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

首次在体内评估促性腺激素释放激素受体 SPECT 脑放射性示踪剂的潜在作用

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作者:Richard Fjellaksel, Ana Oteiza, Montserrat Martin-Armas, Patrick J Riss, Ole Kristian Hjelstuen, Samuel Kuttner, Jørn H Hansen, Rune Sundset

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.

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