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First in vivo evaluation of a potential SPECT brain radiotracer for the gonadotropin releasing hormone receptor.
Fjellaksel, Richard; Oteiza, Ana; Martin-Armas, Montserrat; Riss, Patrick J; Hjelstuen, Ole Kristian; Kuttner, Samuel; Hansen, Jørn H; Sundset, Rune.
Afiliação
  • Fjellaksel R; Medical Imaging Research Group, Department of Clinical Medicine, UiT The Arctic University of Norway, Tromsø, Norway. richard.fjellaksel@uit.no.
  • Oteiza A; Drug Transport and Delivery Research Group, Department of Pharmacy, UiT The Arctic University of Norway, Tromsø, Norway. richard.fjellaksel@uit.no.
  • Martin-Armas M; Organic Chemistry Research Group, Department of Chemistry, UiT The Arctic University of Norway, Tromsø, Norway. richard.fjellaksel@uit.no.
  • Riss PJ; The PET Imaging Center, University Hospital of North Norway, Tromsø, Norway. richard.fjellaksel@uit.no.
  • Hjelstuen OK; Medical Imaging Research Group, Department of Clinical Medicine, UiT The Arctic University of Norway, Tromsø, Norway.
  • Kuttner S; The PET Imaging Center, University Hospital of North Norway, Tromsø, Norway.
  • Hansen JH; Medical Imaging Research Group, Department of Clinical Medicine, UiT The Arctic University of Norway, Tromsø, Norway.
  • Sundset R; The PET Imaging Center, University Hospital of North Norway, Tromsø, Norway.
BMC Res Notes ; 11(1): 811, 2018 Nov 15.
Article em En | MEDLINE | ID: mdl-30442192
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.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Encéfalo / Tomografia Computadorizada de Emissão de Fóton Único / Receptores LHRH Limite: Animals / Humans Idioma: En Ano de publicação: 2018 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Encéfalo / Tomografia Computadorizada de Emissão de Fóton Único / Receptores LHRH Limite: Animals / Humans Idioma: En Ano de publicação: 2018 Tipo de documento: Article