Radiofluoro-tyrosine derivatives, the preparation and use thereo

Drug – bio-affecting and body treating compositions – Radionuclide or intended radionuclide containing; adjuvant...

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562445, A61K 4902, C07C10172

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active

049256513

ABSTRACT:
The use of 2-radiohalogenotyrosine derivatives of the formula I ##STR1## in which X denotes a radioactive halogen, in particular fluorine-18, bromine-75 or iodine-123, and R denotes hydrogen or methyl, in particular of 2-fluoro(18)-tyrosine and -methyltyrosine (II) for emission-tomographic measurement of protein synthesis in vivo, in particular for the purposes of cerebral diagnosis, by means of SPECT and, in particular, by means of PET, provides, in view of the particularly high incorporation rate, especially of II, the possibility of quantitative kinetic evaluation and is thus of great interest, specifically in the framework of tumor diagnosis.

REFERENCES:
patent: 4469680 (1984-09-01), Huffman et al.
patent: 4695449 (1987-09-01), Pawelek
Bustany et al., "Protein Synthesis Evaluation in Brain and Other Organs in uman by PET." Positron Emission Tomography, Dreivich et al. eds, Alan R. Liss, Inc. (1985) pp. 183-201.
Coenen et al., "Synthesis, Autoradiography and Biochemistry of L-.sup.18 F-Fluorophenylalanines for Probing Protein Synthesis," Nuklear medizin, suppl. 22 (1986) pp. 600-602.
Chirakal et al., "Synthesis of 2- and 3-Fluorotyrosine with Dilute Fluorine Gas," Journal of Fluorine Chemistry, vol. 37 (1987) pp. 267-278.
Wagner, J. Nucl. Med., 29(8)1329-1331 (Aug. 1988).

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