Abstract
Chlornaltrexamine (CNA) produces ultralong-lasting (3--6 days) narcotic antagonism in mice and persistent stereospecific binding to rat-brain homogenate. Protection studies in mice suggest that CNA mediates its narcotic antagonist effects by interacting with the same receptors that are occupied by naloxone. A single icv dose of CNA also has been found to inhibit the development of physical dependence in mice for at least 3 days. These studies suggest that CNA exerts its sustained effects by selective covalent association with opioid receptors.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Alkylating Agents / chemical synthesis*
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Analgesics
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Animals
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Humans
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In Vitro Techniques
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Male
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Mice
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Molecular Conformation
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Morphine / antagonists & inhibitors
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Morphine Dependence / prevention & control
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Naloxone / analogs & derivatives*
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Naloxone / metabolism
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Naloxone / pharmacology
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Naltrexone / analogs & derivatives*
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Naltrexone / chemical synthesis
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Naltrexone / metabolism
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Naltrexone / pharmacology
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Narcotic Antagonists / chemical synthesis*
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Nitrogen Mustard Compounds / chemical synthesis
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Nitrogen Mustard Compounds / metabolism
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Nitrogen Mustard Compounds / pharmacology
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Rats
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Receptors, Opioid / metabolism
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Time Factors
Substances
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Alkylating Agents
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Analgesics
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Narcotic Antagonists
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Nitrogen Mustard Compounds
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Receptors, Opioid
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Naloxone
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Naltrexone
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chlornaltrexamine
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Morphine