBICEK, J. et al. Effects of the synthetic enkephalin analogue FK 33-824 in man. Nature 272, 729–730 (1978). https://doi.org/10.1038/272729a0

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  • DOI: https://doi.org/10.1038/272729a0

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