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  • conformational restriction  (2)
  • Modified phase cycle  (1)
  • Partial and full 1H—1H decoupling  (1)
  • 1
    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
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  • 2
    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
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  • 3
    Electronic Resource
    Electronic Resource
    Chichester : Wiley-Blackwell
    Organic Magnetic Resonance 30 (1992), S. S35 
    ISSN: 0749-1581
    Keywords: FLOCK sequence ; Modified phase cycle ; Chemistry ; Analytical Chemistry and Spectroscopy
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: The phase cycle for the FLOCK experiment was modified to provide improved suppression of artifacts and improved signal-to-noise ratios. An alternative version of FLOCK in which the initial BIRD pulse during t1 is replaced by a one-step J filter is shown to give comparable performance, while a phase-sensitive version of FLOCK shows the expected \documentclass{article}\pagestyle{empty}\begin{document}$ \sqrt 2 $\end{document} increase in sensitivity. Finally, while it is shown that phase-sensitive FLOCK without decoupling during acquisition can be used to measure nJ(C,H) (n ≤ 2), there are serious limitations to this approach.
    Additional Material: 5 Ill.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 0749-1581
    Keywords: 13C-Detected ; 13C—1H shift correlation sequence ; Phase-sensitive mode ; Partial and full 1H—1H decoupling ; Partial spectral editing ; Chemistry ; Analytical Chemistry and Spectroscopy
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Several different versions of the 13C-detected 13C—1H shift correlation sequence in phase sensitive mode with partial and full 1H—1H decoupling are described and evaluated. As expected, they show sensitivity advantages over their absolute value analogues. Further, it is possible partially to edit the 2D spectra since CH2 peaks are inverted relative to CH and CH3 peaks.
    Additional Material: 5 Ill.
    Type of Medium: Electronic Resource
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