Radioiodinated benzovesamicol analogs for cholinergic nerve...

Details Radioiodinated benzovesamicol analogs for cholinergic nerve... Radioiodinated benzovesamicol analogs for cholinergic nerve...

C - Chemistry, Metallurgy

07

D

C07D 211/14 (2006.01) A61K 51/04 (2006.01) C07B 59/00 (2006.01) A61K 49/02 (1990.01)

Patent

CA 2082797

2082797 9117776 PCTABS00008 Radioiodinated benzovesamicol analogs which selectively localize in presynaptic cholinergic neurons of general formula (I), where X is selected from the group consisting of H, OH, NH2, 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 if 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.

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