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  • 1
    Electronic Resource
    Electronic Resource
    Conformationally constrained opioid peptide analogs with novel activity profiles (1998)
    Springer
    International journal of peptide research and therapeutics 5 (1998), S. 209-214 
    Details
    ISSN: 1573-3904
    Keywords: conformational restriction ; δ opioid agonists ; δ opioid antagonists ; mixed μ opioid agonist/δ opioid antagonists ; opioid peptides ; receptor-bound conformation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary Novel conformationally constrained opioid peptide analogs with δ antagonist, mixed μ agonist/δ antagonist or δ agonist properties were developed. TIP(P)-related δ antagonists showed unprecedented δ antagonist potency and δ receptor selectivity, and may have potential for use in analgesia in combination with μ agonists. A definitive model of their δ receptor-bound conformation was developed. Three prototype mixed μ agonist/δ antagonists were discovered. They represent the only known compounds with this pharmacological profile and, as expected, one of them was shown to be a potent analgesic and to produce no dependence and less tolerance than morphine. Novel dipeptide derivatives turned out to be potent and selective δ agonists. Because of their low molecular weight and lipophilic character, these compounds may cross the blood-brain barrier and, thus, may have potential as centrally acting analgesics.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02443471
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    Conformationally constrained opioid peptide analogs with novel activity profiles (1998)
    Springer
    International journal of peptide research and therapeutics 5 (1998), S. 209-214 
    Details
    ISSN: 1573-3904
    Keywords: conformational restriction ; δ opioid agonists ; δ opioid antagonists ; mixed μ opioid agonist/δ opioid antagonists ; opioid peptides ; receptor-bound conformation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Novel conformationally constrained opioid peptide analogs with δ antagonist, mixed μ agonist/δ antagonist or δ agonist properties were developed. TIP(P)-related δ antagonists showed unprecedented δ antagonist potency and δ receptor selectivity, and may have potential for use in analgesia in combination with μ agonists. A definitive model of their δ receptor-bound conformation was developed. Three prototype mixed μ agonist/δ antagonists were discovered. They represent the only known compounds with this pharmacological profile and, as expected, one of them was shown to be a potent analgesic and to produce no dependence and less tolerance than morphine. Novel dipeptide derivatives turned out to be potent and selective δ agonists. Because of their low molecular weight and lipophilic character, these compounds may cross the blood-brain barrier and, thus, may have potential as centrally acting analgesics.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1008842411553
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    Enkephalin analogs containing 4,4-difluoro-2-aminobutyric acid: Synthesis and fluorine effect on the biological activity (1998)
    New York, NY [u.a.] : Wiley-Blackwell
    Journal of Peptide Science 4 (1998), S. 496-501 
    Details
    ISSN: 1075-2617
    Keywords: enkephalins ; DPDPE ; opioid agonists ; δ-receptor ; fluorine containing amino acid ; Chemistry ; Biochemistry and Biotechnology
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Analogs of Met-enkephalin and [d-Pen2, d-Pen5]enkephalin (DPDPE) containing the partially fluorinated amino acid 4,4-difluoro-2-aminobutyric acid (DFAB) in the 2- or 3-position of the peptide sequence were synthesized and their opioid activities and receptor selectivities were determined in vitro. The linear fluorinated [d-DFAB2, Met5-NH2]enkephalin showed μ and δ agonist potencies comparable to those of natural [Leu5]enkephalin. The partially fluorinated DPDPE analogs behaved differently as compared with their non-fluorinated correlates. While l-amino acid substitution in position 3 of DPDPE usually resulted in higher δ agonist potency than d-amino acid substitution, [d-DFAB3]DPDPE turned out to be a more potent δ agonist than [l-DFAB3]DPDPE. Furthermore, [d-DFAB3]DPDPE showed over 100-fold higher δ agonist potency than [d-Abu3]DPDPE (Abu=2-aminobutyric acid), indicating that the fluorine substituents interact favorably with a δ opioid receptor subsite. © 1998 European Peptide Society and John Wiley & Sons, Ltd.
    Additional Material: 4 Ill.
    Type of Medium: Electronic Resource
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