This title appears in the Scientific Report :
2006
Please use the identifier:
http://dx.doi.org/10.1016/j.ejmech.2005.07.018 in citations.
Synthesis and evaluation of 7-amino-2(2(3)-furyl)-5-phentylethylaminooxazolo[4,5-d]pyrimidines as potential A2A adenosine receptor antagonist for positron emission tomography (PET)
Synthesis and evaluation of 7-amino-2(2(3)-furyl)-5-phentylethylaminooxazolo[4,5-d]pyrimidines as potential A2A adenosine receptor antagonist for positron emission tomography (PET)
The brain A2A adenosine receptor (A2AAR) participates with the dopamine D2 receptor in the control of movement and also might influence behavior. Because PET is an important tool for studying the roles of receptors in disease, a ligand for imaging the brain A2AAR is desirable. This report describes...
Saved in:
Personal Name(s): | Holschbach, M. H. |
---|---|
Bier, D. / Stüsgen, S. / Wutz, W. / Sihver, W. / Coenen, H. H. / Olsson, R. A. | |
Contributing Institute: |
Institut für Nuklearchemie; INC |
Published in: | European Journal of Medicinal Chemistry, 41 (2006) S. 7 - 15 |
Imprint: |
Amsterdam [u.a.]
Elsevier Science
2006
|
Physical Description: |
7 - 15 |
PubMed ID: |
16289482 |
DOI: |
10.1016/j.ejmech.2005.07.018 |
Document Type: |
Journal Article |
Research Program: |
Funktion und Dysfunktion des Nervensystems |
Series Title: |
European Journal of Medicinal Chemistry
41 |
Subject (ZB): | |
Publikationsportal JuSER |
The brain A2A adenosine receptor (A2AAR) participates with the dopamine D2 receptor in the control of movement and also might influence behavior. Because PET is an important tool for studying the roles of receptors in disease, a ligand for imaging the brain A2AAR is desirable. This report describes the synthesis and A2AAR antagonist activities of a panel of phenyl-substituted 7-amino-2-(2-furyl)-5-phenylethylamino-oxazolo[5,4-d]pyrimidines, 11aa-af, and their 3-furyl congeners, 11ba-bd. In competitive binding studies all compounds displaced [3H]CGS21680 from the A2AAR with Ki values of 14-33 nM with selectivity for the A2AAR over the A1AR of 5- to 94-fold. Autoradiography of brain sections showed a high level of unspecific binding that obscured specific binding. Thus, these compounds are not promising PET ligands. |