Radiosynthesis and in vivo evaluation of a fluorine-18 labeled pyrazine based radioligand for PET imaging of the adenosine A2B receptor

2018 ◽  
Vol 26 (16) ◽  
pp. 4650-4663 ◽  
Author(s):  
Marcel Lindemann ◽  
Sonja Hinz ◽  
Winnie Deuther-Conrad ◽  
Vigneshwaran Namasivayam ◽  
Sladjana Dukic-Stefanovic ◽  
...  
Keyword(s):  
Pet Imaging ◽  
In Vivo Evaluation ◽  
Adenosine A2b Receptor ◽  
A2b Receptor ◽  
Adenosine A2b

scholarly journals Development of a Radiofluorinated Adenosine A2B Receptor Antagonist as Potential Ligand for PET Imaging

2020 ◽  
Vol 21 (9) ◽  
pp. 3197
Author(s):  
Marcel Lindemann ◽  
Rareş-Petru Moldovan ◽  
Sonja Hinz ◽  
Winnie Deuther-Conrad ◽  
Daniel Gündel ◽  
...  
Keyword(s):  
Nucleophilic Aromatic Substitution ◽  
Receptor Subtypes ◽  
Cancer Therapies ◽  
Aromatic Substitution ◽  
Adenosine A2b Receptor ◽  
Positron Emission ◽  
A2b Receptor ◽  
Potential Ligand ◽  
Adenosine A2b

The adenosine A2B receptor has been proposed as a novel therapeutic target in cancer, as its expression is drastically elevated in several tumors and cancer cells. Noninvasive molecular imaging via positron emission tomography (PET) would allow the in vivo quantification of this receptor in pathological processes and most likely enable the identification and clinical monitoring of respective cancer therapies. On the basis of a bicyclic pyridopyrimidine-2,4-dione core structure, the new adenosine A2B receptor ligand 9 was synthesized, containing a 2-fluoropyridine moiety suitable for labeling with the short-lived PET radionuclide fluorine-18. Compound 9 showed a high binding affinity for the human A2B receptor (Ki(A2B) = 2.51 nM), along with high selectivities versus the A1, A2A, and A3 receptor subtypes. Therefore, it was radiofluorinated via nucleophilic aromatic substitution of the corresponding nitro precursor using [18F]F-/K2.2.2./K2CO3 in DMSO at 120 °C. Metabolic studies of [18F]9 in mice revealed about 60% of radiotracer intact in plasma at 30 minutes p.i. A preliminary PET study in healthy mice showed an overall biodistribution of [18F]9, corresponding to the known ubiquitous but low expression of the A2B receptor. Consequently, [18F]9 represents a novel PET radiotracer with high affinity and selectivity toward the adenosine A2B receptor and a suitable in vivo profile. Subsequent studies are envisaged to investigate the applicability of [18F]9 to detect alterations in the receptor density in certain cancer-related disease models.

In vivo adenosine A2B receptor desensitization in guinea-pig airway smooth muscle: Implications for asthma

2007 ◽  
Vol 575 (1-3) ◽  
pp. 149-157 ◽  
Author(s):  
Maria Cristina Breschi ◽  
Corrado Blandizzi ◽  
Stefano Fogli ◽  
Cinzia Martinelli ◽  
Barbara Adinolfi ◽  
...  
Keyword(s):  
Smooth Muscle ◽  
Guinea Pig ◽  
Airway Smooth Muscle ◽  
Receptor Desensitization ◽  
Adenosine A2b Receptor ◽  
A2b Receptor ◽  
Adenosine A2b

scholarly journals In Vivo Hypoxic Preconditioning Protects From Warm Liver Ischemia-Reperfusion Injury Through the Adenosine A2B Receptor

2012 ◽  
Vol 94 (9) ◽  
pp. 894-902 ◽  
Author(s):  
Alexander Choukèr ◽  
Akio Ohta ◽  
André Martignoni ◽  
Dmitriy Lukashev ◽  
Lefteris C. Zacharia ◽  
...  
Keyword(s):  
Reperfusion Injury ◽  
Ischemia Reperfusion Injury ◽  
Ischemia Reperfusion ◽  
Hypoxic Preconditioning ◽  
Liver Ischemia ◽  
Adenosine A2b Receptor ◽  
A2b Receptor ◽  
Warm Liver Ischemia ◽  
Adenosine A2b

scholarly journals Elevated adenosine signaling via adenosine A2B receptor induces normal and sickle erythrocyte sphingosine kinase 1 activity

Blood ◽  
2015 ◽  
Vol 125 (10) ◽  
pp. 1643-1652 ◽  
Author(s):  
Kaiqi Sun ◽  
Yujin Zhang ◽  
Mikhail V. Bogdanov ◽  
Hongyu Wu ◽  
Anren Song ◽  
...  
Keyword(s):  
Sphingosine Kinase ◽  
Sphingosine Kinase 1 ◽  
Adenosine A2b Receptor ◽  
Sickle Erythrocyte ◽  
Key Points ◽  
A2b Receptor ◽  
Specific Antagonist ◽  
Adenosine A2b ◽  
Adenosine Signaling

Key Points Adenosine signaling via ADORA2B induces SphK1 activity in sickle and normal erythrocytes via PKA-mediated ERK1/2 activation. Lowering adenosine by PEG-ADA or interfering ADORA2B activation by specific antagonist decreases SphK1 activity in normal and sickle RBCs.

Novel Adenosine A2B Receptor Signalling in Cardiac Fibroblasts: Uncovering Context-Specific Biased Agonism

2018 ◽  
Vol 27 ◽  
pp. S115-S116
Author(s):  
E. Vecchio ◽  
J. Baltos ◽  
C. Qin ◽  
R. Ritchie ◽  
A. Christopoulos ◽  
...  
Keyword(s):  
Cardiac Fibroblasts ◽  
Adenosine A2b Receptor ◽  
Biased Agonism ◽  
Receptor Signalling ◽  
A2b Receptor ◽  
Context Specific ◽  
Adenosine A2b
Sign in / Sign up

Export Citation Format

Share Document