Downregulation of mu-opioid binding sites following chronic administration of neuropeptide FF (NPFF) and morphine

Downregulation of mu-opioid binding sites following chronic administration of neuropeptide FF... The effect of continuous ICV infusion of NPFF (10 μg/μl) and morphine (40 μg/μl) on mu-opioid binding sites was examined in rats using the in vitro radiolabeled techniques of whole-brain homogenate receptor binding and quantitative autoradiography. Mu receptors were labeled with ( 3 H)( d -Ala 2 -MePhe 4 ,Glyol 5 )enkephalin in the homogenate binding experiments and with ( 125 I)( d -Ala 2 -MePhe 4 ,Gly-ol 5 ) enkephalin in autoradiographic studies. In homogenate binding studies, chronic administration of NPFF or morphine significantly downregulated mu receptors by 20% and 44%, respectively. Quantitative autoradiographic experiments demonstrated downregulation of mu opioid receptors in specific brain nuclei for both NPFF- and morphine-treated animals. Within the striatum and several nuclei of the thalamus, the mu receptors of the NPFF- and morphine-treated animals were decreased by 20–30% and 38–73%, respectively. These results suggest that NPFF may modulate opioid-mediated responses in part by altering the density of mu-opioid receptors. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Peptides Elsevier

Downregulation of mu-opioid binding sites following chronic administration of neuropeptide FF (NPFF) and morphine

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Abstract

The effect of continuous ICV infusion of NPFF (10 μg/μl) and morphine (40 μg/μl) on mu-opioid binding sites was examined in rats using the in vitro radiolabeled techniques of whole-brain homogenate receptor binding and quantitative autoradiography. Mu receptors were labeled with ( 3 H)( d -Ala 2 -MePhe 4 ,Glyol 5 )enkephalin in the homogenate binding experiments and with ( 125 I)( d -Ala 2 -MePhe 4 ,Gly-ol 5 ) enkephalin in autoradiographic studies. In homogenate binding studies, chronic administration of NPFF or morphine significantly downregulated mu receptors by 20% and 44%, respectively. Quantitative autoradiographic experiments demonstrated downregulation of mu opioid receptors in specific brain nuclei for both NPFF- and morphine-treated animals. Within the striatum and several nuclei of the thalamus, the mu receptors of the NPFF- and morphine-treated animals were decreased by 20–30% and 38–73%, respectively. These results suggest that NPFF may modulate opioid-mediated responses in part by altering the density of mu-opioid receptors.

Journal

PeptidesElsevier

Published: Jan 1, 1996

References

  • A review of the role of anti-opioid peptides in morphine tolerance and dependence
    Rothman, R.B.
  • Opioid receptor regulation in mice
    Yoburn, B.C.; Billings, B.; Duttaroy, A.

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