Format

Send to

Choose Destination
BMC Res Notes. 2018 Nov 15;11(1):811. doi: 10.1186/s13104-018-3924-2.

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

Author information

1
Medical Imaging Research Group, Department of Clinical Medicine, UiT The Arctic University of Norway, Tromsø, Norway. richard.fjellaksel@uit.no.
2
Drug Transport and Delivery Research Group, Department of Pharmacy, UiT The Arctic University of Norway, Tromsø, Norway. richard.fjellaksel@uit.no.
3
Organic Chemistry Research Group, Department of Chemistry, UiT The Arctic University of Norway, Tromsø, Norway. richard.fjellaksel@uit.no.
4
The PET Imaging Center, University Hospital of North Norway, Tromsø, Norway. richard.fjellaksel@uit.no.
5
Medical Imaging Research Group, Department of Clinical Medicine, UiT The Arctic University of Norway, Tromsø, Norway.
6
The PET Imaging Center, University Hospital of North Norway, Tromsø, Norway.
7
Department of Neuropsychiatry and Psychosomatic Medicine, Oslo University Hospital, Oslo, Norway.
8
Realomics SFI, Department of Chemistry, University of Oslo, Oslo, Norway.
9
Norsk Medisinsk Syklotronsenter AS, Postboks 4950, Nydalen, Oslo, Norway.
10
Drug Transport and Delivery Research Group, Department of Pharmacy, UiT The Arctic University of Norway, Tromsø, Norway.
11
Organic Chemistry Research Group, Department of Chemistry, UiT The Arctic University of Norway, Tromsø, Norway.

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.

KEYWORDS:

Alpha-halogenation; GnRH; Gonadotropin; Radiotracer; SPECT

PMID:
30442192
PMCID:
PMC6238273
DOI:
10.1186/s13104-018-3924-2
[Indexed for MEDLINE]
Free PMC Article

Supplemental Content

Full text links

Icon for BioMed Central Icon for PubMed Central Icon for Norwegian BIBSYS system
Loading ...
Support Center