Synthesis of18F-labelled cyclooxygenase-2 (COX-2) inhibitors via Stille reaction with 4-[18F]fluoroiodobenzene as radiotracers for positron emission tomography (PET)

2005 ◽  
Vol 3 (3) ◽  
pp. 503-507 ◽  
Author(s):  
Frank R. Wüst ◽  
Aileen Höhne ◽  
Peter Metz
Keyword(s):  
Positron Emission Tomography ◽  
Cyclooxygenase 2 ◽  
Emission Tomography ◽  
Stille Reaction ◽  
Positron Emission ◽  
Cox 2 ◽  
Cox 2 Inhibitors

scholarly journals 2-(4-Methylsulfonylphenyl)pyrimidines as Prospective Radioligands for Imaging Cyclooxygenase-2 with PET—Synthesis, Triage, and Radiolabeling

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2850 ◽  
Author(s):  
Michelle Cortes-Salva ◽  
Stal Shrestha ◽  
Prachi Singh ◽  
Cheryl Morse ◽  
Kimberly Jenko ◽  
...  
Keyword(s):  
Comparative Evaluation ◽  
Cyclooxygenase 2 ◽  
Emission Tomography ◽  
Inhibitory Potency ◽  
Positron Emission ◽  
Positron Emitter ◽  
Cox 2 ◽  
Cox 2 Inhibitors ◽  
Cox 1

Cyclooxygenase 2 (COX-2) is an inducible enzyme responsible for the conversion of arachidonic acid into the prostaglandins, PGG2 and PGH2. Expression of this enzyme increases in inflammation. Therefore, the development of probes for imaging COX-2 with positron emission tomography (PET) has gained interest because they could be useful for the study of inflammation in vivo, and for aiding anti-inflammatory drug development targeting COX-2. Nonetheless, effective PET radioligands are still lacking. We synthesized eleven COX-2 inhibitors based on a 2(4-methylsulfonylphenyl)pyrimidine core from which we selected three as prospective PET radioligands based on desirable factors, such as high inhibitory potency for COX-2, very low inhibitory potency for COX-1, moderate lipophilicity, and amenability to labeling with a positron-emitter. These inhibitors, namely 6-methoxy-2-(4-(methylsulfonyl)phenyl-N-(thiophen-2ylmethyl)pyrimidin-4-amine (17), the 6-fluoromethyl analogue (20), and the 6-(2-fluoroethoxy) analogue (27), were labeled in useful yields and with high molar activities by treating the 6-hydroxy analogue (26) with [11C]iodomethane, [18F]2-fluorobromoethane, and [d2-18F]fluorobromomethane, respectively. [11C]17, [18F]20, and [d2-18F]27 were readily purified with HPLC and formulated for intravenous injection. These methods allow these radioligands to be produced for comparative evaluation as PET radioligands for measuring COX-2 in healthy rhesus monkey and for assessing their abilities to detect inflammation.

Design, Synthesis, and Evaluation of an18F-Labeled Radiotracer Based on Celecoxib-NBD for Positron Emission Tomography (PET) Imaging of Cyclooxygenase-2 (COX-2)

ChemMedChem ◽  
2015 ◽  
Vol 10 (10) ◽  
pp. 1635-1640 ◽  
Author(s):  
Jatinder Kaur ◽  
Ole Tietz ◽  
Atul Bhardwaj ◽  
Alison Marshall ◽  
Jenilee Way ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Pet Imaging ◽  
Cyclooxygenase 2 ◽  
Emission Tomography ◽  
Design Synthesis ◽  
Positron Emission ◽  
Cox 2

Positron Emission Tomography of Cocaine Binding Sites on the Dopamine Transporter

1994 ◽  
Author(s):  
Bertha K. Madras ◽  
◽  
David R. Elmaleh ◽  
Peter C. Meltzer ◽  
Anna Y. Liung ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Dopamine Transporter ◽  
Binding Sites ◽  
Emission Tomography ◽  
Positron Emission
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