Tritiated kappa receptor antagonist norbinal torphimine: synthesis and in vitro binding in three different tissues.
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 kappa-opioid receptors with a high potency and selectivity in guinea pig, frog and rat brain membranes. Our results suggest the kappa1 specificity of the radioligand.
Márki
A
A
Institute of Biochemistry and Isotope Laboratory, Biological Research Center, Hungarian Academy of Sciences, Szeged.
Otvös
F
F
Tóth
G
G
Hosztafi
S
S
Borsodi
A
A
D000818:Animals; D001001:Anura; D001667:Binding, Competitive; D001921:Brain / Q000187:drug effects* / Q000378:metabolism; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D006168:Guinea Pigs; D009271:Naltrexone / Q000031:analogs & derivatives* / Q000494:pharmacology; D009292:Narcotic Antagonists / Q000494:pharmacology*; D011869:Radioligand Assay; D051381:Rats; D017473:Receptors, Opioid, kappa / Q000037:antagonists & inhibitors / Q000187:drug effects / Q000378:metabolism*; D013045:Species Specificity; D014316:Tritium
D009292:Narcotic Antagonists; D017473:Receptors, Opioid, kappa; D014316:Tritium; C051844:norbinaltorphimine; D009271:Naltrexone