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  • Analgesia  (2)
  • D-Met2, Pro5-enkephalinamide  (1)
  • Dopaminergic agonists  (1)
  • 1
    ISSN: 1432-2072
    Keywords: Opioid peptides ; d-Met2,Pro5-enkephalina-mide ; Prolactin ; Growth hormone ; TSH ; Methysergide ; Bromocriptine ; Dopaminergic agonists ; Serotonergic antagonists
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract d-Met2,Pro5-enkephalinamide (EA) 10 mg, given SC, induced a dramatic rise in serum prolactin (PRL) and growth hormone (GH) levels in healthy male volunteers. The TSH content was also moderately elevated. Naloxone 0.8 mg administered IV abolished these effects. Bromocriptine 2.5 mg given per os also antagonized EA-induced PRL and TSH release but potentiated the GH surge. Methysergide 2.0 mg administered orally partially reversed EA-elicited PRL release, further augmented GH liberation and did not modify TSH output. The data indicate that inhibition of the dopaminergic tone and/or activation of certain serotonergic mechanisms play an important role in the EA-induced release of PRL and TSH. However, primarily other neurotransmitters might mediate the GH liberation elicited by this opioid peptide.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-2072
    Keywords: Opiates ; Opioid peptides ; Enkephalin analogues ; β-Endorphin ; Analgesia ; Species differences ; Morphine ; d-Met2, Pro5-enkephalinamide ; Rat ; Mouse ; Opiate receptors
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The analgesic ED50 values of some classical morphine congeners (morphine, methadone, fentanyl, azidomorphine) in the rat and mouse tail-flick tests were found to be similar. However, several synthetic derivatives of the natural enkephalins were more potent in mice than in rats. (These analogs contain d-amino acid in position 2 and d- or l-sulfonic (or phosphonic) acid residue in position 5). β-Endorpin, d-Met2, Pro5-enkephalinamide and two partial agonists showed intermediate interspecies relative potencies. According to the data obtained, similar opiate receptors might mediate the analgesic action of classical opiates in rats and in mice. However, the opiate receptors responsible for the antinociceptive effects of the above mentioned enkephalin analogues must be dissimilar in the two species examined. The results are discussed in terms of the role of μ- and δ-receptors in mediation of the analgesic effect induced by different types of opioids.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1432-2072
    Keywords: Opiates ; Opioid peptides ; Enkephalin analogue ; Pain threshold ; Pain tolerance ; Cognitive functions ; Memory ; Attention ; D-Met2, Pro5-enkephalinamide
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The effects ofd-Met2, Pro5-enkephalinamide (EA) on pain tolerance and some cognitive functions have been examined in healthy male volunteers. Dihydrocodeine (DC) was used as reference substance. Applying the submaximum effort tourniquet technique EA (10 mg SC) was found to elevate the pain threshold similarly to DC (20 mg SC). Neither DC nor EA impaired the performance in the symbol cancellation test, which quantitates the intensity of attention. In this assay rather a slight improvement was detected. In addition the short-term memory performance (Wechsler test) was also improved by EA and DC. No alteration was seen in the word fluency test, an indicator of long-term (semantic) memory. The data show that EA not only improves pain tolerance but some of its mental effects are similar to those of a classical morphine congener DC.
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    Psychopharmacology 53 (1977), S. 65-72 
    ISSN: 1432-2072
    Keywords: Morphine ; Apomorphine ; Analgesia ; Dopaminergic receptors
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Apomorphine pretreatment potentiated the analgesic effect of morphine in a dose-dependent manner both in rats and in mice measured by five different tests (writhing, hot plate, inflamed foot, tail-pinch and tail-flick procedures). Furthermore, apomorphine augmented the antinociceptive activity of morphine in tolerant animals as well. In morphine dependent mice the nalorphine precipitated jumping—a withdrawal symptom—was found inhibited by apomorphine treatment. The results are discussed in the light of the numerous but contradictory data available in the literature.
    Type of Medium: Electronic Resource
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