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首页> 外文期刊>Life sciences >Tritiated kappa receptor antagonist norbinal torphimine: synthesis and in vitro binding in three different tissues.
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Tritiated kappa receptor antagonist norbinal torphimine: synthesis and in vitro binding in three different tissues.

机译:ti化的Kappa受体拮抗剂Norbinal Torphimine:在三种不同组织中的合成和体外结合。

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摘要

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.
机译:最近,开发了一种对κ受体具有高选择性的新型拮抗剂(降冰片碱),并在各种系统中进行了测试。该化合物用tri进行放射性标记,产生高比放射性(47.2 Ci / mmol)。通过体外放射性配体结合测定法表征了[3H]诺必宁吗啡。放射性配体在豚鼠,青蛙和大鼠的脑膜中以高效力和选择性与κ阿片受体结合。我们的结果表明放射性配体的κ特异性。

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