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Related Experiment Videos

Human tolerability studies with D-Met2,Pro5-enkephalinamide.

J Földes, K Török, J I Székely

    Life Sciences
    |January 1, 1983
    PubMed
    Summary

    D-Met2,Pro5-enkephalinamide (EA), an enkephalin analogue, was tested for human tolerability. EA caused autonomic effects and mood changes, with dose-dependent hormonal alterations in male volunteers.

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    Area of Science:

    • Pharmacology
    • Neuroscience
    • Endocrinology

    Background:

    • D-Met2,Pro5-enkephalinamide (EA) is a potent enkephalin analogue.
    • Previous studies established its high activity.

    Purpose of the Study:

    • To evaluate the human tolerability of D-Met2,Pro5-enkephalinamide (EA).
    • To investigate the autonomic, mood, and hormonal effects of EA in male volunteers.

    Main Methods:

    • Male volunteers received subcutaneous injections of EA at increasing doses (0.1-30.0 mg).
    • Autonomic responses, mood, wakefulness, and serum hormone levels (prolactin, HGH, TSH) were monitored.

    Main Results:

    • Observed autonomic effects included limb heaviness, dry mouth, pallor, and conjunctival injection within 15-30 minutes.

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  • Mood changes like drowsiness and emotional detachment occurred later.
  • Serum prolactin increased dose-dependently; HGH showed a biphasic response; TSH elevated at highest doses.

    • Conclusions:

    • EA is generally tolerated in humans, with predictable autonomic and mood effects.
    • EA influences pituitary hormone secretion in a dose-dependent or biphasic manner.