Facilitated Delivery of Endomorphins and Morphine into the CNS

Abstract

Endomorphins, endogenous brain opiates with the highest affinity and specifity for the mu opiate receptor, potently produce analgesia. A rapid brain-to-blood efflux system could give misleading results when entry rates are determined. Preliminary results show that endomorphin-1 and endomorphin-2 are saturably transported from brain to blood, as shown by self-inhibition by an excess of that peptide. There also was cross-inhibition of each endomorphin by the other, indicating shared components for the efflux system. CGRP, substance P, or constriction of the sciatic nerve did not decrease efflux. Furthermore, chronic pain induced by sciatic nerve constriction caused a striking decrease in endomorphin-2 immunoreactivity on the nerve-injured side in the spinal cord.

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Document Details

Document Type
Technical Report
Publication Date
Mar 01, 2001
Accession Number
ADA390342

Entities

People

  • Abba J. Kastin

Organizations

  • Veterans Administration Medical Center

Tags

DTIC Thesaurus Topics

  • Amino Acids
  • Animal Structures
  • Blood
  • Blood-Brain Barrier
  • Brain
  • Central Nervous System
  • Constrictions
  • Dissociation
  • Drug Addiction
  • Inhibition
  • Nerves
  • Nervous System
  • Opioids
  • Pain
  • Peptides
  • Sciatic Nerve
  • Spinal Cord

Fields of Study

  • Biology

Readers

  • Molecular and Cellular Biochemistry
  • Neuroscience
  • Neurotrauma and Rehabilitation Medicine.