Antinociceptive and gastrointestinal effects of opiates

an analysis of the nature of the involvement of mu and delta receptors of the central nervous system in morphine-tolerant and non-tolerant mice

Subbiah Sivam, Ing K. Ho

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

This study attempted to distinguish between μ (morphine) and δ [(D-Ala2-D-Leu5)-enkephalin; DADLE] receptors, with regard to both in vivo effects (analgesia and gastrointestinal motility) and the location of binding activity in the brain. Analgesia and motility are distinguishable both by dose (intracere-broventricular) and by ligand selectivity with μ ligands more potent for the former and δ for the latter. Tolerance and cross-tolerance are exhibited for both effects, with the relationships between μ and δ ligand potencies preserved. In vitro receptor binding revealed an affinity decrease for δ in medulla and an increase in medulla and diencephalon for μ receptors after tolerance development to morphine. The results indicate that the μ receptors in medulla and diencephalon mediate analgesia, while medullary δ receptors control motility.

Original languageEnglish (US)
Pages (from-to)105-108
Number of pages4
JournalNeuropharmacology
Volume23
Issue number1
DOIs
StatePublished - 1984
Externally publishedYes

Fingerprint

Opiate Alkaloids
delta Opioid Receptor
mu Opioid Receptor
Analgesia
Morphine
Diencephalon
Central Nervous System
Ligands
Leucine-2-Alanine Enkephalin
Gastrointestinal Motility
Brain

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Drug Discovery
  • Pharmacology

Cite this

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abstract = "This study attempted to distinguish between μ (morphine) and δ [(D-Ala2-D-Leu5)-enkephalin; DADLE] receptors, with regard to both in vivo effects (analgesia and gastrointestinal motility) and the location of binding activity in the brain. Analgesia and motility are distinguishable both by dose (intracere-broventricular) and by ligand selectivity with μ ligands more potent for the former and δ for the latter. Tolerance and cross-tolerance are exhibited for both effects, with the relationships between μ and δ ligand potencies preserved. In vitro receptor binding revealed an affinity decrease for δ in medulla and an increase in medulla and diencephalon for μ receptors after tolerance development to morphine. The results indicate that the μ receptors in medulla and diencephalon mediate analgesia, while medullary δ receptors control motility.",
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N2 - This study attempted to distinguish between μ (morphine) and δ [(D-Ala2-D-Leu5)-enkephalin; DADLE] receptors, with regard to both in vivo effects (analgesia and gastrointestinal motility) and the location of binding activity in the brain. Analgesia and motility are distinguishable both by dose (intracere-broventricular) and by ligand selectivity with μ ligands more potent for the former and δ for the latter. Tolerance and cross-tolerance are exhibited for both effects, with the relationships between μ and δ ligand potencies preserved. In vitro receptor binding revealed an affinity decrease for δ in medulla and an increase in medulla and diencephalon for μ receptors after tolerance development to morphine. The results indicate that the μ receptors in medulla and diencephalon mediate analgesia, while medullary δ receptors control motility.

AB - This study attempted to distinguish between μ (morphine) and δ [(D-Ala2-D-Leu5)-enkephalin; DADLE] receptors, with regard to both in vivo effects (analgesia and gastrointestinal motility) and the location of binding activity in the brain. Analgesia and motility are distinguishable both by dose (intracere-broventricular) and by ligand selectivity with μ ligands more potent for the former and δ for the latter. Tolerance and cross-tolerance are exhibited for both effects, with the relationships between μ and δ ligand potencies preserved. In vitro receptor binding revealed an affinity decrease for δ in medulla and an increase in medulla and diencephalon for μ receptors after tolerance development to morphine. The results indicate that the μ receptors in medulla and diencephalon mediate analgesia, while medullary δ receptors control motility.

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