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  • Title: Enkephalin-like character and analgesia.
    Author: Rónai AZ, Berzétei IP, Székely JI, Miglécz E, Kurgyis J, Bajusz S.
    Journal: Eur J Pharmacol; 1981 Jan 29; 69(3):263-71. PubMed ID: 7215429.
    Abstract:
    The opioid activities of enkephalin analogues bearing D- or L-aminopentane-sulfonic/phosphonic acid at position 5 were studied in vitro, in electrically stimulated longitudinal muscle strip of guinea-pig ileum and mouse vas deferens preparations and in vivo in the rat tail-flick test. Using their in vitro effects Met-enkephalin-like, beta-endorphin-like, (nor)morphine-like and derivatives of intermediate character could be differentiated. Correlating the in vitro activities with the analgesic activity in vivo it is concluded that the enkephalin-like character in a pentapetide may hinder the expression of analgesic activity, when the compounds are given into the cerebroventricular system.
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