Synthesis and Pharmacologic Characterization of an Alkylating Analog (Chlornaltrexamine), of Naltrexone with Ultralong-Lasting Narcotic Antagonist Properties

Philip S Portoghese, D. L. Larson, J. B. Jiang, T. P. Caruso, A. E. Takemori

Research output: Contribution to journalArticlepeer-review

103 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)168-173
Number of pages6
JournalJournal of medicinal chemistry
Volume22
Issue number2
DOIs
StatePublished - Feb 1 1979

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