Upregulation of opioid receptor subtypes correlates with potency changes of morphine and DADLE. Academic Article uri icon

Overview

abstract

  • Chronic treatment with opioid antagonists increases the potency of opioid agonists and produces an increase in brain opioid binding sites. In the present study, 8 day treatment with naltrexone blocked morphine and DADLE analgesia for the entire treatment period and increased mu 1, mu 2 and delta opioid receptor binding sites in mouse brain. mu 1 and mu 2 binding were increased by 81 and 67%, respectively, while delta binding was increased by 31%. Consistent with these binding changes, the potency of ICV morphine to produce analgesia was increased by over 3-fold, while the potency of ICV DADLE was increased by only 1.7. These findings indicate that relative increases in opioid receptor subtypes agree with pharmacodynamic studies on potency changes of opioid agonists.

publication date

  • January 1, 1988

Research

keywords

  • Enkephalin, Leucine
  • Morphine
  • Naltrexone
  • Receptors, Opioid

Identity

Scopus Document Identifier

  • 0023742942

Digital Object Identifier (DOI)

  • 10.1016/0024-3205(88)90587-5

PubMed ID

  • 2845219

Additional Document Info

volume

  • 43

issue

  • 16