Drug – bio-affecting and body treating compositions – Radionuclide or intended radionuclide containing; adjuvant...
Patent
1990-05-14
1991-12-31
Maples, John S.
Drug, bio-affecting and body treating compositions
Radionuclide or intended radionuclide containing; adjuvant...
546206, A61K 4902, C07D21106
Patent
active
050770357
ABSTRACT:
Radioiodinated benzovesamicol analogs which selectively localize in presynaptic cholinergic neurons of the general formula: ##STR1## where X is selected from the group consisting of H, OH, NH.sub.2, NHCO-3-[I]-Ph, and a radioactive isotope of iodine, and Y is selected from the group of H and a radioactive isotope of iodine, Y being H is X contains iodine. Illustrative examples include: (.+-.)-trans-2-hydroxy-5-iodo-3-(4-phenylpiperidino)tetralin; (.+-.)-trans-3-hydroxy-5-iodo-2-(4-phenylpiperidino)tetralin; (.+-.)-trans-5-amino-2-hydroxy-8-iodo-3-(4-phenylpiperidino)tetralin; and (.+-.)-trans-2-hydroxy-5-(3-iodobenzamido)-3-(4-phenylpiperidino)tetralin. The novel radioiodinated benzovesamicol analogs may be used as radiopharmaceuticals to visualize cholinergic neurons with conventional imaging devices which are typically found in most nuclear medicine or radiology clinics.
REFERENCES:
patent: 4246268 (1981-01-01), Carr
patent: 4435570 (1984-03-01), Nishimura et al.
Rogers et al., J. Med. Chem., vol. 32, No. 6, pp. 1217-1230, (1989).
Gildersleeve David L.
Jung Yong-Woon
Van Dort Marcian E.
Wieland Donald M.
Maples John S.
The University of Michigan
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