(-)[N-(propyl)-14-OH-dihydromorphinan-6-one] = (N-propyl)-noroxymorphone and its multiple tritiated form (molar activity: 126 Ci/mmol; 1 Ci = 37 GBq) was synthesized. According to our knowledge this specific radioactivity exceeds all of the commercially available [3H]opioid ligands. The ligand was found to be a pure opioid antagonist in receptor binding assays performed with rat brain membranes. Scatchard analysis of equilibrium binding isotherms revealed one high affinity (Kd approximately 4 nM) binding site. Reversibility, stereospecificity and opioid nature of the binding was confirmed by ligand binding experiments. Because of its antagonist character combined with high specific radioactivity the ligand might be a useful tool in characterizing and purifying opioid receptors.
|Number of pages||9|
|Journal||Neurobiology (Budapest, Hungary)|
|Publication status||Published - 1993|
ASJC Scopus subject areas