Radioiodinated benzovesamicol analogs for cholinergic nerve mapping

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.

Dependencies are inferred from the claim text.