Preparation of [3H]-oxymorphazone and its binding to rat brain membranes.

A. Borsodi, E. Varga, G. Toth, S. Hosztafi

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

Oxymorphazone is a 14-hydroxydihydromorphinone derivative which contains C-6 hydrazone group and hence could serve as an irreversible label for opioid receptors. 3H-oxymorphazone was synthesized by the reaction of 3H-oxymorphone with excess hydrazine, with 640 GBq/mmol specific radioactivity. Both the unlabelled compound and the tritiated ligand show high affinity to mu and kappa opiate receptor subtypes in rat brain membranes. Two binding sites were detected by equilibrium binding studies. About 60% of the 3H-oxymorphazone specific binding is irreversible at 10nM ligand concentration. Preincubation of the membranes with unlabelled oxymorphazone resulted in an irreversible blockade of the high affinity 3H-naloxone binding sites.

Original languageEnglish
Pages (from-to)220-223
Number of pages4
JournalNIDA research monograph
Volume75
Publication statusPublished - 1986

Fingerprint

Membranes
hydrazine
Brain
Opioid Receptors
Oxymorphone
Binding Sites
Ligands
Hydrazones
kappa Opioid Receptor
Naloxone
Radioactivity
oxymorphazone

ASJC Scopus subject areas

  • Medicine (miscellaneous)

Cite this

Preparation of [3H]-oxymorphazone and its binding to rat brain membranes. / Borsodi, A.; Varga, E.; Toth, G.; Hosztafi, S.

In: NIDA research monograph, Vol. 75, 1986, p. 220-223.

Research output: Contribution to journalArticle

Borsodi, A. ; Varga, E. ; Toth, G. ; Hosztafi, S. / Preparation of [3H]-oxymorphazone and its binding to rat brain membranes. In: NIDA research monograph. 1986 ; Vol. 75. pp. 220-223.
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