Subcutaneous injection of an analog of neuropeptide FF prevents naloxone-precipitated morphine abstinence syndrome

Subcutaneous injection of an analog of neuropeptide FF prevents naloxone-precipitated morphine... There is evidence that neuropeptide FF (NPFF) has antiopiate activity and may play a role in opiate dependence and subsequent abstinence syndrome. A fragment of NPFF was modified at the C-terminal in an effort to convert it to an NPFF antagonist. It was also dansylated at the N-terminal in an effort to render it more lipophilic and increase its penetration of the blood-brain barrier. Third ventricle administration of the resulting compound, dansyl-PQRamide (0.75 μg and 1 μg), dose-dependently antagonized the quasi-morphine abstinence activity of NPFF (10 μg) in opiate-naive rats. Subcutaneous injection of dansyl-PQRamide (13 mg/kg) in chronically morphine-infused rats attenuated opiate dependence as indicated by prevention of naloxone-precipitated abstinence syndrome. Dansyl-PQRamide displaced radiolabelled ligand from NPFF receptors in a concentration-dependent manner with a K i of 13 μM, and had a half-life over 300 times longer than NPFF under aminopeptidase digestion. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Drug and Alcohol Dependence Elsevier

Subcutaneous injection of an analog of neuropeptide FF prevents naloxone-precipitated morphine abstinence syndrome

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Publisher
Elsevier
Copyright
Copyright © 1995 Elsevier Ltd
ISSN
0376-8716
DOI
10.1016/0376-8716(95)01178-1
Publisher site
See Article on Publisher Site

Abstract

There is evidence that neuropeptide FF (NPFF) has antiopiate activity and may play a role in opiate dependence and subsequent abstinence syndrome. A fragment of NPFF was modified at the C-terminal in an effort to convert it to an NPFF antagonist. It was also dansylated at the N-terminal in an effort to render it more lipophilic and increase its penetration of the blood-brain barrier. Third ventricle administration of the resulting compound, dansyl-PQRamide (0.75 μg and 1 μg), dose-dependently antagonized the quasi-morphine abstinence activity of NPFF (10 μg) in opiate-naive rats. Subcutaneous injection of dansyl-PQRamide (13 mg/kg) in chronically morphine-infused rats attenuated opiate dependence as indicated by prevention of naloxone-precipitated abstinence syndrome. Dansyl-PQRamide displaced radiolabelled ligand from NPFF receptors in a concentration-dependent manner with a K i of 13 μM, and had a half-life over 300 times longer than NPFF under aminopeptidase digestion.

Journal

Drug and Alcohol DependenceElsevier

Published: Nov 1, 1995

References

  • Subcutaneous injection of an analog of neuropeptide FF precipitates morphine abstinence syndrome
    Malin, D.H.; Lake, J.R.; Arcangeli, K.R.; Deshotel, K.D.; Hausam, D.D.; Witherspoon, W.E.; Carter, V.A.; Yang, H.-Y.T.; Pal, B.; Burgess, K.
  • Characterization of binding sites for neuropeptide FF on T lymphocytes of the Jurkat cell line
    Minault, M.; Lecron, J.C.; Labrouche, S.; Simonnet, G.; Gombert, J.

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