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Volumn 15, Issue 21, 2005, Pages 4699-4702

Synthesis of 4-(5-[18F]fluoromethyl-3-phenylisoxazol-4-yl) benzenesulfonamide, a new [18F]fluorinated analogue of valdecoxib, as a potential radiotracer for imaging cyclooxygenase-2 with positron emission tomography

Author keywords

COX 2; Fluorine 18; Inhibitor; PET; Radiotracer; Valdecoxib

Indexed keywords

4 (5 FLUOROMETHYL 3 PHENYLISOXAZOL 4 YL)BENZENESULFONAMIDE F 18; CYCLOOXYGENASE 2; FLUORIDE ION; RADIOPHARMACEUTICAL AGENT; TOLUENESULFONIC ACID DERIVATIVE; UNCLASSIFIED DRUG; VALDECOXIB;

EID: 25144508684     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.07.065     Document Type: Article
Times cited : (45)

References (41)
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    • f 0.45; hexanes-EtOAc 1:1 v/v). The total synthesis time was ∼120 min from EOB and the decay-corrected radiochemical yield was ∼40%. The specific activity was determined to be ∼2000 Ci/mmol at EOS based on the UV absorption and concentration standard curve.
  • 33
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    • The product was kept in EtOH until ready for use. For in vivo applications, the solution was diluted with normal saline such that the alcohol concentration was <5%.
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    • 18F]fluoride stays at the origin. The non-radioactive 1 was stable in PBS (pH 7.4).
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    • note
    • 18F (200-300 μCi in 200 μL saline containing <5% EtOH). Dynamic data acquisition commenced in a list mode at the time of injection to obtain a time-dependent organ distribution of radioactivity (frame times and sequence: 10 × 90 s and 21 × 300 s). The data were acquired in a 3-D mode with an axial span of ∼8 cm. The images were reconstructed using well-characterized 3-D filtered back-projection methods. The bony skeleton was visible in 15 min post-injection.
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    • note
    • 18F (∼10 mCi) was followed by the data collection, as described in Ref. 27, except that a series of bed positions was used to cover the entire animal with each position (300-s frames) repeated 3-6 times. The bone structure became visible in 45 min post-injection.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.