Journal article
[ 3H][D-Ala 2,NMePhe 4,Gly-ol 5]-enkephalin (mu-opioid) binding in beige-J mice
Peptides (New York, N.Y. : 1980), v 9(3), pp 637-642
01 May 1988
PMID: 2843835
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Abstract
Tritiated [D-Ala
2,NMePhe
4,Gly-ol
5]-enkephalin [
3H]DAGO) was used to examine mu-opioid receptor number and mu-ligand binding in brain synaptic membranes (P
2 fraction) from C57BL/6J-bg
J/bg
J (beige-J) mice, a strain with combined deficiencies in immunological function (resembling Chediak-Higashi syndrome) and analgesic response to mu-opioid agonists such as morphine and DAGO. As controls, white mice, beige-J littermates (normally responsive to mu-opioid agonists), and a known mu-deficient strain (CXBK) were also examined. Neither the K
D (0.47 to 0.49 nM) nor the B
max (153 to 168 fmol/mg protein) determined for beige-J mice was significantly different from values determined for littermates or white mice. In contrast, the B
max of CXBK mice (66 fmol/mg protein) was clearly less than that of the other strains. The analgesic defect of beige-J mice, therefore, is not likely due to an insufficient number of mu-opioid receptors, as it presumably is in CXBK mice. Carbachol (200 μg/ml), which partly corrects the analgesic defect of beige-J mice, had no effect on [
3H]DAGO binding either acutely in vitro or chronically ex vivo after administration to beige-J mice for three weeks. Hence, the analgesic defect of beige-J mice appears to be due to some defect in the mu-opioid receptor-effector coupling mechanism or to some endogenous substance that inhibits binding of mu-opioid ligands to otherwise functional receptors.
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Details
- Title
- [ 3H][D-Ala 2,NMePhe 4,Gly-ol 5]-enkephalin (mu-opioid) binding in beige-J mice
- Creators
- Robert B. Raffa - JanssenWilliam J. BaldyRichard P. ShankJoanne R. MathiasenJeffry L. VaughtJanssen Research Foundation, Spring House, PA (USA)
- Publication Details
- Peptides (New York, N.Y. : 1980), v 9(3), pp 637-642
- Publisher
- Elsevier
- Number of pages
- 6
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- Pharmacology and Physiology
- Web of Science ID
- WOS:A1988P113200031
- Scopus ID
- 2-s2.0-0024164424
- Other Identifier
- 991021900195404721
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InCites Highlights
Data related to this publication, from InCites Benchmarking & Analytics tool:
- Web of Science research areas
- Biochemistry & Molecular Biology
- Endocrinology & Metabolism
- Pharmacology & Pharmacy