Publication Date:
1980-05-02
Description:
Naloxazone, a hydrazone derivative of the opiate antagonist naloxone, has a high affinity for opiate receptor binding sites. Naloxazone injections reduce opiate receptor binding to extensively washed mouse brain membranes for more than 24 hours, suggesting that the effect is irreversible. High-affinity binding sites are abolished by this treatment, whereas low-affinity sites are unaffected. Naloxazone treatment blocks the analgesic effects of morphine for at least 24 hours but does not prevent death from high doses of morphine. Thus analgesic but nonlethal opiate effects may be mediated by the high-affinity subpopulation of opiate receptors.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Pasternak, G W -- Childers, S R -- Snyder, S H -- New York, N.Y. -- Science. 1980 May 2;208(4443):514-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6245448" target="_blank"〉PubMed〈/a〉
Keywords:
Animals
;
Binding Sites/drug effects
;
Brain/metabolism
;
Mice
;
Morphine/pharmacology/toxicity
;
Naloxone/adverse effects/*analogs & derivatives/pharmacology
;
Receptors, Opioid/classification/*drug effects/physiology
Print ISSN:
0036-8075
Electronic ISSN:
1095-9203
Topics:
Biology
,
Chemistry and Pharmacology
,
Computer Science
,
Medicine
,
Natural Sciences in General
,
Physics
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