The Apparent Affinity of Morphine-3-Glucuronide At Mu(1)-Opioid Receptors Results From Morphine Contamination - Demonstration Using Hplc and Radioligand Binding

Bartlett, SE and Smith, MT (1995) The Apparent Affinity of Morphine-3-Glucuronide At Mu(1)-Opioid Receptors Results From Morphine Contamination - Demonstration Using Hplc and Radioligand Binding. Life Sciences, 57 6: 609-615.

Author Bartlett, SE
Smith, MT
Title The Apparent Affinity of Morphine-3-Glucuronide At Mu(1)-Opioid Receptors Results From Morphine Contamination - Demonstration Using Hplc and Radioligand Binding
Journal name Life Sciences   Check publisher's open access policy
ISSN 0024-3205
Publication date 1995-06-01
Year available 1995
Sub-type Article (original research)
Open Access Status Not yet assessed
Volume 57
Issue 6
Start page 609
End page 615
Total pages 7
Place of publication OXFORD
Publisher PERGAMON-ELSEVIER SCIENCE LTD
Language eng
Abstract Equilibrium binding studies in sheep thalamic homogenates indicated that morphine- 3-glucuronide (M3G) had an apparent affinity for mu(1)-opioid binding sites (IC50 = 1781 +/- 40 nM, K-i = 116 +/- 25 nM, mean +/- s.e.m., n=4) similar to that reported by Pasternak and co-workers (1). However, when the chemical purity of M3G Was investigated using high-performance-liquid-chromatography (HPLC) with electrochemical detection, it was found to be contaminated with 0.5% (molar basis) of morphine. Reduction of the morphine contamination of M3G to 0.08% resulted in a 7.2-fold decrease in apparent binding affinity (IC50 = 1279 +/- 287 nM, K-i = 766 +/- 30 nM, mean +/- s.e.m., n=4), indicating that the small percentage of morphine present in the M3G raw material drug is the likely explanation for M3G's apparent binding to mu(1)-opioid receptors.
Keyword Morphine-3-Glucuronide
Mu(1)-Opioid Receptors
Cns
Morphine
High-Dose Morphine
Opioid Receptor
Morphine-6-Glucuronide
Rats
Mu
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Unknown

Document type: Journal Article
Sub-type: Article (original research)
Collection: ResearcherID Downloads - Archived
 
Versions
Version Filter Type
Citation counts: TR Web of Science Citation Count  Cited 24 times in Thomson Reuters Web of Science Article | Citations
Google Scholar Search Google Scholar
Created: Sat, 02 Jul 2016, 04:17:39 EST by System User