Tritiated Kappa receptor antagonist norbinaltorphimine: Synthesis and in vitro binding in three different tissues

A. Márki, F. Ötvös, G. Tóth, S. Hosztafi, A. Borsodi

Research output: Article

10 Citations (Scopus)

Abstract

Recently a new antagonist with high selectivity for the kappa receptors (norbinaltorphimine) was developed and tested in various systems. This compound was radiolabelled with tritium resulting in high specific radioactivity (47.2 Ci/mmol). [3H]Norbinaltorphimine was characterized by in vitro radioligand binding assays. The radioligand binds to κ-opioid receptors with a high potency and selectivity in guinea pig, frog and rat brain membranes. Our results suggest the κ1 specificity of the radioligand.

Original languageEnglish
Pages (from-to)43-49
Number of pages7
JournalLife Sciences
Volume66
Issue number1
DOIs
Publication statusPublished - nov. 26 1999

Fingerprint

kappa Opioid Receptor
Tissue
Radioligand Assay
Tritium
Radioactivity
Opioid Receptors
Anura
Rats
Assays
Brain
Guinea Pigs
Membranes
norbinaltorphimine
In Vitro Techniques

ASJC Scopus subject areas

  • Pharmacology

Cite this

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T1 - Tritiated Kappa receptor antagonist norbinaltorphimine

T2 - Synthesis and in vitro binding in three different tissues

AU - Márki, A.

AU - Ötvös, F.

AU - Tóth, G.

AU - Hosztafi, S.

AU - Borsodi, A.

PY - 1999/11/26

Y1 - 1999/11/26

N2 - Recently a new antagonist with high selectivity for the kappa receptors (norbinaltorphimine) was developed and tested in various systems. This compound was radiolabelled with tritium resulting in high specific radioactivity (47.2 Ci/mmol). [3H]Norbinaltorphimine was characterized by in vitro radioligand binding assays. The radioligand binds to κ-opioid receptors with a high potency and selectivity in guinea pig, frog and rat brain membranes. Our results suggest the κ1 specificity of the radioligand.

AB - Recently a new antagonist with high selectivity for the kappa receptors (norbinaltorphimine) was developed and tested in various systems. This compound was radiolabelled with tritium resulting in high specific radioactivity (47.2 Ci/mmol). [3H]Norbinaltorphimine was characterized by in vitro radioligand binding assays. The radioligand binds to κ-opioid receptors with a high potency and selectivity in guinea pig, frog and rat brain membranes. Our results suggest the κ1 specificity of the radioligand.

KW - κ-Opioid receptors

KW - Binding studies

KW - Norbinaltorphimine

KW - Tritium labelling

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