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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    International journal of peptide research and therapeutics 5 (1998), S. 395-398 
    ISSN: 1573-3904
    Keywords: antinociception ; interactions between opioids and substance P ; opioids ; substance P
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary Many years preclinical and clinical anatomic, pharmacologic, and physiologic studies suggest that SP- and opioid-expressing neurons produce opposite biological effects at the spinal level, i.e., nociception and antinociception, respectively. However, in certain circumstances intrathecally administered SP is capable of reinforcing of spinal morphine analgesia and may therefore function as an opioid adjuvantin vivo. The SP dose-response curve of spinally administered SP follows a bell-shaped or inverted-U configuration, permitting pharmacological dissociation of opioid-potentiating and analgesic properties of SP from traditional hyperalgesic effects seen at significantly higher concentrations. This analgesic effect is blocked by naloxone but unaffected by transection of the spinal cord, thus demonstrating the lack of supraspinal modulation. The present report briefly describes both reinforcing and opposing interactions between multiple opioid systems and substance P at the spinal level. We propose that a likely mechanism underlying SP-mediated enhancement of opioid analgesia is the ability of SP to release endogenous opioid peptides within the local spinal cord environment.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    International journal of peptide research and therapeutics 5 (1998), S. 395-398 
    ISSN: 1573-3904
    Keywords: antinociception ; interactionsbetween opioids and substance P ; opioids ; substance P
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Many years preclinical and clinical anatomic, pharmacologic, and physiologic studies suggest that SP- and opioid-expressing neurons produce opposite biological effects at the spinal level, i.e., nociception and antinociception, respectively. However, in certain circumstances intrathecally administered SP is capable of reinforcing of spinal morphine analgesia and may therefore function as an opioid adjuvant in vivo. The SP dose-response curve of spinally administered SP follows a bell-shaped or inverted-U configuration, permitting pharmacological dissociation of opioid-potentiating and analgesic properties of SP from traditional hyperalgesic effects seen at significantly higher concentrations. This analgesic effect is blocked by naloxone but unaffected by transection of the spinal cord, thus demonstrating the lack of supraspinal modulation. The present report briefly describes both reinforcing and opposing interactions between multiple opioid systems and substance P at the spinal level. We propose that a likely mechanism underlying SP-mediated enhancement of opioid analgesia is the ability of SP to release endogenous opioid peptides within the local spinal cord environment.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 3
    ISSN: 1573-3904
    Keywords: cis peptide bond conformation ; 1,5-disubstituted tetrazole ring ; Leu-enkephalin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary Six analogs of leucine-enkephalin were synthesized in which a 1,5-disubstituted tetrazole ring was incorporated in order to lock selected peptide bonds in cis geometry. The obtained compounds were examined based on their biological effects in vivo and in vitro. Only one analog was completely inactive in binding assays being very weakly active in the antinociceptive test. The remaining five compounds displayed at least weak receptor affinity and in vivo activity.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 4
    ISSN: 1573-3904
    Keywords: cis ; peptide bond conformation ; 1,5-disubstituted tetrazole ring ; Leu-enkephalin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Six analogs of leucine-enkephalin were synthesized in which a 1,5-disubstituted tetrazole ring was incorporated in order to lock selected peptide bonds in cis geometry. The obtained compounds were examined based on their biological effects in vivo and in vitro. Only one analog was completely inactive in binding assays being very weakly active in the antinociceptive test. The remaining five compounds displayed at least weak receptor affinity and in vivo activity.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
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