Radioiodinated benzamines and method of their use as radioimagin

Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Amino acid sequence disclosed in whole or in part; or...

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514359, 514428, 548567, A61K 5104, A61K 3140, C07D20708, A01N 4336

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active

054806313

ABSTRACT:
Novel, substituted benzamides in radioiodinated form are useful in radiopharmaceutical compositions in nuclear medicine as imaging agents to detect, visualize, and analyze the distribution and function of the dopamine D2 receptor in the mammalian brain. These compounds have a specific combination of lipophilicity and dopamine D2 receptor affinity required to attain a required image contrast. The iodinated benzamides identified by the above discovery can be made by reacting a trialkyltin substituted benzamide with an acid in the presence of radioactive iodine which, in turn, is generated by in situ oxidation of an appropriate iodide nuclide salt.

REFERENCES:
Crawley et al. "Abstract 145 Dopamine Receptors in the Human Brain Imaged w/ a New Ligand Labelled with .sup.123 I", Clin. Sci. 70, Suppl. 13 (1986).
Kung et al., "Preparation & Radiolabelling of IBZM: A Potential D-Z Specific Brain Imaging Agent for SPECT", J. of Labelled Compounds & Radio-Pharmaceuticals, 23:10-12, Oct., 1986, pp. 1318-1319.

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