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Synthesis and evaluation of a beta-adrenergic receptor ligand: Fluorine-18 labeled fluorocarazolol

Zheng, Lei
http://rave.ohiolink.edu/etdc/view?acc_num=case1061219721

Abstract Details

1994, Doctor of Philosophy, Case Western Reserve University, Chemistry.
Fluorocarazolol was synthesized, labeled with fluorine-18, and investigated as a potential radiopharmaceutical for use in positron tomography (PET). S-Fluorocarazolol was found to have a high affinity (K D = 68 pM) for the β-adrenergic receptors, similar to the parent compound, S-carazolol. The material exhibited significant specific binding in mice and in pigs. PET studies with pigs demonstrated an ability to produce clear high contrast images. The majority (80-90%) of the total tissue uptake was attributable to specific binding. The uptake kinetics were suitable for application of current compartmental kinetic models for receptor estimation. R-Fluorocarazolol was also found to have a measurable affinity (K D = 1138 pM) for the receptors, similar to R-carazolol itself. In vivo uptake of R-fluorocarazolol did not have any measurable specific binding component, however, which may allow it to be used for independent measurement of nonspecific binding. Fluorocarazolol was prepared in 58-72% yield by reaction of (18F) -fluoroacetone with previously synthesized R or S -des-isopropyl carazolol. The synthesis of fluoroacetone in 55-60% yield by reaction of (18F) -fluoride with acetol tosylate is also reported. The radiochemical yield of fluorocarazolol from labe led fluoride ion was 37 ± 5% at the end of the 45 min. procedure. Specific activity was 500-1200 Ci/mmol
Marc Berridge (Advisor)
218 p.
Chemistry, Organic
Fluorocarazolol; Fluorine-18; Beta-adrenergic receptor

Recommended Citations

Citations

  • Zheng, L. (1994). Synthesis and evaluation of a beta-adrenergic receptor ligand: Fluorine-18 labeled fluorocarazolol [Doctoral dissertation, Case Western Reserve University]. OhioLINK Electronic Theses and Dissertations Center. http://rave.ohiolink.edu/etdc/view?acc_num=case1061219721

    APA Style (7th edition)

  • Zheng, Lei. Synthesis and evaluation of a beta-adrenergic receptor ligand: Fluorine-18 labeled fluorocarazolol. 1994. Case Western Reserve University, Doctoral dissertation. OhioLINK Electronic Theses and Dissertations Center, http://rave.ohiolink.edu/etdc/view?acc_num=case1061219721.

    MLA Style (8th edition)

  • Zheng, Lei. "Synthesis and evaluation of a beta-adrenergic receptor ligand: Fluorine-18 labeled fluorocarazolol." Doctoral dissertation, Case Western Reserve University, 1994. http://rave.ohiolink.edu/etdc/view?acc_num=case1061219721

    Chicago Manual of Style (17th edition)

case1061219721
422
© 1994, all rights reserved.
This open access ETD is published by Case Western Reserve University School of Graduate Studies and OhioLINK.