Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists.
Bioorg Med Chem Lett
; 20(19): 5690-4, 2010 Oct 01.
Article
em En
| MEDLINE
| ID: mdl-20801028
ABSTRACT
Movement disorders such as Parkinson's disease and Huntington's disease are serious life-limiting and debilitating movement disorders. Their onset typically occurs from mid-life to late in life, and effective diagnostic techniques for detecting and following the disease course are lacking. Our goal is to develop receptor imaging agents for positron emission tomography (PET) that selectively target the most relevant subtype of adenosine receptors (AR) that are highly expressed in the striatum, that is, the A(2A) AR. To further this goal, we have synthesized and characterized pharmacologically a family of high affinity A(2A) AR ligands, based on the known antagonist, SCH 442416 (R=-Me), which have structural variability on the terminus (R=-Et, -i-Pr, -allyl, and others). A O-fluoroethyl analogue suitable for use as a PET tracer had a K(i) value of 12.4 nM and was highly selective for the A(2A) AR in comparison to the A(1) and A(3) ARs.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirimidinas
/
Triazóis
/
Meios de Contraste
/
Receptor A2A de Adenosina
/
Antagonistas do Receptor A2 de Adenosina
Limite:
Humans
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article