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First in vivo evaluation of a potential SPECT brain radiotracer for the gonadotropin releasing hormone receptor

机译:首先在体内评估潜在的SPECT脑放射机构的促进促促毒素释放激素受体

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摘要

Abstract Objectives In vivo evaluations of a gonadotropin releasing hormone-receptor single photon emission computed tomography radiotracer for non-invasive detection of gonadotropin releasing homone-receptors in brain. Results We have used a simple, robust and high-yielding procedure to radiolabel an alpha-halogenated bioactive compound with high radiochemical yield. Literature findings showed similar alpha-halogenated compounds suitable for in vivo evaluations. The compound was found to possess nano molar affinity for the gonadotropin releasing hormone-receptor in a competition dependent inhibition study. Furthermore, liquid chromatography-mass spectrometry analysis in saline, human and rat serum resulted in 46%, 52% and 44% stability after incubation for 1 h respectively. In addition, rat brain single photon emission computed tomography and biodistribution studies gave further insight into the nature of the compound as a radiotracer.
机译:摘要目的在促性腺激素释放激素受体单光子发射计算断层灭火器的体内评价,用于脑脑内促进脑内促进促性腺素受体的无侵袭性检测。结果我们利用简单,鲁棒和高产的方法来放射性标记具有高放射化学产率的α-卤代生物活性化合物。文献结果显示了适用于体内评价的类似α-卤代化合物。发现该化合物对竞争依赖性研究中的促进促性腺激素释放激素受体具有纳米摩尔亲和力。此外,盐水中的液相色谱 - 质谱分析分别孵育1小时后产生46%,52%和44%的稳定性。此外,大鼠脑单光子发射计算断层扫描和生物分布研究进一步了解化合物作为放射性机构的性质。

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