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Updated: Aug 9, 2026

Assessment of Morphine-induced Hyperalgesia and Analgesic Tolerance in Mice Using Thermal and Mechanical Nociceptive Modalities
07:23

Assessment of Morphine-induced Hyperalgesia and Analgesic Tolerance in Mice Using Thermal and Mechanical Nociceptive Modalities

Published on: July 29, 2014

Limited phase I study of morphine-3-glucuronide

R T Penson1, S P Joel, S Clark

  • 1Division of Hematology/Oncology, Massachusetts General Hospital, 100 Blossom Street, Cox 640, Boston, Massachusetts 02114, USA. rpenson@partners.org

Journal of Pharmaceutical Sciences
|December 18, 2001
PubMed

Insights

Morphine-3-glucuronide (M3G) showed minimal toxicity in healthy volunteers at tested doses. This study found no significant adverse effects or changes in vital signs, indicating M3G is well-tolerated.

Area of Science:

  • Pharmacology
  • Clinical Toxicology

Background:

  • Morphine-3-glucuronide (M3G) is a major metabolite of morphine.
  • Understanding M3G toxicity is crucial for pain management and opioid pharmacokinetics.

Purpose of the Study:

  • To investigate the toxicity and pharmacokinetics of intravenous morphine-3-glucuronide (M3G) in healthy volunteers.
  • To assess potential neuroexcitatory and opioid effects of M3G at single doses.

Main Methods:

  • Open, uncontrolled, single-blinded, single-dose study.
  • Three cohorts of healthy volunteers (n=3 per cohort) received 7.5, 15, or 30 mg/70 kg IV M3G.
  • Plasma M3G concentrations measured via HPLC; subjective toxicity and vital signs recorded over 24 hours.

Main Results:

  • No significant changes in cardiovascular or respiratory parameters were observed.
  • Subjective toxicity assessments revealed virtually no adverse effects.
  • Pharmacokinetics followed a two-compartment model with a mean elimination half-life of 1.66 hours.

Conclusions:

  • M3G demonstrated a favorable safety profile at the investigated doses.
  • No clear neuroexcitatory or opioid effects were detected.
  • M3G pharmacokinetics were comparable to those of morphine-6-glucuronide (M6G).

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