Márki A, Otvös F, Tóth G, Hosztafi S, Borsodi A
Institute of Biochemistry and Isotope Laboratory, Biological Research Center, Hungarian Academy of Sciences, Szeged.
Life Sci. 2000;66(1):43-9. doi: 10.1016/s0024-3205(99)00560-3.
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.
最近，一种对κ受体具有高选择性的新型拮抗剂（诺宾烷托啡尼）被研发出来并在各种系统中进行了测试。该化合物用氚进行放射性标记，产生了高比放射性（47.2 Ci/mmol）。[3H]诺宾烷托啡尼通过体外放射性配体结合试验进行了表征。该放射性配体在豚鼠、青蛙和大鼠脑膜中以高效力和选择性与κ阿片受体结合。我们的结果表明该放射性配体具有κ1特异性。
