Binding of 3H-naloxone in the mouse brain: Effect of ions and tolerance development

Robert J. Hitzemann, Barbara A. Hitzemann, Horace H. Loh

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The binding of 3H-naloxone (spec. act. 5.2 Ci/mmol) in a crude mitochondrial fraction of the whole mouse brain was examined. Binding was reversed by the narcotic agonists levorphanol, morphine and 1-methadone but not by dextrorphan. Levorphanol sensitive (specific) 3H-naloxone binding was blocked by Na+, Li+, Ca++, Mg++ and Mn++ but not by K+. When the crude mitochondrial fraction was separated on a discontinuous sucrose gradient, the highest activity of specific binding was found in the nerve ending particle fraction. Animals made physically dependent by 3 day morphine pellet implantation did not show an increased binding affinity for 3H-nalovxone. The implantation of a 10 mg naloxone pellet increased the apparent total number of binding sites on the second and third day of implantation.

Original languageEnglish (US)
Pages (from-to)2393-2404
Number of pages12
JournalLife Sciences
Issue number12
StatePublished - Jun 16 1974

Bibliographical note

Funding Information:
1 This study was supported in part by USPHS Grant DA-00564 and Contract DADA-17-73-C-03006 .


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