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Metabolism of enkephalins and its inhibition

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IUPHAR 9th International Congress of Pharmacology London 1984

Abstract

The enkephalins can be cleaved by a variety of peptidases but it increasingly appears that two enzyme activities are mainly, if not solely, involved in their physiological inactivation (for reviews see Schwartz et al., 1981, 1982, 1983; Hui & Lajtha, 1983; Schwartz, 1983). The first, responsible for the cleavage of the Gly3-Phe4 amide bond of the opioid pentapeptides, is generally termed ‘enkephalinase’ (Malfroy et al., 1978). It is primarily associated with synaptic membranes (De La Baume et al., 1980) and is potently and selectively inhibited by Thiorphan® (Roques et al., 1980). Its inhibition allows an increased recovery of enkephalins released from striatal slices and, in vivo, a diminished responsiveness to various nociceptive stimuli (Patey et al., 1981; De La Baume et al., 1983; Chaillet et al., 1983a).

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Authors and Affiliations

  1. Unité 109 de Neurobiologie, Centre Paul Broca de l’INSERM, 2 ter rue d’Alésia, 75014, Paris, France

    J. C. Schwartz, B. Giros, C. Gros, C. Llorens & B. Malfroy

Authors
  1. J. C. Schwartz
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  2. B. Giros
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  3. C. Gros
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  4. C. Llorens
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  5. B. Malfroy
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Editor information

William Paton James Mitchell Paul Turner Cheryl Padgham Eileen Ashcroft

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© 1984 Macmillan Publishers Limited

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Schwartz, J.C., Giros, B., Gros, C., Llorens, C., Malfroy, B. (1984). Metabolism of enkephalins and its inhibition. In: Paton, W., Mitchell, J., Turner, P., Padgham, C., Ashcroft, E. (eds) IUPHAR 9th International Congress of Pharmacology London 1984. Palgrave Macmillan, London. https://doi.org/10.1007/978-1-349-17615-1_40

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