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

被引：0

作者：

Fjellaksel R. ^{[1
,2
,3
,4
]}

Oteiza A. ^{[1
,4
]}

Martin-Armas M. ^{[1
,4
]}

Riss P.J. ^{[5
,6
,7
]}

Hjelstuen O.K. ^{[2
]}

Kuttner S. ^{[1
,4
]}

Hansen Jø.H. ^{[3
]}

Sundset R. ^{[1
,4
]}

机构：

[1] Medical Imaging Research Group, Department of Clinical Medicine, UiT, Arctic University of Norway, Tromsø

[2] Drug Transport and Delivery Research Group, Department of Pharmacy, UiT, Arctic University of Norway, Tromsø

[3] Organic Chemistry Research Group, Department of Chemistry, UiT, Arctic University of Norway, Tromsø

[4] PET Imaging Center, University Hospital of North Norway, Tromsø

[5] Department of Neuropsychiatry and Psychosomatic Medicine, Oslo University Hospital, Oslo

[6] Realomics SFI, Department of Chemistry, University of Oslo, Oslo

[7] Norsk Medisinsk Syklotronsenter AS, Postboks 4950, Nydalen, Oslo

来源：

BMC Research Notes | / 11卷 / 1期

关键词：

Alpha-halogenation; GnRH; Gonadotropin; Radiotracer; SPECT;

D O I：

10.1186/s13104-018-3924-2

中图分类号：

学科分类号：

摘要：

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. © 2018 The Author(s).

引用

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