Azidomorphine is an agonist of high-affinity opioid receptor binding sites

Azidomorphine at low concentration (10(-9) M) inhibits the high-affinity binding site of labeled naloxone in rat brain membrane preparations. In the presence of Na+ and guanine nucleotides the displacement curves of azidomorphine are increased toward high concentrations, whereas Mg2+ ions decrease t...

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Bibliographic Details
Published in:Neurochemical research 1986-11, Vol.11 (11), p.1565-1569
Main Authors: HORVATH, K, WOLLEMANN, M
Format: Article
Language:English
Subjects:
Analgesics
Analgesics - pharmacology
Animals
azidomorphine
Binding, Competitive
Biological and medical sciences
brain
Brain - metabolism
Cell Membrane - metabolism
Dihydromorphine - metabolism
Guanylyl Imidodiphosphate - pharmacology
Kinetics
Medical sciences
Morphine - pharmacology
Morphine Derivatives - pharmacology
naloxone
Naloxone - metabolism
Neuropharmacology
opiates
Pharmacology. Drug treatments
Rats
Receptors, Opioid - drug effects
Receptors, Opioid - metabolism
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Summary:Azidomorphine at low concentration (10(-9) M) inhibits the high-affinity binding site of labeled naloxone in rat brain membrane preparations. In the presence of Na+ and guanine nucleotides the displacement curves of azidomorphine are increased toward high concentrations, whereas Mg2+ ions decrease the IC50 values; This demonstrates the agonist behavior of azidomorphine in binding experiments. When compared with morphine, azidomorphine displayed five-fold lower IC50 values. Based on the presented results, azidomorphine appears to be a good candidate for photoaffinity labeling of opiate receptors.
ISSN:0364-3190
1573-6903
DOI:10.1007/BF00965775