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Synthesis and evaluation of the novel 2-[¹8F]fluoro-3-propoxy-triazole-pyridine-substituted losartan for imaging AT1 receptors.
Arksey, Natasha; Hadizad, Tayebeh; Ismail, Basma; Hachem, Maryam; Valdivia, Ana C; Beanlands, Rob S; deKemp, Robert A; DaSilva, Jean N.
Afiliación
  • Arksey N; Cardiac PET Centre, University of Ottawa Heart Institute, 40 Ruskin St., Ottawa, ON, Canada; Department of Cellular and Molecular Medicine, University of Ottawa, Ottawa, ON, Canada.
  • Hadizad T; Cardiac PET Centre, University of Ottawa Heart Institute, 40 Ruskin St., Ottawa, ON, Canada.
  • Ismail B; Cardiac PET Centre, University of Ottawa Heart Institute, 40 Ruskin St., Ottawa, ON, Canada; Department of Cellular and Molecular Medicine, University of Ottawa, Ottawa, ON, Canada.
  • Hachem M; Cardiac PET Centre, University of Ottawa Heart Institute, 40 Ruskin St., Ottawa, ON, Canada; Department of Cellular and Molecular Medicine, University of Ottawa, Ottawa, ON, Canada.
  • Valdivia AC; Cardiac PET Centre, University of Ottawa Heart Institute, 40 Ruskin St., Ottawa, ON, Canada; Department of Cellular and Molecular Medicine, University of Ottawa, Ottawa, ON, Canada.
  • Beanlands RS; Cardiac PET Centre, University of Ottawa Heart Institute, 40 Ruskin St., Ottawa, ON, Canada; Department of Cellular and Molecular Medicine, University of Ottawa, Ottawa, ON, Canada.
  • deKemp RA; Cardiac PET Centre, University of Ottawa Heart Institute, 40 Ruskin St., Ottawa, ON, Canada.
  • DaSilva JN; Cardiac PET Centre, University of Ottawa Heart Institute, 40 Ruskin St., Ottawa, ON, Canada; Department of Cellular and Molecular Medicine, University of Ottawa, Ottawa, ON, Canada; Department of Radiology, Radio-Oncology and Nuclear Medicine, University of Montreal, University of Montreal Hospital
Bioorg Med Chem ; 22(15): 3931-7, 2014 Aug 01.
Article en En | MEDLINE | ID: mdl-25023539
ABSTRACT
The 2-[(18)F]fluoro-3-pent-4-yn-1-yloxypyridine ([(18)F]FPyKYNE) analog of the potent non-peptide angiotensin II type 1 receptor (AT1R) blocker losartan was produced via click chemistry linking [(18)F]FPyKYNE to azide-modified tetrazole-protected losartan followed by TFA deprotection. Preliminary small animal imaging with positron emission tomography (PET) in rats displayed high uptake in the kidneys with good contrast to surrounding tissue. Rat metabolism displayed the presence of 23% unchanged tracer in plasma at 30 min. Upon co-administration with AT1R blocker candesartan (2.5, 5 and 10 mg/kg), a dose-dependent reduction (47-65%) in tracer uptake was observed in the kidney, while no difference was observed following AT2R blocker PD123,319 (5 mg/kg), indicating binding selectivity for AT1R over AT2R and potential for imaging AT1R using PET.
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Losartán / Receptor de Angiotensina Tipo 1 / Bloqueadores del Receptor Tipo 1 de Angiotensina II Límite: Animals Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article País de afiliación: Canadá
Texto completo
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Losartán / Receptor de Angiotensina Tipo 1 / Bloqueadores del Receptor Tipo 1 de Angiotensina II Límite: Animals Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article País de afiliación: Canadá