Record number :
1306436
Title of article :
PET-compatible endothelin receptor radioligands: Synthesis and first in vitro and in vivo studies Original Research Article
Author/Authors :
Carsten H?ltke، نويسنده , , Marilyn P. Law، نويسنده , , Stefan Wagner، نويسنده , , Klaus Kopka، نويسنده , , Andreas Faust، نويسنده , , Hans-J?rg Breyholz، نويسنده , , Otmar Schober، نويسنده , , Christoph Bremer، نويسنده , , Burkhard Riemann، نويسنده , , Michael Sch?fers، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2009
Pages :
12
From page :
7197
To page :
7208
Abstract :
The expression and function of endothelin (ET) receptors is abnormal in cardiovascular diseases, tumor progression, and tumor metastasis. In this study, we prepared two [18F]-fluorinated derivatives of the non-peptide ETA receptor antagonist PD 156707 and evaluated their ET receptor binding potencies. Ex vivo as well as in vivo biodistribution studies in mice were performed, as well as the metabolism of the radiotracer, which was examined by metabolite analysis in mice and rats. All tested derivatives of PD 156707 exhibited potent in vitro pharmacological characteristics with Ki values comparable to that of the lead compound. The biodistribution studies showed a high accumulation of the tracer in bile and intestine. In vivo we were able to show that the visualization of the heart as a major target organ with high ETAR expression is possible.
Keywords :
Biodistribution studies , Binding studies , Endothelin axis , Radiofluorination , PET imaging
Journal title :
Bioorganic and Medicinal Chemistry
Serial Year :
2009
Link To Document :
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